Combinations of DGK (diacylglycerol kinase) inhibitors

Abstract

The present invention encompasses combinations comprising one or more DGK [alpha] inhibitors and one or more DGK [zeta] inhibitors. Another aspect of the invention encompasses the use of the above combination for the preparation of a medicament for the treatment or prophylaxis of a disease, in particular a condition with a dysregulated immune response, in particular cancer, or a viral infection or other disorder associated with abnormal DGK [alpha] and / or DGK [zeta] signaling.

Description

Technical Field

[0001] The present invention encompasses a combination comprising one or more DGKα inhibitors and one or more DGKζ inhibitors, in particular a combination comprising a DGKα inhibitor compound of formula (I) as described herein and a DGKζ inhibitor compound of formula (II) as described herein, more particularly a combination comprising a DGKα inhibitor A and a DGKζ inhibitor A' as described herein. In addition, the present invention relates to a DGKα inhibitor for use in a method for treating or preventing a disease, in particular a condition in a mammal (including a human) with a dysregulated immune response (in particular cancer), a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling, characterized in that the method for treating or preventing the disease comprises administering at least one DGKζ inhibitor. The present invention also provides a DGKζ inhibitor for use in a method for treating or preventing a disease, in particular a condition in a mammal (including a human) with a dysregulated immune response (in particular cancer), a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling, characterized in that the method for treating or preventing the disease comprises administering at least one DGKα inhibitor. Another aspect of the present invention encompasses the use of the combination comprising one or more DGKα inhibitors and one or more DGKζ inhibitors in the preparation of a medicament for the treatment or prevention of a disease, particularly a condition in mammals (including humans) with a dysregulated immune response (particularly cancer), a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling. Background Art

[0002] Cancer is the second most common cause of death in the United States, killing 450,000 people annually. While substantial progress has been made in identifying some of the possible environmental and genetic causes of cancer, additional treatment modalities for cancer and related diseases remain unmet. In particular, there is a need for therapies that can reactivate a patient's immune system, particularly exhausted and suppressed T cells, to kill tumors.

[0003] Diacylglycerol kinases (DGKs) represent a family of enzymes that catalyze the phosphorylation of the membrane lipid sn-1,2-diacylglycerol (DAG) to form phosphatidic acid (PA) (T. O. Eichmann and A. Lass, Cell. Mol. Life Sci. 2015, 72, 3931-3952). In T cells, DAG is formed downstream of the T cell receptor (TCR) following activation of the gamma 1 isoform of phospholipase C (PLCyl) and cleavage of phosphatidylinositol 4,5-bisphosphate (PIP2) to DAG and the additional second messenger inositol 1,4,5-trisphosphate (IP3) (S. Krishna and X.-P. Zhong, Front. Immunol. 2013, 4, 178). While IP3 is important in facilitating the release of calcium from the endoplasmic reticulum, DAG interacts with other important proteins in TCR signaling, such as protein kinase C theta (E. J. Quann et al., Nat. Immunol. 2011, 12(7), 647-654) and the Ras-activating protein RasGRP1 (S.

[0004] Three isoforms of DGK are known to exist within T cells: DGKa (DGK alpha), DGK5 (DGK delta), and DGKz (DGK zeta). Two of these, DGKa and DGKz, are believed to play important roles in promoting DAG metabolism downstream of the TCR (R. P. Joshi and G. A. Koretzky, Int. J. Mol. Sci. 2013, 14(4), 6649-6673).

[0005] Targeting the activity of DGKa or DGKz in T cells through germline deletion or chemical inhibitors results in enhanced and sustained signaling downstream of T cells, as assessed by prolonged phosphorylation of downstream molecules such as extracellular signal-related kinase 1 / 2 (ERK 1 / 2) and NFKB (X.-P.-Zhong et al., Nat. Immunol. 2003, 4, 882-890; B. A. Olenchock et al., Nat. Immunol. 2006, 7(11), 1174-1181; M. J. Riese et al., J. Biol.

[0006] Chem. 2011, 286, 5254-5265; E. M. Wesley et al., Immuno Horizons 2018, 2(4), 107-118).

[0007] Deletion of DGKz or DGKa in T cells leads to enhanced production of effector cytokines (such as IL2, IFNy) and enhanced proliferation (X.-P. Zhong et al., Nat. Immunol. 2003, 4, 882-890; B. A. Olenchock et al., Nat. Immunol. 2006, 7(11), 1174-1181, E. M. Riese et al., J. Biol. Chem. 2011, 286, 5254-5264). Furthermore, overexpression of DGKa induced a state of reduced functionality similar to anergy-like state (Zha et al., Nat Immunol 2006, 7, 1166).

[0008] Adoptive transfer of DGKz-deficient T cells reduced the leukemia burden after inoculation with C1498.SIY leukemia cells compared to controls. Furthermore, DGKz-deficient T cells were at least partially resistant to PD1 -mediated inhibitory signals (W. Jing et al., Cancer Res. 2017, 77(20), 5676-5686). Moreover, DGKz-deficient mice had reduced tumor size compared to controls after orthotopic tumor injection in a pancreatic tumor model (E. M. Wesley et al., Immuno Horizons, 2018, 2(4), 107-118). Furthermore, S. Wee et al. inoculated C57BL / 6 mice with various syngeneic tumor cell lines (MC38 colon carcinoma, B16F1 melanoma and C1498 leukemia) and analyzed survival and tumor growth in the presence or absence of anti-PD1 treatment. DGKz- / - mice inhibited growth of subcutaneously implanted tumor cells in all three model systems and the combination of DGKz-deficiency and anti-PD1 was additive in tumor control (S. Wee et al., Proceedings of the American Association for Cancer Research Annual Meeting 2019; Cancer Res. 2019, 79(13 Suppl): Abstract nr 936).

[0009] C57BL / 6 mice and analyzed survival and tumor growth in the presence or absence of anti-PD1 treatment. DGKz- / - mice inhibited growth of subcutaneously implanted tumor cells in all three model systems and the combination of DGKz-deficiency and anti-PD1 was additive in tumor control (S. Wee et al., Proceedings of the American Association for Cancer Research Annual Meeting 2019; Cancer Res. 2019, 79(13 Suppl): Abstract nr 936).

[0010] The role of DGKa in anti-tumor responses was also investigated in human tumor-infiltrating CD8+ T cells (CD8-TIL) from renal cell carcinoma (RCC) patients (Prinz et al., J. Immunol 2012, 188, 5990). CD8-TIL from RCCs have a defect in lytic granule exocytosis and their ability to kill target cells. While proximal signaling events are intact upon TCR engagement, CD8-TILs exhibit reduced ERK phosphorylation compared to non-tumor infiltrating CD8+ T cells. Treatment of CD8-TILs with DGKa activity inhibitors can rescue the killing ability of target cells, enhance basal levels of ERK phosphorylation, and enhance PMA / ionomycin-stimulated ERK phosphorylation.

[0011] Thus, DGKz and DGKa can be useful targets to enhance T cell anti-tumor activity.

[0012] In addition, the adoptive transfer of DGKz and / or DGKa deficient CAR (chimeric antigen receptor)-T cells showed enhanced efficacy in the treatment of a mouse mesothelioma (M. J. Riese et al., Cancer Res. 2013, 73(12), 3566-3577) and a glioblastoma xenograft mouse model (I.-Y. Jung et al., Cancer Res. 2018, 78(16), 4692-4703) in combination with DGKa knock-out.

[0013] Furthermore, DGK inhibitors not only promote Ras / ERK signaling, but also AP-1 (activator protein-1) transcription, promote DGKa membrane localization, reduce the requirement for costimulation, and synergize with activation enhancement upon DGKz silencing / deletion. In contrast to pharmacological inhibition triggering activation enhancement, DGKa silencing / gene deletion leads to impaired Lck (lymphocyte-specific protein tyrosine kinase) activation and limited costimulatory responses (Arranz-Nicolas et al., Cancer Immun, Immunother 2018, 67(6), 965).

[0014] In addition, DGKa- / - and DGKz- / - Antigen-specific CD8-positive T cells of mice show enhanced expansion and cytokine production after infection with (lymphocytic choriomeningitis virus) (Shin et al. J. Immunol, 2012). Furthermore, DGKz-deficient mice developed a stronger immune response to lymphocytic choriomeningitis virus infection than wild-type mice (X.-P. Zhong et al., Nat. Immunol. 2003, 4, 882-890).

[0015] DGKz is also associated with natural killer cells (NK). Upon stimulation through multiple activating receptors, NK cells of DGKz-deficient mice showed enhanced cytokine production and degranulation in an ERK-dependent manner. Furthermore, they had enhanced cytotoxic function against tumor cell lines (E. Yang et al. J. Immunol. 2016, 197(3), 934-41.).

[0016] In addition to immune cell modulation, DGKz also plays a role in cancer, mediating many aspects of cancer cell development, including proliferation, apoptosis, survival, invasion, and tumorigenicity, for example in models of osteosarcoma, colon cancer, breast cancer, prostate cancer, glioma, and leukemia (W. Yu et al., Front. Oncol. 2019, 8:655; K. Cai et al., BMC Cancer 2014, 14:208; J. Diao et al., Mol. Neurobiol. 2016; 53, 5425-35; H. Li et al. Pharmazie 2019, 74(7):418-422). DGKa also plays a role in cancer, mediating many aspects of cancer cell development, including survival (Bacchiocchi et al., Blood, 2005, 106(6), 2175; Yanagisawa et al. Biochim Biophys Acta 2007, 1771, 462) of cancer cells, migration, and invasion (Baldanzi et al., Oncogene 2008, 27, 942; Filigheddu et al., Anticancer Res 2007, 27, 1489; Rainero et al., J Cell Biol 2012, 196(2):277) of cancer cells. In particular, DGKa has been reported to be overexpressed in hepatocellular carcinoma (Takeishi et al., J Hepatol 2012, 57, 77) and melanoma cells (Yanagisawa et al., Biochim Biophys Acta 2007, 1771, 462), while other reports indicate that growth of colon and breast cancer cell lines was significantly inhibited by DGKa-siRNA16 and that the DGKa / noncanonical PKC / b1 integrin signaling pathway is critical for matrix invasion of breast cancer cells (Rainero et al., PLoS One 2014, 9(6):e97144). Furthermore, expression was also higher in lymph node metastases than in breast primary tumors (Hao et al., Cancer 2004, 100, 1110).

[0017] In addition, a study testing the importance of DGKa in glioblastoma multiforme (GBM) cells found that concurrent administration of the relatively non-specific DGKa inhibitor R59022 resulted in reduced growth of intracranially injected GBM tumors (Dominguez et al. Cancer Discov 2013, 3(7):782).

[0018] Likewise, DGKa promotes the development of esophageal squamous cell carcinoma (ESCC), supporting DGKa as a potential target for the treatment of ESCC (Chen et al., Oncogene, 2019, 38(14) 2533).

[0019] Furthermore, pharmacological inhibition of DGKs reduces airway inflammation and airway hyperresponsiveness in mice and attenuates T helper 2 (Th2)-driven immune pathology in a mouse model of allergic asthma by blocking T H 2) differentiation reduces bronchoconstriction in human airway samples in vitro (Singh et al., Sci Signal. 2019, 12, eaax3332).

[0020] Moreover, inhibition of DGKa has the potential to reverse life-threatening Epstein-Barr virus (EBV)-related immunopathology occurring in patients with X-linked lymphoproliferative disease (XLP-1)

[0021] (Ruffo et al., Sci Transl Med. 2016, 13, 8, 321; Velnati et al., Eur J Med Chem. 2019, 164, 378).

[0022] Furthermore, DGKa exacerbates cardiac injury after ischemia / reperfusion heart disease (Sasaki et al., Heart Vessels, 2014, 29, 110).

[0023] In summary, the results of these studies suggest that inhibition of DGKz and / or DGKa activity in T cells and tumor cells can prove valuable in generating a stronger immune response against tumors and in ameliorating Th2-driven (auto)immune diseases (rebalancing the immune system). Furthermore, inhibition of DGKz and / or DGKa activity has therapeutic potential in directly targeting tumors as well as in addressing fibrotic disorders, pathologies associated with viral infections, heart disease, and lymphoproliferative disorders.

[0024] Inhibitors of DGKs have been previously disclosed, such as aminochinolone DGKa inhibitors (see WO 2021 / 105115, WO 2021 / 105116 and WO 2021 / 105117), and aminothiazole DGKz inhibitors (see WO 2021 / 214019 and WO 2021 / 214020).

[0025] Further inhibitors of DGK a are disclosed in WO2021 / 130638, WO2022 / 271650, WO2022 / 271659, WO2022 / 271677, WO2022 / 271684, WO2022 / 114812, WO2023 / 165504, WO2023 / 165509 and WO2023 / 165525.

[0026] Further inhibitors of DGK zeta are disclosed in WO2021 / 132422 and WO2022 / 114164.

[0027] Inhibitors of DGK a and / or DGK zeta are disclosed in WO2020 / 006016, WO2020 / 006018, WO2021 / 041588, WO2021 / 133748, WO2021 / 133749, WO2021 / 133750, WO2021 / 133751, WO2021 / 133752, WO2021 / 258010, WO2022 / 133083, WO2022 / 171745, WO2023 / 011456, WO2023 / 122772, WO2023 / 122777, WO2023 / 122778, WO2023 / 184327 and WO2023 / 186060.

[0028] Further inhibitors / modulators of DGK activity are disclosed in WO2023 / 023376, WO2023 / 023664, WO2023 / 150186, CN116969943 and CN117088874.

[0029] Combinations of DGK inhibitors and immune checkpoint antagonists are disclosed in WO2021 / 127554.

[0030] Combinations of T cell therapies with DGK inhibitors are disclosed in WO2022 / 187406.

[0031] Wichroski et al., Sci. Transl. Med. 15, eadh1892 (2023) 25 October 2023 disclose studies of dual DGK a / zeta inhibitors in combination with aPD-(L)1.

[0032] Chupak et al., ACS Med. Chem. Lett. 2023, 14, 929-935 disclose the discovery of dual DGK a / zeta inhibitors. SUMMARY

[0033] Surprisingly, when a DGK a inhibitor is administered in combination with a DGK z inhibitor, a superior effect is observed in in vitro and in vivo tumor models.

[0034] According to a first aspect, the present application provides a combination comprising one or more DGK a inhibitors and one or more DGK z inhibitors.

[0035] According to a second aspect, the present application provides a kit comprising:

[0036] a DGK a inhibitor compound of general formula (I) as described herein, more specifically DGK a inhibitor A, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same,

[0037] a DGK z inhibitor compound of general formula (II) as described herein, more specifically DGK z inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[0038] According to a third aspect, the present application provides a pharmaceutical composition comprising a combination of one or more DGK a inhibitors and one or more DGK z inhibitors, and one or more pharmaceutically acceptable excipients.

[0039] According to a fourth aspect, there is provided a DGK a inhibitor for use in a method of treatment or prevention of a disease, preferably a condition with dysregulated immune response (in particular cancer), a viral infection or other disorder associated with abnormal DGK a and / or DGK z signaling, in a mammal, including a human, as described herein before, characterized in that the method comprises administering at least one DGK z inhibitor.

[0040] According to a fifth aspect, there is provided a DGK z inhibitor for use in a method of treatment or prevention of a disease, preferably a condition with dysregulated immune response (in particular cancer), a viral infection or other disorder associated with abnormal DGK a and / or DGK z signaling, in a mammal, including a human, as described herein before, characterized in that the method comprises administering at least one DGK a inhibitor.

[0041] According to a sixth aspect, the present application provides a combination of the present application as described herein before for use in a method of treatment or prevention of a disease, preferably a condition with dysregulated immune response (in particular cancer), a viral infection or other disorder associated with abnormal DGK a and / or DGK z signaling, in a mammal, including a human, as described herein below.

[0042] According to a seventh aspect, the present application provides a kit as described above for use in the treatment or prevention of a disease, preferably a condition with a dysregulated immune response (in particular cancer), a viral infection or other disorder associated with abnormal DGK a and / or DGK z signaling in a mammal, including a human, as described below.

[0043] According to an eighth aspect, the present application provides a pharmaceutical composition as described above for use in the treatment or prevention of a disease, preferably a condition with a dysregulated immune response (in particular cancer), a viral infection or other disorder associated with abnormal DGK a and / or DGK z signaling in a mammal, including a human, as described below.

[0044] According to a ninth aspect, the present application provides a method of treating or preventing a disease, preferably a condition with a dysregulated immune response (in particular cancer), a viral infection or other disorder associated with abnormal DGK a and / or DGK z signaling in a mammal, including a human, as described below, comprising:

[0045] a) administering a DGK a inhibitor A as described herein, or a tautomer, N-oxide, hydrate, solvate, or salt thereof, or a mixture of same, and

[0046] b) administering a DGK z inhibitor A' as described herein, or a stereoisomer, tautomer, N-oxide, hydrate, solvate, or salt thereof, or a mixture of same.

[0047] Technical problem

[0048] While treating cancer by stimulating immune cells against tumors has achieved remarkable clinical success

[0049] (e.g. by treatment with humanized antibodies against the PD-1 / PD-L1 axis in a fraction of the respective patient population), many patients' tumors have developed resistance to the treatment, while many other patients have not responded at all. Therefore, there is a need for further improving cancer therapy, including those acting by activating immune cells against the respective tumor. Furthermore, there is a need to provide solutions to prevent tumor recurrence, e.g. formation of metastases. As described above, there is a large body of evidence supporting that inhibition of some DGK isoforms, in particular DGK a and DGK z, can influence such stimulation, and efforts have been initiated to develop

[0050] Multiple clinical studies of DGKa, DGKz inhibitors and DGKa / z dual inhibitors. However, little is known about how to best balance the effects of inhibiting DGKa and DGKz, and "further study of DGKa and DGKz selective inhibitors is needed to disentangle the contributions of these DGK isozyme components to T cell signaling and tumor immunity" (Wichroski et al., Sci. Transl. Med. 15, eadh1892 (2023) 25 October 2023).

[0051] Problem solution

[0052] It is now surprisingly found in preclinical experiments that combination therapy with a DGKa inhibitor and a DGKz inhibitor provides a beneficial and surprising technical effect. In syngeneic murine tumor models (e.g. EMT6, MC38, Hepa 1-6) it was found that combination therapy with a DGKa inhibitor and a DGKz inhibitor resulted in a significant reduction of tumor growth, which clearly exceeded the additive of the effects produced by monotherapy with the respective DGKa inhibitor and the respective DGKz inhibitor. Furthermore, in the MC38 syngeneic murine tumor model, under combination therapy with a DGKa inhibitor and a DGKz inhibitor, an increase in survival was found that exceeded either monotherapy, and those surviving animals showed no substantial tumor growth upon re-challenge with inoculation of MC38 cells after recovery from the experiment described in Example 6.

[0053] Since any drug can reach a dose-limiting toxicity at some point after increasing the dose, it can be expected in a clinical setting that replacing some of the anti-tumor effect of a given dose of a DGKz inhibitor with combination therapy with a reduced dose of a DGKa inhibitor and a DGKz inhibitor will result in a reduction of DGKz inhibitor related toxicity while efficacy will at least remain unchanged, and vice versa, i.e. replacing some of the anti-tumor effect of a given dose of a DGKa inhibitor with combination therapy with a reduced dose of a DGKa inhibitor and a DGKz inhibitor will result in a reduction of DGKa inhibitor related toxicity while efficacy will at least remain unchanged.

[0054] A further benefit of combination therapy with a DGKa inhibitor and a DGKz inhibitor compared to therapy with one dual DGKa / z inhibitor includes the option to dose each independently flexibly and to allow for optimal treatment of individual patients in terms of the amount of each dose, and in terms of the sequence and timing of each dose, depending on the individual patient's response to the treatment, maximizing the beneficial effects of inhibiting either DGK isoform while minimizing potential undesired effects. DETAILED DESCRIPTION

[0055] Definitions

[0056] General definitions

[0057] Unless otherwise defined, all scientific and technical terms used in the specification, drawings, and claims are intended to have the general meanings that are commonly understood by one of ordinary skill in the art. All publications, patent applications, patents, and other references mentioned herein are incorporated by reference in their entirety. In case of conflict between the disclosure of the present specification (including the definitions) and the disclosure of such incorporated references, the present specification (including the definitions) shall control. If two or more documents incorporated by reference include conflicting and / or inconsistent disclosure, the document having the later effective date shall control. The materials, methods, and examples are illustrative only and not intended to be limiting. Unless otherwise indicated, the following terms used in the present document (including the specification and claims) have the definitions given below.

[0058] As used herein, the word “about” or “~” means a value within an acceptable error range for a particular value as determined by one of ordinary skill in the art, which will depend on how the value is measured or determined, i.e., the limitations of the measurement system. For example, “about” can mean within 1 or more than 1 standard deviation, per the practice in the art. The term “about” is also used to indicate that an amount, or a value, or a property that is close to a specified value or an approximate one. The phrase is intended to convey that similar values promote the same outcome or effect as described herein. In the context of a range, “about” can mean up to 10% higher and / or lower. Whenever the term “about” is specified for a certain measurement or implementation, that definition applies to the particular context.

[0059] The term “about” means + / - 10% of the value provided, if not otherwise defined.

[0060] The terms “comprising,” “including,” “containing,” “having,” and the like are to be construed open-ended, or as “including but not limited to,” unless otherwise noted. As used in the specification, the term “comprising” includes “consisting of.”

[0061] If any item referred to in this document is “as mentioned herein” or “as described herein,” it means that it can be mentioned anywhere in this document.

[0062] The singular forms “a,” “an,” and “the” include plural referents unless the context clearly dictates otherwise. Thus, for example, reference to “a monoclonal antibody” includes a single monoclonal antibody as well as a plurality of monoclonal antibodies, identical or different. Likewise, reference to “a cell” includes a single cell as well as a plurality of cells.

[0063] Unless specified otherwise, the term “at least” preceding a series of elements is to be understood to refer to every element in the series. The terms “at least one” and “at least one of’ include, for example, one, two, three, four, five or more elements.

[0064] It is also to be understood that slight variations of the ranges specified can be used to achieve essentially the same results as the values within the ranges. Furthermore, except where otherwise provided, the disclosure of ranges includes every value within the range.

[0065] The term "amino acid" or "amino acid residue" as used herein generally refers to naturally occurring amino acids. Single letter codes are used herein to refer to the corresponding amino acid. As used herein, "charged amino acids" are amino acids that are either negatively charged or positively charged. "Negatively charged amino acids" are aspartic acid (D) and glutamic acid (E). "Positively charged amino acids" are arginine (R), lysine (K), and histidine (H). "Polar amino acids" are all amino acids that form hydrogen bonds as donors or acceptors. They are all charged amino acids and asparagine (N), glutamine (Q), serine (S), threonine (T), tyrosine (Y), and cysteine (C).

[0066] "Polar uncharged amino acids" are asparagine (N), glutamine (Q), serine (S), threonine (T), tyrosine (Y), and cysteine (C). "Amphipathic amino acids" are tryptophan (W), tyrosine (Y), and methionine (M). "Aromatic amino acids" are phenylalanine (F), tyrosine (Y), and tryptophan (W). "Hydrophobic amino acids" are glycine (G), alanine (A), valine (V), leucine (L), isoleucine (I), proline (P), phenylalanine (F), methionine (M), and cysteine. "Small amino acids" are glycine (G), alanine (A), serine (S), proline (P), threonine (T), aspartic acid (D), and asparagine (N).

[0067] "Polar uncharged amino acids" are asparagine (N), glutamine (Q), serine (S), threonine (T), tyrosine (Y), and cysteine (C). "Amphipathic amino acids" are tryptophan (W), tyrosine (Y), and methionine (M). "Aromatic amino acids" are phenylalanine (F), tyrosine (Y), and tryptophan (W). "Hydrophobic amino acids" are glycine (G), alanine (A), valine (V), leucine (L), isoleucine (I), proline (P), phenylalanine (F), methionine (M), and cysteine. "Small amino acids" are glycine (G), alanine (A), serine (S), proline (P), threonine (T), aspartic acid (D), and asparagine (N).

[0068] The term "DGK", also known as DAGK, refers to the diacylglycerol kinase family, a family of enzymes that catalyze the conversion of diacylglycerol (DAG) to phosphatidic acid (PA). Members of this family use ATP as a source of phosphate. DGKs can be divided into five classes. The type 1 DGK group includes DGK-alpha, DGK-beta, and DGK-gamma, members of which include EF-hand motifs and recoverin homology domains. The type 2 DGK group includes DGK-delta and DGK-eta, members of which include plleckstrin homology domains. The type 3 DGK group includes DGK-epsilon, which has specificity for arachidonate-containing DAG. The type 4 DGK group includes DGK-zeta and DGK-ι, members of which include MARCKS homology domains, ankyrin repeats, a C-terminal nuclear localization signal, and a PDZ binding motif. The type 5 DGK group includes DGK-theta, which includes a third cysteine-rich domain, a plleckstrin homology domain, and a proline-rich region. A DGK inhibitor is an inhibitor of at least one or more members of the DGK family. For example, a DGK inhibitor can be an inhibitor of one or more of DGK-alpha, DGK-beta, DGK-gamma, DGK-delta, DGK-eta, DGK-epsilon, DGK-zeta, DGK-ι, and DGK-theta.

[0069] The term "DGK alpha", also known as DGK-alpha or DGK a, refers to the DGK family member diacylglycerol kinase alpha. The DGK alpha protein is encoded by the gene DGKA (also known as DAGK, DAGK1, NCBI Gene ID 1606). Synonyms for DGK alpha are, among others, DAG kinase alpha, 80 kDa diacylglycerol kinase, and diglyceride kinase alpha. The DGK alpha protein includes human, murine, rat, rhesus, and other mammalian and non-mammalian homologs. The sequence of human DGK alpha is available through

[0070] UniProt identifier P23743 (DGKA_HUMAN), for example isoform P23743-1 or P23743-2 or P23743-3 (UniProt, February 1, 2023). Different isoforms and variants can exist for different species, and are all encompassed by the term DGK alpha. In addition, synthetic variants of the DGK alpha protein can be generated and are encompassed by the term DGK alpha. The protein DGK alpha can also be subjected to various modifications, for example synthetic or naturally occurring modifications, such as post-translational modifications. A DGK alpha inhibitor is a compound or antibody that at least partially inhibits the functional activity of at least one isoform of DGK alpha.

[0071] The term "DGK alpha", also known as DGK-alpha or DGK a, refers to the DGK family member diacylglycerol kinase alpha. The DGK alpha protein is encoded by the gene DGKA (also known as DAGK, DAGK1, NCBI Gene ID 1606). Synonyms for DGK alpha are, among others, DAG kinase alpha, 80 kDa diacylglycerol kinase, and diglyceride kinase alpha. The DGK alpha protein includes human, murine, rat, rhesus, and other mammalian and non-mammalian homologs. The sequence of human DGK alpha is available through

[0072] The term "DGKzeta", also called DGK-zeta or DGKζ, refers to the DGK family member diacylglycerol kinase zeta. The DGKζ protein is encoded by the gene DGKZ (also called DAGK6, DAGK5, DGK-ZETA, hDGKζ, NCBI Gene ID 8525). Synonyms for DGKζ are, in particular, DAG kinase zeta and diglyceride kinase zeta. The DGKζ protein includes human, murine, rat, rhesus, as well as other mammalian and non-mammalian homologues. The sequence of human DGKζ is available under UniProt identifier Q13574 (DGKZ_HUMAN), e.g. the canonical human isoform Q13574-2

[0073] (UniProt, February 1, 2023). Different isoforms and variants exist for different species and are all encompassed by the term DGKζ. Furthermore, synthetic variants of the DGKζ protein can be generated and are encompassed by the term DGKζ. The protein DGKζ can also be subject to various modifications, e.g. synthetic or naturally occurring modifications, like post-translational modifications. A DGKζ inhibitor is a compound or antibody that at least partially inhibits the functional activity of at least one isoform of DGKζ.

[0074] An "isoform control" is an antibody or fragment that does not bind the target but is of the same class and type as the reference antibody or fragment that recognizes the target.

[0075] The "half maximal effective concentration" (EC50) refers to the concentration of a drug, antibody, fragment, conjugate or molecule that induces a half of the response between baseline and maximum after a specified incubation time. Thus, in the case of antibody binding, the EC50reflects the antibody concentration required for half maximal binding. The EC50can be determined if the inflection point can be determined by mathematical modeling, e.g. non-linear regression, of a dose-response curve that describes the relationship between the concentration of the applied drug, antibody, fragment, conjugate or molecule and the signal. For example, the EC50can be determined if the dose-response curve follows a sigmoidal curve. When the response is inhibition, the EC50is called half maximal inhibitory concentration (IC50). The EC80can be determined by making the necessary adjustments or accommodations.

[0076] The term "linker" or "spacer" as used herein refers to any molecule that is capable of making a direct topological connection between two moieties. The moieties can be, in particular, polypeptides, proteins, antibodies, antibody fragments, cytotoxic moieties, binding moieties, moieties for detection, like fluorophores, moieties for immobilization or recovery, like beads or magnetic beads, reactive moieties or any other molecule. The two moieties can be of the same type or of different types. The linker can be part of a conjugate and can even contribute to their functionality. For example, for a conjugate comprising a polypeptide and biotin, there is a distance of about 1.5 A between the carboxyl group of biotin and the first bulky amino acid of the peptide. The spacer region of (~5 atoms) allows the biotin to reach the (streptavidin) avidin binding pocket. Various linkers are known in the art and can be selected based on the moieties to be connected. Linker lengths typically range between 4 atoms and more than 200 atoms. Linkers with a length of more than 60 atoms typically comprise a population of compounds with an average length.

[0077] In the context of the present application, the term "treatment" or "treating" includes inhibiting, retarding, arresting, ameliorating, attenuating, limiting, reducing, suppressing, fighting or curing the development, progression or advancement of a disease or such state and / or symptoms of such state. The term "disease" includes, but is not limited to, a condition, disorder, injury or health problem. The term "therapy" is herein understood to be synonymous with the term "treatment".

[0078] The terms "prevent", "preventing" or "prevention" are used synonymously in the context of the present application and refer to avoiding or reducing the risk of developing or progressing of an infection, experiencing, having or having symptoms of a disease or such state.

[0079] The treatment or prevention of a disease can be partial or total.

[0080] The terms "effective amount" or "therapeutically effective amount" are used interchangeably herein and refer to an amount that is sufficient to achieve a particular biological result or to modulate or improve the symptoms or the time of onset of symptoms in a subject, typically by at least about 10%; typically by at least about 20%, preferably by at least about 30%, or more preferably by at least about 50%. The efficacy of an antibody used in the treatment of cancer can be assessed based on changes in tumor burden. Both tumor shrinkage (objective remission) and time to disease progression are important endpoints in cancer clinical trials. A standardized response criteria, called RECIST (Response Evaluation Criteria in Solid Tumors), was published in 2000. An updated version (RECIST 1.1) was released in 2009. The RECIST criteria are commonly used in clinical trials with objective remission as the primary study endpoint, as well as in trials where disease stabilization assessment, tumor progression or time to progression analysis is performed, as these outcome measures are based on the assessment of anatomic tumor burden and its changes over the course of the trial. The effective amount for a particular subject can vary according to factors such as the condition being treated, the overall health status of the subject, the method, route and dose of administration and the severity of side effects, among others. When co-administered, the effective amount is proportionate to the combination of the components and the effect is not limited to the individual components alone. Whenever an antibody is administered as part of a medical use, it is clear to the skilled person that the antibody needs to be administered in an effective amount.

[0081] If not defined otherwise, a "complete response" (CR) is defined as the disappearance of all target lesions. The short axis of any pathological lymph node (whether target or non-target) must be reduced to <10 mm. For a "partial response" (PR), the sum of the diameters of the target lesions must be reduced by at least 30%, with the baseline sum of diameters as a reference. For "progressive disease" (PD), the sum of the diameters of the target lesions must increase by at least 20%, with the minimum sum on study as a reference (including the baseline sum if it is the minimum on study). In addition to the 20% relative increase, the sum must also demonstrate an absolute increase of at least 5 mm. In "stable disease" (SD), neither a shrinkage sufficient to qualify as a PR nor an increase sufficient to qualify as a PD is observed, with the minimum sum of diameters during the study as a reference.

[0082] Secondary outcome measures that can be used to determine the therapeutic benefit of the antibodies of the invention described herein include the following: "Objective response rate" (ORR) is defined as achieving complete remission (CR) or partial remission (PR)

[0083] The proportion of subjects who achieved a PR. "Progression-free survival" (PFS) was defined as the time from the first dose of the antibody to disease progression or death, whichever occurred first. "Overall survival"

[0084] (OS) is defined as the length of time a patient diagnosed with the disease remains alive from the date of diagnosis or the start of treatment for the disease. "Overall duration of response" (DOR) is defined as the time from the subject's initial CR or PR to disease progression. "Depth of response" (DpR) is defined as the percentage of tumor shrinkage observed at the point of maximum response compared to baseline tumor burden. The clinical endpoints of ORR and PFS can be determined according to the above-mentioned RECIST 1.1 criteria.

[0085] The parameters described above for determining efficacy and benefit must be adjusted when analyzing non-human subjects.

[0086] As used herein, the terms "patient" or "subject" are used interchangeably and refer to a mammal, including but not limited to a human or a non-human mammal, such as a cow, horse, dog, sheep or cat. Preferably, the patient is a human.

[0087] As used herein, a "lesion" refers to an area of ​​abnormal tissue. A lesion can be benign or malignant (a "cancerous lesion," also called a "tumor lesion").

[0088] In the context of cells, structures, proteins, antibodies or markers, the term “intratumoral

[0089] "intra-tumoral," "tumor-infiltrating," or "neoplastic" refer to their localization within tumor tissue.

[0090] A cell that is "positive" or "+" for a certain marker or protein is a cell that is characterized by substantial expression of that marker or protein. Marker or protein expression can be determined and quantified as known in the art, for example to define different cell populations. For characterizing (immune) cell populations, marker expression can be determined by FACS or using any other technique described herein.

[0091] A "leukocyte" is an immune cell that expresses CD45.

[0092] As used herein, "CD45+ cells" refer to all leukocytes. CD45 can serve as a marker to distinguish immune cells from non-immune cells.

[0093] The term "lymphocyte" refers to all immature, mature, undifferentiated, and differentiated populations of white lymphocytes, including tissue-specific and specialized classes. It includes, by way of non-limiting example, B cells, T cells, NKT cells, and NK cells. In some embodiments, lymphocytes include all B cell lineages, including pro-B cells, progenitor B cells, early progenitor B cells, late progenitor B cells, large pro-B cells, small pro-B cells, immature B cells, mature B cells, plasma B cells, memory B cells, B-1 cells, B-2 cells, and anergic AN1 / T3 cell populations.

[0094] A "T cell" is an immune cell that expresses TCR alpha beta, CD3, and CD8 or CD4. As used herein, the term includes naive T cells, CD4+ T cells, CD8+ T cells, regulatory T cells, memory T cells, activated T cells, anergic T cells, tolerant T cells, chimeric B cells, and antigen-specific T cells, as well as other T cell populations known in the art. In some embodiments, the presence of a T cell receptor (TCR) on the cell surface distinguishes T cells from other lymphocytes.

[0095] A "CD8+ T cell" (also known as a "cytotoxic T cell," "TC," "cytotoxic T lymphocyte," "CTL," "T killer cell," "cytolytic T cell," "CD8+ T cell," or "killer T cell") is a T cell that expresses CD3, CD45, and CD8. CD8+ T cells can kill cancer cells, infected (particularly, virally infected) cells, or other damaged cells.

[0096] A "CD4+ T cell" (also known as a "T helper cell," "Th cell") is an immune cell that expresses CD3, CD4, and CD45. There are several subpopulations of helper T cells, such as, but not limited to

[0097] Th1, Th2, and Th17. CD4+ T cells help suppress or regulate immune responses. They are required in B cell antibody class switching, activation and growth of cytotoxic T cells, and maximizing the bactericidal activity of phagocytes such as macrophages.

[0098] “NK cells” (also known as natural killer cells) are immune cells that express CD45, CD16, CD56, NKG2D, but are CD3 negative. NK cells can kill cells lacking MHC class I without activation.

[0099] MHC class I “self”-labeled cells. NCR1 (also known as CD335 or NKp46) is expressed on NK cells and a subset of NKT cells.

[0100] Natural killer T (NKT) cells are a heterogeneous group of T cells with properties of both T cells and natural killer cells.

[0101] “iNKT cells” (also known as “invariant natural killer T cells”) express an invariant alpha beta TCR (Valpha24-Jalpha18, CD24lo), CD44hi, NK1.1 (mouse), and NKG2D. The invariant TCR recognizes glycolipid antigens presented by the non-polymorphic MHC class I molecule CD1d. These cells can influence immune responses by rapidly producing large amounts of cytokines (i.e., IFNy).

[0102] As known in the art, “effector cells” are immune cells that actively support an immune response upon stimulation. As used herein, effector cells refer to immune cells that express Fcy receptors and are thus capable of mediating ADCC or ADCP. Non-limiting examples of effector cells are monocytes, neutrophils, mast cells, and preferably macrophages and natural killer cells.

[0103] As used herein, the term “chimeric antigen receptor” or “CAR” refers to an artificial T cell surface receptor engineered to be expressed on an immune effector cell and specifically bind to an antigen. CARs can be used as a therapy with adoptive cell transfer. Mononuclear cells are taken from a patient (blood, tumor, or ascites) and modified to express a receptor specific for a particular form of an antigen. In some embodiments, the CAR has been expressed to be specific for a tumor-associated antigen. CARs can also comprise an intracellular activation domain, a transmembrane domain, and an extracellular domain comprising a tumor-associated antigen binding region. In certain aspects, the CAR comprises a fusion of a single-chain variable region fragment (scFv) derived from a monoclonal antibody fused to a CD3-zeta transmembrane and intracellular domain. The specificity of the CAR design can be derived from the ligand of the receptor (e.g., a peptide). In some embodiments, the CAR can target cancer by redirecting mononuclear cells / macrophages expressing a CAR specific for a tumor-associated antigen.

[0104] If not otherwise stated, dosing schedules are abbreviated as known in the art, e.g. daily

[0105] (QD), every 2 days (Q2D) or every 3 days (Q3D). In this context, “QW” means once a week, “Q2W” means once every two weeks, “Q3W” means once every three weeks,

[0106] “Q4W” means once every four weeks, “Q5W” means once every five weeks, “Q6W” means once every six weeks. “BIW” means once every two weeks, “BIW x 4” means once every two weeks for a total of 4 doses, i.e. 4 doses within two weeks.

[0107] The dose ratio referred to as “dose ratio (mg or mg / kg of DGK alpha inhibitor A: mg or mg / kg of DGK zeta inhibitor A’)” relates to the ratio of mg of DGK alpha inhibitor A: mg of DGK zeta inhibitor A’, or to the ratio of mg / kg of DGK alpha inhibitor A: mg / kg of DGK zeta inhibitor A’.

[0108] A “dosing cycle” or “treatment cycle” is a treatment period followed by a rest period (no treatment), which is repeated on a regular schedule. When this cycle is repeated a number of times on a regular schedule, it constitutes a course of treatment.

[0109] An intravenous line or “IV line” is a tube or cannula that can be used for intravenous infusion.

[0110] Definition of the DGK inhibitors of formula (I)

[0111] The terms mentioned herein in the context of the DGK inhibitors of formula (I) have the following meanings:

[0112] The term “substituted” means that one or more hydrogen atoms on the designated atom or group is replaced with the designated group, provided that the normal valency of the designated atom is not exceeded. Combinations of substituents and / or variables are permissible.

[0113] The term “optionally substituted” means that the number of substituents can or can not equal zero. Unless otherwise indicated, an optionally substituted group can be substituted with as many optional substituents as available carbon or nitrogen atoms can accommodate by replacing a hydrogen atom with a non-hydrogen substituent. Typically, the number of optional substituents, when present, can be 1, 2, 3, or 4, especially 1, 2, or 3.

[0114] When a group in a compound according to the application is substituted, the group can be mono- or poly-substituted with substituents, unless indicated otherwise. Within the scope of the application, the meaning of all groups recurring is independent of each other. A group in a compound according to the application can be substituted with one, two or three identical or different substituents, in particular with one substituent.

[0115] As used herein, an oxo substituent denotes an oxygen atom which is bound to a carbon atom or a sulfur atom by a double bond.

[0116] A complex substituent shall consist of more than one moiety, for example (Ci-C2-alkoxy)-(Ci-C6-alkyl)-, the given moieties can be attached at any suitable position of said complex substituent, for example the Ci-C2-alkoxy moiety can be attached to any suitable carbon atom of the Ci-C6-alkyl moiety of said (Ci-C2-alkoxy)-(Ci-C6-alkyl)- group. The hyphen at the beginning or end of such a complex substituent indicates the point of attachment of said complex substituent to the rest of the molecule. A ring comprising carbon atoms and optionally one or more heteroatoms, for example a nitrogen, oxygen or sulfur atom, is substituted with a substituent, then said substituent can be bound at any suitable position of said ring, which can be bound to a suitable carbon atom and / or to a suitable heteroatom.

[0117] The term “comprising” when used in the specification, includes “consisting of”. If any item is referred to herein as being “as described herein”, then it is by reference to the description of it in any of the foregoing embodiments, which are all incorporated herein by reference.

[0118] The terms mentioned herein have the following meanings:

[0119] The term “halogen atom” means a fluorine, chlorine, bromine or iodine atom, in particular a fluorine, chlorine or bromine atom.

[0120] The term “Ci-C6-alkyl” means a straight-chain or branched saturated monovalent hydrocarbon group having 1, 2, 3, 4, 5 or 6 carbon atoms, for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, tert-butyl, pentyl, isopentyl, 2-methylbutyl, 1 -methylbutyl, 1 -ethylpropyl, 1,2-dimethylpropyl, neopentyl, 1,1 -dimethylpropyl, hexyl, 1 -methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1 -ethylbutyl, 2-ethylbutyl, 1,1 -dimethylbutyl, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 2,3-dimethylbutyl, 1,2-dimethylbutyl or 1,3-dimethylbutyl or an isomer thereof. In particular, the group has 1, 2, 3, 4 or 5 carbon atoms

[0121] ("C1-C5-alkyl"), for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, tert-butyl, pentyl, isopentyl, 2-methylbutyl, 1-methylbutyl, 1-ethylpropyl, 1,2-dimethylpropyl, neopentyl, 1,1-dimethylpropyl. More particularly, the radicals have 1, 2, 3 or 4 carbon atoms ("C1-C4-alkyl"), for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl or tert-butyl, more particularly 1, 2 or 3 carbon atoms ("C1-C3-alkyl"), for example methyl, ethyl, n-propyl or isopropyl, more particularly 1 or 2 carbon atoms ("C1-C2-alkyl"), for example methyl or ethyl.

[0122] The term "C2-C4-alkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group having 2, 3 or 4 carbon atoms, for example ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl or tert-butyl.

[0123] The term "C1-C6-hydroxyalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group, wherein the term "C1-C6-alkyl" has been defined above, and wherein 1 or 2 hydrogen atoms are replaced by a hydroxyl group, for example hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxyprop-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl, 1-hydroxy-2-methyl-propyl, 1-hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl, 4-hydroxybutyl, 1-hydroxypentyl, 2-hydroxypentyl, 3-hydroxypentyl, 4-hydroxypentyl, 5-hydroxypentyl, 1-hydroxyhexyl, 2-hydroxyhexyl, 3-hydroxyhexyl, 4-hydroxyhexyl, 5-hydroxyhexyl, 6-hydroxyhexyl or an isomer thereof. Particularly, the radicals have 1, 2, 3 or 4 carbon atoms

[0124] ("C1-C4-hydroxyalkyl"), for example hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxyprop-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl, 1-hydroxy-2-methyl-propyl, 1-hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl, 4-hydroxybutyl or an isomer thereof.

[0125] The term "C2-C4-hydroxyalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group having 2, 3 or 4 carbon atoms, wherein the term "C2-C4-alkyl" has been defined above, and wherein one or two hydrogen atoms are replaced by a hydroxyl group, for example 1 -hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1 -hydroxypropyl, 1 -hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxyprop-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl, 1 -hydroxy-2-methyl-propyl, 1 -hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl or 4-hydroxybutyl or an isomer thereof.

[0126] The term "C1-C6-haloalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group, wherein the term "C1-C6-alkyl" is as defined above, and wherein one or more hydrogen atoms are replaced by the same or different halogen atom. In particular, the halogen atom is a fluorine atom. The C1-C6-haloalkyl is for example fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl, 1,3-difluoroprop-2-yl, 4,4,4-trifluorobutyl, 5,5,5-trifluoropentyl or 6,6,6-trifluorohexyl. In particular, the group has 1, 2, 3 or 4 carbon atoms ("C1-C4-haloalkyl"), for example fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl, 1,3-difluoroprop-2-yl or 4,4,4-trifluorobutyl.

[0127] The term "C1-C6-alkoxy" refers to a straight-chain or branched saturated monovalent group of formula (C1-C6-alkyl)-O-, wherein the term "C1-C6-alkyl" is as defined above, for example methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, s-butoxy, i-butoxy, t-butoxy, pentoxy, iso-pentoxy or n-hexoxy or an isomer thereof. In particular, the group has 1, 2, 3 or 4 carbon atoms ("C1-C4-alkoxy"), for example methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, s-butoxy, i-butoxy or t-butoxy.

[0128] The term "C1-C6-haloalkoxy" refers to a straight-chain or branched saturated monovalent C1-C6-alkoxy group as defined above, wherein one or more hydrogen atoms are replaced by the same or different halogen atom. In particular, the halogen atom is a fluorine atom. The C1-C6-haloalkoxy is for example fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy.

[0129] The term "C2-C6-alkenyl" refers to a straight-chain or branched single bond monohydrocarbon group containing one or two double bonds and having 2, 3, 4, 5, or 6 carbon atoms, it being understood that in the case where the alkenyl group contains two double bonds, the double bonds can be mutually conjugated or form a cumulated diene. The alkenyl group is, for example, ethenyl (or "vinyl"), prop-2-en-1-yl (or "allyl"), prop-1-en-1-yl, but-3-enyl, but-2-enyl, but-1-enyl, pent-4-enyl, pent-3-enyl, pent-2-enyl, pent-1-enyl, hex-5-enyl, hex-4-enyl, hex-3-enyl, hex-2-enyl, hex-1-enyl, prop-1-en-2-yl (or "isopropenyl"), 2-methylprop-2-enyl, 1-methylprop-2-enyl, 2-methylprop-1-enyl, 1-methylprop-1-enyl, 3-methylbut-3-enyl, 2-methylbut-3-enyl, 1-methylbut-3-enyl, 3-methylbut-2-enyl, 2-methylbut-2-enyl, 1-methylbut-2-enyl, 3-methylbut-1-enyl, 2-methylbut-1-enyl, 4-methylpent-4-enyl, 3-methylpent-4-enyl, 1-methylpent-4-enyl, 1-methylpent-4-enyl, 1-methylbut-1-enyl, 1,1-dimethylprop-2-enyl, 1-ethylprop-1-enyl, 1-propylvinyl, 1-isopropylvinyl, 4-methylpent-4-enyl, 3-methylpent-4-enyl, 2-methylpent-4-enyl, 4-methylpent-3-enyl, 3-methylpent-3-enyl, 2-methylpent-3-enyl, 1-methylpent-3-enyl, 4-methylpent-2-enyl, 3-methylpent-2-enyl, 2-methylpent-2-enyl, 1-methylpent-2-enyl, 4-methylpent-1-enyl, 3-methylpent-1-enyl, 2-methylpent-1-enyl, 1-methylpent-1-enyl, 3-ethylbut-3-enyl, 2-ethylbut-3-enyl, 1-ethylbut-3-enyl, 3-ethyl-but-2-enyl, 2-ethylbut-2-enyl, 1-ethylbut-2-enyl, 3-ethylbut-1-enyl, 2-ethylbut-1-enyl, 1-ethylbut-1-enyl, 2-propylprop-2-enyl, 1-propylprop-2-enyl, 2-isopropylprop-2-enyl, 1-isopropylprop-2-enyl, 2-isopropylprop-1-enyl, 1-propylprop-1-enyl, 2-isopropylprop-1-enyl, 1-isopropylprop-1-enyl, 3,3-dimethylprop-1-enyl, 1-(1,1-dimethylethyl)vinyl, but-1,3-dienyl, pent-1,4-dienyl, or hex-1,5-dienyl group.

[0130] The term "C2-C6-alkynyl" refers to linear or branched monovalent hydrocarbon groups containing one triple bond and 2, 3, 4, 5, or 6 carbon atoms, in particular 2, 3, or 4 carbon atoms ("C2-C4-alkynyl"). Said C2-C6-alkynyl group is, for example, ethynyl, prop-1 -ynyl, prop-2-ynyl (or "propargyl"), but-1 -ynyl, but-2-ynyl, but-3-ynyl, pent-1 -ynyl, pent-2-ynyl, pent-3-ynyl, pent-4-ynyl, hex-1 -ynyl, hex-2-ynyl, hex-3-ynyl, hex-4-ynyl, hex-5-ynyl, 1 -methylprop-2-ynyl, 2-methylbut-3-ynyl, 1 -methylbut-3-ynyl, 1 -methylbut-2-ynyl, 3-methylbut-1 -ynyl, 1 -ethylprop-2-ynyl, 3-methylpent-4-ynyl, 2-methylpent-4-ynyl, 1 -methylpent-4-ynyl, 2-methylpent-3-ynyl, 1 -methylpent-3-ynyl, 4-methylpent-2-ynyl, 1 -methylpent-2-ynyl, 4-methylpent-1 -ynyl, 3-methylpent-1 -ynyl, 2-ethylbut-3-ynyl, 1 -ethylbut-3-ynyl, 1 -ethylbut-2-ynyl, 1 -propylprop-2-ynyl, 1 -isopropylprop-2-ynyl, 2,2-dimethylbut-3-ynyl, 1,1 -dimethylbut-3-ynyl, 1,1 -dimethylbut-2-ynyl or 3,3-dimethylbut-1 -ynyl group.

[0131] The term "C3-C6-cycloalkyl" refers to saturated monovalent monocyclic hydrocarbon rings containing 3, 4, 5, or 6 carbon atoms. Said C3-C6-cycloalkyl is, for example, a cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl group. In particular, said group has 3, 4, or 5 carbon atoms ("C3-C5-cycloalkyl"), such as a cyclopropyl, cyclobutyl, or cyclopentyl group. In particular, said group has 3 or 4 carbon atoms ("C3-C4-cycloalkyl"), such as a cyclopropyl or cyclobutyl group.

[0132] The term "C4-C6-cycloalkenyl" refers to monocyclic hydrocarbon rings containing 4, 5, or 6 carbon atoms and one double bond. In particular, said ring contains 5 or 6 carbon atoms ("C5-C6-cycloalkenyl"). Said C4-C6-cycloalkenyl is, for example, a monocyclic hydrocarbon ring, such as a cyclobutenyl, cyclopentenyl, cyclohexenyl, or cycloheptenyl group.

[0133] The term "C3-C6-cycloalkoxy" refers to saturated monovalent groups of the formula (C3-C6-cycloalkyl)-O-, wherein the term "C3-C6-cycloalkyl" is as defined above, for example a cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, or cyclohexyloxy group.

[0134] The term "4- to 7-membered heterocycloalkyl" refers to a monocyclic, saturated heterocyclic ring containing 4, 5, 6 or 7 ring atoms in total, comprising one or two identical or different ring heteroatoms from the series N, O and S.

[0135] The heterocycloalkyl group can be a 4-membered ring, such as azetidinyl, oxetanyl or thietanyl; or a 5-membered ring, such as tetrahydrofuranyl, 1,3-dioxolanyl, thiolanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,1-dioxothiolanyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl or 1,3-thiazolidinyl; or a 6-membered ring, such as tetrahydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl, 1,3-dioxanyl, 1,4-dioxanyl or 1,2-oxazinyl, or a 7-membered ring, such as, for example, azepanyl, 1,4-diazepanyl or 1,4-oxazepanyl, but is not limited thereto.

[0136] The term "5- to 7-membered heterocycloalkenyl" refers to a monocyclic, unsaturated, non-aromatic heterocyclic ring having 5, 6 or 7 ring atoms in total, comprising one or two double bonds and one or two identical or different ring heteroatoms from the series N, O and S.

[0137] The heterocycloalkenyl group is, for example, 4H-pyranyl, 2H-pyranyl, 2,5-dihydro-1H-pyrrolyl, [1,3]dioxolane, 4H-[1,3,4]thiadiazolyl, 2,5-dihydrofuranyl, 2,3-dihydrofuranyl, 2,5-dihydrothiophenyl, 2,3-dihydrothiophenyl, 4,5-dihydrooxazolyl or 4H-[1,4]thiazinyl.

[0138] The term "(4- to 7-membered heterocycloalkyl)oxy" refers to a monocyclic, saturated heterocycloalkyl group of the formula (4- to 7-membered heterocycloalkyl)-O-, wherein the term "4- to 7-membered heterocycloalkyl" is as defined above.

[0139] The term "nitrogen-containing 4- to 7-membered heterocycloalkyl" refers to a monocyclic, saturated heterocyclic ring having 4, 5, 6 or 7 ring atoms in total, comprising one ring nitrogen atom and optionally one further ring heteroatom from the series N, O and S.

[0140] The nitrogen-containing 4- to 7-membered heterocycloalkyl group can be, for example, a 4-membered ring, such as azetidinyl; or a 5-membered ring, such as pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl or 1,3-thiazolidinyl; or a 6-membered ring, such as piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl or 1,2-oxazinyl, or a 7-membered ring, such as azepanyl, 1,4-diazepanyl or 1,4-oxazepanyl, but is not limited thereto.

[0141] The term "heteroaryl" refers to a monovalent, monocyclic or bicyclic aromatic ring ("5- to 10-membered heteroaryl" group) having 5, 6, 8, 9, or 10 ring atoms, which includes at least one ring heteroatom and optionally one, two, or three additional ring heteroatoms from the series N, O, and / or S, and which is bound via a ring carbon atom.

[0142] The heteroaryl group can be a 5-membered heteroaryl group, such as thienyl, furanyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, or tetrazolyl; or a 6-membered heteroaryl group, such as pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, or triazinyl; or a 9-membered heteroaryl group, such as benzofuranyl, benzothienyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzothiazolyl, benzotriazolyl, thiazolopyridinyl, indazolyl, indolyl, isoindolyl, indolizinyl, or purinyl; or a 10-membered heteroaryl group, such as quinolinyl, quinazolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, or pteridinyl.

[0143] Generally, unless otherwise stated, the heteroaryl or heteroarylene groups include all possible isomeric forms thereof, such as: tautomers and position isomers with respect to the point of attachment of the remainder of the molecule. Thus, for some illustrative, non-limiting examples, the term pyridyl includes pyrid-2-yl, pyrid-3-yl, and pyrid-4-yl; or the term thienyl includes thien-2-yl and thien-3-yl.

[0144] The term "C1-C6", as used herein, e.g. in the definition of "C1-C6-alkyl", "C1-C6-haloalkyl", "C1-C6-hydroxyalkyl", "C1-C6-alkoxy" or "C1-C6-haloalkoxy", refers to an alkyl group having a finite number of carbon atoms of 1 to 6, i.e. 1, 2, 3, 4, 5 or 6 carbon atoms.

[0145] Furthermore, as used herein, the term "C3-C8", as used herein, e.g. in the definition of "C3-C6-cycloalkyl" in the context of the present application, refers to a cycloalkyl group having a finite number of carbon atoms of 3 to 6, i.e. 3, 4, 5 or 6 carbon atoms.

[0146] When a range of values is given, the range includes every value and sub-range within the range.

[0147] For example:

[0148] "C1-C6" includes C1, C2, C3, C4, C5, C6, C1-C6, C1-C5, C1-C4, C1-C3, C1-C2, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5 and C5-C6;

[0149] "C2-C6" includes C2, C3, C4, C5, C6, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5, and C5-C6;

[0150] "C3-C6" includes C3, C4, C5, C6, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5, and C5-C6;

[0151] As used herein, the term "leaving group" refers to an atom or group of atoms which is displaced as a stable species in a chemical reaction, which carries a bonding electron. In particular, such leaving group is selected from the group consisting of halogen, in particular fluorine, chlorine, bromine or iodine, (methylsulfonyl)oxy, [(trifluoromethyl)sulfonyl]oxy, [(nonafluorobutyl)sulfonyl]oxy, (phenylsulfonyl)oxy, [(4-methylphenyl)sulfonyl]oxy, [(4-bromophenyl)sulfonyl]oxy, [(4-nitrophenyl)sulfonyl]oxy, [(2-nitrophenyl)sulfonyl]oxy, [(4-isopropylphenyl)sulfonyl]oxy, [(2,4,6-triisopropylphenyl)sulfonyl]oxy, [(2,4,6-trimethylphenyl)sulfonyl]oxy, [(4-tert-butylphenyl)sulfonyl]oxy, and [(4-methoxyphenyl)sulfonyl]oxy.

[0152] [(2,4,6-trimethylphenyl)sulfonyl]oxy, [(4-tert-butylphenyl)sulfonyl]oxy, and [(4-methoxyphenyl)sulfonyl]oxy.

[0153] Definition of DGK inhibitors of formula (II)

[0154] The terms mentioned herein in the context of DGK inhibitors of formula (II) have the following meanings:

[0155] The term "substituted" means that one or more hydrogen atoms on the designated atom or group is replaced with a designated group, provided that the atom's normal valency is not exceeded. Combinations of substituents and / or variables are permissible.

[0156] The term "optionally substituted" means that the number of substituents can or can not equal zero. Unless otherwise indicated, an optionally substituted group can be substituted with as many optional substituents as available, which can be accommodated by replacing a hydrogen atom with a non-hydrogen substituent on any available carbon or nitrogen atom. Typically, the number of optional substituents, when present, can be 1, 2, 3, or 4, particularly 1, 2, or 3.

[0157] When a group in a compound according to the application is substituted, the group can be mono- or poly-substituted with substituents, unless indicated otherwise. Within the scope of the application, the meaning of all groups recurring is independent of each other. The groups in the compounds according to the application can be substituted with one, two or three identical or different substituents, in particular with one substituent.

[0158] As used herein, an oxo substituent denotes an oxygen atom which is bound to a carbon atom or a sulfur atom by a double bond.

[0159] A complex substituent shall consist of more than one moiety, for example (Ci-C2-alkoxy)-(Ci-C6-alkyl)-, the given moiety can be attached at any suitable position of said complex substituent, for example the Ci-C2-alkoxy moiety can be attached to any suitable carbon atom of the Ci-C6-alkyl moiety of said (Ci-C2-alkoxy)-(Ci-C6-alkyl)- group. The hyphen at the beginning or end of such a complex substituent indicates the point of attachment of said complex substituent to the rest of the molecule. A ring comprising carbon atoms and optionally one or more heteroatoms, for example nitrogen, oxygen or sulfur atoms, is substituted with a substituent, then said substituent can be bound at any suitable position of said ring, which can be bound to a suitable carbon atom and / or to a suitable heteroatom.

[0160] The term "comprising" when used in the specification, includes "consisting of". If any item is referred to as being "as herein described", this is meant to refer to that item as described at any place in this text.

[0161] The terms mentioned herein have the following meanings:

[0162] The term "halogen atom" means a fluorine, chlorine, bromine or iodine atom, in particular a fluorine, chlorine or bromine atom.

[0163] The term "C1-C6-hydroxyalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group, wherein the term "C1-C6-alkyl" has been defined above, and wherein one or two hydrogen atoms are replaced by a hydroxyl group, for example hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxyprop-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl, 1-hydroxy-2-methyl-propyl, 1-hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl or 4-hydroxybutyl or an isomer thereof.

[0164] The term "C1-C4-hydroxyalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group, wherein the term "C1-C4-alkyl" has been defined above, and wherein one or two hydrogen atoms are replaced by a hydroxyl group, for example hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxyprop-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl, 1-hydroxy-2-methyl-propyl, 1-hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl or 4-hydroxybutyl or an isomer thereof.

[0165] The term "C1-C6-haloalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group, wherein the term "C1-C6-alkyl" is defined above, and wherein one or more hydrogen atoms are replaced by identical or different halogen atoms. In particular, the halogen atoms are fluorine atoms. The C1-C6-haloalkyl is for example fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoroprop-2-yl.

[0166] The term "C1-C6-hydroxyalkyl" refers to a straight-chain or branched saturated monovalent hydrocarbon group, wherein the term "C1-C6-alkyl" has been defined above, and wherein one or two hydrogen atoms are replaced by a hydroxyl group, for example hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxyprop-2-yl, 2-hydroxyprop-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxyprop-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl, 1-hydroxy-2-methyl-propyl, 1-hydroxybutyl, 2-hydroxybutyl, 3-hydroxybutyl or 4-hydroxybutyl or an isomer thereof.

[0167] The term "C1-C6-haloalkyl" refers to a straight-chained or branched saturated monovalent hydrocarbon group as defined above, wherein one or more hydrogen atoms are replaced with the same or different halogen atom. In particular, the halogen atom is a fluorine atom. The C1-C6-haloalkyl group is, for example, fluoromethyl, difluoromethyl, trifluoromethyl, 2,2,2-trifluoroethyl, or pentafluoroethyl.

[0168] The term "C3-C4-alkenyl" refers to a straight-chained or branched monovalent hydrocarbon group containing one or two double bonds and having 3 or 4 carbon atoms. The alkenyl group is, for example, prop-2-en-1-yl (or "allyl"), prop-1-en-1-yl, but-3-enyl, but-2-enyl, or but-1-enyl.

[0169] The term "C3-C4-alkynyl" refers to a straight-chained or branched monovalent hydrocarbon group containing one triple bond and having 3 or 4 carbon atoms. The C3-C4-alkynyl group is, for example, prop-1-ynyl, prop-2-ynyl (or "propargyl"), but-1-ynyl, but-2-ynyl, or but-3-ynyl.

[0170] The term "C3-C7-cycloalkyl" refers to a saturated monovalent monocyclic hydrocarbon ring ("C3-C7-cycloalkyl") containing 3, 4, 5, 6, or 7 carbon ring atoms. The C3-C7-cycloalkyl group is, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl group.

[0171] The term "bicyclic C6-C 11 -cycloalkyl" refers to a spirocycloalkyl group, a fused C6-C 10 -cycloalkyl, or a bridged C7-C 10 -cycloalkyl group as defined below:

[0172] The term "spirocycloalkyl" refers to a bicyclic saturated monovalent C5-C 11 hydrocarbon group, wherein two rings share one common ring carbon atom, and wherein the bicyclic hydrocarbon group contains 5, 6, 7, 8, 9, 10, or 11 carbon atoms, the spirocycloalkyl group can be attached to the rest of the molecule through any one of the carbon atoms except the spiro carbon atom. The spirocycloalkyl group is, for example, spiro[2.6]nonanyl, spiro[3.3]heptanyl, spiro[3.4]octanyl, spiro[3.5]nonanyl, spiro[3.6]decanyl, spiro[4.4]nonanyl, spiro[4.5]decanyl, spiro[4.6]undecanyl, or spiro[5.5]undecanyl.

[0173] The term "fused C6-C 10 -cycloalkyl" refers to a bicyclic saturated monovalent hydrocarbon group, wherein two rings share two adjacent ring atoms, for example bicyclo[4.2.0]octanyl, octahydropentalenyl, or decahydronaphthyl.

[0174] The term "bridged C7-C 10 "-Cycloalkyl" refers to a bicyclic saturated monovalent hydrocarbon radical in which the two rings share two non-adjacent ring atoms in common, for example, bicyclo[2.2.1]heptyl (also known as norbornyl).

[0175] The term "bicyclic C5-C 11 -cycloalkyl" refers to a spirocycloalkyl group, a fused C5-C 10 -cycloalkyl or bridged C5-C 10 -Cycloalkyl group:

[0176] The term "spiroalkyl" refers to a bicyclic saturated monovalent C5-C 11 Hydrocarbyl groups, wherein two rings share a common ring carbon atom, and wherein the bicyclic hydrocarbon group contains 5,6,7,8,9,10 or 11 carbon atoms, and the spiroalkyl group can be connected to the rest of the molecule by any one carbon atom except the spiral carbon atom. The spiroalkyl group is for example spiral [2.6] nonyl, spiral [3.3] heptyl, spiral [3.4] octyl, spiral [3.5] nonyl, spiral [3.6] decyl, spiral [4.4] nonyl, spiral [4.5] decyl, spiral [4.6] undecyl or spiral [5.5] undecyl.

[0177] The term "fused C5-C 10 "-Cycloalkyl" refers to a bicyclic saturated monovalent hydrocarbon radical in which the two rings share two adjacent ring atoms, for example, bicyclo[4.2.0]octyl, octahydropentalenyl or decahydronaphthyl.

[0178] The term "bridged C5-C 10 "-Cycloalkyl" refers to a bicyclic saturated monovalent hydrocarbon radical in which the two rings share two non-adjacent ring atoms in common, for example, bicyclo[2.2.1]heptyl (also known as norbornyl).

[0179] The term "monocyclic 4- to 7-membered heterocycloalkyl" refers to a monocyclic saturated heterocycle containing a total of 4, 5, 6 or 7 ring atoms including one or two identical or different ring heteroatoms from the series N, O and S.

[0180] The monocyclic heterocycloalkyl group can be a 4-membered ring, such as azetidinyl, oxetanyl or thietanyl; or a 5-membered ring, such as tetrahydrofuranyl, 1,3-dioxolanyl, thiolanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,1-dioxothiolanyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl or 1,3-thiazolidinyl; or a 6-membered ring, such as tetrahydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl, 1,3-dioxanyl, 1,4-dioxanyl or 1,2-oxazinyl, or a 7-membered ring, such as azepanyl, 1,4-diazepanyl or 1,4-oxazepanyl, but is not limited thereto.

[0181] The term "monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl" refers to a monocyclic saturated heterocycle having a total of 4, 5, 6 or 7 ring atoms, which contains one ring nitrogen atom and optionally one further ring heteroatom from the series of N, O and S.

[0182] The monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group can be, for example, a 4-membered ring, such as azetidinyl; or a 5-membered ring, such as pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl or 1,3-thiazolidinyl; or a 6-membered ring, such as piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl or 1,2-oxazinyl, or a 7-membered ring, such as azepanyl, 1,4-diazepanyl or 1,4-oxazepanyl, but is not limited thereto.

[0183] The term "monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl" refers to a monocyclic saturated heterocycle having a total of 4, 5, 6 or 7 ring atoms, which contains one ring nitrogen atom and optionally one further ring heteroatom from the series of N, O and S.

[0184] The term "bicyclic 6- to 11-membered heterocycloalkyl" refers to a 6- to 11-membered heterospirocycloalkyl, 6- to 10-membered fused heterocycloalkyl or 7- to 10-membered bridged heterocycloalkyl group as defined hereinafter:

[0185] The term "6- to 11-membered heterospirocycloalkyl" refers to a bicyclic saturated heterocyclic ring having a total of 6, 7, 8, 9, 10, or 11 ring atoms, wherein two rings share one common ring carbon atom, said "heterospirocycloalkyl" containing one or two ring heteroatoms, identical or different, selected from N, O, S; said heterospirocycloalkyl can be attached to the rest of the molecule through any one of the carbon atoms, except the spiro carbon atom, or the nitrogen atom, if present.

[0186] Said heterospirocycloalkyl group is, for example, azaspiro[2.3]hexyl, azaspiro[3.3]heptyl, oxazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, oxaspiro[3.3]heptyl, oxazaspiro[5.3]nonyl, oxazaspiro[4.3]octyl, azaspiro[4.5]decyl, oxazaspiro[5.5]undecyl, diazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, thiazaspiro[4.3]octyl, azaspiro[5.5]undecyl, or one of the other homologues, such as spiro[3.4]-, spiro[4.4]-, spiro[2.4]-, spiro[2.5]-, spiro[2.6]-, spiro[3.5]-, spiro[3.6]-, spiro[4.5]- and spiro[4.6]-.

[0187] The term "6- to 10-membered fused heterocycloalkyl" refers to a bicyclic saturated heterocyclic ring having a total of 6, 7, 8, 9, or 10 ring atoms, wherein two rings share two adjacent ring atoms, said "fused heterocycloalkyl" containing one or two ring heteroatoms, identical or different, selected from N, O, S; said fused heterocycloalkyl can be attached to the rest of the molecule through any one of the carbon atoms or the nitrogen atom, if present.

[0188] Said fused heterocycloalkyl is, for example, azabicyclo[3.3.0]octyl, azabicyclo[4.3.0]nonyl, diazabicyclo[4.3.0]nonyl, oxazabicyclo[4.3.0]nonyl, thiazabicyclo[4.3.0]nonyl, or azabicyclo[4.4.0]decyl.

[0189] The term "7- to 10-membered bridged heterocycloalkyl" refers to a bicyclic saturated heterocyclic ring having a total of 7, 8, 9, or 10 ring atoms, wherein two rings share two non-adjacent common ring atoms, said "bridged heterocycloalkyl" containing one or two ring heteroatoms, identical or different, selected from N, O, S; said bridged heterocycloalkyl can be attached to the rest of the molecule through any one of the carbon atoms, except the spiro carbon atom, or the nitrogen atom, if present.

[0190] (if present).

[0191] The bridged heterocycloalkyl group is, for example, azabicyclo[2.2.1]heptyl, oxazabicyclo[2.2.1]heptyl, thiazabicyclo[2.2.1]heptyl, diazabicyclo[2.2.1]heptyl, azabicyclo[2.2.2]octyl, diazabicyclo[2.2.2]octyl, oxazabicyclo[2.2.2]octyl, thiazabicyclo[2.2.2]octyl, azabicyclo[3.2.1]octyl, diazabicyclo[3.2.1]octyl, oxazabicyclo[3.2.1]octyl, thiazabicyclo[3.2.1]octyl, azabicyclo[3.3.1]nonyl, diazabicyclo[3.3.1]nonyl, oxazabicyclo[3.3.1]nonyl, thiazabicyclo[3.3.1]nonyl, azabicyclo[4.2.1]nonyl, diazabicyclo[4.2.1]nonyl, oxazabicyclo[4.2.1]nonyl, thiazabicyclo[4.2.1]nonyl, azabicyclo[3.3.2]decyl, diazabicyclo[3.3.2]decyl, oxazabicyclo[3.3.2]decyl, thiazabicyclo[3.3.2]decyl or azabicyclo[4.2.2]decyl.

[0192] The term "bicyclic nitrogen-containing 6- to 11-membered heterocycloalkyl" means a 6- to 11-membered heterospirocycloalkyl, 6- to 10-membered fused heterocycloalkyl or 7- to 10-membered bridged heterocycloalkyl as defined above, but containing one ring nitrogen atom and optionally one or two further ring heteroatoms selected from the series consisting of N, O and S; the bicyclic nitrogen-containing 6- to 11-membered heterocycloalkyl group can be attached to the remainder of the molecule by the nitrogen atom or by any one of the carbon atoms other than the spiro carbon atom.

[0193] The term "bicyclic 5- to 11-membered heterocycloalkyl" means a 5- to 11-membered heterospirocycloalkyl, 5- to 11-membered fused heterocycloalkyl or 5- to 11-membered bridged heterocycloalkyl group as defined below:

[0194] The term "5- to 11-membered heterospirocycloalkyl" means a bicyclic saturated heterocycle having a total of 5, 6, 7, 8, 9, 10 or 11 ring atoms, wherein the two rings share one common ring carbon atom, the "heterospirocycloalkyl" containing one or two ring heteroatoms which are the same or different selected from N, O, S; the heterospirocycloalkyl can be attached to the remainder of the molecule by any one of the carbon atoms other than the spiro carbon atom or by the nitrogen atom if present.

[0195] The heterospirocycloalkyl radicals are, for example, azaspiro[2.2]pentyl, azaspiro[2.3]hexyl, azaspiro[3.3]heptyl, oxazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, oxazaspiro[5.3]nonyl, oxazaspiro[4.3]octyl, azaspiro[4.5]decyl, oxazaspiro[5.5]undecyl, , diazaspiro[3.3]heptyl, thiaazaspiro[3.3]heptyl, thiaazaspiro[4.3]octyl, azaspiro[5.5]undecyl or one of the other homologues, such as spiro[3.4]-, spiro[4.4]-, spiro[2.4]-, spiro[2.5]-, spiro[2.6]-, spiro[3.5]-, spiro[3.6]-, spiro[4.5]- and spiro[4.6]-.

[0196] The term "5- to 11-membered fused heterocycloalkyl" refers to a bicyclic saturated heterocycle having a total of 5, 6, 7, 8, 9 or 10 ring atoms, wherein the two rings share two adjacent ring atoms, and the "fused heterocycloalkyl" contains one or two identical or different ring heteroatoms selected from N, O, and S; the fused heterocycloalkyl may be attached to the rest of the molecule via any one carbon atom or nitrogen atom (if present).

[0197] The fused heterocycloalkyl group is, for example, azabicyclo[3.1.0]hexyl, azabicyclo[3.3.0]octyl, azabicyclo[4.3.0]nonyl, diazabicyclo[4.3.0]nonyl, oxazabicyclo[4.3.0]nonyl, thiazabicyclo[4.3.0]nonyl or azabicyclo[4.4.0]decyl.

[0198] The term "5- to 11-membered bridged heterocycloalkyl" refers to a bicyclic saturated heterocycle having a total of 5, 6, 7, 8, 9 or 10 ring atoms, wherein the two rings share two non-adjacent common ring atoms, and the "bridged heterocycloalkyl" contains one or two identical or different ring heteroatoms selected from N, O, and S; the bridged heterocycloalkyl can be attached to the rest of the molecule through any carbon atom other than the spiro carbon atom or the nitrogen atom (if present).

[0199] The bridged heterocycloalkyl group is, for example, azabicyclo[2.2.1]heptyl, oxazabicyclo[2.2.1]heptyl, thiazabicyclo[2.2.1]heptyl, diazabicyclo[2.2.1]heptyl, azabicyclo[2.2.2]octyl, diazabicyclo[2.2.2]octyl, oxazabicyclo[2.2.2]octyl, thiazabicyclo[2.2.2]octyl, azabicyclo[3.2.1]octyl, diazabicyclo[3.2.1]octyl, oxazabicyclo[3.2.1]octyl, thiazabicyclo[3.2.1]octyl, azabicyclo[3.3.1]nonyl, diazabicyclo[3.3.1]nonyl, oxazabicyclo[3.3.1]nonyl, thiazabicyclo[3.3.1]nonyl, azabicyclo[4.2.1]nonyl, diazabicyclo[4.2.1]nonyl, oxazabicyclo[4.2.1]nonyl, thiazabicyclo[4.2.1]nonyl, azabicyclo[3.3.2]decyl, diazabicyclo[3.3.2]decyl, oxazabicyclo[3.3.2]decyl, thiazabicyclo[3.3.2]decyl, or azabicyclo[4.2.2]decyl.

[0200] The term "bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl" refers to a 5- to 11-membered heterospirocycloalkyl, 5- to 10-membered fused heterocycloalkyl, or 5- to 11-membered bridged heterocycloalkyl as defined above, but containing one ring nitrogen atom and optionally one or two additional ring heteroatoms selected from the series consisting of N, O, and S; which bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl group can be attached to the remainder of the molecule through the nitrogen atom or any one of the carbon atoms other than the spiro carbon atom.

[0201] The term "heteroaryl" refers to a monovalent, monocyclic or bicyclic aromatic ring ("5- to 10-membered heteroaryl" group) having 5, 6, 8, 9, or 10 ring atoms, which contains at least one ring heteroatom and optionally one, two, or three additional ring heteroatoms from the series consisting of N, O, and / or S, and which is bound through a ring carbon atom or a nitrogen atom, if valence allows, for example in pyrrol-1-yl.

[0202] The heteroaryl group can be a 5-membered heteroaryl group, for example thienyl, furanyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, or tetrazolyl; or a 6-membered heteroaryl group, for example pyridinyl (also referred to herein as pyridyl), pyridazinyl, pyrimidinyl, pyrazinyl, or triazinyl; or a 9-membered heteroaryl group, for example benzofuranyl, benzothiophenyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzothiazolyl, benzotriazolyl, thiazolopyridinyl, indazolyl, indolyl, isoindolyl, indolizinyl, or purinyl; or a 10-membered heteroaryl group, for example quinolinyl, quinazolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, or pteridinyl.

[0203] Generally, unless otherwise indicated, the heteroaryl or heteroarylene groups include all possible isomeric forms thereof, such as tautomers and position isomers with respect to the point of attachment of the remainder of the molecule. Thus, for some illustrative, non-limiting examples, the term pyridyl includes pyrid-2-yl, pyrid-3-yl and pyrid-4-yl; or the term thienyl includes thien-2-yl and thien-3-yl.

[0204] The term "C1-C6", as used herein, e.g. in the definition of "C1-C6-alkyl", "C1-C6-haloalkyl", "C1-C6-hydroxyalkyl", "C1-C6-alkoxy" or "C1-C6-haloalkoxy", means an alkyl group having a finite number of carbon atoms of 1 to 6, i.e. 1, 2, 3, 4, 5 or 6 carbon atoms.

[0205] Furthermore, as used herein, the term "C3-C7", as used herein, e.g. in the definition of "C3-C7-cycloalkyl" above and below, means a cycloalkyl group having a finite number of carbon atoms of 3 to 7, i.e. 3, 4, 5, 6 or 7 carbon atoms.

[0206] When a range of values is given, the range includes every value and sub-range within the range.

[0207] For example:

[0208] "C1-C6" includes C1, C2, C3, C4, C5, C6, C1-C6, C1-C5, C1-C4, C1-C3, C1-C2, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5 and C5-C6;

[0209] "C2-C6" includes C2, C3, C4, C5, C6, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5 and C5-C6;

[0210] "C3-C6" includes C3, C4, C5, C6, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5 and C5-C6;

[0211] As used herein, the term "leaving group" refers to an atom or atom group which is replaced by a stable species in a chemical reaction, which carries a bonding electron. In particular, such leaving group is selected from the group consisting of a halogen atom, in particular a fluorine atom, a chlorine atom, a bromine atom or an iodine atom, which is displaced as a halide, in particular a fluoride, a chloride, a bromide or an iodide, a (methylsulfonyl)oxy group, a [(trifluoromethyl)sulfonyl]oxy group, a [(nonafluorobutyl)sulfonyl]oxy group, a (phenylsulfonyl)oxy group, a [(4-methylphenyl)sulfonyl]oxy group, a [(4-bromophenyl)sulfonyl]oxy group, a [(4-nitrophenyl)sulfonyl]oxy group, a [(2-nitrophenyl)sulfonyl]oxy group, a [(4-isopropylphenyl)sulfonyl]oxy group, a [(2,4,6-triisopropylphenyl)sulfonyl]oxy group, a [(2,4,6-trimethylphenyl)sulfonyl]oxy group, a [(4-tert-butylphenyl)sulfonyl]oxy group and a [(4-methoxyphenyl)sulfonyl]oxy group.

[0212] As used herein, the term "dipolar aprotic solvent" refers to a solvent selected from the group consisting of acetone, acetonitrile, propionitrile, dimethyl sulfoxide, diethyl sulfoxide, N,N-dimethylformamide, N,N-dimethylacetamide, N,N-diethylformamide, N,N-diethylacetamide, 1-methyl-2-pyrrolidinone, 1-ethyl-2-pyrrolidinone, 1-methyl-2-piperidinone and 1-ethyl-2-piperidinone or mixtures thereof. In particular, the dipolar aprotic solvent is acetonitrile, dimethyl sulfoxide, N,N-dimethylformamide, N,N-dimethylacetamide or 1-methyl-2-pyrrolidinone.

[0213] As used herein, the term "room temperature" refers to a temperature in the range of 15 °C to 25 °C.

[0214] Further definitions of DGK inhibitors

[0215] As used herein, the term "one or more", for example in the definition of substituents of the DGK inhibitors of the general formula of the present application, is to be understood as meaning "one, two, three, four or five, in particular one, two, three or four, more particularly one, two or three, even more particularly one or two".

[0216] The definition of the respective DGK inhibitor of formula (I) or (II) also includes all suitable isotopic variants of the respective DGK inhibitor of formula (I) or (II). Thus an "isotopic variant" is defined as a variant in which at least one atom is replaced by an atom having the same atomic number but an atomic mass different from the atomic mass usually or predominantly found in nature. Examples of isotopes that can be suitably replaced in a DGK inhibitor of formula (I) or (II) include isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorus, sulphur, fluorine, chlorine, bromine and iodine, such as2H,3H,13C,14C,15N,17O,18O,31P,32P,35S,18F,36Cl,82Br and125I, respectively. 2 H (deuterium), 3 H (tritium),11 C, 13 C, 14 C, 15 N, 17 O, 18 O, 32 P, 33 P, 33 S, 34 S, 35 S, 36 S, 18 F, 36 Cl, 82 Br, 123 I, 124 I, 129 I and 131 I. Certain isotopic variants of the DGK inhibitors of Formula (I) or (II), for example, those in which one or more radioactive isotopes

[0217] (e.g. 3 H or 14 C) are incorporated can be used in the study of drug and / or substrate tissue distribution. Tritiated and carbon-14 (i.e. 14 C) isotopes are particularly preferred due to their ease of preparation and detectability. Further, substitution with isotopes such as deuterium can afford certain therapeutic advantages resulting from greater metabolic stability, for example, increased in vivo half-life or reduced dosage requirements, and hence can be preferred in some circumstances. Isotopic variants of the DGK inhibitors of Formula (I) or (II) can generally be prepared by conventional procedures known to those skilled in the art (e.g., by the illustrative processes or by the methods of preparation described in the Examples below) using the appropriate isotopic variants of suitable reagents.

[0218] When the plural form is used in reference to a compound, salt, polymorph, hydrate, solvate or the like, this is intended to also include a single compound, salt, polymorph, isomer, hydrate, solvate or the like.

[0219] Depending on the location and nature of the various substituents required, the DGK inhibitors of Formula (I) and (II) can contain one or more asymmetric centers. Asymmetric carbon atoms can exist in either the (R) or (S) configuration, leading to racemic mixtures in the case of a single asymmetric center, and diastereomeric mixtures in the case of multiple asymmetric centers. In certain cases, asymmetry can also exist due to restricted rotation about a given bond (e.g., a central bond adjacent to two substituted aromatic rings of a specified compound).

[0220] Substituents on rings can also exist in either the cis or trans form. All such configurations (including enantiomers and diastereomers) are included within the definition of the corresponding DGK inhibitor.

[0221] Preferred DGK inhibitors of formula (I) and (II) are those that produce more desirable biological activity. Separated, pure or partially purified isomers and stereoisomers or racemic or diastereomeric mixtures of the DGK inhibitors of formula (I) and (II) are also included within the scope of the present invention. Purification and isolation of these substances can be accomplished by standard techniques known in the art.

[0222] Optical isomers can be obtained by resolving the racemic mixture according to conventional methods, for example, by forming diastereomeric salts or forming covalent diastereomers using optically active acids or bases. Examples of suitable acids are tartaric acid, diacetyltartaric acid, ditoluoyltartaric acid and camphorsulfonic acid. A mixture of diastereoisomers can be separated into its respective diastereoisomers by methods known in the art (for example, by chromatography or partial crystallization) based on its physical and / or chemical differences. The optically active base or acid is then released from the separated diastereomeric salts. The different methods for separating optical isomers include using chiral chromatography (for example, chiral HPLC columns), whether or not conventional derivatization is performed, optimally selected to maximize the separation of enantiomers. Suitable chiral HPLC columns are manufactured by Daicel, such as Chiracel OD and Chiracel OJ and many other products, which are all conventionally optional. Enzymatic separation is useful whether or not derivatization is performed. The optically active compounds of the present invention can also be obtained by using chiral synthesis of optically active raw materials.

[0223] In order to define isomers that are different types from each other, reference is made to IUPAC Rules Section E (Pure Appl Chem 45, 11-30, 1976).

[0224] The definition of DGK inhibitors described in accordance with the present invention includes, but is not limited to, all possible stereoisomers of the DGK inhibitors of formula (I) and (II), which are single stereoisomers, or any mixture of said stereoisomers, such as R or S isomers, or E or Z isomers in any ratio. Separation of single stereoisomers (e.g., single enantiomers or single diastereomers) of the DGK inhibitors of formula (I) and (II) can be achieved by any suitable prior art method, such as chromatography, in particular chiral chromatography.

[0225] In addition, some of the DGK inhibitors of formula (I) and (II) may exist as "tautomers". For example, the DGK inhibitors of the present invention may contain a pyridone moiety and may exist as a pyridone or as a hydroxypyridine or even as a mixture of the two tautomers in any amount, i.e.:

[0226]

[0227] The present definition of DGK inhibitors includes, but is not limited to, all possible tautomers of the DGK inhibitors of formula (I) and (II), which are single tautomers or any mixture of said tautomers in any ratio.

[0228] Furthermore, the DGK inhibitors of formula (I) and (II) can exist as "N-oxides", which are defined in that at least one nitrogen of the compounds of the present application is oxidized. The combinations of the present application include, but are not limited to, all possible N-oxides of the DGK inhibitors of formula (I) and (II).

[0229] The present definition of DGK inhibitors also relates to useful forms of the DGK inhibitors of formula (I) and (II) as disclosed herein, such as metabolites, hydrates, solvates, prodrugs, salts, in particular pharmaceutically acceptable salts, and co-precipitates.

[0230] The DGK inhibitors of formula (I) and (II) can exist as "hydrates" or "solvates", wherein the compounds described herein contain a polar solvent, in particular, for example, water, methanol or ethanol, as a structural element of the crystal lattice of the compounds. The amount of the polar solvent, in particular water, can be present in stoichiometric or non-stoichiometric amounts. In the case of stoichiometric solvates, for example, hemi-, (hemi)-, mono-, sesqui-, di-, tri-, tetra-, penta-solvates or hydrates are possible. The DGK inhibitors of formula (I) and (II) include all such hydrates or solvates.

[0231] Furthermore, the DGK inhibitors of formula (I) and (II) can exist in free form, for example, as a free base, or as a free acid, or as a zwitterion, or can exist in the form of a salt. The salt can be any salt, an organic or inorganic addition salt, in particular any pharmaceutically acceptable organic or inorganic addition salt, which is customarily used.

[0232] The DGK inhibitors of formula (I) and (II) include all possible salts of the DGK inhibitors of formula (I) and (II), which are single salts or any mixture of said salts in any ratio.

[0233] The term "pharmaceutically acceptable salts" of the DGK inhibitors of formula (I) and (II) refers to relatively non-toxic, inorganic or organic acid addition salts of the compounds of the present application. For example, see S. M. Berge, et al.

[0234] "Pharmaceutical Salts," J. Pharm. Sci. 1977, 66, 1-19. Pharmaceutically acceptable salts include those obtained by reacting a parent compound with a suitable inorganic or organic acid such as hydrochloric, sulfuric, phosphoric, methanesulfonic, camphorsulfonic, oxalic, maleic, succinic, and citric acid. Pharmaceutically acceptable salts also include those obtained by reacting a parent compound with a suitable base such as the alkali and alkaline earth metal hydroxides, ammonium hydroxide, and organic basic such as dicyclohexyl amine. Those skilled in the art will further recognize that acid addition salts of the claimed compounds can be prepared by reaction of the compound with the appropriate inorganic or organic acid via any of a number of known methods. Alternatively, alkali and alkaline earth metal salts of acidic compounds of the present application are prepared by reacting the compound of the present application with the appropriate base via a variety of known methods.

[0235] Representative salts of the DGK inhibitors of formula (I) and (II) include the conventional nontoxic salts and the quaternary ammonium salts that are formed, for example, from inorganic or organic acids or bases by means known in the art. For example, such acid addition salts include acetate, adipate, alginate, ascorbate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, citrate, camphorate, camphorsulfonate, cinnamate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, fumarate, glucoheptanoate, glycerophosphate, hemisulfate, heptanoate, hexanoate, chloride, bromide, iodide, 2-hydroxyethanesulfonate, itaconate, lactate, maleate, mandelate, methanesulfonate, 2-naphthalenesulfonate, nicotinate, nitrate, oxalate, pamoate, pectinate, persulfate, 3-phenylpropionate, picrate, pivalate, propionate, succinate, sulfonate, sulfate, tartrate, thiocyanate, tosylate, and undecanoate. Base salts include alkali metal salts such as potassium and sodium salts, alkaline earth metal salts such as calcium and magnesium salts, and salts with organic bases such as dicyclohexyl amine salts and N-methyl-D-glucamine salts. Additionally, the basic nitrogen-containing groups can be quaternized with such agents as lower alkyl halides, such as methyl, ethyl, propyl, and butyl chlorides, bromides and iodides; dialkyl sulfates like dimethyl, diethyl, dibutyl, and diamyl sulfates; long chain halides such as decyl, lauryl, myristyl and stearyl chlorides, bromides and iodides; aralkyl halides like benzyl and phenethyl bromides; and others.

[0236] In addition, the DGK inhibitors of formula (I) and (II) include all possible crystalline forms or polymorphs of the DGK inhibitors of formula (I) and (II), either as a single polymorph or as a mixture of more than one polymorph in any proportion.

[0237] When the groups in the DGK inhibitors of formula (I) and (II) are substituted, the groups can be mono- or polysubstituted, unless otherwise indicated. In the DGK inhibitors of formula (I) and (II), all groups occurring more than once are defined independently of each other. Preferred is substitution by one, two or three identical or different substituents.

[0238] DGK alpha inhibitors and DGK zeta inhibitors

[0239] In the following, DGK alpha inhibitors and DGK zeta inhibitors which can preferably be used in the present application are described according to any one of aspect 1, aspect 2, aspect 3, aspect 4, aspect 5, aspect 6, aspect 7, aspect 8 or aspect 9 of the present application. In the following, the terms "inhibitor of DGK alpha" and "DGK alpha inhibitor" are used interchangeably. Likewise, in the following, the terms "inhibitor of DGK zeta" and "DGK zeta inhibitor" are used interchangeably.

[0240] Inhibitors of DGK have been previously disclosed as listed above.

[0241] Two members of the DGK family, DGK alpha and DGK zeta, specifically regulate the DAG pool generated as a second messenger upon T cell receptor

[0242] (TCR) stimulation. Inhibitors of both members are therefore preferred.

[0243] Furthermore, as used herein, the term "DGK inhibitor" refers to a compound which inhibits one or more isoforms of DGK. A DGK alpha inhibitor inhibits the DGK alpha isoform and can be a selective DGK alpha inhibitor or, in addition to its DGK alpha inhibitory activity, can inhibit other DGK isoforms, e.g. DGK zeta. Likewise, a DGK zeta inhibitor inhibits the DGK zeta isoform and can be a selective DGK zeta inhibitor or, in addition to its DGK zeta inhibitory activity, can inhibit other DGK isoforms, e.g. DGK alpha. In the present application, a DGK alpha inhibitor is preferably selective for DGK zeta and a DGK zeta inhibitor is preferably selective for DGK alpha.

[0244] More preferably, a DGK alpha inhibitor is characterized by a selectivity for DGK zeta of 20-fold or more, i.e. the IC 50 value for DGK zeta is 20-fold or more higher compared to the IC 50 value for DGK alpha, and a DGK zeta inhibitor is characterized by a selectivity for DGK alpha of 20-fold or more, i.e. the IC 50 value for DGK alpha is 20-fold or more higher compared to the IC 50 value for DGK zeta.

[0245] Even more preferably, the DGK alpha inhibitors are characterized by a selectivity of 100-fold or more for DGKzeta, i.e. the IC50value for DGKzeta is 100-fold or more higher compared to the IC50value for DGK alpha, e.g. in the in vitro assay described in the experimental section, and the DGKzeta inhibitors are characterized by a selectivity of 100-fold or more for DGK alpha, i.e. the IC50value for DGK alpha is 100-fold or more higher compared to the IC50value for DGKzeta, e.g. in the in vitro assay described in the experimental section. 50 50 50 50

[0246] As used herein, the compounds of general formula (I) are typically DGK alpha inhibitors, and as used herein, the compounds of general formula (II) are typically DGKzeta inhibitors. As shown below, particularly preferred DGK alpha inhibitors A are characterized by a selectivity of more than 100-fold for DGKzeta, and particularly preferred DGKzeta inhibitors A' are characterized by a selectivity of more than 100-fold for DGK alpha.

[0247] DGK alpha inhibitors

[0248] DGK alpha inhibitor embodiment A

[0249] In the following, DGK alpha inhibitors are described, which can preferably be used in accordance with any one of the first, second, third, fourth, fifth, sixth, seventh, eighth or ninth aspect of the present application.

[0250] In some embodiments of the present application, the DGK alpha inhibitors are compounds of formula (I)

[0251]

[0252] wherein:

[0253] R 1 represents a group selected from cyano, -C(=O)NH2, -C(=O)N(H)CH3, -C(=O)N(H)C2H5, -C(=O)N(CH3)2and -C(=O)OR 15 ;

[0254] R 2 represents a group selected from phenyl, naphthyl and 5- to 10-membered heteroaryl,

[0255] wherein the 5- to 10-membered heteroaryl group is attached to the remainder of the molecule via a carbon atom of said 5- to 10-membered heteroaryl group,

[0256] and ​​​​

[0257] wherein the phenyl, naphthyl and 5- to 10-membered heteroaryl group is optionally substituted one, two, three or four times, each substituent independently being selected from a halogen atom or a group selected from: Ci-C6-alkyl, C3-C6-cycloalkyl, Ci-C6-hydroxyalkyl, Ci-C6-haloalkyl, (Ci-C2-alkoxy)-(Ci-C6-alkyl)-, Ci-C6-alkoxy, (Ci-C2-alkoxy)-(Ci-C6-alkoxy)-, Ci-C6-haloalkoxy, C3-C6-cycloalkoxy, phenyloxy, -SR 14 , -S(=O)R 14 , -S(=O)2R 14 , -P(=O)(R 14 )2, cyano, hydroxy, -N(R 9 )(R 10 ), -C(=O)N(R 9 )(R 10 ), -C(=O)R 11 , -N(R 12 )C(=O)R 13 , -N(R 12 )S(=O)2R 14 , -N=S(=NH)(R 14 )2, -N=S(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl and 5- or 6-membered heteroaryl,

[0258] or two substituents of the phenyl group, when they are attached to adjacent ring atoms, are optionally mutually connected in such a way that they together form a group selected from: -(CH2)3-, -CH2-CH(OH)-CH2-, -(CH2)4-, -O-(CH2)2-, -(CH2)2-O-, -CH2-CH(CH3)-O-, -CH2-O-CH2-, -O-(CH2)3-, -(CH2)3-O-, -CH2-O-(CH2)2-, -(CH2)2-O-CH2-, -O-CH2-O-, -O-C(CH3)2-O-, -O-(CH2)2-O-, -N(R 18 )-C(=O)-(C(R 18 )(R 19 )) m -, -N(R 18 )-C(=O)-(C(CH2)3)-, -N(R 18 )-(C(R 18 )(R 19 )) m -, -N(R18 )-C(=O)-O- and -N(R 18 )-C(=O)-N(R 18 )-,

[0259] wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group,

[0260] as well as

[0261] wherein the 4- to 7-membered heterocycloalkyl group, the 5- to 7-membered heterocycloalkenyl group and the (4- to 7-membered heterocycloalkyl)oxy group are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0262] as well as

[0263] wherein the C1-C6-alkyl and C1-C6-alkoxy groups are optionally selected from

[0264] C3-C4-cycloalkyl, phenyl and 4- to 7-membered heterocycloalkyl groups,

[0265] wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0266] as well as

[0267] wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0268] as well as

[0269] The phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0270] as well as

[0271] wherein the C3-C4-cycloalkyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano and hydroxy,

[0272] and

[0273] wherein the C3-C6-cycloalkyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a Ci-C4-alkyl group,

[0274] and

[0275] wherein the phenyl, phenoxy and 5- or 6-membered heteroaryl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from Ci-C2-alkyl, Ci-C2-haloalkyl, cyano, hydroxy, Ci-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0276] R 3 represents a hydrogen atom or a halogen atom or a group selected from Ci-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C6-cycloalkenyl, Ci-C6-hydroxyalkyl, Ci-C6-haloalkyl, (Ci-C2-alkoxy)-(Ci-C6-alkyl)-, Ci-C6-alkoxy, (Ci-C2-alkoxy)-(Ci-C6-alkoxy)-, Ci-C4-haloalkoxy, C3-C6-cycloalkoxy, phenoxy, -SR 14 , -S(=0)R 14 , -S(=0)2R 14 , cyano, hydroxy, -N(R 9 )(R 10 ), -C(=0)N(R 9 )(R 10 ), -C(=0)R 11 , -N(R 12 )C(=0)R 13 , -N(R 12 )S(=0)2R 14 , -N=S(=NH)(R 14 )2, -N=S(=0)(R 14 )2, -P(=0)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl and 5- or 6-membered heteroaryl,

[0277] wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group,

[0278] as well as

[0279] wherein the 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, and (4- to 7-membered heterocycloalkyl)oxy groups are optionally substituted once, twice, or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0280] as well as

[0281] wherein the C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C1-C6-alkoxy groups are optionally substituted by groups selected from the group consisting of C3-C4-cycloalkyl, phenyl and 4- to 7-membered heterocycloalkyl,

[0282] wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0283] as well as

[0284] wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0285] as well as

[0286] wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0287] as well as

[0288] wherein the C3-C4-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of a cyano group and a hydroxyl group,

[0289] as well as

[0290] wherein the C2-C6-alkenyl group is optionally substituted by a C1-C4-haloalkyl group,

[0291] as well as

[0292] wherein the C3-C6-cycloalkyl and C4-C6-cycloalkenyl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl,

[0293] as well as

[0294] wherein the phenyl, phenoxy and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0295] R 4 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C6-cycloalkenyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, (C1-C2-alkoxy)-(C1-C6-alkyl)-, C1-C6-alkoxy, (C1-C2-alkoxy)-(C1-C6-alkoxy)-, C1-C4-haloalkoxy, -O-(C1-C4-alkyl)-C(=O)OR 15 、-O-(C1-C4-alkyl)-C(=O)N(R 9 )(R 10 ), C3-C6-cycloalkyloxy, -S(=O)R 14 、-S(=O)2R 14 , cyano, nitro, hydroxyl, -N(R 9 )(R 10 )、-N(R 16 )(R 17 )、-N(R 16 )(R 20 )、-C(=O)N(R 9 )(R 10 ),-C(=O)R 11 、-N(R 12 )C(=O)R 13 、-N(R 12 )S(=O)2R 14 、-N=S(=NH)(R 14 )2、-N=S(=O)(R14 )2、-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl, and 5- or 6-membered heteroaryl,

[0296] wherein the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups,

[0297] as well as

[0298] wherein the 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, and (4- to 7-membered heterocycloalkyl)oxy groups are optionally substituted once, twice, or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0299] as well as

[0300] wherein the C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C1-C6-alkoxy groups are optionally substituted by groups selected from C3-C4-cycloalkyl and 4- to 7-membered heterocycloalkyl,

[0301] wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0302] as well as

[0303] wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0304] as well as

[0305] wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0306] as well as

[0307] wherein the C3-C4-cycloalkyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano and hydroxy,

[0308] and

[0309] wherein the C1-C6-alkyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano and hydroxy,

[0310] and

[0311] wherein the C3-C6-cycloalkyl and C4-C6-cycloalkenyl groups are optionally substituted one or two times, each substituent being independently selected from a halogen atom or a C1-C4-alkyl group,

[0312] and

[0313] wherein the phenyl and 5- or 6-membered heteroaryl groups are optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0314] R 5 represents a hydrogen atom or a halogen atom or a group selected from C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C6-cycloalkenyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, (C1-C2-alkoxy)-(C1-C6-alkyl)-, C1-C6-alkoxy, (C1-C2-alkoxy)-(C2-C6-alkoxy)-, C1-C4-haloalkoxy, C3-C6-cycloalkoxy, phenoxy, -SR 14 , -S(=O)R 14 , -S(=O)2R 14 , cyano, hydroxy, -N(R 9 )(R 10 ), -C(=O)N(R 9 )(R 10 ), -C(=O)R 11 , -N(R 12 )C(=O)R 13 , -N(R 12 )S(=O)2R 14 , -N=S(=NH)(R 14 )2, -N=S(=O)(R 14 )2, -P(=O)(R 14)2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl, and 5- or 6-membered heteroaryl,

[0315] wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group,

[0316] as well as

[0317] wherein the 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, and (4- to 7-membered heterocycloalkyl)oxy groups are optionally substituted once, twice, or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0318] as well as

[0319] wherein the C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C1-C6-alkoxy groups are optionally substituted by groups selected from the group consisting of C3-C4-cycloalkyl, phenyl and 4- to 7-membered heterocycloalkyl,

[0320] wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0321] as well as

[0322] wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo,

[0323] as well as

[0324] wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0325] as well as

[0326] wherein the C3-C4-cycloalkyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano and hydroxy,

[0327] and

[0328] wherein the C3-C6-cycloalkyl and C4-C6-cycloalkenyl groups are optionally substituted one or two times, each substituent being independently selected from a halogen atom or a C1-C4-alkyl group,

[0329] and

[0330] wherein the phenyl, phenoxy and 5 or 6 membered heteroaryl groups are optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0331] R 6 represents a hydrogen atom or a fluorine atom or a group selected from C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, hydroxy and oxo,

[0332] R 7 represents a hydrogen atom or a halogen atom or a group selected from C1-C4-alkyl, C1-C4-alkoxy, hydroxy and cyano,

[0333] R 8 represents a group selected from methyl and ethyl,

[0334] R 9 and R 10 independently from each other represent a hydrogen atom or a group selected from C1-C4-alkyl, C2-C4-hydroxyalkyl, N≡C-(C1-C4-alkyl)-, (C1-C4-alkoxy)-(C2-C4-alkyl)-, C3-C4-cycloalkyl and C2-C4-haloalkyl,

[0335] or

[0336] R 9 and R 10 together with the nitrogen to which they are attached represent a nitrogen containing 4 to 7 membered heterocycloalkyl group,

[0337] wherein the nitrogen containing 4 to 7 membered heterocycloalkyl group is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl, C3-C4-cycloalkyl, hydroxy and oxo,

[0338] or

[0339] two substituents connected to the same carbon atom of the nitrogen containing 4- to 7-membered heterocycloalkyl group together with the carbon atom to which they are attached represent a 4- to 7-membered heterocycloalkyl group,

[0340] wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or from the group consisting of Ci-C4-alkyl, C3-C4-cycloalkyl, Ci-C4-haloalkyl, hydroxyl and oxo,

[0341] R 11 represents a hydrogen atom or a group selected from Ci-C4-alkyl, Ci-C4-hydroxyalkyl, Ci-C4-haloalkyl, phenyl and 5- or 6-membered heteroaryl,

[0342] wherein the phenyl group and 5- or 6-membered heteroaryl group are optionally substituted one or two times, each substituent being independently selected from a halogen atom or from the group consisting of Ci-C2-alkyl, Ci-C2-haloalkyl, cyano, hydroxyl, Ci-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ),

[0343] R 12 represents a hydrogen atom or a Ci-C4-alkyl group,

[0344] R 13 represents a hydrogen atom or a group selected from Ci-C6-alkyl, phenyl and 5- or 6-membered heteroaryl,

[0345] wherein the phenyl group and 5- or 6-membered heteroaryl group are optionally substituted one or two times, each substituent being independently selected from a halogen atom or from the group consisting of:

[0346] Ci-C2-alkyl, Ci-C2-haloalkyl, cyano, hydroxyl, Ci-C2-alkoxy,

[0347] C3-C4-cycloalkyl and -N(R 9 )(R 10 ,

[0348] R 14 represents a group selected from Ci-C6-alkyl, Ci-C6-haloalkyl, C3-C6-cycloalkyl, phenyl and 5- or 6-membered heteroaryl,

[0349] wherein the phenyl group and 5- or 6-membered heteroaryl group are optionally substituted one or two times, each substituent being independently selected from a halogen atom or from the group consisting of Ci-C2-alkyl, Ci-C2-haloalkyl, cyano, hydroxyl, Ci-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9) (R 10 ),

[0350] R 15 represents a hydrogen atom or a C1-C4-alkyl group,

[0351] R 16 represents a hydrogen atom or a group selected from C1-C4-alkyl, C3-C4-cycloalkyl and C2-C4-haloalkyl,

[0352] R 17 represents a 4- to 7-membered heterocycloalkyl group,

[0353] wherein said 4- to 7-membered heterocycloalkyl group is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl, C3-C4-cycloalkyl, C1-C4-alkoxy, hydroxyl and oxo,

[0354] and

[0355] wherein said 4- to 7-membered heterocycloalkyl group is attached to the rest of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0356] R 18 represents a hydrogen atom or a group selected from methyl and ethyl,

[0357] R 19 represents a hydrogen atom or a group selected from methyl and ethyl,

[0358] R 20 represents a (4- to 7-membered heterocycloalkyl)-(C1-C4-alkyl)- group,

[0359] wherein the (4- to 7-membered heterocycloalkyl) part of said group is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl, C3-C4-cycloalkyl, C1-C4-alkoxy, hydroxyl and oxo,

[0360] m represents an integer selected from 1, 2 and 3,

[0361] and

[0362] n represents an integer selected from 1, 2 and 3,

[0363] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[0364] In a preferred embodiment, the at least one DGK a inhibitor is characterized by having the formula (I) as defined under this heading.

[0365] DGK alpha inhibitor embodiment B

[0366] In some other embodiments of the application, the DGKa inhibitor is a compound of formula (I) as described above, wherein

[0367] R 1 represents a group selected from cyano, -C(=O)NH2, -C(=O)N(H)CH3and -C(=O)N(CH3)2;

[0368] R 2 represents a group selected from phenyl, naphthyl and 5- to 10-membered heteroaryl,

[0369] wherein the 5- to 10-membered heteroaryl group is attached to the remainder of the molecule by a carbon atom of said 5- to 10-membered heteroaryl group,

[0370] and

[0371] wherein the phenyl, naphthyl and 5- to 10-membered heteroaryl groups are optionally substituted one, two, three or four times, each substituent being independently selected from a halogen atom or a group selected from C1-C6-alkyl, C3-C5-cycloalkyl, C1-C4-haloalkyl, (C1-C2-alkoxy)-(C1-C2-alkyl)-, C1-C4-alkoxy, C1-C4-haloalkoxy, phenyloxy, -S(=O)2R 14 , -P(=O)(R 14 )2, cyano, hydroxy, -N(R 9 )(R 10 ), -C(=O)N(R 9 )(R 10 ), -C(=O)R 11 , -N(R 12 )C(=O)R 13 , -N(R 12 )S(=O)2R 14 , -N=S(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, phenyl and 5- or 6-membered heteroaryl,

[0372] or two substituents of said phenyl group, when they are attached to adjacent ring atoms, are optionally mutually linked in such a way that they together form a group selected from -CH2-CH(OH)-CH2-, -CH2-CH(CH3)-O-, -O-C(CH3)2-O-, -N(R 18 )-C(=O)-(C(R 18 )(R 19 )) m -, -N(R 18 )-C(=O)-(C(CH2)3)-, -N(R 18)-(C(R 18 )(R 19 )) m -、-N(R 18 )-C(=O)-O- and -N(R 18 )-C(=O)-N(R 18 )-,

[0373] wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0374] as well as

[0375] wherein the C1-C4-alkoxy group is optionally substituted by a group selected from 4- to 7-membered heterocycloalkyl and phenyl,

[0376] wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0377] as well as

[0378] wherein the phenyl and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl and C1-C2-alkoxy,

[0379] R 3 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C2-C4-alkenyl, C3-C5-cycloalkyl, (C1-C2-alkoxy)-(C1-C4-alkyl)-, C1-C4-alkoxy, C1-C4-haloalkoxy, C3-C5-cycloalkyloxy, -S(=O)2R 14 , cyano, hydroxyl, -N(R 9 )(R 10 )、-C(=O)N(R 9 )(R 10 ),-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy and phenyl,

[0380] wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group,

[0381] as well as

[0382] wherein the C1-C6-alkyl and C1-C4-alkoxy groups are optionally substituted by groups selected from C3-C4-cycloalkyl and 4- to 7-membered heterocycloalkyl groups,

[0383] wherein said 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule by a carbon atom of said 4- to 7-membered heterocycloalkyl group,

[0384] and wherein said C3-C4-cycloalkyl group is optionally substituted one or two times, independently, by a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl,

[0385] wherein said C2-C4-alkenyl group is optionally substituted by a C1-C4-haloalkyl group,

[0386] and wherein said C3-C5-cycloalkyl group is optionally substituted one or two times, independently, by a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl,

[0387] wherein said C2-C4-alkenyl group is optionally substituted by a C1-C4-haloalkyl group,

[0388] and wherein said C3-C5-cycloalkyl group is optionally substituted one or two times, independently, by a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl,

[0389] wherein said C3-C5-cycloalkyl group is optionally substituted one or two times, independently, by a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl,

[0390] R 4 represents a hydrogen atom or a halogen atom or a group selected from C1-C6-alkyl, C1-C6-haloalkyl, C3-C5-cycloalkyl, (C1-C2-alkoxy)-(C1-C4-alkyl)-, C1-C4-alkoxy, (C1-C2-alkoxy)-(C1-C4-alkoxy)-, -0-(C1-C4-alkyl)-C(=0)OR 15 , -0-(C1-C4-alkyl)-C(=0)N(R 9 )(R 10 ), C3-C5-cycloalkoxy, -S(=0)2R 14 , cyano, nitro, hydroxy, -N(R 9 )(R 10 ), -N(R 16 )(R 17 ), -N(R 16 )(R 20 ), -N=S(=NH)(R 14 )2, -N=S(=0)(R 14 )2, -P(=0)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy and phenyl,

[0391] wherein said 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl group is attached to the remainder of the molecule by a carbon atom of said 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl group,

[0392] and wherein said C3-C5-cycloalkyl group is optionally substituted one or two times, independently, by a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl,

[0393] wherein said C1-C6-alkyl and C1-C4-alkoxy groups are optionally substituted, identically or differently, with one or more substituents selected from the group consisting of

[0394] C3-C4-cycloalkyl and 4- to 7-membered heterocycloalkyl,

[0395] wherein said 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule by a carbon atom of said 4- to 7-membered heterocycloalkyl group,

[0396] and wherein said C3-C4-cycloalkyl group is optionally substituted, identically or differently, one or more times by a halogen atom or a group selected from cyano and hydroxy,

[0397] wherein said C1-C4-alkoxy group is optionally substituted with an oxirane-2-yl group,

[0398] and wherein said C3-C5-cycloalkyl group is optionally substituted, identically or differently, one or more times by a halogen atom or a C1-C4-alkyl group,

[0399] wherein said C3-C4-cycloalkyl group is optionally substituted, identically or differently, one or more times by a halogen atom or a group selected from cyano and hydroxy,

[0400] and wherein said C1-C4-alkoxy group is optionally substituted with an oxirane-2-yl group,

[0401] wherein said C3-C5-cycloalkyl group is optionally substituted, identically or differently, one or more times by a halogen atom or a C1-C4-alkyl group,

[0402] R 5 represents a hydrogen atom or a halogen atom or a group selected from C1-C5-alkyl, C3-C5-cycloalkyl, C1-C4-alkoxy, C3-C5-cycloalkoxy, -S(=O)2R 14 , cyano, hydroxy, -N(R 9 )(R 10 ), 4- to 7-membered heterocycloalkyl and (4- to 7-membered heterocycloalkyl)oxy,

[0403] wherein said 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule by a carbon atom of said 4- to 7-membered heterocycloalkyl group,

[0404] R 6 represents a hydrogen atom or a group selected from C1-C4-alkyl and C1-C4-hydroxyalkyl,

[0405] R 7 represents a hydrogen atom or a halogen atom or a group selected from C1-C4-alkyl, C1-C4-alkoxy and hydroxy,

[0406] R 8 represents a group selected from methyl and ethyl,

[0407] R 9 and R 10independently of one another represent a hydrogen atom or a group selected from among C1-C4-alkyl, C2-C4-hydroxyalkyl, N≡C-(C1-C4-alkyl)-, (C1-C4-alkoxy)-(C2-C4-alkyl)- and C3-C4-cycloalkyl,

[0408] or

[0409] R 9 and R 10 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group,

[0410] wherein said nitrogen-containing 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or thrice, each substituent being independently selected from among a halogen atom or a group selected from among C1-C4-alkyl, hydroxyl and oxo,

[0411] or

[0412] two substituents attached to the same carbon atom of said nitrogen-containing 4- to 7-membered heterocycloalkyl group, together with the carbon atom to which they are attached, represent a 4- to 7-membered heterocycloalkyl group,

[0413] wherein said 4- to 7-membered heterocycloalkyl group is optionally substituted once or twice by a C1-C4-alkyl group,

[0414] R 11 represents a group selected from among C1-C4-alkyl and C1-C4-haloalkyl,

[0415] R 12 represents a hydrogen atom,

[0416] R 13 represents a phenyl group,

[0417] R 14 represents a group selected from among C1-C4-alkyl and phenyl,

[0418] R 15 represents a hydrogen atom or a C1-C4-alkyl group,

[0419] R 16 represents a hydrogen atom or a C1-C4-alkyl group,

[0420] R 17 represents a 4- to 7-membered heterocycloalkyl group,

[0421] wherein said 4- to 7-membered heterocycloalkyl is optionally substituted once or twice by a C1-C4-alkyl group,

[0422] and

[0423] wherein said 4- to 7-membered heterocycloalkyl group is attached to the rest of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group,

[0424] R 18 represents a hydrogen atom or a methyl group,

[0425] R 19 represents a hydrogen atom or a methyl group,

[0426] R 20 represents a (4- to 7-membered heterocycloalkyl)-(Ci-C4-alkyl)- group,

[0427] wherein the (4- to 7-membered heterocycloalkyl) part of said group is optionally substituted one or two times by a Ci-C4-alkyl group,

[0428] m represents an integer selected from 1 and 2,

[0429] wherein the 4- to 7-membered heterocycloalkyl is optionally substituted one or two times by a Ci-C4-alkyl,

[0430] and

[0431] n represents an integer selected from 1, 2 and 3,

[0432] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[0433] In some preferred embodiments, the DGK a inhibitors are characterized by having the formula (I) as defined under this heading.

[0434] DGK alpha inhibitor embodiment C

[0435] In some other embodiments of the application, the DGK a inhibitors are compounds of formula (I) as described above, wherein

[0436] R 1 represents a group selected from cyano, -C(=0)NH2, -C(=0)N(H)CH3 and -C(=0)N(CH3)2

[0437] R 2represents a group selected from phenyl, 1 -naphthyl, 2-naphthyl, 1 H-pyrazol-3-yl, 1 H-pyrazol-4-yl, 1 H-pyrazol-5-yl, 1,2,4-oxadiazol-5-yl, 1,3,4-oxadiazol-2-yl, 1 H-1,2,3-triazol-4-yl, 2H-1,2,3-triazol-4-yl, 1,3-thiazol-2-yl, pyridin-3-yl, pyrazin-2-yl, 1 H-indol-5-yl, 1 -benzofuran-4-yl, 1 -benzofuran-7-yl, 1 H-indol-6-yl, benzothiophen-2-yl, 1,3-benzoxazol-2-yl, 1,3-benzoxazol-5-yl, 1,3-benzoxazol-6-yl, 1,3-benzoxazol-7-yl, 1 H-indazol-5-yl, 1 H-benzoimidazol-2-yl, 1 H-benzoimidazol-4-yl, 1,3-benzothiazol-2-yl, 1,3-benzothiazol-4-yl, 1,3-benzothiazol-5-yl, 1,3-benzothiazol-6-yl, 1,3-benzothiazol-7-yl, 1 H-pyrrolo[2,3-b]pyridin-3-yl, quinolin-2-yl, quinolin-4-yl, quinolin-6-yl, quinolin-7-yl, isoquinolin-5-yl, isoquinolin-7-yl, isoquinolin-8-yl, quinoxalin-2-yl, quinoxalin-5-yl and 1,3-thiazolo[5,4-b]pyridin-2-yl,

[0438] wherein the group is optionally substituted once or twice, each substituent being independently selected from a fluorine, chlorine or bromine atom or from a group selected from methyl, propyl, isopropyl, tert-butyl, cyclopropyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, propyloxy, (propan-2-yl)oxy, methoxymethyl, 2-methoxyethyl, benzyloxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, phenoxy, (oxolan-2-yl)methoxy, (tetrahydrofuran-2-yl)methoxy, methylsulfonyl, dimethylphosphoryl, cyano, hydroxy, dimethylamino, oxetan-3-yl, 2-oxopyrrolidin-1 -yl, 4-methyl-2-oxopiperazin-1 -yl, 4-methyl-3-oxopiperazin-1 -yl, morpholino-4-yl, 7-oxo-2-oxa-6-azaspiro[3.4]octan-6-yl, 8-methyl-3-oxo-2,8-diazaspiro[4.5]dec-2-yl, carbamoyl, acetyl, trifluoroacetyl, benzamido, benzenesulfonylamido, [dimethyl(oxo)-lambda 6 -phenyl, 3-chlorophenyl, 4-chlorophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 3-trifluoromethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl and pyridin-3-yl,

[0439] or

[0440] two substituents of the phenyl group, when they are attached to adjacent ring atoms, are mutually attached in such a way that they together form a group selected from -CH2-CH(OH)-CH2-, -CH2-CH(CH3)-O-, -O-C(CH3)2-O-, -NH-C(=O)-CH(CH3)-, -N(CH3)-C(=O)-C(CH3)2-, -NH-C(=O)-(C(CH2)3)-, -NH-CH2-C(CH3)2-, -N(CH3)-C(=O)-O-, and -N(CH3)-C(=O)-N(CH3)-,

[0441] R 3 represents a hydrogen atom or a fluorine, chlorine or bromine atom or a group selected from methyl, sec-butyl, (oxetan-3-yl)methyl, 3,3,3-trifluoroprop-1-en-2-yl, cyclopropyl, (trifluoromethyl)cyclopropyl, cyclobutyl, 2,2-dimethylcyclobutyl, 3,3-difluorocyclobutyl, methoxymethyl, methoxy, ethoxy, propoxy, 2,2-difluoroethoxy, 2,2-difluoropropoxy, cyclopropylmethoxy, (1-cyanocyclopropyl)methoxy, cyclopropyloxy, cyclobutyloxy, methylsulfonyl, cyano, hydroxy, 4-hydroxy-2-oxo-pyrrolidin-1-yl, 7-oxo-2-oxa-6-azaspiro[3.4]octan-6-yl, carbamoyl, dimethylphosphoryl, oxetan-3-yl, 3,6-dihydro-2H-pyran-4-yl, (oxetan-3-yl)oxy, and phenyl,

[0442] R 4 represents a hydrogen atom or a fluorine, chlorine or bromine atom or a group selected from methyl, sec-butyl, (oxetan-3-yl)methyl, trifluoromethyl, cyclopropyl, 3,3-difluorocyclobutyl, methoxymethyl, methoxy, propoxy, 2-methoxyethoxy, (1-hydroxycyclopropyl)methoxy, (1-cyanocyclopropyl)methoxy, (oxirane-2-yl)methoxy, carboxymethoxy, 2-tert-butoxy-2-oxo-ethoxy, 2-amino-2-oxo-ethoxy, cyclopropyloxy, cyclobutyloxy, methylsulfonyl, dimethylphosphoryl, cyano, nitro, hydroxy, (cyanomethyl)(methyl)amino, (2-hydroxyethyl)amino, (2-hydroxyethyl)(methyl)amino, (2-methoxyethyl)amino, (2-methoxyethyl)(methyl)amino, cyclopropylamino, (oxetan-3-yl)amino, methyl(oxetan-3-yl)amino, methyl(oxolan-3-yl)amino, 3-hydroxyazetidin-1-yl, 2-oxopyrrolidin-1-yl, morpholino, 1,1-dioxidothiomorpholin-4-yl, 4-hydroxy-2-oxo-pyrrolidin-1-yl, 7-oxo-2-oxa-6-azaspiro[3.4]octan-6-yl, 2,2-dimethyl-2lambda 6-diaza-1,2-dien-1-yl, [dimethyl(oxo)-λ 6 -sulfydene]amino, methyl(tetrahydrofuran-3-yl)amino, tetrahydrofuran-3-ylmethoxy, (tetrahydrofuran-3-ylmethyl)amino, oxetan-3-yl, 3,6-dihydro-2H-pyran-4-yl, (oxetan-3-yl)oxy, (tetrahydrofuran-3-yl)oxy, (tetrahydro-2H-pyran-3-yl)oxy, (tetrahydro-2H-pyran-4-yl)oxy and phenyl groups,

[0443] R 5 represents a hydrogen atom or a fluorine, chlorine or bromine atom or a group selected from a methyl group, a cyclopropyl group, a methoxy group, a propoxy group, a cyclopropyloxy group, a methanesulfonyl group, a cyano group, a hydroxyl group, an oxetan-3-yl group and an oxetan-3-yloxy group,

[0444] R 6 represents a hydrogen atom or a group selected from a methyl group and a hydroxymethyl group,

[0445] R 7 represents a hydrogen atom or a fluorine atom or a group selected from methyl, ethyl, methoxy and hydroxyl groups,

[0446] R 8 represents a group selected from methyl and ethyl,

[0447] as well as

[0448] n represents an integer selected from 1, 2 and 3,

[0449] or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[0450] In some preferred embodiments, the DGKa inhibitor is characterized by Formula (I) with the limitations defined under this heading.

[0451] DGK alpha inhibitor embodiment D

[0452] In some other embodiments of the present invention, the DGKa inhibitor is a compound selected from the group consisting of:

[0453] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0454] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0455] • 4-[4-(7-fluoro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0456] • 4-[4-(6-fluoro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0457] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0458] • 4-[4-(5-fluoro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0459] • 1 -Methyl-4-[4-(6-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0460] • 1 -Methyl-2-oxo-4-{4-[5-(propan-2-yl)- 1,3-benzoxazol-2-yl]piperidin- 1 -yl}- 1,2- dihydroquinoline-3-carbonitrile,

[0461] • 4-[4-(6-chloro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0462] • 4-[4-(5-bromo-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0463] • 4-[4-(5-chloro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0464] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile, • 4-[4-(5-fluoro-l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0465] • 4-[4-(6-bromo-l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0466] • 1 -Methyl-4-[4-(7-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0467] • 4-[4-(5-Chloro- 1,3-benzothiazol-2-yl)piperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0468] • 1 -Methyl-4-[4-(4-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0469] • 4-[4-(5-Chloro- 1,3-benzothiazol-2-yl)piperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0470] • 4-[4-(5-Chloro- 1,3-benzothiazol-2-yl)piperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0471] • 1 -Methyl-4-{4-methyl-4-[6-(trifluoromethoxy)- 1,3-benzoxazol-2-yl]piperidin- 1 - yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0472] • 1 -Methyl-4-{4-methyl-4-[5-(prop-2-yl)- 1,3-benzoxazol-2-yl]piperidin- 1 -yl}-2- oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0473] • 4-[4-(5,6-Difluoro- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0474] • 1 -Methyl-2-oxo-4-{4-[5-(trifluoromethyl)- 1,3-benzothiazol-2-yl]piperidin- 1 -yl}- 1,2-dihydroquinoline-3-carbonitrile,

[0475] • 4-[4-(5-tert-Butyl- 1,3-benzoxazol-2-yl)-4-methylpiperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0476] • 4-{4-[5-(Methylsulfonyl)- 1,3-benzoxazol-2-yl]-4-methylpiperidin- 1 -yl}- 1 -methyl- 2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0477] • 4-[4-(4-fluoro-1,3-benzoxazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0478] • 4-[4-(1,3-benzoxazol-2-yl)piperidin-1 -yl]-7-bromo-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0479] • 7-bromo-1 -methyl-4-{4-methyl-4-[6-(trifluoromethoxy)-1,3-benzoxazol-2-yl]piperidin- 1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0480] • 7-bromo-4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0481] • 7-bromo-1 -methyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1 -yl}- 1,2-dihydroquinoline-3-carbonitrile,

[0482] • 7-bromo-4-[4-(5,6-difluoro-1,3-benzoxazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0483] • 7-bromo-4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0484] • 4-[4-(1,3-benzothiazol-2-yl)piperidin-1 -yl]-7-bromo-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0485] • 7-bromo-1 -methyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1 -yl}- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0486] • 4-[4-(1,3-benzoxazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-7-(2-oxopyrrolidin-1 -yl)- 1,2-dihydroquinoline-3-carbonitrile,

[0487] • 4-[4-(1,3-benzothiazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-7-(2-oxopyrrolidin-1 -yl)- 1,2-dihydroquinoline-3-carbonitrile,

[0488] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0489] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0490] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0491] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0492] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0493] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0494] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0495] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0496] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0497] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0498] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0499] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0500] • 1 -Methyl-2-oxo-4-(4-{4-[2-(trifluoromethyl)pyrimidin-5- yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3-carbonitrile,

[0501] • 1 -Methyl-4-[4-(1 -methyl-1 H-indol-5-yl)piperidin-1 -yl]-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0502] • 4-[4-(3-Fluoro-5-methylphenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0503] • 4-[4-(2-Methoxyphenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0504] • 4-[4-([1,1 '-Biphenyl]-4-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0505] • 4-[4-(4-Chlorophenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0506] • 4-[4-(3-Methoxyphenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0507] • 1 -Methyl-2-oxo-4-[4-(4-phenoxyphenyl)piperidin-1 -yl]-1,2-dihydroquinoline-3-carbonitrile,

[0508] • 1 -Methyl-2-oxo-4-(4-phenylpiperidin-1 -yl)-1,2-dihydroquinoline-3-carbonitrile,

[0509] • 1 -Methyl-4-(4-methyl-4-phenylpiperidin-1 -yl)-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0510] • 1 -Methyl-2-oxo-4-{4-[4-(2-oxopyrrolidin-1 -yl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3- carbonitrile,

[0511] • 4-[4-(2-Fluorophenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0512] • 1 -Methyl-2-oxo-4-{4-[4-(trifluoromethyl)phenyl]piperidin-1 -yl}-1,2-dihydroquinoline-3- carbonitrile,

[0513] • 4-[4-(3-Fluorophenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0514] • 1 -Methyl-4-{4-[4-(morpholin-4-ylmethyl)phenyl]piperidin-1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0515] • 4-[4-(3-Cyano-2-methylphenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0516] • 4-{4-[4-(Methylsulfonyl)phenyl]piperidin-1 -yl}-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0517] • 1 -Methyl-4-{4-[4-(4-methyl-2-oxopiperazin-1 -yl)phenyl]piperidin-1 -yl}-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0518] • 4-[4-(1,3-Benzoxazol-5-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0519] • N-{3-[1 -(3-Cyano-1 -methyl-2-oxo-1,2-dihydroquinolin-4-yl)piperidin-4- yl]phenyl}benzenesulfonamide,

[0520] • 4-[4-(3-{[Dimethyl(oxo)-lambda 6 - Sulfuryl]amino}phenyl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0521] • 1 -Methyl-4-[4-(naphthalen-1 -yl)piperidin-1 -yl]-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0522] • 4-[4-(1,3-Benzothiazol-4-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0523] • 1 -Methyl-4-{4-[1 -methyl-3-(trifluoroacetyl)-1 H-indol-5-yl]piperidin-1 -yl}-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0524] • 4-[4-(1 -Benzofuran-7-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline- 3-carbonitrile,

[0525] • 4-[4-(Isoquinolin-7-yl)piperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0526] • 4-[4-(l,3-benzothiazol-7-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0527] • N-{3-[l-(3-cyano-l-methyl-2-oxo-l,2-dihydroquinolin-4-yl)piperidin-4-yl]phenyl}benzamide,

[0528] • 4-[4-(isoquinolin-8-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0529] • 4-[4-(isoquinolin-5-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0530] • l-methyl-2-oxo-4-[4-(quinoxalin-5-yl)piperidin-l-yl]-l,2-dihydroquinoline-3- carbonitrile,

[0531] • 4-{4-[3-(methylsulfonyl)phenyl]piperidin-l-yl}-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0532] • 4-[4-(4-fluorophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0533] • l-methyl-4-[4-(2-methylphenyl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0534] • l-methyl-4-[4-(4-methylphenyl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0535] • 4-[4-(3,5-dichlorophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0536] • 4-[4-(3-bromophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0537] • 4-[4-(4-cyanophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0538] • 4-{4-[3-(difluoromethyl)phenyl]piperidin-l-yl}-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile, • 4-[4-(4-bromophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0539] • 7-bromo-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0540] • 7-bromo-l-methyl-2-oxo-4-(4-phenylpiperidin-l-yl)-l,2-dihydroquinoline-3- carbonitrile,

[0541] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l,7-dimethyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0542] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-7-phenyl-l,2- dihydroquinoline-3-carbonitrile,

[0543] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3,7- dicarbonitrile,

[0544] • 7-cyclopropyl-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0545] • 7-(2,2-dimethyl-2λ 6 - diazasulfur- 1,2-dien- 1 -yl)-4-[4-(4-methoxyphenyl)piperidin- 1 -yl]- 1 -methyl-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0546] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-7-(2-oxopyrrolidin-l-yl)- l,2-dihydroquinoline-3-carbonitrile,

[0547] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-7-(oxetan-3-yl)-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0548] • 7-(methylsulfonyl)-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0549] • 7-{[dimethyl(oxo)-λ 6 - sulfido]amino}-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0550] • 7-(3,6-dihydro-2H-pyran-4-yl)-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0551] • 4-[4-(l-benzofuran-4-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0552] • 1 -methyl-2-oxo-4-(4-{4-[(prop-2-yl)oxy]phenyl}piperidin- 1 -yl)- 1,2-dihydroquinoline- 3-carboxamide,

[0553] • 1 -methyl-4-{4-methyl-4-[5-(prop-2-yl)- 1,3-benzoxazol-2-yl]piperidin- 1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0554] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-7-bromo-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carboxamide,

[0555] • 4-[4-(l,3-benzoxazol-2-yl)-4-methylpiperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carboxamide,

[0556] • 4-[4-(l,3-benzoxazol-2-yl)-4-ethylpiperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0557] • 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3- carboxamide,

[0558] • 1 -methyl-2-oxo-4-{4-[4-(trifluoromethoxy)phenyl]piperidin- 1 -yl}- 1,2-dihydroquinoline-3- carboxamide,

[0559] • 4-[4-(5,6-difluoro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carboxamide,

[0560] • 7-bromo- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0561] • 1 -methyl-4-[3-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline- 3-carbonitrile, mixture of stereoisomers,

[0562] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carboxamide,

[0563] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carboxamide,

[0564] • 1 -methyl-2-oxo-4-(4-phenylpiperidin- 1 -yl)- 1,2-dihydroquinoline-3 -carboxamide,

[0565] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-7-(oxetan-3-yl)-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0566] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-7-(2-oxopyrrolidin-l-yl)- 1,2-dihydroquinoline-3-carboxamide,

[0567] • (rac)-l-methyl-2-oxo-4-{4-[4-(propan-2-yl)phenyl]azepan-l-yl}-l,2-dihydroquinoline- 3-carbonitrile,

[0568] • l-methyl-2-oxo-4-{(4S)-4-[4-(propan-2-yl)phenyl]azepan-l-yl}-l,2-dihydroquinoline- 3-carbonitrile,

[0569] • l-methyl-2-oxo-4-{(4R)-4-[4-(propan-2-yl)phenyl]azepan-l-yl}-l,2-dihydroquinoline- 3-carbonitrile,

[0570] • (rac)-4-[4-(l,3-benzoxazol-2-yl)azepan-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0571] • l-methyl-2-oxo-4-[4-{4-[(propan-2-yl)oxy]phenyl}azepan-l-yl]-l,2-dihydroquinoline- 3-carbonitrile,

[0572] • (rac)-4-[4-(4-methoxyphenyl)azepan-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0573] • 4-[(4R)-4-(4-methoxyphenyl)azepan-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0574] • 4-[(4S)-4-(4-methoxyphenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0575] • (rac)-4-[4-(1,3-benzoxazol-2-yl)azepan-1-yl]-7-bromo-1-methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0576] • 4-[(4R)-4-(1,3-benzoxazol-2-yl)azepan-1-yl]-7-bromo-1-methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0577] • 4-[(4S)-4-(1,3-benzoxazol-2-yl)azepan-1-yl]-7-bromo-1-methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0578] • (rac)-4-[4-(4-chlorophenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0579] • 4-[(4R)-4-(4-chlorophenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0580] • 4-[(4SR)-4-(4-chlorophenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3- carbonitrile,

[0581] • (rac)-1-methyl-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile,

[0582] • (rac)-7-bromo-1-methyl-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3- carbonitrile,

[0583] • (rac)-1-methyl-7-(oxetan-3-yl)-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline- 3-carbonitrile,

[0584] • (rac)-1-methyl-7-(morpholin-4-yl)-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline- 3-carbonitrile,

[0585] • (rac)-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-4-[4-phenylazepan-1-yl]-1,2- dihydroquinoline-3-carbonitrile,

[0586] • (rac)-7-(l,l-dioxo-l lambda 6 • 7-bromo-4-[4-ethyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-l- methyl-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0587] • (rac)-7-bromo-l-methyl-2-oxo-4-[4-(5-phenyl-l,3-benzoxazol-2-yl)piperidin- 1-yl] - 1,2-dihydroquinoline-3-carboxamide,

[0588] • 7-bromo-l-methyl-2-oxo-4-[(4S)-4-phenylazepan-l-yl]-l,2-dihydroquinoline-3- carboxamide,

[0589] • 7-bromo-l-methyl-2-oxo-4-[(4S)-4-phenylazepan-l-yl]-l,2-dihydroquinoline-3- carboxamide,

[0590] • 4-[4-ethyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0591] • 7-bromo-4-[4-ethyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2- oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0592] • 4-[4-(6-methoxypyridin-3-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0593] • l-methyl-4-[4-(6-methylpyridin-3-yl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0594] • l-methyl-2-oxo-4-[4-(pyridin-3-yl)piperidin-l-yl]-l,2-dihydroquinoline-3- carbonitrile,

[0595] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-N,l-dimethyl-2-oxo-l,2-dihydroquinoline- 3-carboxamide,

[0596] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-N,N,l-trimethyl-2-oxo-l,2-dihydroquinoline- 3-carboxamide,

[0597] • l-methyl-4-[4-(l-methyl-lH-benzoimidazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0598] ●1-methyl-2-oxo-4-[4-(3-propyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile,

[0599] ●1-methyl-4-[4-(1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0600] ●1-methyl-2-oxo-4-[4-(pyrazin-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile,

[0601] ●4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0602] ●4-{4-hydroxy-4-[3-(trifluoromethyl)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0603] ●8-fluoro-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0604] ●4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-8-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0605] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-8-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0606] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-8-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0607] ●8-Bromo-4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0608] ●8-Bromo-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0609] ●8-Bromo-4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0610] • 8-bromo-4-[4-(5,6-difluoro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0611] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-8-bromo-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0612] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-8-chloro-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0613] • 1-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo- 1,2-dihydroquinoline-3,8-dicarbonitrile,

[0614] • 8-(methylsulfonyl)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)- piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0615] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-l,6-dimethyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0616] • 1,6-dimethyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0617] • 6-bromo-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0618] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-6-bromo-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0619] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-6-bromo-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0620] • 6-bromo-l-methyl-2-oxo-4-{4-[5-(propan-2-yl)-l,3-benzoxazol-2-yl]piperidin-l- yl}-l,2-dihydroquinoline-3-carbonitrile,

[0621] • 6-bromo-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0622] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l,6-dimethyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0623] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3,6- dicarbonitrile,

[0624] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-l,6-dimethyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0625] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3,6- dicarbonitrile,

[0626] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3,6- dicarbonitrile,

[0627] • 6-cyclopropyl-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0628] • 6-(methylsulfonyl)-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0629] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-6-(oxetan-3-yl)-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0630] • 6-(3,6-dihydro-2H-pyran-4-yl)-4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo- l,2-dihydroquinoline-3-carbonitrile,

[0631] • 4-[4-(4-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-6-phenyl-l,2-dihydroquinoline-3- carbonitrile,

[0632] • 6-(methylsulfonyl)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0633] • 4-[4-(6-chloro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l,6-dimethyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0634] • 1,6-Dimethyl-4-[4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0635] • 4-[4-(5-Chloro-1,3-benzoxazol-2-yl)piperidin-1 -yl]-1,6-dimethyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0636] • 1,6-Dimethyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1 - yl}-1,2-dihydroquinoline-3-carbonitrile,

[0637] • 1,6-Dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0638] • 1,6-Dimethyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0639] • 1,6-Dimethyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1 - yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0640] • 6-Methoxy-1 -methyl-4-[4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0641] • 6-Methoxy-1 -methyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0642] • 6-Chloro-1 -methyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1 - yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0643] • 4-[4-(1,3-Benzoxazol-2-yl)piperidin-1 -yl]-1,6-dimethyl-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0644] • 1,6-Dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0645] • 4-[4-(l,3-benzoxazol-2-yl)-4-methylpiperidin-l-yl]-l,6-dimethyl-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0646] • 1,6-dimethyl-4-[4-(6-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0647] • 1,6-dimethyl-4-[4-methyl-4-(6-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0648] • 1,6-dimethyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0649] • 1,6-dimethyl-4-{4-methyl-4-[5-(propan-2-yl)-l,3-benzoxazol-2-yl]piperidin- 1-yl}-2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0650] • 1,6-dimethyl-2-oxo-4-{4-[5-(propan-2-yl)-l,3-benzoxazol-2-yl]piperidin-l- yl}-l,2-dihydroquinoline-3-carboxamide,

[0651] • 4-[4-(5-chloro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l,6-dimethyl-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0652] • 4-[4-(6-chloro-l,3-benzoxazol-2-yl)piperidin-l-yl]-l,6-dimethyl-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0653] • 6-bromo-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin- 1-yl]-2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0654] • 4-[4-(l,3-benzoxazol-2-yl)azepan-l-yl]-l,6-dimethyl-2-oxo-l,2-dihydro- quinoline-3-carbonitrile,

[0655] • 4-[4-(l,3-benzoxazol-2-yl)azepan-l-yl]-l,6-dimethyl-2-oxo-l,2-dihydro- quinoline-3-carboxamide,

[0656] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-6-fluoro-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0657] • 1 -Methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin- 1 -yl]-2- oxo- 1,2-dihydroquinoline-3,6-dicarbonitrile,

[0658] • 6-Cyano-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l- yl]-2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0659] • 6-(3,3-Difluorocyclobutyl)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol- 2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0660] • 6-Cyclopropyl-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0661] • 6-(Butan-2-yl)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0662] • 7-(Methoxymethyl)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0663] • 6-(Methoxymethyl)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0664] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-l,6-dimethyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0665] • 6-Fluoro-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0666] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-6-fluoro-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0667] ●6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0668] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0669] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0670] ●1,7-dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0671] ●1,7-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0672] ●4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0673] ●4-[4-(1,3-benzoxazol-2-yl)-4-ethylpiperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0674] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0675] ●8-Bromo-1,6-dimethyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0676] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0677] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0678] • 7-Chloro-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0679] • 7-Chloro-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0680] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-8-chloro-l-methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0681] • 8-Chloro-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l- yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0682] • 8-Chloro-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0683] • 8-Bromo-l-methyl-4-{4-methyl-4-[5-methyl-4-(trifluoromethyl)-l,3-benzoxazol- 2-yl]piperidin-l-yl}-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0684] • 1-Methyl-4-[(2S,4S)-2-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0685] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-7-fluoro-l-methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0686] • 4-[4-(l,3-Benzoxazol-2-yl)piperidin-l-yl]-7-fluoro-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0687] • 7-Fluoro-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l- yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0688] • 7-Fluoro-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0689] • 7-[(1 -hydroxycyclopropyl)methoxy]- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3- benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0690] • 4-[4-( 1,3 -benzoxazol-2-yl)piperidin- 1 -yl]-7-methoxy- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0691] • 1 -Methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7- [(oxetan-3-yl)oxy]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0692] • 6-Hydroxy- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 - yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0693] • 4-[4-( 1,3 -benzoxazol-2-yl)piperidin- 1 -yl]-7-methoxy- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0694] • 7-(Cyclopropyloxy)- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2- yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0695] • 1 -Methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-8- (oxetan-3-yl)-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0696] • 6-Methoxy- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 - yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0697] • 7-(Cyclobutyloxy)- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2- yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0698] • 7-Methoxy- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 - yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0699] • 1 -Methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3,7-dicarbonitrile,

[0700] • 7-Cyclopropyl- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 - yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0701] • 7-[(l-Cyanocyclopropyl)methoxy]- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2- yl)piperidin- 1 -yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0702] • 7-(3,3-Difluorocyclobutyl)- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0703] • 1 -Methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-8-[(oxetan-3- yl)oxy]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0704] • 4-[4-(5,6-Difluoro- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-methoxy- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0705] • 1,7-Dimethyl-2-oxo-4-(4-phenylpiperidin- 1 -yl)- 1,2-dihydroquinoline-3-carbonitrile,

[0706] • 7-Methoxy- 1 -methyl-2-oxo-4-(4-phenylpiperidin- 1 -yl)- 1,2-dihydroquinoline-3- carbonitrile,

[0707] • 1 -Methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-7- propoxy- 1,2-dihydroquinoline-3-carbonitrile,

[0708] • 4-[4-(6-Chloro- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-methoxy- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0709] • 4-[4-(5-Chloro- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-methoxy- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0710] • 8-methoxy- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]- 2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0711] • 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-(oxetan-3- yl)-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0712] • 8-(cyclopropyloxy)- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 - yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0713] • 1,8-dimethyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0714] • 7-(cyclopropyloxy)- 1 -methyl-2-oxo-4-(4-phenylpiperidin- 1 -yl)- 1,2-dihydroquinoline-3- carbonitrile,

[0715] • 4-{4-[4-(2-methoxyethyl)- 1,3-benzoxazol-2-yl]piperidin- 1 -yl}- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0716] • 7-[(2S)-butan-2-yl]- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 - yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0717] • 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-6-[(oxetan-3- yl)oxy]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0718] • 6-[( 1 -cyanocyclopropyl)methoxy]- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2- yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0719] • 7-[(4R)-4-hydroxy-2-oxopyrrolidin- 1 -yl]- 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol- 2-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0720] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0721] • 8-hydroxy-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0722] • 8-cyclopropyl-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0723] • 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-8-propoxy- 1,2- dihydroquinoline-3-carbonitrile,

[0724] • 6-(cyclopropyloxy)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0725] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3,7- dicarbonitrile,

[0726] • 4-[4-(l,3-benzothiazol-2-yl)piperidin-l-yl]-6-cyclopropyl-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0727] • 6-[(4R)-4-hydroxy-2-oxopyrrolidin-l-yl]-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol- 2-yl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0728] • 6-(cyclobutyloxy)-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carbonitrile,

[0729] • 1 -methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-6-propoxy- 1,2- dihydroquinoline-3-carbonitrile,

[0730] • 6-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-1-methyl-4-[4-methyl-4-(5-methyl-1,3- benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0731] • 7-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0732] • 7-(dimethylphosphoryl)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0733] • 4-{4-[5-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0734] • 4-{4-[6-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0735] • 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxetan-3- yl)methyl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0736] • 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-[(oxetan-3- yl)methyl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0737] • 1-methyl-4-{4-[5-(oxetan-3-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0738] • 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2- dihydroquinoline-3-carbonitrile,

[0739] • 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(trifluoromethyl)- 1,2-dihydroquinoline-3-carbonitrile,

[0740] ●1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile,

[0741] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile,

[0742] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile,

[0743] ●7-hydroxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0744] ●4-[4-(6-bromo-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0745] ●4-{4-[5-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0746] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-6-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0747] ●4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0748] ●6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0749] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-6-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0750] ●4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0751] • 7-Chloro-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0752] • 1 -Methyl-4-[4-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0753] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-7-fluoro-l-methyl-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0754] • 7-Fluoro-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0755] • 4-[4-(l,3-Benzoxazol-2-yl)piperidin-l-yl]-7-fluoro-l-methyl-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0756] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-l-methyl-2-oxo-7- (trifluoromethyl)- 1,2-dihydroquinoline-3-carboxamide,

[0757] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-7- (trifluoromethyl)- 1,2-dihydroquinoline-3-carboxamide,

[0758] • 4-[4-(l,3-Benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-7-(trifluoromethyl)- 1,2- dihydroquinoline-3-carboxamide,

[0759] • 4-[4-(l,3-Benzoxazol-2-yl)piperidin-l-yl]-8-chloro-l-methyl-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0760] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-8-chloro-l-methyl-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0761] • 4-[4-(l,3-Benzoxazol-2-yl)-4-methylpiperidin-l-yl]-l,7-dimethyl-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0762] • 1,7-Dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0763] • 1,7-Dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0764] • 4-[4-(1,3-Benzoxazol-2-yl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline- 3-carboxamide,

[0765] • 4-{4-[4-(2-Methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0766] • 4-[4-(1,3-Benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3- carboxamide,

[0767] • 4-{4-[6-(2-Methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0768] • 4-[4-(1,3-Benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)- 1,2-dihydroquinoline-3-carboxamide,

[0769] • 8-Chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0770] • 4-[4-(4,5-Dimethyl-1,3-thiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline- 3-carbonitrile,

[0771] • 1-Methyl-2-oxo-4-[4-(quinoxalin-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile,

[0772] • 1-Methyl-2-oxo-4-[4-(1H-pyrazol-3-yl)piperidin-1-yl]-1,2-dihydroquinoline-3- carbonitrile,

[0773] • 1-Methyl-4-[4-(1-methyl-1H-pyrazol-4-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline- 3-carbonitrile,

[0774] • 4-[4-(3,4-dimethoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carbonitrile,

[0775] • 4-[4-(3-chlorophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0776] • 1 -methyl-4-[(2S,4S)-2-methyl-4-(5-methyl- 1,3-benzoxazol-2-yl)- 1 -piperidinyl]-2- oxo-quinoline-3-carbonitrile,

[0777] • 4-[4-(3-cyanophenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0778] • 8-fluoro-l-methyl-2-oxo-4-[(4S)-4-phenylazepan-l-yl]-l,2-dihydroquinoline-3- carbonitrile,

[0779] • 1 -methyl-4-[rac-(2R,3S)-2-methyl-3-phenylpyrrolidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline- 3-carbonitrile,

[0780] • 4-[l-(3-cyano-l-methyl-2-oxo-l,2-dihydroquinolin-4-yl)piperidin-4-yl]benzamide,

[0781] • 4-[4-hydroxy-4-(2-methoxyphenyl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0782] • 4-[4-(l,3-benzoxazol-2-yl)piperidin-l-yl]-l-ethyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0783] • 4-[4-(4-chlorophenyl)piperidin-l-yl]-l-ethyl-2-oxo-l,2-dihydroquinoline-3- carbonitrile,

[0784] • 1 -methyl-2-oxo-4-{4-[5-(2-oxopyrrolidin- 1 -yl)- 1,3-benzoxazol-2-yl]piperidin- 1 -yl}- 1,2- dihydroquinoline-3-carbonitrile,

[0785] • 4-[4-(4-acetylphenyl)-4-methylpiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0786] • 4-[4-(3-chlorophenyl)-4-methoxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0787] • 6-(dimethylphosphoryl)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0788] • 6-(dimethylphosphoryl)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0789] • 6-(dimethylphosphoryl)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0790] • 4-[4-(l-benzothiophen-2-yl)-4-hydroxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0791] • 4-[4-(l-benzothiophen-2-yl)-4-hydroxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0792] • 4-[4-(l-benzothiophen-2-yl)-4-hydroxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0793] • 4-[4-(l-benzothiophen-2-yl)-4-hydroxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0794] • 6-[l-(3-cyano-l-methyl-2-oxo-l,2-dihydroquinolin-4-yl)piperidin-4-yl]-2-methylquinoline- 4-carbonitrile,

[0795] • 1 -methyl-4-[4-(2-methyl- 1,3-benzoxazol-5-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline- 3-carbonitrile,

[0796] • 1 -methyl-4-[4-(2-methyl- 1,3-benzoxazol-5-yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline- 3-carbonitrile,

[0797] • (rac)-l-methyl-4-[4-(3-methyl-2-oxo-2,3-dihydro-lH-indol-5-yl)piperidin-l-yl]-2-oxo- l,2-dihydroquinoline-3-carbonitrile,

[0798] • 1 -Methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0799] • 4-{4-[3-(4-Methoxyphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 -yl}-1 -methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0800] • 1 -Methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0801] • 1 -Methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0802] • 1 -Methyl-4-{4-[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0803] • 1 -Methyl-4-{4-[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0804] • 4-{4-[5-(3-Chlorophenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}-1 -methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0805] • 4-{4-[5-(3-Chlorophenyl)-1,3,4-oxadiazol-2-yl]-4-methylpiperidin-1 -yl}-1 -methyl- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0806] • 4-[4-(3,3-Dimethyl-2,3-dihydro-1 H-indol-5-yl)piperidin-1 -yl]-1 -methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0807] • 1 -Methyl-4-{4-[(2R)-2-methyl-2,3-dihydro-1 -benzofuran-5-yl]piperidin-1 -yl}-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0808] • 1 -Methyl-2-oxo-4-[4-(1,3,3-trimethyl-2-oxo-2,3-dihydro-1 H-indol-5-yl)piperidin-1 - yl]-1,2-dihydroquinoline-3-carbonitrile,

[0809] • 4-[4-(2-hydroxy-2,3-dihydro-lH-inden-5-yl)piperidin-l-yl]-l-methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0810] • 4-[4-(2,2-dimethyl-2H-l,3-benzodioxol-5-yl)piperidin-l-yl]-l-methyl-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0811] • 1 -methyl-2-oxo-4-[4-(2'-oxo- 1 ',2'-dihydrospiro[cyclobutane- 1,3 '-indol]-5'- yl)piperidin-l-yl]-l,2-dihydroquinoline-3-carbonitrile,

[0812] • 1 -methyl-4-[4-(3-methyl-2-oxo-2,3-dihydro- 1,3-benzoxazol-6-yl)piperidin- 1 -yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0813] • 4-[4-(l,3-dimethyl-2-oxo-2,3-dihydro-lH-benzimidazol-5-yl)piperidin-l-yl]-l- methyl-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0814] • 1 -methyl-4-[4-methyl-4-(4-methylquinolin-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0815] • 4-[4-(4-fluoro-l-methyl-lH-indol-6-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0816] • 1 -methyl-4-{4-[ 1 -(3-methylphenyl)- 1 H-pyrazol-3 -yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0817] • 1 -methyl-4-{4-[ 1 -(2-methylphenyl)- 1 H-pyrazol-3 -yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carbonitrile,

[0818] • 4-{4-[l-(3-chlorophenyl)-lH-pyrazol-3-yl]piperidin-l-yl}-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0819] • 4-{4-[l-(4-chlorophenyl)-lH-pyrazol-3-yl]piperidin-l-yl}-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0820] ●1-methyl-2-oxo-4-{4-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile,

[0821] ●1-methyl-4-[4-(2-methylquinolin-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0822] ●4-{4-[4-(3-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0823] ●4-{4-[4-(2-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0824] ●1-methyl-4-{4-[4-(4-methylphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0825] ●4-[4-(1,3-dimethyl-1H-indazol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0826] ●1-methyl-4-[4-(2-methyl-1,3-benzoxazol-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0827] ●1-methyl-4-[4-(2-methyl-1,3-benzothiazol-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0828] ●4-{4-[3-(difluoromethyl)quinolin-7-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0829] ●(rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[0830] ●1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile,

[0831] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0832] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0833] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0834] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0835] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0836] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0837] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0838] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0839] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0840] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0841] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{[(3S)- oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[0842] • 4-{4-[6-(methyloxy methyl)-l,3-benzoxazol-2-yl]-4-methylpiperidin-l-yl}-l- methyl-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0843] • 4-[4-(5-cyclopropyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0844] • 4-[4-(5-cyclopropyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0845] • 4-[4-(5-cyclopropyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0846] • 6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0847] • 6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0848] • 6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0849] • 6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0850] • 6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0851] • 6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3-carbonitrile,

[0852] • 6-ethoxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0853] • 1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-6-(3,3,3- trifluoroprop-1 -en-2-yl)-1,2-dihydroquinoline-3-carbonitrile,

[0854] • 3-cyano-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-1,2- dihydroquinoline-6-carboxamide,

[0855] • 6-ethoxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0856] • 6-(2,2-difluoropropoxy)-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 - yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0857] • 6-(2,2-difluoroethoxy)-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 - yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0858] • 6-(cyclopropylmethoxy)-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 - yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0859] • 6-cyclobutyl-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carbonitrile,

[0860] • 6-[2,2-dimethylcyclobutyl]-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0861] • 1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-6-(3,3,3- trifluoroprop-1 -en-2-yl)-1,2-dihydroquinoline-3-carbonitrile,

[0862] • 1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-6-[1 -(trifluoro- methyl)cyclopropyl]-1,2-dihydroquinoline-3-carbonitrile,

[0863] • 2-({3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2- oxo-1,2-dihydroquinolin-7-yl}oxy)acetamide,

[0864] • 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{[oxan-3- yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0865] • (rac)-({3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2- oxo-1,2-dihydroquinolin-7-yl}oxy)acetic acid tert-butyl ester,

[0866] • ({3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo- 1,2-dihydroquinolin-7-yl}oxy)acetic acid,

[0867] • (rac)-4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2- oxo-7-(tetrahydrofuran-3-yloxy)-1,2-dihydroquinoline-3-carbonitrile,

[0868] • 7-(cyclopropylamino)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2- yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0869] • 7-methoxy-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0870] • 6-bromo-4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7- methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0871] • 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-nitro-2- oxo-1,2-dihydroquinoline-3-carbonitrile,

[0872] • 6-bromo-7-hydroxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1- yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0873] • 6-bromo-7-hydroxy-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[0874] • (rac)-6-bromo-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-7-[(oxolan-3- yl)oxy]-l,2-dihydroquinoline-3-carbonitrile,

[0875] • (rac)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-7-[tetrahydrofuran-3- yloxy]-l,2-dihydroquinoline-3,6-dicarbonitrile,

[0876] • 7-hydroxy-l-methyl-4-[4-methyl-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2- dihydroquinoline-3,6-dicarbonitrile,

[0877] • (rac)-6-ethoxy-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-7-[tetrahydro- furan-3-yloxy]-l,2-dihydroquinoline-3-carbonitrile,

[0878] • 7-hydroxy-l,6-dimethyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2-dihydro- quinoline-3-carbonitrile,

[0879] • (rac)-l,6-dimethyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo-7-[tetrahydrofuran- 3-yloxy]-l,2-dihydroquinoline-3-carbonitrile,

[0880] • (rac)-6-(2,2-difluoroethoxy)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2-oxo- 7-[tetrahydrofuran-3-yloxy]-l,2-dihydroquinoline-3-carbonitrile,

[0881] • (rac)-4-[4-fluoro-4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-6-methoxy-l-methyl-2-oxo-7- [tetrahydrofuran-3-yloxy]-l,2-dihydroquinoline-3-carbonitrile,

[0882] • (rac)-1 -Methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- [(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3,6-dicarbonitrile,

[0883] • (rac)-1 -Methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- [(oxolan-3-yl)oxy]-6-(3,3,3-trifluoroprop-1 -en-2-yl)-1,2-dihydroquinoline-3-carbonitrile,

[0884] • (rac)-1 -Methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- [(oxolan-3-yl)oxy]-6-[1 -(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carbonitrile,

[0885] • 6-Bromo-1 -methyl-2-oxo-4-(4-{5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2- yl}piperidin-1 -yl)-1,2-dihydroquinoline-3-carbonitrile,

[0886] • 6-Methoxy-1 -methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 -yl}- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0887] • 6-Methoxy-1 -methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1 -yl]- 1,2-dihydroquinoline-3-carbonitrile,

[0888] • 6-Methoxy-1 -methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 -yl}- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0889] • 6-Methoxy-1 -methyl-2-oxo-4-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)piperidin-1 -yl]- 1,2-dihydroquinoline-3-carbonitrile,

[0890] • 6-Bromo-1 -methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1 -yl]- 1,2-dihydroquinoline-3-carbonitrile,

[0891] • 6-Bromo-1 -methyl-2-oxo-4-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)piperidin-1 -yl]- 1,2-dihydroquinoline-3-carbonitrile,

[0892] • 6-bromo-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin- 1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0893] • 6-bromo-1 -methyl-4-{4-[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin- 1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0894] • 7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin- 1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0895] • 6-bromo-7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0896] • (rac)-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}- 7-{[oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0897] • 4-[4-(1,3-benzoxazol-2-yl)piperidin-1 -yl]-N,1 -dimethyl-2-oxo-1,2-dihydro- quinoline-3-carboxamide,

[0898] • N,1 -dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0899] • 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1 -yl]-N,1 -dimethyl-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0900] • 1 -methyl-2-oxo-4-{4-[5-(2-oxopyrrolidin-1 -yl)-1,3-benzoxazol-2-yl]piperidin- 1 -yl}-1,2-dihydroquinoline-3-carboxamide,

[0901] • 4-[4-(3-chlorophenyl)-4-methoxypiperidin-1 -yl]-1 -methyl-2-oxo-1,2-dihydro- quinoline-3-carboxamide,

[0902] • 6-(dimethylphosphoryl)-1 -methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2- yl)piperidin-1 -yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0903] • 6-(dimethylphosphoryl)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]- 2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0904] • 6-(methylsulfonyl)-l-methyl-4-[4-(5-methyl-l,3-benzoxazol-2-yl)piperidin-l-yl]-2- oxo-l,2-dihydroquinoline-3-carboxamide,

[0905] • 4-[4-(l-benzothiophen-2-yl)-4-methoxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0906] • 4-[4-(l-benzothiophen-2-yl)-4-hydroxypiperidin-l-yl]-l-methyl-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0907] • 4-[4-(6-methoxynaphthalen-2-yl)piperidin-l-yl]-l-methyl-2-oxo-l,2-dihydroquinoline- 3-carboxamide,

[0908] • 1 -methyl-4-{4-[3-(2-methylphenyl)- 1,2,4-oxadiazol-5-yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0909] • 4-{4-[3-(4-methoxyphenyl)-l,2,4-oxadiazol-5-yl]piperidin-l-yl}-l-methyl-2-oxo-l,2- dihydroquinoline-3-carboxamide,

[0910] • 1 -methyl-4-{4-[3-(3-methylphenyl)- 1,2,4-oxadiazol-5-yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0911] • 1 -methyl-4-{4-[5-(2-methylphenyl)- 1,3,4-oxadiazol-2-yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0912] • 1 -methyl-4-{4-[5-(4-methylphenyl)- 1,3,4-oxadiazol-2-yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0913] • 1 -methyl-4-{4-[5-(3-methylphenyl)- 1,3,4-oxadiazol-2-yl]piperidin- 1 -yl}-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0914] ●4-{4-[5-(3-chlorophenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0915] ●4-{4-[5-(3-chlorophenyl)-1,3,4-oxadiazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0916] ●1-methyl-4-{4-[2-methyl-2,3-dihydro-1-benzofuran-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0917] ●4-[4-(2-hydroxy-2,3-dihydro-1H-inden-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0918] ●4-[4-(2,2-dimethyl-2H-1,3-benzodioxol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0919] ●1-methyl-2-oxo-4-[4-(2'-oxo-1',2'-dihydrospiro[cyclobutane-1,3'-indole]-5'-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide,

[0920] ●1-methyl-4-[4-methyl-4-(4-methylquinolin-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0921] ●4-[4-(4-fluoro-1-methyl-1H-indol-6-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0922] ●1-methyl-4-{4-[1-(3-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0923] ●1-methyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0924] ●4-{4-[1-(3-chlorophenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0925] ●1-methyl-2-oxo-4-{4-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carboxamide,

[0926] ●4-{4-[4-(3-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0927] ●4-{4-[4-(2-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0928] ●1-methyl-4-{4-[4-(4-methylphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0929] ●1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxan-4-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0930] ●7-(2-methoxyethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0931] ●1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{[oxiran-2-yl]methoxy}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0932] ●(rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0933] ●(-)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0934] ●(+)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0935] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-[(oxetan-3- yl)methoxy]-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0936] • 4-[4-(5-Methoxy- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0937] • 1 -Methyl-2-oxo-4-(4-{5-[(oxetan-2-yl)methoxy]- 1,3-benzoxazol-2-yl}piperidin- 1 - yl)- 1,2-dihydroquinoline-3-carboxamide,

[0938] • 4-[4-( 1,3-Benzoxazol-2-yl)-4-fluoropiperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0939] • 4-[4-( 1,3-Benzoxazol-2-yl)-4-methoxypiperidin- 1 -yl]- 1 -methyl-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0940] • 4-{4-[5-(Methoxymethyl)- 1,3-benzoxazol-2-yl]-4-methylpiperidin- 1 -yl}- 1 -methyl- 2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0941] • 4-{4-[6-(Methoxymethyl)- 1,3-benzoxazol-2-yl]-4-methylpiperidin- 1 -yl}- 1 -methyl- 2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0942] • 6-Bromo- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0943] • 8-Bromo- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0944] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-[methyl(oxetan-3- yl)amino]-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0945] • 7-[(2-Hydroxyethyl)(methyl)amino]- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2- yl)piperidin- 1 -yl]-2-oxo- 1,2-dihydroquinoline-3-carboxamide,

[0946] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{methyl[(3R)- oxolane-3-yl]amino}-2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0947] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-7-{methyl[(3S)- oxolane-3-yl]amino}-2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0948] • 6-Cyano- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0949] • 1 -Methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-l,2-dihydroquinoline- 3,6-dicarboxamide,

[0950] • 7-[(Cyanomethyl)(methyl)amino]- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0951] • 6-Methoxy- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0952] • 6-Ethoxy- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo- 1,2- dihydroquinoline-3-carboxamide,

[0953] • 6-(2,2-Difluoropropoxy)- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]- 2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0954] • 6-(2,2-Difluoroethoxy)- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]- 2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0955] • 6-(Cyclopropylmethoxy)- 1 -methyl-4-[4-(5-methyl- 1,3-benzoxazol-2-yl)piperidin- 1 -yl]- 2-oxo-l,2-dihydroquinoline-3-carboxamide,

[0956] • 6-cyclobutyl-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0957] • 1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-6-[1 -(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carboxamide,

[0958] • 7-(2-amino-2-oxoethoxy)-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 - yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0959] • 4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-1 -methyl-2-oxo-7- [(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0960] • 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-7-nitro-2-oxo-1,2- dihydroquinoline-3-carboxamide,

[0961] • 6-bromo-7-hydroxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0962] • 6-bromo-7-hydroxy-1 -methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0963] • (rac)-6-bromo-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo- 7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0964] • (rac)-6-cyano-1 -methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 - yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0965] • 6-cyano-1 -methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2- oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0966] ●6-cyano-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0967] ●(rac)-6-(2,2-difluoroethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0968] ●(rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-6-[1-(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carboxamide,

[0969] ●6-bromo-1-methyl-2-oxo-4-(4-{5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl}piperidin-1-yl)-1,2-dihydroquinoline-3-carboxamide,

[0970] ●6-methoxy-1-methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0971] ●6-methoxy-1-methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide,

[0972] ●6-methoxy-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0973] ●6-bromo-1-methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide,

[0974] ●6-bromo-1-methyl-2-oxo-4-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide,

[0975] • 6-bromo-7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0976] • 6-bromo-7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0977] • 1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}-7-{[(3R)- oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0978] • 1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1 -yl}-7-{[(3S)- oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0979] • 6-bromo-7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0980] • 6-bromo-7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0981] • 6-bromo-7-hydroxy-1 -methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide,

[0982] • (rac)-6-bromo-1 -methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 - yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[0983] • (rac)-6-bromo-1 -methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1 - yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[0984] • (rac)-6-cyano-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}- 2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0985] • 6-cyano-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo- 7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0986] • 6-cyano-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo- 7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0987] • (-)-6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)- oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile,

[0988] • (rac)-6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7- [(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0989] • 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)- oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0990] • 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)- oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0991] • 6-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)- oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile,

[0992] • 6-methoxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- [(oxan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0993] • 6-methoxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- [(oxan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0994] • (rac)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7-[(oxan- 3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[0995] • 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7-{[(3R)- oxan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0996] • 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7-{[(3S)- oxan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[0997] • 7-[(2-methoxyethyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0998] • 7-(3-hydroxyazetidin-1 -yl)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[0999] • 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-7-[(oxetan-3-yl)amino]- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[1000] • 7-[(2-hydroxyethyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin- 1 -yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[1001] • 7-[(2-hydroxyethyl)(methyl)amino]-l,6-dimethyl-4-[4-(5-methyl-l,3- benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[1002] • 7-[(2-hydroxyethyl)(methyl)amino]-l,6-dimethyl-4-[4-(5-methyl-l,3- benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[1003] • 7-[(2-hydroxyethyl)(methyl)amino]-l,6-dimethyl-4-[4-(5-methyl-l,3- benzoxazol-2-yl)piperidin-l-yl]-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[1004] • (rac)-l,6-dimethyl-4-{4-[3-(2-methylphenyl)-l,2,4-oxadiazol-5-yl]piperidin-l-yl}- 2-oxo-7-[(oxolan-3-yl)oxy]-l,2-dihydroquinoline-3-carbonitrile,

[1005] • 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-l,2,4-oxadiazol-5-yl]piperidin-l-yl}-2- oxo-7-{[(3R)-oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[1006] • 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-l,2,4-oxadiazol-5-yl]piperidin-l-yl}-2- oxo-7-{[(3S)-oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[1007] • 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-l,2,4-oxadiazol-5-yl]piperidin-l-yl}-2- oxo-7-{[(3R)-oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[1008] • 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-l,2,4-oxadiazol-5-yl]piperidin-l-yl}-2- oxo-7-{[(3S)-oxolan-3-yl]oxy}-l,2-dihydroquinoline-3-carbonitrile,

[1009] • 7-[(2-hydroxyethyl)(methyl)amino]-l,6-dimethyl-4-{4-[3-(2-methylphenyl)-l,2,4- oxadiazol-5-yl]piperidin-l-yl}-2-oxo-l,2-dihydroquinoline-3-carbonitrile,

[1010] • 7-bromo-1,6-dimethyl-4-{4-[1 -(2-methylphenyl)-1 H-pyrazol-3-yl]piperidin- 1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[1011] • 7-[(2-hydroxyethyl)amino]-1,6-dimethyl-4-{4-[1 -(2-methylphenyl)-1 H-pyrazol-3- yl]piperidin-1 -yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[1012] • 6-bromo-7-fluoro-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carboxamide,

[1013] • 6-cyano-7-fluoro-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carboxamide,

[1014] • (rac)-6-cyano-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2- oxo-7-{[(oxolan-3-yl)methyl]amino}-1,2-dihydroquinoline-3-carboxamide,

[1015] • 6-cyano-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- ({[(3R)-oxolan-3-yl]methyl}amino)-1,2-dihydroquinoline-3-carboxamide,

[1016] • 6-cyano-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-7- ({[(3S)-oxolan-3-yl]methyl}amino)-1,2-dihydroquinoline-3-carboxamide,

[1017] • 6-chloro-7-methoxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[1018] • 6-chloro-7-hydroxy-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]- 2-oxo-1,2-dihydroquinoline-3-carbonitrile,

[1019] • (rac)-6-chloro-1 -methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2- oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[1020] ●(rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide,

[1021] ●6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[1022] ●6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide,

[1023] ●(rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)methoxy]-1,2-dihydroquinoline-3-carbonitrile,

[1024] ●(rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)methoxy]-1,2-dihydroquinoline-3-carboxamide,

[1025] ●6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]methoxy}-1,2-dihydroquinoline-3-carboxamide,

[1026] ●6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]methoxy}-1,2-dihydroquinoline-3-carboxamide,

[1027] ●(rac)-6-bromo-1-methyl-2-oxo-7-[(oxolan-3-yl)oxy]-4-{4-[2-(pyridin-3-yl)-2H-1,2,3-triazol-4-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile,

[1028] • (rac)-6-bromo-1 -methyl-4-{4-[1 -(2-methylphenyl)-1 H-1,2,3-triazol-4-yl]piperidin- 1 -yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[1029] • (rac)-1,6-dimethyl-4-{4-[1 -(2-methylphenyl)-1 H-1,2,3-triazol-4-yl]piperidin-1 -yl}-2- oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[1030] • 7-bromo-1,6-dimethyl-4-{4-[1 -(2-methylphenyl)-1 H-pyrazol-4-yl]piperidin-1 -yl}-2- oxo-1,2-dihydroquinoline-3-carbonitrile, and

[1031] • (rac)-1,6-dimethyl-4-{4-[1 -(2-methylphenyl)-1 H-pyrazol-4-yl]piperidin-1 -yl}-2-oxo-7- [(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile,

[1032] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1033] In some preferred embodiments, the DGK a inhibitor is a compound according to this list.

[1034] DGK a inhibitor A

[1035] In a preferred embodiment of the application, the DGK a inhibitor is 6-fluoro-1 -methyl-4-[4-(5- methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, or a tautomer, N-oxide, hydrate, solvate, or salt thereof, or a mixture of same.

[1036] In another preferred embodiment of the application, the DGK a inhibitor is 6-fluoro-1 -methyl-4-[4-(5- methyl-1,3-benzoxazol-2-yl)piperidin-1 -yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide.

[1037] In another preferred embodiment of the application, the DGK a inhibitor is DGK a inhibitor A of the following structure

[1038]

[1039] or a tautomer, N-oxide, hydrate, solvate, or salt thereof, or a mixture of same.

[1040] In another preferred embodiment of the application, the DGK a inhibitor is DGK a inhibitor A of the following structure:

[1041]

[1042] The synthesis of DGK a inhibitor A is described in International Patent Application PCT / EP2020 / 083198, published as WO 2021 / 105117 Al, Example 298. International Patent Application PCT / EP2020 / 083198 also discloses methods of preparing other compounds of formula (I) mentioned herein.

[1043] DGK z inhibitor

[1044] DGK zeta inhibitor embodiment A

[1045] In the following, DGK z inhibitors are described, which can preferably be used in the application according to any one of the first, second, third, fourth, fifth, sixth, seventh, eighth or ninth aspect of the application.

[1046] In some embodiments of the application, the DGK z inhibitor is a compound of formula (II)

[1047]

[1048] wherein:

[1049] R 1 represents a phenyl or 6-membered heteroaryl group, optionally substituted once, twice or thrice, each substituent being independently selected from a halogen atom or from a group consisting of hydroxyl, cyano, nitro, Ci-C6-alkyl, (phenyl)-(Ci-C3-alkyl)-, Ci-C6-haloalkyl, Ci-C6-alkoxy, (phenyl)-(Ci-C3-alkoxy)-, Ci-C6-haloalkoxy, -N(R 5 )(R 6 ),

[1050] wherein the phenyl group in said (phenyl)-(Ci-C3-alkyl)- and (phenyl)-(Ci-C3-alkoxy)- groups is optionally substituted once or twice, each substituent being independently selected from a halogen atom or from a group consisting of cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[1051] or two substituents linked to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a bivalent radical selected from -(CH2)3-, -(CH2)4-, -(CH2)2-0-, -(CH2)3-0-, -CH2-0-CH2-, -(CH2)2-0-CH2-, -0-CH2-0-, -0-CH2-CH2-0-, -0-CF2-0-, -0-CH2-CF2-0-, and -0-CF2-CF2-0-, or two substituents linked to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a bivalent radical of the formula -(C=0)-(CH2)2-0-CH2-CH2-;

[1052] or

[1053] R 1 represents a 5-membered heteroaryl group, optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano, C1-C3-alkyl and C1-C3-alkoxy;

[1054] R 2 represents a group,

[1055] wherein the “*” represents the site of attachment to the nitrogen atom; 2 ;

[1056] R 3 represents a group selected from methyl and -NH2;

[1057] R 4 represents a phenyl or 6-membered heteroaryl group, optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, nitro, C1-C6-alkyl, (phenyl)-C1-C3-alkyl)-, (5 or 6-membered heteroaryl)-(C1-C3-alkyl)-, (C3-C7-cycloalkyl)-(C1-C3-alkyl)-, ((R 9 )O)-(C1-C6-alkyl)-, C1-C6-haloalkyl, C3-C7-cycloalkyl, -OR 9 , -N(R 10 )(R 11 ), ((R 10 )(R 11 )N)-(C1-C3-alkyl)-, -C(=0)-N(R 12 )(R 13 ), -S(=0)n-R 14 , -C(=0)R 14 , -C(=0)-OR 17 and 5 or 6-membered heteroaryl optionally substituted with one or two substituents selected from a halogen atom and a methyl group,

[1058] or two substituents attached to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a bivalent radical selected from -(CH2)3-, -(CH2)4-, -(CH2)2-0-, -(CH2)3-0-, -CH2-0-CH2-, -(CH2)2-0-CH2-, -0-CH2-0-, -0-CH2-CH2-0-, -0-CF2-0-, -0-CH2-CF2-0-, and -0-CF2-CF2-0-;

[1059] R 5 and R 6 independently of one another represent a hydrogen atom or a radical selected from among C1-C4-alkyl, (C1-C4-alkyl)-C(=0)-, C3-C4-cycloalkyl and (phenyl)-(C1-C3-alkyl)-, or

[1060] R 5 and R 6 together with the nitrogen atom to which they are attached represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once, twice or thrice, each substituent being independently selected from a halogen atom or a radical selected from among oxo, hydroxyl, C1-C4-alkyl, (C1-C4-alkyl)-C(=0)-, C3-C4-cycloalkyl and C1-C4-alkoxy;

[1061] R 7 represents a hydrogen atom or a C1-C2-alkyl radical;

[1062] R 8 represents a radical selected from -C(=0)-NH2and -S(=0)2-NH2;

[1063] R 9 represents a hydrogen atom or a radical selected from among C1-C6-alkyl, (5- or 6-membered heteroaryl)-(C1-C3-alkyl)-, (phenyl)-(C1-C3-alkyl)-, C1-C6-haloalkyl, C2-C4-hydroxyalkyl, (C1-C3-alkoxy)-C2-C3-alkyl-, ((C1-C3-alkyl)-C(=0)-0)-C2-C3-alkyl-, C(R 18 )(R 19 -C(=0)-OR 17 , -C(R 18 )(R 19 -C(=0)-N(R 20 )(R 21 ), -C(=0)-N(R 20 )(R 21 ), phenyl and 5- or 6-membered heteroaryl,

[1064] wherein the phenyl group in said (phenyl)-(Ci-C3-alkyl)- group and said phenyl group itself, and the 5 or 6 membered heteroaryl group in said (5 or 6 membered heteroaryl)-(Ci-C3-alkyl)- group and said 5 or 6 membered heteroaryl group itself are optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy;

[1065] R 10 and R 11 independently of one another represent a hydrogen atom or a group selected from Ci-C4-alkyl, Ci-C4-haloalkyl, C2-C4-hydroxyalkyl, (Ci-C3-alkoxy)-C2-C3-alkyl-, ((R 22 )(R 23 )N)-C2-C3-alkyl, (C3-C7-cycloalkyl)-(Ci-C3-alkyl)-, (Ci-C4-alkyl)-C(=0)-, C3-C7-cycloalkyl, (C3-C7-cycloalkyl)-C(=0)-, (phenyl)-(Ci-C3-alkyl)-, (phenyl)-(Ci-C3-alkyl)-C(=0)-, (phenyl)-(Ci-C3-alkyl)-0-C(=0)-, phenyl and 5 or 6 membered heteroaryl,

[1066] wherein the C3-C7-cycloalkyl group and the C3-C7-cycloalkyl groups in said (C3-C7-cycloalkyl)-(Ci-C3-alkyl)- and (C3-C7-cycloalkyl)-C(=0)- groups are optionally substituted one or two times, each substituent being independently selected from a fluorine atom or a group selected from cyano, Ci-C2-alkyl and Ci-C2-haloalkyl,

[1067] and wherein said phenyl and said 5 or 6 membered heteroaryl groups, and the phenyl groups in said (phenyl)-(Ci-C3-alkyl)-, (phenyl)-(Ci-C3-alkyl)-C(=0)- and (phenyl)-(Ci-C3-alkyl)-0-C(=0)- groups are optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[1068] or

[1069] R 10 and R 11together with the nitrogen atom to which they are attached, represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group or a bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl group, which is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or from a group selected from cyano, oxo, hydroxyl, C1-C4-alkyl, C1-C4-haloalkyl, (C1-C4-alkyl)-C(=0)-, C3-C7-cycloalkyl, C1-C4-alkoxy, -N(R 22 23 ) and a monocyclic 4- to 7-membered heterocycloalkyl group;

[1070] R 12 and R 13 independently of one another represent a hydrogen atom or a group selected from C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-hydroxyalkyl, (C1-C4-alkoxy)-C2-C3-alkyl-, (C1-C4-haloalkoxy)-C2-C3-alkyl-, (phenoxy)-C2-C3-alkyl-, C3-C7-cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C1-C3-alkyl)-,

[1071] wherein said C3-C7-cycloalkyl and monocyclic 4- to 7-membered heterocycloalkyl groups are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or from a group selected from cyano, oxo, hydroxyl, C1-C4-alkyl, (C1-C4-alkyl)-C(=0)-, C3-C4-cycloalkyl and C1-C4-alkoxy,

[1072] and wherein the phenyl group of said (phenoxy)-C2-C3-alkyl- group and said (phenyl)-(C1-C3-alkyl)- group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or from a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[1073] or

[1074] R 12 and R 13 together with the nitrogen atom to which they are attached, represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group, which is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or from a group selected from cyano, oxo, hydroxyl, C1-C4-alkyl, (C1-C4-alkyl)-C(=0)-, C3-C4-cycloalkyl and C1-C4-alkoxy;

[1075] R 14 represents a group selected from C1-C4-alkyl, C1-C4-haloalkyl and phenyl,

[1076] ​wherein said phenyl group is optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy;

[1077] R 17 represents a hydrogen atom or a group selected from C1-C4-alkyl, C3-C4-alkenyl, C3-C4-alkynyl, C1-C3-alkoxy, C3-C7-cycloalkyl, bicyclic C5-C

[1078] R 18 and R 19 independently of one another represent a hydrogen atom or a C1-C4-alkyl group;

[1079] R 20 represents a hydrogen atom or a group selected from C1-C6-alkyl, C3-C4-alkenyl, C3-C4-alkynyl, C1-C3-alkoxy, C3-C7-cycloalkyl, bicyclic C5-C 11 -alkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 11-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1080] wherein said C1-C6-alkyl group is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from hydroxy, cyano, C1-C3-alkoxy, -N(R 22 )(R 23 ), C3-C7-cycloalkyl, bicyclic C5-C 11 -alkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 11-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, the phenyl and 5- to 10-membered heteroaryl substituents themselves being optionally substituted one or two times, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[1081] and wherein said C3-C7-cycloalkyl, bicyclic C5-C 11 -alkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl and bicyclic 5- to 11-membered heterocycloalkyl groups are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, oxo, hydroxy, C1-C4-alkyl, (C1-C4-alkyl)-C(=O)-, C3-C4-cycloalkyl and C1-C4-alkoxy,

[1082] and wherein said phenyl, naphthyl and 5- to 10-membered heteroaryl groups are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, -N(R 22 )(R 23) and -C(=O)-N(R 24 )(R 25 ) of the group,

[1083] R 21 represents a hydrogen atom or a C1-C4-alkyl group,

[1084] or

[1085] R 20 and R 21 together with the nitrogen atom to which they are attached represent an optionally benzo-fused monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group, and which is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or from a cyano group, an oxo group, a hydroxyl group, a C1-C4-alkyl group, a C1-C4-haloalkyl group, a (phenyl)-(C1-C3-alkyl)- group, a (C1-C4-alkyl)-C(=O)- group, a C3-C4-cycloalkyl group, a C1-C4-alkoxy group, a C1-C3-haloalkoxy group, a -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ) group;

[1086] R 22 and R 23 independently of one another represent a hydrogen atom or a group selected from a C1-C2-alkyl group and a (C1-C2-alkyl)-C(=O)- group;

[1087] R 24 and R 25 independently of one another represent a hydrogen atom or a C1-C4-alkyl group; and

[1088] n represents an integer 0, 1 or 2,

[1089] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1090] DGK zeta inhibitor embodiment B

[1091] In some embodiments of the application, the DGKz inhibitor is a compound of formula (II) above, wherein:

[1092] R 1 represents a phenyl or a pyridyl group optionally substituted one, two or three times, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom or from a group selected from a hydroxyl group, a cyano group, a C1-C4-alkyl group, a C1-C2-fluoroalkyl group, a C1-C2-alkoxy group, a (phenyl)-(C1-C2-alkoxy)- group, a C1-C2-fluoroalkoxy group and a -N(R 5 )(R 6 ) group,

[1093] or two substituents attached to adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group selected from: -(CH2)3-, -O-CH2-O- and -O-CF2-O-,

[1094] or

[1095] R 1 represents a pyrazolyl group optionally substituted by a methyl group;

[1096] R 2 express Group,

[1097] Where "*" represents R 2 The site of attachment to the nitrogen atom;

[1098] R 3 represents a group selected from methyl and -NH2;

[1099] R 4 represents a phenyl or pyridyl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or from a cyano group, a C1-C3-alkyl group, ((R 9 )O)-(C1-C3-alkyl)-, C1-C3-fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ), -S(=O) n -R 14 and -C(=O)-OR 17 , or two substituents attached to adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group selected from the group consisting of: -(CH2)3-, -O-CH2-O-, and -O-CF2-O-;

[1100] R 5 and R 6 independently of one another represent a hydrogen atom or a C1-C2-alkyl group,

[1101] or

[1102] R 5 and R 6 together with the nitrogen atom to which they are attached represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from hydroxy and C1-C2-alkyl;

[1103] R 7 represents a hydrogen atom or a C1-C2-alkyl group;

[1104] R 8 represents a -C(=O)-NH2group;

[1105] R 9 represents a hydrogen atom or a group selected from C1-C2-alkyl, benzyl, C1-C2-fluoroalkyl, C2-hydroxyalkyl, (C1-C2-alkoxy)-C2-alkyl-, ((C1-C2-alkyl)-C(=O)-O)-C2-alkyl-, C(R 18 )(R 19 )-C(=O)-OR 17 , -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ), -C(=O)-N(R 20 )(R 21 ) and phenyl,

[1106] wherein the phenyl group in the benzyl group and the phenyl group itself are optionally substituted one or two times, each substituent being independently selected from a fluorine atom or a chlorine atom or a group selected from cyano and methyl;

[1107] R 10 and R 11 independently from each other represent a hydrogen atom or a group selected from C1-C2-alkyl, C1-C2-fluoroalkyl, (C3-C5-cycloalkyl)-(C1-C2-alkyl)-, (C1-C2-alkyl)-C(=O)-, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C(=O)-, (phenyl)-(C1-C2-alkyl)-, (phenyl)-(C1-C2-alkyl)-C(=O)- and (phenyl)-(C1-C2-alkyl)-O-C(=O)-,

[1108] wherein the C3-C7-cycloalkyl group and the C3-C5-cycloalkyl group in the (C3-C5-cycloalkyl)-(C1-C2-alkyl)- and the C3-C7-cycloalkyl group in the C3-C7-cycloalkyl-C(=O)- group are optionally substituted one or two times, each substituent being independently selected from a fluorine atom or a group selected from cyano, C1-C2-alkyl and C1-C2-fluoroalkyl, and wherein the phenyl group in the (phenyl)-(C1-C2-alkyl)-, (phenyl)-(C1-C2-alkyl)-C(=O)- and (phenyl)-(C1-C2-alkyl)-O-C(=O)- groups is optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1109] or

[1110] R10 and R 11 together with the nitrogen atom to which they are attached, represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a group selected from cyano, oxo, C1-C2-alkyl, C1-C2-fluoroalkyl and (C1-C2-alkyl)-C(=0)-;

[1111] R 12 and R 13 independently of one another represent a hydrogen atom or a group selected from C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-hydroxyalkyl, (C1-C4-alkoxy)-C2-C3-alkyl-, (C1-C2-fluoroalkoxy)-C2-C3-alkyl-, (phenoxy)-C2-C3-alkyl-, C3-C7-cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C1-C2-alkyl)-,

[1112] wherein said C3-C7-cycloalkyl and monocyclic 4- to 7-membered heterocycloalkyl groups are optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a group selected from oxo, C1-C2-alkyl and (C1-C2-alkyl)-C(=0)-,

[1113] and wherein the phenyl groups in said (phenoxy)-C2-C3-alkyl- group and said (phenyl)-(C1-C2-alkyl)- group are optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom or from a group selected from methyl, trifluoromethyl and methoxy,

[1114] or

[1115] R 12 and R 13 together with the nitrogen atom to which they are attached, represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group optionally substituted once or twice, each substituent being independently selected from a halogen atom or from a group selected from oxo, C1-C2-alkyl and (C1-C2-alkyl)-C(=0)-;

[1116] R 14 represents a group selected from methyl and trifluoromethyl;

[1117] R 17 represents a C1-C2-alkyl group;

[1118] R 18 and R 19 independently of one another represent a hydrogen atom or a methyl group;

[1119] R 20represents a hydrogen atom or a group selected from an optionally substituted C1-C3-alkyl group, an unsubstituted C4-C6-alkyl group, prop-2-ynyl, methoxy, C3-C6-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1120] wherein said C1-C3-alkyl group is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from hydroxyl, cyano, C1-C3-alkoxy, -N(R 22 )(R 23 ), C3-C6-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, said phenyl and 5- to 10-membered heteroaryl substituents themselves being optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1121] and wherein said C3-C6-cycloalkyl, adamantyl and monocyclic 4- to 7-membered heterocycloalkyl groups are optionally substituted one or two or three times, each substituent being independently selected from a fluorine atom or a group selected from oxo, C1-C2-alkyl and (C1-C2-alkyl)-C(=O)-,

[1122] and wherein said phenyl and 5- to 10-membered heteroaryl groups are optionally substituted one, two or three times, each substituent being independently selected from a fluorine atom and a chlorine atom or a group selected from cyano, C1-C2-alkyl, C1-C2-fluoroalkyl, C1-C2-alkoxy, C1-C2-fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1123] R 21 represents a hydrogen atom or a C1-C2-alkyl group,

[1124] or

[1125] R 20 and R 21 together with the nitrogen atom to which they are attached represent an optionally benzo-fused monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group, and which is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, oxo, hydroxyl, C1-C2-alkyl, C1-C2-fluoroalkyl, benzyl, (C1-C2-alkyl)-C(=O)-, C3-C4-cycloalkyl, C1-C2-alkoxy, C1-C2-fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ;

[1126] R 22 and R 23 independently of one another represent a hydrogen atom or a group selected from among Ci-C2-alkyl and (Ci-C2-alkyl)-C(=0)-;

[1127] R 24 and R 25 independently of one another represent a hydrogen atom or a group selected from among Ci-C2-alkyl groups; and

[1128] n represents an integer 2,

[1129] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or mixtures thereof.

[1130] DGK zeta inhibitor embodiment C

[1131] In some embodiments of the application, the DGKz inhibitor is a compound of formula (II) above, wherein:

[1132] R 1 represents a group

[1133] wherein "**" represents the point of attachment of R 1 to the nitrogen atom;

[1134] R 2 represents a group

[1135] wherein "*" represents the point of attachment of R 2 to the nitrogen atom;

[1136] R 3 represents a group selected from among methyl and -NH2;

[1137] R 4 represents a group

[1138] wherein "#" represents the point of attachment of R 4 to the carbonyl group;

[1139] R 7 represents a hydrogen atom or a Ci-C2-alkyl group;

[1140] R 8 represents a -C(=0)-NH2 group;

[1141] R 9represents a hydrogen atom or is selected from C1-C2-alkyl, benzyl, C1-C2-fluoroalkyl, (C1-C2-alkoxy)-C2-alkyl-, ((C1-C2-alkyl)-C(=O)-O)-C2-alkyl-, -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ) and a phenyl group,

[1142] wherein the phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or a group selected from cyano and methyl;

[1143] R 10 and R 11 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C2-alkyl, C3-C7-cycloalkyl and (benzyl)-OC(=O)-,

[1144] wherein the C3-C7-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from methyl and trifluoromethyl,

[1145] and wherein the phenyl group within the (benzyl)-OC(=O)- group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1146] or

[1147] R 10 and R 11 Together with the nitrogen atom to which they are attached, they represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from a cyano group, a methyl group and a trifluoromethyl group;

[1148] R 12 and R 13 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C1-C2-fluoroalkyl, C1-C2-hydroxyalkyl, (C1-C4-alkoxy)-C2-alkyl-, (C1-C2-fluoroalkoxy)-C2-alkyl-, (phenoxy)-C2-alkyl-, C3-C7-cycloalkyl and (phenyl)-(C1-C2-alkyl)-,

[1149] wherein the phenyl group in said (phenyl)-(C1-C2-alkyl)- group is optionally substituted one or two times, each substituent being independently selected from a fluorine atom and a chlorine atom or from a group selected from methyl, trifluoromethyl and methoxy;

[1150] R 17 represents a hydrogen atom or a methyl group;

[1151] R 18 and R 19 independently from each other represent a hydrogen atom or a methyl group;

[1152] R 20 represents a group selected from benzyl and phenyl,

[1153] wherein the phenyl group in said benzyl group is optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1154] R 21 represents a hydrogen atom or a methyl group,

[1155] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[1156] Y 2 represents -C(H)= or -N=;

[1157] Y 3 represents -C(R 27 )= or -N=;

[1158] provided that if Y 2 represents -N=, then Y 3 represents -C(R 27 )=, and if Y 3 represents -N=, then Y 2 represents -C(H)=;

[1159] R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or a group selected from methyl, difluoromethyl, trifluoromethyl, methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy,

[1160] R 27 represents a halogen atom or a group selected from C1-C2-alkyl, C1-C2-fluoroalkyl, -OR 9 , -N(R 10 )(R 11 ), -C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR17 The group,

[1161] or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[1162] DGK zeta inhibitor embodiment D

[1163] In some other embodiments of the present invention, the DGKζ inhibitor is a compound selected from the group consisting of:

[1164] ●rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methoxy-2-methyl-anilino)propionamide,

[1165] ●rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(dimethylamino)anilino]propionamide,

[1166] ●rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-isopropoxy-anilino)propionamide,

[1167] ●rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2,4,6-trifluoro-anilino)propionamide,

[1168] ●rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-bromo-4-fluoro-anilino)propionamide,

[1169] ●rac-2-(N-[4-amino-5-(6-methylpyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1170] ●rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1171] ●rac-2-(N-[4-amino-5-(2-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1172] ●rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-cyano-anilino)propionamide,

[1173] ●rac-2-(N-[4-amino-5-[4-chloro-3-(trifluoromethyl)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1174] ●rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-fluoro-anilino)propionamide,

[1175] • rac-2-(N-[4-amino-5-(3-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1176] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(dimethylamino)anilino]propanamide,

[1177] • rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1178] • rac-4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5- carbonyl]-N-methyl-benzamide,

[1179] • rac-2-(N-[4-amino-5-(3-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1180] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-methoxy-anilino)propanamide,

[1181] • rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-methoxy-anilino)propanamide,

[1182] • rac-2-(N-[4-amino-5-(4-methylsulfonylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1183] • rac-2-(N-[4-amino-5-(4-imidazol-1-ylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1184] • rac-2-(N-[4-amino-5-(4-cyano-3-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1185] • (R)-2-(N-[4-amino-5-(4-cyano-3-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1186] • (S)-2-(N-[4-amino-5-(4-cyano-3-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1187] • rac-2-(N-[4-amino-5-(2-fluoro-4-methoxy-benzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1188] • rac-2-(N-[4-amino-5-(2-fluoro-4-methoxy-benzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1189] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(trifluoromethoxy)anilino]propanamide,

[1190] • rac-2-(N-[4-amino-5-(3,4-difluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1191] • rac-2-(N-[4-amino-5-(3,4-dichlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1192] • rac-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propanamide,

[1193] • (R)-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propanamide,

[1194] • (S)-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propanamide,

[1195] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(trifluoromethyl)anilino]propanamide,

[1196] • rac-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1197] • (R)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1198] • (S)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1199] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-2-fluoro-anilino)propanamide,

[1200] • rac-2-(N-[4-amino-5-(indan-5-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1201] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3,4-difluoro-anilino)propanamide,

[1202] • (R)-2-(N-[4-amino-5-(4-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1203] • (S)-2-(N-[4-amino-5-(4-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1204] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-anilino)propanamide,

[1205] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3,4-dichloro-anilino)propanamide,

[1206] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-fluoro-anilino)propanamide,

[1207] • rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1208] • (R)-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1209] • (S)-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1210] • rac-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1211] • (R)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1212] • (S)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1213] • rac-2-[4-[4-amino-2-(N-[2-amino-1 -methyl-2-oxo-ethyl]-4-fluoro- anilino)thiazole-5-carbonyl]phenoxy]-2-methyl-propionic acid ethyl ester,

[1214] • rac-2-(N-[4-amino-5-[4-(trifluoromethoxy)benzoyl]thiazol-2-yl]-4- fluoro-anilino)propionamide,

[1215] • (R)-2-(N-[4-amino-5-[4-(trifluoromethoxy)benzoyl]thiazol-2-yl]-4- fluoro-anilino)propionamide,

[1216] • (S)-2-(N-[4-amino-5-[4-(trifluoromethoxy)benzoyl]thiazol-2-yl]-4- fluoro-anilino)propionamide,

[1217] • rac-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide,

[1218] • (R)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide,

[1219] • (S)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide,

[1220] • rac-2-(N-[4-amino-5-[4-(trifluoromethyl)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propionamide,

[1221] • rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- (trifluoromethyl)anilino]propionamide,

[1222] • (R)-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- (trifluoromethyl)anilino]propionamide,

[1223] • (S)-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- (trifluoromethyl)anilino]propionamide,

[1224] • rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propionamide,

[1225] • (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1226] • (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1227] • 2-(N-[4-amino-5-[4-[2-amino-1-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]- anilino)propanamide (mixture of stereoisomers),

[1228] • (2R)-(N-[4-amino-5-[4-[2-amino-(1 R)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2- yl]anilino)propanamide,

[1229] • (2R)-(N-[4-amino-5-[4-[2-amino-(1 S)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2- yl]anilino)propanamide,

[1230] • (2S)-(N-[4-amino-5-[4-[2-amino-(1 R)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2- yl]anilino)propanamide,

[1231] • (2S)-(N-[4-amino-5-[4-[2-amino-(1 S)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2- yl]anilino)propanamide,

[1232] • rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-2- fluoro-anilino)propanamide,

[1233] • (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-2- fluoro-anilino)propanamide,

[1234] • (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-2- fluoro-anilino)propanamide,

[1235] • rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro- anilino)propanamide,

[1236] • (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro- anilino)propanamide,

[1237] • (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-3- fluoro-anilino)propanamide,

[1238] • rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3,4-difluoro- anilino)propanamide,

[1239] • (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3,4-difluoro- anilino)propanamide,

[1240] • (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3,4-difluoro- anilino)propanamide,

[1241] • rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1242] • (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1243] • (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1244] • rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1245] • (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1246] • (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1247] • rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1248] • (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1249] • (S)-2-(N-[4-amino-5-(6-methoxy-pyridine-3-carbonyl)-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1250] • rac-2-(N-[4-amino-5-(6-methoxy-pyridine-3-carbonyl)-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1251] • (R)-2-(N-[4-amino-5-(6-methoxy-pyridine-3-carbonyl)-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1252] • (S)-2-(N-[4-amino-5-(6-methoxy-pyridine-3-carbonyl)-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1253] • rac-2-(N-[4-amino-5-[6-(trifluoromethyl)-pyridine-3-carbonyl]-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1254] • (R)-2-(N-[4-amino-5-[6-(trifluoromethyl)-pyridine-3-carbonyl]-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1255] • (S)-2-(N-[4-amino-5-[6-(trifluoromethyl)-pyridine-3-carbonyl]-thiazol-2-yl]-3,4- difluoro-anilino)-propionamide,

[1256] • rac-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-4-fluoro- anilino)-propionamide,

[1257] • rac-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-3,4-difluoro- anilino)-propionamide,

[1258] • (R)-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-3,4-difluoro- anilino)-propionamide,

[1259] • (S)-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-3,4-difluoro- anilino)-propionamide,

[1260] • rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)-thiazol-2-yl]-4-chloro-3-fluoro- anilino)-propionamide,

[1261] • (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide,

[1262] • (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide,

[1263] • rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1264] • (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1265] • (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1266] • rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1267] • (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1268] • (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propanamide,

[1269] • rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide,

[1270] • (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide,

[1271] • (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide,

[1272] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)anilino)propanamide,

[1273] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propanamide,

[1274] • (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propanamide,

[1275] • (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propanamide,

[1276] • rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1277] • (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1278] • (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1279] • rac-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1280] • (R)-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1281] • (S)-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1282] • rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1283] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2,4-difluoro-anilino)propanamide,

[1284] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methoxy-anilino)propanamide,

[1285] • rac-2-[(4-amino-5-benzoyl-l,3-thiazol-2-yl)(phenyl)amino]butyramide,

[1286] • rac-2-[(4-amino-5-benzoyl-l,3-thiazol-2-yl)(4-fluorophenyl)amino]butyramide,

[1287] • 2-(N-[4-amino-5-[4-(2-amino-l-methyl-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide (mixture of stereoisomers),

[1288] • rac-2-{[4-amino-5-(4-methoxybenzoyl)-l,3-thiazol-2-yl](4-fluorophenyl)amino}butanamide,

[1289] • 2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)acetamide,

[1290] • 2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)acetamide,

[1291] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methyl-anilino)propanamide,

[1292] • (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methyl-anilino)propanamide,

[1293] • (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methyl-anilino)propanamide,

[1294] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propanamide,

[1295] • (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propanamide,

[1296] • (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propanamide,

[1297] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propanamide,

[1298] • (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propanamide,

[1299] • (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propanamide,

[1300] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-methyl-anilino)propanamide,

[1301] • (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-methyl-anilino)propanamide,

[1302] • (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-methyl-anilino)propanamide,

[1303] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-methyl-anilino)propanamide,

[1304] • (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-methyl-anilino)propanamide,

[1305] • (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-methyl-anilino)propanamide,

[1306] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1-methylpyrazol-4-yl)amino]propanamide,

[1307] • (R)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1-methylpyrazol-4-yl)amino]propanamide,

[1308] • (S)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1-methylpyrazol-4-yl)amino]propanamide,

[1309] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propanamide,

[1310] • (R)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propanamide,

[1311] • (S)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propanamide,

[1312] • rac-2-(N-[4-amino-5-(4-bromobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1313] • rac-2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5- carbonyl]phenoxy]ethyl acetate,

[1314] • (S)-2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole- 5-carbonyl]phenoxy]acetic acid ethyl ester,

[1315] • (S)-2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole- 5-carbonyl]phenoxy]acetic acid ethyl ester,

[1316] • rac-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]- 4-fluoro-anilino)propanamide,

[1317] • rac-2-(N-[4-amino-5-[4-[2-(m-tolylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1318] • rac-2-(N-[4-amino-5-[4-[2-(o-tolylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1319] • rac-2-(N-[4-amino-5-[4-[2-[(3-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thi azol-2-yl]-4-fluoro-anilino)propanamide,

[1320] • rac-2-(N-[4-amino-5-[4-[2-(4-methylpiperazin-1-yl)-2-oxo-ethoxy]benzoyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1321] • rac-2-(N-[4-amino-5-[4-[2-(3-methylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]- 4-fluoro-anilino)propanamide,

[1322] • rac-2-(N-[4-amino-5-[4-(2-morpholino-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1323] • rac-2-(N-[4-amino-5-[4-[2-oxo-2-[2-(1-piperidinyl)ethylamino]ethoxy]benzoyl]thi azol-2-yl]-4-fluoro-anilino)propanamide,

[1324] • rac-2-(N-[4-amino-5-[4-[2-(4-benzyl-l-piperidinyl)-2-oxo-ethoxy]benzoyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1325] • rac-2-(N-[4-amino-5-[4-[2-(2-methoxyethylamino)-2-oxo-ethoxy]benzoyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1326] • rac-2-(N-[4-amino-5-[4-[2-(4-cyanoanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]- 4-fluoro-anilino)propanamide,

[1327] • rac-2-(N-[4-amino-5-[4-[2-[methyl(prop-2-ynyl)amino]-2-oxo-ethoxy]benzoyl]thi- azol-2-yl]-4-fluoro-anilino)propanamide,

[1328] • rac-2-(N-[4-amino-5-[4-[2-[(2-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1329] • rac-2-(N-[4-amino-5-[4-[2-[(3-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1330] • rac-2-(N-[4-amino-5-[4-[2-[(2-fluorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thi- azol-2-yl]-4-fluoro-anilino)propanamide,

[1331] • rac-2-(N-[4-amino-5-[4-[2-[(4-fluorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thi- azol-2-yl]-4-fluoro-anilino)propanamide,

[1332] • rac-2-(N-[4-amino-5-[4-[2-(lH-benzimidazol-2-ylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1333] • rac-2-(N-[4-amino-5-[4-[2-oxo-2-(2,2,2-trifluoroethylamino)ethoxy]benzoyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1334] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1335] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1336] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1337] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1338] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1339] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1340] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1341] • rac-3-[[2-[4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5- carbonyl]phenoxy]acetyl]amino]benzamide,

[1342] • rac-2-(N-[4-amino-5-[4-[2-(dimethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1343] • rac-4-[[2-[4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5- carbonyl]phenoxy]acetyl]amino]benzamide,

[1344] • (2S)-1 -[2-[4-[4-amino-2-(N-[2-amino-(1 RS)-methyl-2-oxo-ethyl]-4- fluoro-anilino)thiazole-5-carbonyl]phenoxy]acetyl]pyrrolidine-2-carboxamide (mixture of two diastereoisomers),

[1345] • rac-2-(N-[4-amino-5-[4-[2-[ethyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1346] • rac-2-(N-[4-amino-5-[4-[2-[(3-methylisoxazol-5-yl)amino]-2-oxo-ethoxy]benzoyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1347] • rac-2-(N-[4-amino-5-[4-[2-[3-(dimethylamino)propyl-methyl-amino]-2-oxo- ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1348] • rac-2-(N-[5-[4-[2-(4-acetylpiperazin-1-yl)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1349] • rac-2-(N-[4-amino-5-[4-[2-oxo-2-(3-pyridinylmethylamino)ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1350] • 2-(N-[4-amino-5-[4-[2-(2,3-dihydroxypropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide (mixture of stereoisomers),

[1351] • rac-2-(N-[4-amino-5-[4-[2-(4-methoxyanilino)-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1352] • rac-2-(N-[4-amino-5-[4-[2-[benzyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1353] • rac-2-(N-[4-amino-5-[4-[2-(4-chloroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1354] • rac-2-(N-[4-amino-5-[4-[2-[(2-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1355] • rac-2-(N-[4-amino-5-[4-[2-[(4-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1356] • rac-2-(N-[4-amino-5-[4-[2-(4-fluoroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1357] • rac-2-(N-[4-amino-5-[4-[2-(azepan-1-yl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1358] • rac-2-(N-[4-amino-5-[4-[2-[(4-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1359] • 2-(N-[4-amino-5-[4-[2-oxo-2-(1-phenylethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (mixture of stereoisomers),

[1360] • rac-2-(N-[4-amino-5-[4-[2-oxo-2-(p-tolylmethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1361] • rac-2-(N-[4-amino-5-[4-[2-[methyl(2-phenylethyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1362] • 2-(N-[4-amino-5-[4-[2-(3-methyl-1-piperidinyl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (mixture of stereoisomers),

[1363] • rac-2-(N-[4-amino-5-[4-[2-(4-methyl-1-piperidinyl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1364] • rac-2-(N-[5-[4-[2-(4-acetamidophenylamino)-2-oxo-ethoxy]benzoyl]-4- amino-thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1365] • rac-2-(N-[4-amino-5-[4-[2-oxo-2-(1 H-pyrazolo[3,4-d]pyrimidin-4- ylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1366] • rac-2-(N-[4-amino-5-[4-[2-(cyclopentylamino)-2-oxo-ethoxy]benzoyl]thiazol-2- yl]-4-fluoro-phenylamino)propanamide,

[1367] • rac-2-(N-[4-amino-5-[4-[2-(3,4-dihydro-1 H-isoquinolin-2-yl)-2-oxo-ethoxy]benzoyl] thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1368] • rac-2-(N-[4-amino-5-[4-(2-isoindolin-2-yl-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4- fluoro-phenylamino)propanamide,

[1369] • rac-2-(N-[4-amino-5-[4-[2-[2-furanylmethyl(methyl)amino]-2-oxo-ethoxy]benzoyl] thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1370] • rac-2-(N-[4-amino-5-[4-[2-[4-(dimethylamino)-1 -piperidinyl]-2-oxo-ethoxy]benzoyl] thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1371] • rac-2-(N-[4-amino-5-[4-[2-[methyl(3-pyridinylmethyl)amino]-2-oxo-ethoxy]benzoyl] thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1372] • rac-2-(N-[4-amino-5-[4-[2-(N,2-dimethylaminophenylamino)-2-oxo-ethoxy]benzoyl] thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1373] • rac-2-(N-[4-amino-5-[4-[2-(N,4-dimethylaminophenylamino)-2-oxo-ethoxy]benzoyl] thiazol-2-yl]-4-fluoro-phenylamino)propanamide,

[1374] • rac-2-(N-[4-amino-5-[4-[2-(N,3-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1375] • rac-2-(N-[4-amino-5-[4-[2-(2,2-dimethylpropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1376] • 2-(N-[5-[4-[2-(1-adamantylamino)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4-fluoro- anilino)propanamide (single stereoisomer),

[1377] • 2-(N-[5-[4-[2-(1-adamantylmethylamino)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4- fluoro-anilino)propanamide (single stereoisomer),

[1378] • 2-(N-[5-[4-[2-[2-(1-adamantyl)ethylamino]-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4- fluoro-anilino)propanamide (single stereoisomer),

[1379] • 2-(N-[4-amino-5-[4-[2-(4-chloroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino) propanamide (single stereoisomer),

[1380] • 4-[[2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5- carbonyl]phenoxy]acetyl]amino]benzamide (single stereoisomer),

[1381] • 2-(N-[4-amino-5-[4-[2-((2RS),3-dihydroxypropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide (mixture of two diastereoisomers),

[1382] • 2-(N-[4-amino-5-[4-[2-oxo-2-[2-(1-piperidyl)ethylamino]ethoxy]benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide (single stereoisomer),

[1383] • 2-(N-[4-amino-5-[4-(2-amino-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propanamide (single stereoisomer),

[1384] • (R)-2-(N-[4-amino-5-[4-[2-(methylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1385] • (S)-2-(N-[4-amino-5-[4-[2-(methylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1386] • (R)-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1387] • (S)-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1388] • rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5- carbonyl]phenoxy]-N-isopropyl-2-methyl-propanamide,

[1389] • rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5- carbonyl]phenoxy]-2-methyl-propanamide,

[1390] • rac-2-(N-(5-benzoyl-4-methyl-thiazol-2-yl)-4-fluoro-anilino)propanamide,

[1391] • rac-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1392] • rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1393] • rac-2-(N-[4-amino-5-[6-(difluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1394] • rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propanamide,

[1395] • (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro- anilino)propanamide,

[1396] • (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro- anilino)propanamide,

[1397] • rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro- anilino)propanamide,

[1398] • (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro- anilino)propanamide,

[1399] • (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro- anilino)propanamide,

[1400] • rac-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1401] • (R)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1402] • (S)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1403] • rac-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3,4- difluoro-anilino)propanamide,

[1404] • (R)-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3,4- difluoro-anilino)propanamide,

[1405] • (S)-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3,4- difluoro-anilino)propanamide,

[1406] • rac-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4- chloro-3-fluoro-anilino)propanamide,

[1407] • (R)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4- chloro-3-fluoro-anilino)propanamide,

[1408] • (S)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4- chloro-3-fluoro-anilino)propanamide,

[1409] • rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1410] • (R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1411] • (S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propanamide,

[1412] • rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide,

[1413] • (R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide,

[1414] • (S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propanamide,

[1415] • rac-N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5- carbonyl]phenyl]benzylcarbamate,

[1416] • (R)-N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5- carbonyl]phenyl]benzylcarbamate,

[1417] • (S)-N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5- carbonyl]phenyl]benzylcarbamate,

[1418] • rac-2-[4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]phenoxy]acetic acid ethyl ester,

[1419] • rac-N-[4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]phenyl]benzylcarbamate,

[1420] • (R)-N-[4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]phenyl]benzylcarbamate,

[1421] • (S)-N-[4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]phenyl]benzylcarbamate,

[1422] • rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1423] • (R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1424] • (S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1425] • rac-2-(N-[4-amino-5-(4-iodobenzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1426] • rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4- chloro-3-fluoro-anilino)propanamide,

[1427] • (R)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4- chloro-3-fluoro-anilino)propanamide,

[1428] • (S)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4- chloro-3-fluoro-anilino)propanamide,

[1429] • rac-2-(N-[4-amino-5-(4-phenoxybenzoyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1430] • rac-2-(N-[4-amino-5-[4-(dimethylamino)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1431] • (R)-2-(N-[4-amino-5-[4-(dimethylamino)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1432] • (S)-2-(N-[4-amino-5-[4-(dimethylamino)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1433] • rac-2-(N-[4-amino-5-(4-nitrobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1434] • rac-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propanamide,

[1435] • (R)-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propanamide,

[1436] • (S)-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propanamide,

[1437] • rac-4-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole- 5-carbonyl]phenyl]cyclopropanecarboxamide,

[1438] • rac-2-(N-[4-amino-5-(4-morpholinobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1439] • rac-2-(N-[4-amino-5-[4-(pyrazol-1-ylmethyl)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1440] • rac-2-(N-[4-amino-5-[4-(dimethylamino)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1441] • rac-2-(N-[4-amino-5-(4-pyrrolidin-1-ylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1442] • rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- benzyloxy-anilino)propanamide,

[1443] • (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- benzyloxy-anilino)propanamide,

[1444] • (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- benzyloxy-anilino)propanamide,

[1445] • rac-2-(N-[4-amino-5-[3-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1446] • rac-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro- anilino)propanamide,

[1447] • (R)-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro- anilino)propanamide,

[1448] • (S)-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro- anilino)propanamide,

[1449] • rac-2-(N-[5-(4-acetamidobenzoyl)-4-amino-thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1450] • rac-2-(N-[4-amino-5-(2-chloropyridine-4-carbonyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1451] • rac-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1452] • (R)-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1453] • (S)-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1454] • rac-2-(N-[4-amino-5-[2-(difluoromethyl)pyridine-4-carbonyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1455] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(2,2-difluoro-l,3-benzodioxol-5-yl)amino]propanamide,

[1456] • rac-2-(N-[4-amino-5-(2-methoxypyridine-4-carbonyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1457] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-4-methoxy-anilino)propanamide,

[1458] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-cyano-3-fluoro-anilino)propanamide,

[1459] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-bromo-anilino)propanamide,

[1460] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(difluoromethoxy)anilino]propanamide,

[1461] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-ethoxy-anilino)propanamide,

[1462] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(l,3-benzodioxol-5-yl)amino]propanamide,

[1463] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(2,2-difluoro-l,3-benzodioxol-5-yl)amino]propanamide,

[1464] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(difluoromethoxy)-3-fluoro-anilino]propanamide,

[1465] • rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-benzyloxy-anilino)propanamide,

[1466] • rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4- (difluoromethoxy)anilino]propanamide,

[1467] rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide,

[1468] rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide,

[1469] ●rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide,

[1470] ●rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide,

[1471] rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide,

[1472] ●rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide,

[1473] ●rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide,

[1474] ●rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide,

[1475] ●rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide,

[1476] ●rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(trifluoromethoxy)anilino]propionamide,

[1477] ●rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide,

[1478] • rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-(2,2-difluoro-l,3- benzodioxol-5-yl)amino]propanamide,

[1479] • rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-(2,2-difluoro-l,3- benzodioxol-5-yl)amino]propanamide,

[1480] • rac-2-[[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-(2,2-difluoro-l,3-benzodioxol-5- yl)amino]propanamide,

[1481] • rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-(2,2-difluoro- 1,3-benzodioxol-5-yl)amino]propanamide,

[1482] • rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-fluoro-4- (trifluoromethoxy)anilino]propanamide,

[1483] • rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-fluoro-4- (trifluoromethoxy)anilino]propanamide,

[1484] • rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3-fluoro-4- (trifluoromethoxy)anilino]propanamide,

[1485] • rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-fluoro-4- (trifluoromethoxy)anilino]propanamide,

[1486] • rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3-fluoro- 4-(trifluoromethoxy)anilino]propanamide,

[1487] • rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4- (trifluoromethoxy)anilino]propanamide,

[1488] • rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-chloro-4- (trifluoromethoxy)anilino]propanamide,

[1489] • rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4- (trifluoromethoxy)anilino]propanamide,

[1490] • rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4- (trifluoromethoxy)anilino]propanamide,

[1491] • rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4- (trifluoromethoxy)anilino]propanamide,

[1492] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1493] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1494] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1495] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1496] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1497] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1498] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1499] • rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridyl)amino]propanamide,

[1500] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-3-(trifluoromethoxy)anilino]propanamide,

[1501] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-3-(trifluoromethoxy)anilino]propanamide,

[1502] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-(difluoromethoxy)-4-fluoro- anilino]propionamide,

[1503] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-(difluoromethoxy)- anilino]propionamide,

[1504] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-4-(trifluoromethoxy)- anilino]propionamide,

[1505] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-(trifluoromethoxy)- anilino]propionamide,

[1506] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(difluoromethoxy)-2-fluoro- anilino]propionamide,

[1507] • rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-(difluoromethoxy)- anilino]propionamide,

[1508] • rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4- (difluoromethyl)anilino]propionamide,

[1509] • rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4- (difluoromethyl)anilino]propionamide,

[1510] • rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4- (difluoromethyl)anilino]propionamide,

[1511] • rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4- (difluoromethyl)anilino]propionamide,

[1512] • rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]- 4-(difluoromethyl)anilino]propionamide,

[1513] • rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-[6-(trifluoromethoxy)- 3-pyridyl]amino]propionamide,

[1514] • rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-[6-(trifluoromethoxy)-3- pyridyl]amino]propanamide,

[1515] • rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-[6- (trifluoromethoxy)-3-pyridyl]amino]propanamide,

[1516] • rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-[6- (trifluoromethoxy)-3-pyridyl]amino]propanamide,

[1517] • rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-[6-(difluoromethoxy)-3- pyridyl]amino]propanamide,

[1518] • rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-[6-(difluoromethoxy)-3- pyridyl]amino]propanamide,

[1519] • rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-[6- (difluoromethoxy)-3-pyridyl]amino]propanamide,

[1520] • rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-[6- (difluoromethoxy)-3-pyridyl]amino]propanamide,

[1521] • rac-N-[5-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole- 5-carbonyl]-2-pyridyl]benzylcarbamate,

[1522] • rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole- 5-carbonyl]benzoic acid ethyl ester,

[1523] • rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro- anilino)thiazole-5-carbonyl]benzoic acid ethyl ester,

[1524] • rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole- 5-carbonyl]phenoxy]-2-methyl-propanoic acid ethyl ester,

[1525] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide,

[1526] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide,

[1527] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide,

[1528] • 4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole- 5-carbonyl]-N-[(2S)-2-hydroxypropyl]benzamide (mixture of stereoisomers),

[1529] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide,

[1530] • 4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole- 5-carbonyl]-N-[(2S)-2-hydroxypropyl]benzamide (mixture of stereoisomers),

[1531] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide,

[1532] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide,

[1533] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-chloro-3-fluoro- anilino)thiazole-5-carbonyl]-N-(2-phenoxyethyl)benzamide,

[1534] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-chloro-3-fluoro- anilino)thiazole-5-carbonyl]-N-[2-(trifluoromethoxy)ethyl]benzamide,

[1535] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-chloro-3-fluoro- anilino)thiazole-5-carbonyl]-N-[2-(dimethylamino)ethyl]benzamide,

[1536] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-chloro-3-fluoro- anilino)thiazole-5-carbonyl]-N-(2-tert-butoxyethyl)benzamide,

[1537] • rac-4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-chloro-3-fluoro- anilino)thiazole-5-carbonyl]-N-(2-methoxyethyl)benzamide,

[1538] • rac-2-[4-[4-amino-2-(N-(2-amino-l-methyl-2-oxo-ethyl)-4-fluoro- anilino)thiazole-5-carbonyl]phenoxy]-N-[(4-chlorophenyl)methyl]-2-methyl- propanamide,

[1539] • rac-2-(N-[4-amino-5-(6-bromopyridine-3-carbonyl)thiazol-2-yl]-4-fluoro- anilino)propanamide,

[1540] • rac-2-(N-[4-amino-5-[6-[4-(trifluoromethyl)-l-piperidyl]pyridine-3- carbonyl]thiazol-2-yl]-4-fluoro-anilino)propanamide,

[1541] • rac-2-(N-[4-amino-5-[6-(4-methyl-l-piperidyl)pyridine-3-carbonyl]thiazol-2- yl]-4-fluoro-anilino)propanamide,

[1542] • rac-2-(N-[4-amino-5-[6-[4-(oxetan-3-yl)-l-piperidyl]pyridine-3-carbonyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1543] • rac-2-(N-[4-amino-5-[6-(dimethylamino)pyridine-3-carbonyl]thiazol-2-yl]-4- fluoro-anilino)propanamide,

[1544] • rac-2-(N-[4-amino-5-[6-(4,4-dimethyl-l-piperidyl)pyridine-3-carbonyl]thiazol- 2-yl]-4-fluoro-anilino)propanamide,

[1545] ●rac-2-(N-[4-amino-5-[6-(3-azabicyclo[3.2.1]octane-3-yl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1546] ●rac-2-(N-[4-amino-5-[6-(3,5-dimethyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1547] ●rac-2-(N-[4-amino-5-[6-(3-azabicyclo[3.1.0]hexane-3-yl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1548] ●rac-2-(N-[4-amino-5-[6-(1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1549] ●rac-2-(N-[4-amino-5-[6-(4,4-difluoro-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1550] ●rac-2-(N-[4-amino-5-[6-(4-cyano-4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1551] ●(R)-2-(N-[4-amino-5-[6-(4-cyano-4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1552] ●(S)-2-(N-[4-amino-5-[6-(4-cyano-4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide,

[1553] ●2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide (single enantiomer),

[1554] ●(R)-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide,

[1555] ●(S)-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide,

[1556] • 2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide (enantiomer 1),

[1557] • 2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide (enantiomer 2),

[1558] • 2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide (enantiomer 2),

[1559] • rac-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro- anilino)propanamide,

[1560] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1561] In some preferred embodiments, the DGKz inhibitor is a compound according to this list.

[1562] DGK zeta inhibitor A'

[1563] In a preferred embodiment of the application, the DGKz inhibitor is (R)-(N-[4-amino-5-(4- methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1564] In another preferred embodiment of the application, the DGKz inhibitor is (R)-2-(N-[4-amino-5-(4- methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide, or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1565] In another preferred embodiment of the application, the DGKz inhibitor is (R)-2-(N-[4-amino-5-(4- methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide.

[1566] In another preferred embodiment of the application, the DGKz inhibitor is DGKz inhibitor A’ of the following structure:

[1567]

[1568] or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1569] In another preferred embodiment of the application, the DGKz inhibitor is DGKz inhibitor A’ of the following structure:

[1570]

[1571] or a tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture of same.

[1572] In another preferred embodiment of the application, the DGKz inhibitor is DGKz inhibitor A’ of the following structure:

[1573]

[1574] The synthesis of DGKz inhibitor A’ is described in International Patent Application PCT / EP2021 / 060167, Example 62.2. International Patent Application PCT / EP2021 / 060167 also discloses methods of preparing other compounds of formula (II) mentioned herein.

[1575] Embodiment

[1576] Embodiments of the combination

[1577] Aspect 1

[1578] According to a first aspect, the present application provides a combination comprising one or more DGK a inhibitors and one or more DGKz inhibitors.

[1579] In another embodiment, the present application provides a combination comprising one DGK a inhibitor and one DGKz inhibitor.

[1580] In another embodiment, the present application provides a combination comprising one DGK a inhibitor and one DGKz inhibitor.

[1581] In another embodiment, the present application provides a combination comprising one DGK a inhibitor and one DGKz inhibitor.

[1582] In another embodiment, the present application provides a combination comprising one DGK a inhibitor and one DGKz inhibitor.

[1583] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein.

[1584] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is from 20: 1 to 1 :20.

[1585] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is from 12: 1 to 1 :12.

[1586] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is from 12: 1 to 8: 1.

[1587] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is from 10: 1 to 1 : 1.

[1588] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 10: 1.

[1589] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is from 4: 1 to 2: 1.

[1590] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 3: 1.

[1591] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is in the range of 2: 1 to 1 :2.

[1592] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 : 1.

[1593] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is in the range of 1 :2 to 1 :4.

[1594] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 :3.

[1595] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is in the range of 1 :8 to 1 : 12.

[1596] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is in the range of 1 : 1 to 1 : 10.

[1597] In another embodiment, the present application provides a combination comprising a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 : 10.

[1598] In another embodiment, the present application provides a combination consisting of one or more DGK alpha inhibitors and one or more DGK zeta inhibitors.

[1599] In another embodiment, the present application provides a combination consisting of one DGK alpha inhibitor and one DGK zeta inhibitor.

[1600] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture thereof.

[1601] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1602] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1603] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1604] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1605] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1606] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1607] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1608] In another embodiment, the present application provides a combination consisting of one DGKalpha inhibitor compound of general formula (I) as described herein and one DGKzeta inhibitor compound of general formula (II) as described herein.

[1609] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is about 10: 1.

[1610] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is 4: 1 to 2: 1.

[1611] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is about 3: 1.

[1612] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is 2: 1 to 1:2.

[1613] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is about 1: 1.

[1614] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is 1:2 to 1:4.

[1615] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is about 1:3.

[1616] In another embodiment, the present application provides a combination consisting of a DGK a Inhibitor A and a DGK z Inhibitor A' described herein, wherein the dose ratio (mg or mg / kg of DGK a Inhibitor A : mg or mg / kg of DGK z Inhibitor A') is 1:8 to 1: 12.

[1617] In another embodiment, the present application provides a combination consisting of a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 : 1 to about 1 : 10.

[1618] In another embodiment, the present application provides a combination consisting of a DGK alpha inhibitor A and a DGK zeta inhibitor A' as described herein, wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 : 10.

[1619] In another preferred embodiment, the combination of the present application comprises a DGK alpha inhibitor A and a DGK zeta inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a salt thereof, or a mixture of same.

[1620] In another preferred embodiment, the combination of the present application consists of a DGK alpha inhibitor A and a DGK zeta inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a salt thereof, or a mixture of same.

[1621] In another preferred embodiment, the combination of the present application comprises a DGK alpha inhibitor A and a DGK zeta inhibitor A'.

[1622] In another preferred embodiment, the combination of the present application consists of a DGK alpha inhibitor A and a DGK zeta inhibitor A'.

[1623] In another preferred embodiment, the combination of the present application comprises 6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide and (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoroanilino)propanamide, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a salt thereof, or a mixture of same.

[1624] In another preferred embodiment, the combination of the present application consists of 6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide and (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoroanilino)propanamide, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a salt thereof, or a mixture of same.

[1625] In another preferred embodiment, the combination of the present application consists of 6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide and (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoroanilino)propanamide.

[1626] In another preferred embodiment, the combination of the present application consists of 6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide and (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoroanilino)propanamide.

[1627] The combination of the present application can be administered by oral, intravenous, topical, local implantation, intraperitoneal or intranasal route.

[1628] The DGK alpha inhibitor can be administered by oral, intravenous, topical, local implantation, intraperitoneal or intranasal route.

[1629] The DGK zeta inhibitor can be administered by oral, intravenous, topical, local implantation, intraperitoneal or intranasal route.

[1630] The DGK alpha inhibitor can be in the form of a pharmaceutical formulation which can be used directly, can be administered simultaneously, concurrently, separately or sequentially with the DGK zeta inhibitor and optional component C described below. The DGK alpha inhibitor, the DGK zeta inhibitor and the optional component C can be administered independently from each other by oral, intravenous, topical, local implantation, intraperitoneal or intranasal route.

[1631] As described and defined herein, the combination comprising one or more DGK alpha inhibitors and one or more DGK zeta inhibitors is also referred to as "combination of the present application".

[1632] The surprising effect of the combination of the present application is demonstrated herein with DGK inhibitors (DGK alpha inhibitor A and DGK zeta inhibitor A') and is specifically disclosed in the Examples section.

[1633] Embodiments of kits

[1634] Aspect 2

[1635] According to a second aspect, the present application provides a kit comprising:

[1636] a DGK alpha inhibitor compound of general formula (I) as described herein, more specifically DGK alpha inhibitor A, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same,

[1637] a DGKz inhibitor compound of general formula (II) as described herein, more specifically DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1638] In another preferred embodiment, the present application provides a kit comprising:

[1639] DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1640] DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1641] In another preferred embodiment, the present application provides a kit comprising:

[1642] DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1643] DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

[1644] In another preferred embodiment, the present application provides a kit comprising:

[1645] DGKz inhibitor A',

[1646] DGKz inhibitor A'.

[1647] In another preferred embodiment, the present application provides a kit comprising:

[1648] DGKz inhibitor A',

[1649] DGKz inhibitor A',

[1650] wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK z inhibitor A') is from 20: 1 to 1 :20.

[1651] In another preferred embodiment, the present application provides a kit comprising:

[1652] DGKz inhibitor A',

[1653] DGKz inhibitor A',

[1654] The dose ratio (mg or mg / kg of DGKα inhibitor A:mg or mg / kg of DGKζ inhibitor A') is 12:1 to 1:12.

[1655] In another preferred embodiment, the present invention provides a kit comprising:

[1656] DGKα inhibitor A,

[1657] DGKζ inhibitor A',

[1658] The dose ratio (mg or mg / kg of DGKα inhibitor A:mg or mg / kg of DGKζ inhibitor A') is 12:1 to 8:1.

[1659] In another preferred embodiment, the present invention provides a kit comprising:

[1660] DGKα inhibitor A,

[1661] DGKζ inhibitor A',

[1662] The dose ratio (mg or mg / kg of DGKα inhibitor A:mg or mg / kg of DGKζ inhibitor A') is 10:1 to 1:1.

[1663] In another preferred embodiment, the present invention provides a kit comprising:

[1664] DGKα inhibitor A,

[1665] DGKζ inhibitor A',

[1666] The dose ratio (mg or mg / kg of DGKα inhibitor A:mg or mg / kg of DGKζ inhibitor A') was approximately 10:1.

[1667] In another preferred embodiment, the present invention provides a kit comprising:

[1668] DGKα inhibitor A,

[1669] DGKζ inhibitor A',

[1670] The dose ratio (mg or mg / kg of DGKα inhibitor A:mg or mg / kg of DGKζ inhibitor A') is 4:1 to 2:1.

[1671] In another preferred embodiment, the present invention provides a kit comprising:

[1672] DGKα inhibitor A,

[1673] DGKζ inhibitor A',

[1674] wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 3: 1.

[1675] In another preferred embodiment, the present application provides a kit comprising:

[1676] a DGK alpha inhibitor A,

[1677] a DGK zeta inhibitor A',

[1678] wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is 2: 1 to 1 :2.

[1679] In another preferred embodiment, the present application provides a kit comprising:

[1680] a DGK alpha inhibitor A,

[1681] a DGK zeta inhibitor A',

[1682] wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 : 1.

[1683] In another preferred embodiment, the present application provides a kit comprising:

[1684] a DGK alpha inhibitor A,

[1685] a DGK zeta inhibitor A',

[1686] wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is 1 :2 to 1 :4.

[1687] In another preferred embodiment, the present application provides a kit comprising:

[1688] a DGK alpha inhibitor A,

[1689] a DGK zeta inhibitor A',

[1690] wherein the dose ratio (mg or mg / kg of DGK alpha inhibitor A : mg or mg / kg of DGK zeta inhibitor A') is about 1 :3.

[1691] In another preferred embodiment, the present application provides a kit comprising:

[1692] a DGK alpha inhibitor A,

[1693] DGKz inhibitor A',

[1694] wherein the dose ratio (mg or mg / kg of DGK a inhibitor A : mg or mg / kg of DGKz inhibitor A') is from 1 :8 to 1 :12.

[1695] In another preferred embodiment, the present application provides a kit comprising:

[1696] DGK a inhibitor A,

[1697] DGKz inhibitor A',

[1698] wherein the dose ratio (mg or mg / kg of DGK a inhibitor A : mg or mg / kg of DGKz inhibitor A') is from 1 :1 to 1 :10.

[1699] In another preferred embodiment, the present application provides a kit comprising:

[1700] DGK a inhibitor A,

[1701] DGKz inhibitor A',

[1702] wherein the dose ratio (mg or mg / kg of DGK a inhibitor A : mg or mg / kg of DGKz inhibitor A') is about 1 :10.

[1703] In said kit, either or both of said one DGK a inhibitor compound and said one DGKz inhibitor compound in any of the above combinations are optionally in the form of a pharmaceutical composition, which can be used at the time of administration for simultaneous, concurrent, separate or sequential administration. Said one DGK a inhibitor compound and said one DGKz inhibitor compound can be administered independently of each other by oral, intravenous, topical, local implantation, intraperitoneal or intranasal route. Preferably, said one DGK a inhibitor compound and said one DGKz inhibitor compound are both administered by oral route, or said one DGK a inhibitor compound is administered by oral route and said one DGKz inhibitor compound is administered by intravenous route, or vice versa.

[1704] In another embodiment, the present application provides a kit comprising:

[1705] one DGK a inhibitor compound of general formula (I) as described herein, more particularly DGK a inhibitor A, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same,

[1706] a DGKz inhibitor compound of general formula (II) as described herein, more specifically DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same, and optionally,

[1707] component C: one or more, preferably one, other agent, and / or a CAR-T cell,

[1708] wherein optionally, any of the one DGKa inhibitor compound, the one DGKz inhibitor compound, and the component C in any of the above combinations are in the form of a pharmaceutical composition which can be used at any time for simultaneous, concurrent, separate or sequential administration. The one DGKa inhibitor compound, the one DGKz inhibitor compound, and optionally the component C, can be administered independently from each other by oral, intravenous, topical, local implantation, intraperitoneal or intranasal route.

[1709] In another embodiment, the present application provides a kit comprising:

[1710] DGKa inhibitor A, or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same,

[1711] DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same, and optionally,

[1712] component C: one or more, preferably one, other agent, and / or a CAR-T cell,

[1713] wherein optionally, any of the DGKa inhibitor A, or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same, the DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same, and the component C in any of the above combinations are in the form of a pharmaceutical composition which can be used at any time for simultaneous, concurrent, separate or sequential administration. The DGKa inhibitor A, or a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same, the DGKz inhibitor A', or a stereoisomer, a tautomer, an N-oxide, a hydrate, a...

Claims

1. A combination comprising one or more DGKα inhibitors and one or more DGKζ inhibitors.

2. The combination according to claim 1, comprising a DGKα inhibitor and a DGKζ inhibitor.

3. The combination according to claim 1 or 2, comprising a DGKα inhibitor compound of the general formula (I), in: R 1 represents a group selected from cyano, -C(=O)NH2, -C(=O)N(H)CH3, -C(=O)N(H)C2H5, -C(=O)N(CH3)2 and -C(=O)OR 15 Groups; R 2 represents a group selected from phenyl, naphthyl and 5- to 10-membered heteroaryl, wherein the 5- to 10-membered heteroaryl group is attached to the remainder of the molecule via a carbon atom of said 5- to 10-membered heteroaryl group, as well as wherein phenyl, naphthyl and 5- to 10-membered heteroaryl groups are optionally substituted once, twice, three times or four times, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C6-alkyl, C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, (C1-C2-alkoxy)-(C1-C6-alkyl)-, C1-C6-alkoxy, (C1-C2-alkoxy)-(C1-C6-alkoxy)-, C1-C6-haloalkoxy, C3-C6-cycloalkyloxy, phenoxy, -SR 14 、-S(=O)R 14 、-S(=O)2R 14 、-P(=O)(R 14 )2, cyano, hydroxyl, -N(R 9 )(R 10 )、-C(=O)N(R 9 )(R 10 ),-C(=O)R 11 、-N(R 12 )C(=O)R 13 、-N(R 12 )S(=O)2R 14 、-N=S(=NH)(R 14 )2、-N=S(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl, and 5- or 6-membered heteroaryl, or two substituents of the phenyl group, when they are attached to adjacent ring atoms, are optionally linked to each other in such a way that they together form a group selected from the group consisting of: -(CH2)3-, -CH2-CH(OH)-CH2-, -(CH2)4-, -O-(CH2)2-, -(CH2)2-O-, -CH2-CH(CH3)-O-, -CH2-O-CH2-, -O-(CH2)3-, -(CH2)3-O-, -CH2-O-(CH2)2-, -(CH2)2-O-CH2-, -O-CH2-O-, -OC(CH3)2-O-, -O-(CH2)2-O-, -N(R 18 )-C(=O)-(C(R 18 )(R 19 )) m -、-N(R 18 )-C(=O)-(C(CH2)3)-、-N(R 18 )-(C(R 18 )(R 19 )) m -、-N(R 18 )-C(=O)-O- and -N(R 18 )-C(=O)-N(R 18 )-, wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, as well as wherein the 4- to 7-membered heterocycloalkyl group, the 5- to 7-membered heterocycloalkenyl group and the (4- to 7-membered heterocycloalkyl)oxy group are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, as well as wherein the C1-C6-alkyl and C1-C6-alkoxy groups are optionally substituted by groups selected from C3-C4-cycloalkyl, phenyl and 4- to 7-membered heterocycloalkyl, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, as well as The phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), as well as wherein the C3-C4-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of a cyano group and a hydroxyl group, as well as wherein the C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a C1-C4-alkyl group, as well as wherein the phenyl, phenoxy and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 3 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C6-cycloalkenyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, (C1-C2-alkoxy)-(C1-C6-alkyl)-, C1-C6-alkoxy, (C1-C2-alkoxy)-(C1-C6-alkoxy)-, C1-C4-haloalkoxy, C3-C6-cycloalkyloxy, phenoxy, -SR 14 、-S(=O)R 14 、-S(=O)2R 14 , cyano, hydroxyl, -N(R 9 )(R 10 )、-C(=O)N(R 9 )(R 10 ),-C(=O)R 11 、-N(R 12 )C(=O)R 13 、-N(R 12 )S(=O)2R 14 、-N=S(=NH)(R 14 )2、-N=S(=O)(R 14 )2、-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl, and 5- or 6-membered heteroaryl, wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, as well as wherein the 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, and (4- to 7-membered heterocycloalkyl)oxy groups are optionally substituted once, twice, or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, as well as wherein the C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C1-C6-alkoxy groups are optionally substituted by groups selected from the group consisting of C3-C4-cycloalkyl, phenyl and 4- to 7-membered heterocycloalkyl, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, and wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), as well as wherein the C3-C4-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of a cyano group and a hydroxyl group, as well as wherein the C2-C6-alkenyl group is optionally substituted by a C1-C4-haloalkyl group, as well as wherein the C3-C6-cycloalkyl and C4-C6-cycloalkenyl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl, as well as wherein the phenyl, phenoxy and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 4 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C6-cycloalkenyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, (C1-C2-alkoxy)-(C1-C6-alkyl)-, C1-C6-alkoxy, (C1-C2-alkoxy)-(C1-C6-alkoxy)-, C1-C4-haloalkoxy, -O-(C1-C4-alkyl)-C(=O)OR 15 、-O-(C1-C4-alkyl)-C(=O)N(R 9 )(R 10 ), C3-C6-cycloalkyloxy, -S(=O)R 14 、-S(=O)2R 14 , cyano, nitro, hydroxyl, -N(R 9 )(R 10 )、-N(R 16 )(R 17 )、-N(R 16 )(R 20 )、-C(=O)N(R 9 )(R 10 ),-C(=O)R 11 、-N(R 12 )C(=O)R 13 、-N(R 12 )S(=O)2R 14 、-N=S(=NH)(R 14 )2、-N=S(=O)(R 14 )2、-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl, and 5- or 6-membered heteroaryl, wherein the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups, as well as wherein the 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, and (4- to 7-membered heterocycloalkyl)oxy groups are optionally substituted once, twice, or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, as well as wherein the C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C1-C6-alkoxy groups are optionally substituted by groups selected from C3-C4-cycloalkyl and 4- to 7-membered heterocycloalkyl, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, as well as wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), as well as wherein the C3-C4-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of a cyano group and a hydroxyl group, as well as wherein the C1-C6-alkoxy group is optionally replaced by an oxiran-2-yl group generation, as well as wherein the C3-C6-cycloalkyl and C4-C6-cycloalkenyl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a C1-C4-alkyl group, as well as wherein the phenyl and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 5 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C6-cycloalkenyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, (C1-C2-alkoxy)-(C1-C6-alkyl)-, C1-C6-alkoxy, (C1-C2-alkoxy)-(C2-C6-alkoxy)-, C1-C4-haloalkoxy, C3-C6-cycloalkyloxy, phenoxy, -SR 14 、-S(=O)R 14 、-S(=O)2R 14 , cyano, hydroxyl, -N(R 9 )(R 10 )、-C(=O)N(R 9 )(R 10 ),-C(=O)R 11 、-N(R 12 )C(=O)R 13 、-N(R 12 )S(=O)2R 14 、-N=S(=NH)(R 14 )2、-N=S(=O)(R 14 )2、-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy, phenyl, and 5- or 6-membered heteroaryl, wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, as well as wherein the 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, and (4- to 7-membered heterocycloalkyl)oxy groups are optionally substituted once, twice, or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, as well as wherein the C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl and C1-C6-alkoxy groups are optionally substituted by groups selected from the group consisting of C3-C4-cycloalkyl, phenyl and 4- to 7-membered heterocycloalkyl, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl, -N(R 9 )(R 10 ) and oxo, and wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), as well as wherein the C3-C4-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of a cyano group and a hydroxyl group, as well as wherein the C3-C6-cycloalkyl and C4-C6-cycloalkenyl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a C1-C4-alkyl group, as well as wherein the phenyl, phenoxy and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxy, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 6 represents a hydrogen atom or a fluorine atom or a group selected from the group consisting of C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, hydroxy and oxo, R 7 represents a hydrogen atom or a halogen atom or a radical selected from the group consisting of C1-C4-alkyl, C1-C4-alkoxy, hydroxy and cyano, R 8 represents a group selected from methyl and ethyl, R 9 and R 10 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C2-C4-hydroxyalkyl, N≡C-(C1-C4-alkyl)-, (C1-C4-alkoxy)-(C2-C4-alkyl)-, C3-C4-cycloalkyl and C2-C4-haloalkyl, or R 9 and R 10 Together with the nitrogen to which they are attached, they represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group, wherein the nitrogen-containing 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl, C3-C4-cycloalkyl, hydroxyl and oxo, or Two substituents attached to the same carbon atom of the nitrogen-containing 4- to 7-membered heterocycloalkyl group together with the carbon atom to which they are attached represent a 4- to 7-membered heterocycloalkyl group, wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C4-alkyl, C3-C4-cycloalkyl, C1-C4-haloalkyl, hydroxyl and oxo, R 11 represents a hydrogen atom or a radical selected from C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-haloalkyl, phenyl and 5- or 6-membered heteroaryl, wherein the phenyl group and the 5- or 6-membered heteroaryl group are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 12 represents a hydrogen atom or a C1-C4-alkyl group, R 13 represents a hydrogen atom or a group selected from the group consisting of C1-C6-alkyl, phenyl and 5- or 6-membered heteroaryl, wherein the phenyl group and the 5- or 6-membered heteroaryl group are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 14 represents a radical selected from C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, phenyl and 5- or 6-membered heteroaryl, wherein the phenyl group and the 5- or 6-membered heteroaryl group are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C2-alkyl, C1-C2-haloalkyl, cyano, hydroxyl, C1-C2-alkoxy, C3-C4-cycloalkyl and -N(R 9 )(R 10 ), R 15 represents a hydrogen atom or a C1-C4-alkyl group, R 16 represents a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C3-C4-cycloalkyl and C2-C4-haloalkyl, R 17 represents a 4- to 7-membered heterocycloalkyl group, wherein the 4- to 7-membered heterocycloalkyl is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: C1-C4-alkyl, C3-C4-cycloalkyl, C1-C4-alkoxy, hydroxyl and oxo, as well as wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, R 18 represents a hydrogen atom or a group selected from a methyl group and an ethyl group, R 19 represents a hydrogen atom or a group selected from a methyl group and an ethyl group, R 20 represents a (4- to 7-membered heterocycloalkyl)-(C1-C4-alkyl)- group, wherein the (4- to 7-membered heterocycloalkyl) portion of the group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C4-alkyl, C3-C4-cycloalkyl, C1-C4-alkoxy, hydroxy and oxo, m represents an integer selected from 1, 2 and 3, as well as n represents an integer selected from 1, 2 and 3, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof; as well as A DGKζ inhibitor compound of general formula (II), in: R 1 represents a phenyl group or a 6-membered heteroaryl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: hydroxyl, cyano, nitro, C1-C6-alkyl, (phenyl)-(C1-C3-alkyl)-, C1-C6-haloalkyl, C1-C6-alkoxy, (phenyl)-(C1-C3-alkoxy)-, C1-C6-haloalkoxy, -N(R 5 )(R 6 ), wherein the phenyl groups in the (phenyl)-(C1-C3-alkyl)- and (phenyl)-(C1-C3-alkoxy)- groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy, or two substituents attached to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a divalent group selected from the group consisting of: -(CH2)3-, -(CH2)4-, -(CH2)2-O-, -(CH2)3-O-, -CH2-O-CH2-, -(CH2)2-O-CH2-, -O-CH2-O-, -O-CH2-CH2-O-, -O-CF2-O-, -O-CH2-CF2-O-, and -O-CF2-CF2-O-, or R 1 represents a 5-membered heteroaryl group which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from cyano, C1-C3-alkyl and C1-C3-alkoxy; R 2 express Group, Where "*" represents R 2 The site of attachment to the nitrogen atom; R 3 represents a group selected from methyl and -NH2; R 4 represents a phenyl or 6-membered heteroaryl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or from a cyano group, a nitro group, a C1-C6-alkyl group, a (phenyl)-C1-C3-alkyl)-, a (5- or 6-membered heteroaryl)-(C1-C3-alkyl)-, a (C3-C7-cycloalkyl)-(C1-C3-alkyl)-, a (R 9 )O)-(C1-C6-alkyl)-, C1-C6-haloalkyl, C3-C7-cycloalkyl, -OR 9 、-N(R 10 )(R 11 )、((R 10 )(R 11 )N)-(C1-C3-alkyl)-, -C(=O)-N(R 12 )(R 13 ), -S(=O) n -R 14 、-C(=O)R 14 、-C(=O)-OR 17 and a 5- or 6-membered heteroaryl group optionally substituted by one or two substituents selected from halogen atoms and methyl groups, or two substituents attached to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a divalent group selected from the group consisting of: -(CH2)3-, -(CH2)4-, -(CH2)2-O-, -(CH2)3-O-, -CH2-O-CH2-, -(CH2)2-O-CH2-, -O-CH2-O-, -O-CH2-CH2-O-, -O-CF2-O-, -O-CH2-CF2-O-, and -O-CF2-CF2-O-; R 5 and R 6 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, (C1-C4-alkyl)-C(═O)-, C3-C4-cycloalkyl and (phenyl)-(C1-C3-alkyl)-, or R 5 and R 6 together with the nitrogen atom to which they are attached represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from oxo, hydroxy, C1-C4-alkyl, (C1-C4-alkyl)-C(═O)-, C3-C4-cycloalkyl and C1-C4-alkoxy; R 7 represents a hydrogen atom or a C1-C2-alkyl group; R 8 represents a group selected from -C(=O)-NH2 and -S(=O)2-NH2; R 9 represents a hydrogen atom or is selected from C1-C6-alkyl, (5- or 6-membered heteroaryl)-(C1-C3-alkyl)-, (phenyl)-(C1-C3-alkyl)-, C1-C6-haloalkyl, C2-C4-hydroxyalkyl, (C1-C3-alkoxy)-C2-C3-alkyl-, ((C1-C3-alkyl)-C(=O)-O)-C2-C3-alkyl-, C(R 18 )(R 19 )-C(=O)-OR 17 、-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ), phenyl and 5- or 6-membered heteroaryl groups, wherein the phenyl group of the (phenyl)-(C1-C3-alkyl)-group and the phenyl group itself, and the 5- or 6-membered heteroaryl group of the (5- or 6-membered heteroaryl)-(C1-C3-alkyl)-group and the 5- or 6-membered heteroaryl group itself are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy; R 10 and R 11 independently of one another represent a hydrogen atom or a member selected from the group consisting of C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-hydroxyalkyl, (C1-C3-alkoxy)-C2-C3-alkyl-, ((R 22 )(R 23 )N)-C2-C3-alkyl, (C3-C7-cycloalkyl)-(C1-C3-alkyl)-, (C1-C4-alkyl)-C(═O)-, C3-C7-cycloalkyl, (C3-C7-cycloalkyl)-C(═O)-, (phenyl)-(C1-C3-alkyl)-, (phenyl)-(C1-C3-alkyl)-C(═O)-, (phenyl)-(C1-C3-alkyl)-OC(═O)-, phenyl and 5- or 6-membered heteroaryl groups, wherein the C3-C7-cycloalkyl group and the C3-C7-cycloalkyl group in the (C3-C7-cycloalkyl)-(C1-C3-alkyl)- and (C3-C7-cycloalkyl)-C(═O)- groups are optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from a cyano group, a C1-C2-alkyl group and a C1-C2-fluoroalkyl group, and wherein the phenyl and the 5- or 6-membered heteroaryl groups, and the phenyl groups in the (phenyl)-(C1-C3-alkyl)-, (phenyl)-(C1-C3-alkyl)-C(═O)- and (phenyl)-(C1-C3-alkyl)-OC(═O)- groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy, or R 10 and R 11 Together with the nitrogen atom to which they are attached, they represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group or a bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or selected from cyano, oxo, hydroxyl, C1-C4-alkyl, C1-C4-haloalkyl, (C1-C4-alkyl)-C(=O)-, C3-C7-cycloalkyl, C1-C4-alkoxy, -N(R 22 )(R 23 ) and a monocyclic 4- to 7-membered heterocycloalkyl group; R 12 and R 13 each independently represents a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-hydroxyalkyl, (C1-C4-alkoxy)-C2-C3-alkyl-, (C1-C4-haloalkoxy)-C2-C3-alkyl-, (phenoxy)-C2-C3-alkyl-, C3-C7-cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C1-C3-alkyl)-, wherein the C3-C7-cycloalkyl and monocyclic 4 to 7-membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, oxo, hydroxyl, C1-C4-alkyl, (C1-C4-alkyl)-C(=O)-, C3-C4-cycloalkyl and C1-C4-alkoxy, and wherein the (phenoxy)-C2-C3-alkyl-group and the phenyl group in the (phenyl)-(C1-C3-alkyl)-group are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy, or R 12 and R 13 together with the nitrogen atom to which they are attached represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, oxo, hydroxy, C1-C4-alkyl, (C1-C4-alkyl)-C(═O)-, C3-C4-cycloalkyl and C1-C4-alkoxy; R 14 represents a group selected from C1-C4-alkyl, C1-C4-haloalkyl and phenyl, wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy; R 17 represents a C1-C4-alkyl group; R 18 and R 19 independently of one another represent a hydrogen atom or a C1-C4-alkyl group; R 20 represents a hydrogen atom or is selected from C1-C6-alkyl, C3-C4-alkenyl, C3-C4-alkynyl, C1-C3-alkoxy, C3-C7-cycloalkyl, bicyclo C5-C 11 - a group of cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 11-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl, wherein the C1-C6-alkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or from a hydroxyl group, a cyano group, a C1-C3-alkoxy group, -N(R 22 )(R 23 ), C3-C7-cycloalkyl, bicyclic C5-C 11 - a radical of cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 11-membered heterocycloalkyl, phenyl, and 5- to 10-membered heteroaryl, said phenyl and 5- to 10-membered heteroaryl substituents themselves being optionally substituted once or twice, each substituent being independently selected from a halogen atom or a radical selected from cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino, and trifluoromethoxy, And wherein the C3-C7-cycloalkyl, bicyclic C5-C 11 -cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl and bicyclic 5- to 11-membered heterocycloalkyl groups are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from cyano, oxo, hydroxyl, C1-C4-alkyl, (C1-C4-alkyl)-C(=O)-, C3-C4-cycloalkyl and C1-C4-alkoxy, and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl groups are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or selected from a cyano group, a C1-C4-alkyl group, a C1-C4-haloalkyl group, a C1-C4-alkoxy group, a C1-C4-haloalkoxy group, a -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ), R 21 represents a hydrogen atom or a C1-C4-alkyl group, or R 20 and R 21 together with the nitrogen atom to which they are attached, represents an optionally benzo-fused monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group, and which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or from cyano, oxo, hydroxyl, C1-C4-alkyl, C1-C4-haloalkyl, (phenyl)-(C1-C3-alkyl)-, (C1-C4-alkyl)-C(=O)-, C3-C4-cycloalkyl, C1-C4-alkoxy, C1-C3-haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ); R 22 and R 23 independently of one another represent a hydrogen atom or a group selected from C1-C2-alkyl and (C1-C2-alkyl)-C(═O)-; R 24 and R 25 independently of one another represent a hydrogen atom or are selected from C1-C4-alkyl groups; and n represents an integer 0, 1 or 2, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

4. A combination according to any one of claims 1, 2 or 3, comprising a DGKα inhibitor compound of the general formula (I), in: R 1 represents a group selected from cyano, -C(=O)NH2, -C(=O)N(H)CH3 and -C(=O)N(CH3)2; R 2 represents a group selected from phenyl, naphthyl and 5- to 10-membered heteroaryl, wherein the 5- to 10-membered heteroaryl group is attached to the remainder of the molecule via a carbon atom of said 5- to 10-membered heteroaryl group, as well as wherein phenyl, naphthyl and 5- to 10-membered heteroaryl groups are optionally substituted once, twice, three times or four times, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C6-alkyl, C3-C5-cycloalkyl, C1-C4-haloalkyl, (C1-C2-alkoxy)-(C1-C2-alkyl)-, C1-C4-alkoxy, C1-C4-haloalkoxy, phenoxy, -S(=O)2R 14 、-P(=O)(R 14 )2, cyano, hydroxyl, -N(R 9 )(R 10 )、-C(=O)N(R 9 )(R 10 ),-C(=O)R 11 、-N(R 12 )C(=O)R 13 、-N(R 12 )S(=O)2R 14 、-N=S(=O)(R 14 ) 2, 4 to 7 membered heterocycloalkyl, phenyl and 5 or 6 membered heteroaryl, or two substituents of the phenyl group, when they are attached to adjacent ring atoms, are optionally linked to each other in such a way that they together form a group selected from the group consisting of: -CH2-CH(OH)-CH2-, -CH2-CH(CH3)-O-, -OC(CH3)2-O-, -N(R 18 )-C(=O)-(C(R 18 )(R 19 )) m -、-N(R 18 )-C(=O)-(C(CH2)3)-、-N(R 18 )-(C(R 18 )(R 19 )) m -、-N(R 18 )-C(=O)-O- and -N(R 18 )-C(=O)-N(R 18 )-, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the C1-C4-alkoxy group is optionally substituted by a group selected from 4- to 7-membered heterocycloalkyl and phenyl, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the phenyl and 5- or 6-membered heteroaryl groups are optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of C1-C2-alkyl, C1-C2-haloalkyl and C1-C2-alkoxy, R 3 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C2-C4-alkenyl, C3-C5-cycloalkyl, (C1-C2-alkoxy)-(C1-C4-alkyl)-, C1-C4-alkoxy, C1-C4-haloalkoxy, C3-C5-cycloalkyloxy, -S(=O)2R 14 , cyano, hydroxyl, -N(R 9 )(R 10 )、-C(=O)N(R 9 )(R 10 ),-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy and phenyl, wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, as well as wherein the C1-C6-alkyl and C1-C4-alkoxy groups are optionally substituted by groups selected from C3-C4-cycloalkyl and 4- to 7-membered heterocycloalkyl groups, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the C3-C4-cycloalkyl group is optionally substituted once or twice by a cyano group, as well as wherein the C2-C4-alkenyl group is optionally replaced by a C1-C4-haloalkyl group generation, as well as wherein the C3-C5-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl and C1-C4-haloalkyl, R 4 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C6-alkyl, C1-C6-haloalkyl, C3-C5-cycloalkyl, (C1-C2-alkoxy)-(C1-C4-alkyl)-, C1-C4-alkoxy, (C1-C2-alkoxy)-(C1-C4-alkoxy)-, -O-(C1-C4-alkyl)-C(=O)OR 15 、-O-(C1-C4-alkyl)-C(=O)N(R 9 )(R 10 ), C3-C5-cycloalkyloxy, -S(=O)2R 14 , cyano, nitro, hydroxyl, -N(R 9 )(R 10 )、-N(R 16 )(R 17 )、-N(R 16 )(R 20 ),-N=S(=NH)(R 14 )2、-N=S(=O)(R 14 )2、-P(=O)(R 14 )2, 4- to 7-membered heterocycloalkyl, 5- to 7-membered heterocycloalkenyl, (4- to 7-membered heterocycloalkyl)oxy and phenyl, wherein the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups, as well as wherein the C1-C6-alkyl and C1-C4-alkoxy groups are optionally substituted by groups selected from C3-C4-cycloalkyl and 4- to 7-membered heterocycloalkyl groups, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, as well as wherein the C3-C4-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of a cyano group and a hydroxyl group, as well as wherein the C1-C4-alkoxy group is optionally substituted by an oxiran-2-yl group, as well as wherein the C3-C5-cycloalkyl radical is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a C1-C4-alkyl radical, R 5 represents a hydrogen atom or a halogen atom or a group selected from the following: C1-C5-alkyl, C3-C5-cycloalkyl, C1-C4-alkoxy, C3-C5-cycloalkoxy, -S(=O)2R 14 , cyano, hydroxyl, -N(R 9 )(R 10 ), 4- to 7-membered heterocycloalkyl, and (4- to 7-membered heterocycloalkyl)oxy, wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group, R 6 represents a hydrogen atom or a group selected from the group consisting of C1-C4-alkyl and C1-C4-hydroxyalkyl, R 7 represents a hydrogen atom or a halogen atom or a radical selected from the group consisting of C1-C4-alkyl, C1-C4-alkoxy and hydroxy, R 8 represents a group selected from methyl and ethyl, R 9 and R 10 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C2-C4-hydroxyalkyl, N≡C-(C1-C4-alkyl)-, (C1-C4-alkoxy)-(C2-C4-alkyl)- and C3-C4-cycloalkyl, or R 9 and R 10 Together with the nitrogen to which they are attached, they represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group, wherein the nitrogen-containing 4- to 7-membered heterocycloalkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C4-alkyl, hydroxyl and oxo, or Two substituents attached to the same carbon atom of the nitrogen-containing 4- to 7-membered heterocycloalkyl group together with the carbon atom to which they are attached represent a 4- to 7-membered heterocycloalkyl group, wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once or twice by a C1-C4-alkyl group, R 11 represents a group selected from C1-C4-alkyl and C1-C4-haloalkyl, R 12 represents a hydrogen atom, R 13 represents a phenyl group, R 14 represents a group selected from C1-C4-alkyl and phenyl, R 15 represents a hydrogen atom or a C1-C4-alkyl group, R 16 represents a hydrogen atom or a C1-C4-alkyl group, R 17 represents a 4- to 7-membered heterocycloalkyl group, wherein the 4- to 7-membered heterocycloalkyl radical is optionally substituted once or twice by a C1-C4-alkyl radical, as well as wherein the 4- to 7-membered heterocycloalkyl group is attached to the remainder of the molecule via a carbon atom of the 4- to 7-membered heterocycloalkyl group, R 18 represents a hydrogen atom or a methyl group, R 19 represents a hydrogen atom or a methyl group, R 20 represents a (4- to 7-membered heterocycloalkyl)-(C1-C4-alkyl)- group, wherein the (4- to 7-membered heterocycloalkyl) part of the group is optionally substituted once or twice by a C1-C4-alkyl group, m represents an integer selected from 1 and 2, wherein the 4- to 7-membered heterocycloalkyl group is optionally substituted once or twice by C1-C4-alkyl, as well as n represents an integer selected from 1, 2 and 3, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof; as well as A DGKζ inhibitor compound of general formula (II), in: R 1 represents a phenyl or pyridyl group which is optionally substituted once, twice or three times, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom or a group selected from the group consisting of hydroxyl, cyano, C1-C4-alkyl, C1-C2-fluoroalkyl, C1-C2-alkoxy, (phenyl)-(C1-C2-alkoxy)-, C1-C2-fluoroalkoxy and -N(R 5 )(R 6 ), or two substituents attached to adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group selected from: -(CH2)3-, -O-CH2-O- and -O-CF2-O-, or R 1 represents a pyrazolyl group optionally substituted by a methyl group; R 2 express Group, Where "*" represents R 2 The site of attachment to the nitrogen atom; R 3 represents a group selected from methyl and -NH2; R 4 represents a phenyl or pyridyl group which is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or from a cyano group, a C1-C3-alkyl group, ((R 9 )O)-(C1-C3-alkyl)-, C1-C3-fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ), -S(=O) n -R 14 and -C(=O)-OR 17 , or two substituents attached to adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group selected from: -(CH2)3-, -O-CH2-O-, and -O-CF2-O-; R 5 and R 6 independently of one another represent a hydrogen atom or a C1-C2-alkyl group, or R 5 and R 6 together with the nitrogen atom to which they are attached represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from hydroxy and C1-C2-alkyl; R 7 represents a hydrogen atom or a C1-C2-alkyl group; R 8 represents a -C(=O)-NH2 group; R 9 represents a hydrogen atom or is selected from C1-C2-alkyl, benzyl, C1-C2-fluoroalkyl, C2-hydroxyalkyl, (C1-C2-alkoxy)-C2-alkyl-, ((C1-C2-alkyl)-C(=O)-O)-C2-alkyl-, C(R 18 )(R 19 )-C(=O)-OR 17 、-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ) and a phenyl group, wherein the phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a chlorine atom or a group selected from a cyano group and a methyl group; R 10 and R 11 each independently represents a hydrogen atom or a group selected from C1-C2-alkyl, C1-C2-fluoroalkyl, (C3-C5-cycloalkyl)-(C1-C2-alkyl)-, (C1-C2-alkyl)-C(═O)-, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C(═O)-, (phenyl)-(C1-C2-alkyl)-, (phenyl)-(C1-C2-alkyl)-C(═O)- and (phenyl)-(C1-C2-alkyl)-OC(═O)-, wherein the C3-C7-cycloalkyl group and the C3-C5-cycloalkyl group in the (C3-C5-cycloalkyl)-(C1-C2-alkyl)- and the C3-C7-cycloalkyl group in the C3-C7-cycloalkyl-C(═O)- group are optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from a cyano group, a C1-C2-alkyl group and a C1-C2-fluoroalkyl group, and wherein the phenyl groups in the (phenyl)-(C1-C2-alkyl)-, (phenyl)-(C1-C2-alkyl)-C(═O)- and (phenyl)-(C1-C2-alkyl)-OC(═O)- groups are optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl groups, or R 10 and R 11 together with the nitrogen atom to which they are attached, represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from cyano, oxo, C1-C2-alkyl, C1-C2-fluoroalkyl and (C1-C2-alkyl)-C(═O)—; R 12 and R 13 each independently represents a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-hydroxyalkyl, (C1-C4-alkoxy)-C2-C3-alkyl-, (C1-C2-fluoroalkoxy)-C2-C3-alkyl-, (phenoxy)-C2-C3-alkyl-, C3-C7-cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C1-C2-alkyl)-, wherein the C3-C7-cycloalkyl and monocyclic 4 to 7-membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from oxo, C1-C2-alkyl and (C1-C2-alkyl)-C(=O)-, and wherein the (phenoxy)-C2-C3-alkyl-group and the phenyl group in the (phenyl)-(C1-C2-alkyl)-group are optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms or from a group selected from methyl, trifluoromethyl and methoxy, or R 12 and R 13 together with the nitrogen atom to which they are attached, represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from oxo, C1-C2-alkyl and (C1-C2-alkyl)-C(═O)—; R 14 represents a group selected from methyl and trifluoromethyl; R 17 represents a C1-C2-alkyl group; R 18 and R 19 independently of one another represent a hydrogen atom or a methyl group; R 20 represents a hydrogen atom or a radical selected from optionally substituted C1-C3-alkyl, unsubstituted C4-C6-alkyl, prop-2-ynyl, methoxy, C3-C6-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, wherein the C1-C3-alkyl group is optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or from a hydroxyl group, a cyano group, a C1-C3-alkoxy group, -N(R 22 )(R 23 ), C3-C6-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl groups, said phenyl and 5- to 10-membered heteroaryl substituents themselves being optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl groups, and wherein the C3-C6-cycloalkyl, adamantyl and monocyclic 4 to 7-membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from a fluorine atom or a group selected from oxo, C1-C2-alkyl and (C1-C2-alkyl)-C(═O)-, and wherein the phenyl and 5- to 10-membered heteroaryl groups are optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms and chlorine atoms or selected from cyano, C1-C2-alkyl, C1-C2-fluoroalkyl, C1-C2-alkoxy, C1-C2-fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ), R 21 represents a hydrogen atom or a C1-C2-alkyl group, or R 20 and R 21 Together with the nitrogen atom to which they are attached, they represent an optionally benzo-fused monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group, and they are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or selected from cyano, oxo, hydroxyl, C1-C2-alkyl, C1-C2-fluoroalkyl, benzyl, (C1-C2-alkyl)-C(=O)-, C3-C4-cycloalkyl, C1-C2-alkoxy, C1-C2-fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ); R 22 and R 23 independently of one another represent a hydrogen atom or a group selected from C1-C2-alkyl and (C1-C2-alkyl)-C(═O)-; R 24 and R 25 independently of one another represent a hydrogen atom or are selected from C1-C2-alkyl groups; and n represents the integer 2, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

5. The combination according to any one of claims 1 to 4, comprising a DGKα inhibitor compound of the general formula (I), in: R 1 represents a group selected from cyano, -C(=O)NH2, -C(=O)N(H)CH3 and -C(=O)N(CH3)2, R 2 represents a group selected from phenyl, 1-naphthyl, 2-naphthyl, 1H-pyrazol-3-yl, 1H-pyrazol-4-yl, 1H-pyrazol-5-yl, 1,2,4-oxadiazol-5-yl, 1,3,4-oxadiazol-2-yl, 1H-1,2,3-triazol-4-yl, 2H-1,2,3-triazol-4-yl, 1,3-thiazol-2-yl, pyridin-3-yl, pyrazin-2-yl, 1H-indol-5-yl, 1-benzofuran-4-yl, 1-benzofuran-7-yl, 1H-indol-6-yl, benzothiophene-2-yl, 1,3-benzoxazol-2-yl, 1,3-benzoxazol-5-yl, 1,3-benzoxazol-6-yl, 1 ,3-benzoxazol-7-yl, 1H-indazol-5-yl, 1H-benzimidazol-2-yl, 1H-benzimidazol-4-yl, 1,3-benzothiazol-2-yl, 1,3-benzothiazol-4-yl, 1,3-benzothiazol-5-yl, 1,3-benzothiazol-6-yl, 1,3-benzothiazol-7-yl, 1H-pyrrolo[2,3-b]pyridin-3-yl, quinolin-2-yl, quinolin-4-yl, quinolin-6-yl, quinolin-7-yl, isoquinolin-5-yl, isoquinolin-7-yl, isoquinolin-8-yl, quinoxalin-2-yl, quinoxalin-5-yl and 1,3-thiazolo[5,4-b]pyridin-2-yl groups, wherein the group is optionally substituted once or twice, each substituent being independently selected from a fluorine, chlorine or bromine atom or a group selected from the group consisting of methyl, propyl, isopropyl, tert-butyl, cyclopropyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, propoxy, (prop-2-yl)oxy, methoxymethyl, 2-methoxyethyl, benzyloxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, phenoxy, (oxolan-2-yl)methoxy, (tetrahydrofuran-2-yl)methoxy, methanesulfonyl, dimethylphosphoryl yl, cyano, hydroxy, dimethylamino, oxetan-3-yl, 2-oxopyrrolidin-1-yl, 4-methyl-2-oxopiperazin-1-yl, 4-methyl-3-oxopiperazin-1-yl, morpholino-4-yl, 7-oxo-2-oxa-6-azaspiro[3.4]octan-6-yl, 8-methyl-3-oxo-2,8-diazaspiro[4.5]decan-2-yl, carbamoyl, acetyl, trifluoroacetyl, benzamido, benzylsulfonylamino, [dimethyl(oxo)-λ 6 -thiophenyl]amino, phenyl, 3-chlorophenyl, 4-chlorophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 3-trifluoromethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl and pyridin-3-yl, or Two substituents of the phenyl group, when they are attached to adjacent ring atoms, are linked to one another in such a way that they together form a group selected from the group consisting of -CH2-CH(OH)-CH2-, -CH2-CH(CH3)-O-, -OC(CH3)2-O-, -NH-C(=O)-CH(CH3)-, -N(CH3)-C(=O)-C(CH3)2-, -NH-C(=O)-(C(CH2)3)-, -NH-CH2-C(CH3)2-, -N(CH3)-C(=O)-O- and -N(CH3)-C(=O)-N(CH3)-, R 3 represents a hydrogen atom or a fluorine, chlorine or bromine atom or is selected from methyl, sec-butyl, (oxetan-3-yl)methyl, 3,3,3-trifluoroprop-1-en-2-yl, cyclopropyl, (trifluoromethyl)cyclopropyl, cyclobutyl, 2,2-dimethylcyclobutyl, 3,3-difluorocyclobutyl, methoxymethyl, methoxy, ethoxy, propoxy, 2,2-difluoroethoxy, 2,2-difluoropropoxy, cyclopropylmethoxy, (1-cyanocyclopropyl)methoxy, cyclopropyloxy, cyclobutyloxy, methanesulfonyl, cyano, hydroxy, 4-hydroxy-2-oxo-pyrrolidin-1-yl, 7-oxo-2-oxa-6-azaspiro[3.4]octan-6-yl, carbamoyl, dimethylphosphoryl, oxetan-3-yl, 3,6-dihydro-2H-pyran-4-yl, (oxetan-3-yl)oxy and phenyl radicals, R 4 represents a hydrogen atom or a fluorine, chlorine or bromine atom or is selected from methyl, sec-butyl, (oxetan-3-yl)methyl, trifluoromethyl, cyclopropyl, 3,3-difluorocyclobutyl, methoxymethyl, methoxy, propoxy, 2-methoxyethoxy, (1-hydroxycyclopropyl)methoxy, (1-cyanocyclopropyl)methoxy, (oxiran-2-yl)methoxy, carboxymethoxy, 2-tert-butoxy-2-oxo-ethoxy, 2-amino-2-oxo-ethoxy, cyclopropyloxy, cyclobutyloxy, methanesulfonyl, dimethylphosphoryl, cyano, nitro, hydroxy, (cyanomethyl)(methyl)amino, (2- hydroxyethyl)amino, (2-hydroxyethyl)(methyl)amino, (2-methoxyethyl)amino, (2-methoxyethyl)(methyl)amino, cyclopropylamino, (oxetan-3-yl)amino, methyl(oxetan-3-yl)amino, methyl(oxolan-3-yl)amino, 3-hydroxyazetidin-1-yl, 2-oxopyrrolidin-1-yl, morpholino, 1,1-dioxidothiomorpholin-4-yl, 4-hydroxy-2-oxo-pyrrolidin-1-yl, 7-oxo-2-oxa-6-azaspiro[3.4]octan-6-yl, 2,2-dimethyl-2λ 6 -diaza-1,2-dien-1-yl, [dimethyl(oxo)-λ 6 -sulfydene]amino, methyl(tetrahydrofuran-3-yl)amino, tetrahydrofuran-3-ylmethoxy, (tetrahydrofuran-3-ylmethyl)amino, oxetan-3-yl, 3,6-dihydro-2H-pyran-4-yl, (oxetan-3-yl)oxy, (tetrahydrofuran-3-yl)oxy, (tetrahydro-2H-pyran-3-yl)oxy, (tetrahydro-2H-pyran-4-yl)oxy and phenyl groups, R 5 represents a hydrogen atom or a fluorine, chlorine or bromine atom or a group selected from a methyl group, a cyclopropyl group, a methoxy group, a propoxy group, a cyclopropyloxy group, a methanesulfonyl group, a cyano group, a hydroxyl group, an oxetan-3-yl group and an oxetan-3-yloxy group, R 6 represents a hydrogen atom or a group selected from a methyl group and a hydroxymethyl group, R 7 represents a hydrogen atom or a fluorine atom or a group selected from methyl, ethyl, methoxy and hydroxyl groups, R 8 represents a group selected from methyl and ethyl, as well as n represents an integer selected from 1, 2 and 3, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof; as well as A DGKζ inhibitor compound of general formula (II), in: R 1 Representing group Where "**" represents R 1 The site of attachment to the nitrogen atom; R 2 Representing group Where "*" represents R 2 The site of attachment to the nitrogen atom; R 3 represents a group selected from methyl and -NH2; R 4 Representing group Where "#" represents R 4 the site of attachment to the carbonyl group; R 7 represents a hydrogen atom or a C1-C2-alkyl group; R 8 represents a -C(=O)-NH2 group; R 9 represents a hydrogen atom or is selected from C1-C2-alkyl, benzyl, C1-C2-fluoroalkyl, (C1-C2-alkoxy)-C2-alkyl-, ((C1-C2-alkyl)-C(=O)-O)-C2-alkyl-, -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ) and a phenyl group, wherein the phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or a group selected from cyano and methyl; R 10 and R 11 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C2-alkyl, C3-C7-cycloalkyl and (benzyl)-OC(=O)-, wherein the C3-C7-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from methyl and trifluoromethyl, and wherein the phenyl group within the (benzyl)-OC(=O)- group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group, or R 10 and R 11 Together with the nitrogen atom to which they are attached, they represent a monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from a cyano group, a methyl group and a trifluoromethyl group; R 12 and R 13 independently of one another represent a hydrogen atom or a radical selected from the group consisting of C1-C4-alkyl, C1-C2-fluoroalkyl, C1-C2-hydroxyalkyl, (C1-C4-alkoxy)-C2-alkyl-, (C1-C2-fluoroalkoxy)-C2-alkyl-, (phenoxy)-C2-alkyl-, C3-C7-cycloalkyl and (phenyl)-(C1-C2-alkyl)-, wherein the (phenoxy)-C2-alkyl-group and the phenyl group in the (phenyl)-(C1-C2-alkyl)-group are optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms or a group selected from methyl, trifluoromethyl and methoxy; R 17 represents a C1-C2-alkyl group; R 18 and R 19 independently of one another represent a hydrogen atom or a methyl group; R 20 represents a group selected from benzyl and phenyl, wherein the phenyl group and the phenyl group in the benzyl group are optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group, R 21 represents a hydrogen atom or a methyl group, Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=; Y 2 represents -C(H)= or -N=; Y 3 Indicates -C(R 27 )=or-N=; The condition is that if Y 2 Indicates -N=, then Y 3 Indicates -C(R 27 )=, and if Y 3 Indicates -N=, then Y 2 represents -C(H)=; R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or a group selected from a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group, R 27 represents a halogen atom or is selected from C1-C2-alkyl, C1-C2-fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR 17 The group, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

6. The combination according to any one of claims 1 to 5, comprising a DGKα inhibitor compound of the general formula (I) selected from the group consisting of: 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(7-fluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-fluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-fluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-bromo-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-fluoro-1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-bromo-1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(7-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)-4-fluoropiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(4-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-chloro-1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-chloro[1,3]thiazolo[5,4-b]pyridin-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-methyl-4-[6-(trifluoromethoxy)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5,6-difluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-tert-butyl-1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[5-(methylsulfonyl)-1,3-benzoxazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-fluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-1-methyl-4-{4-methyl-4-[6-(trifluoromethoxy)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-1-methyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-4-[4-(5,6-difluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-1-methyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[4-(2,2,2-trifluoroethoxy)phenyl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-(4-{4-[(propan-2-yl)oxy]phenyl}piperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-ethoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-cyclopropylphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(4-propoxyphenyl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, N-{4-[1-(3-cyano-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)piperidin-4-yl]phenyl}benzenesulfonamide, 4-[4-(3-cyclopropylphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[4-(dimethylamino)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[4-(propan-2-yl)phenyl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[4-(Benzyloxy)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, N-{4-[1-(3-cyano-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)piperidin-4-yl]phenyl}benzamide, 1-methyl-4-[4-(1-methyl-1H-indol-5-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-fluoro-5-methylphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(2-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-([1,1'-biphenyl]-4-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-chlorophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(4-phenoxyphenyl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-(4-phenylpiperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-(4-methyl-4-phenylpiperidin-1-yl)-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[4-(2-oxopyrrolidin-1-yl)phenyl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(2-fluorophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[4-(trifluoromethyl)phenyl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-fluorophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[3-(morpholin-4-yl)phenyl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-cyano-2-methylphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[4-(methylsulfonyl)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[4-(4-methyl-2-oxopiperazin-1-yl)phenyl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, N-{3-[1-(3-cyano-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)piperidin-4-yl]phenyl}benzenesulfonamide, 4-[4-(3-{[dimethyl(oxo)-λ 6 -sulfydene]amino}phenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(naphthalen-1-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-4-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[1-methyl-3-(trifluoroacetyl)-1H-indol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1-benzofuran-7-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(Isoquinolin-7-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-7-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, N-{3-[1-(3-cyano-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)piperidin-4-yl]phenyl}benzamide, 4-[4-(Isoquinolin-8-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(Isoquinolin-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(quinoxalin-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[3-(methylsulfonyl)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-Fluorophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(2-methylphenyl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(4-methylphenyl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3,5-dichlorophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-bromophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-cyanophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[3-(difluoromethyl)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-bromophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-1-methyl-2-oxo-4-(4-phenylpiperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-7-phenyl-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3,7-dicarbonitrile, 7-cyclopropyl-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(2,2-dimethyl-2λ 6 -diazathia-1,2-dien-1-yl)-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-7-(oxetan-3-yl)-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(Methylsulfonyl)-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-{[dimethyl(oxo)-λ 6 -sulfydene]amino}-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(3,6-dihydro-2H-pyran-4-yl)-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1-benzofuran-4-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-(4-{4-[(propan-2-yl)oxy]phenyl}piperidin-1-yl)-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-ethylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-2-oxo-4-{4-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}-1,2-dihydroquinoline-3-carboxamide, 4-[4-(5,6-difluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-bromo-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-Methyl-4-[3-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, a mixture of stereoisomers, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-2-oxo-4-(4-phenylpiperidin-1-yl)-1,2-dihydroquinoline-3-carboxamide, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-7-(oxetane-3-yl)-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-1,2-dihydroquinoline-3-carboxamide, (rac)-1-methyl-2-oxo-4-{4-[4-(propan-2-yl)phenyl]azepan-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{(4S)-4-[4-(propan-2-yl)phenyl]azepan-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{(4R)-4-[4-(propan-2-yl)phenyl]azepan-1-yl}-1,2-dihydroquinoline-3-carbonitrile, (rac)-4-[4-(1,3-benzoxazol-2-yl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-{4-[(propyl-2-yl)oxy]phenyl}azepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-4-[4-(4-methoxyphenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[(4R)-4-(4-methoxyphenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[(4S)-4-(4-methoxyphenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-4-[4-(1,3-benzoxazol-2-yl)azepan-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[(4R)-4-(1,3-benzoxazol-2-yl)azepan-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[(4S)-4-(1,3-benzoxazol-2-yl)azepan-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-4-[4-(4-chlorophenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[(4R)-4-(4-chlorophenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[(4SR)-4-(4-chlorophenyl)azepan-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-7-bromo-1-methyl-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-7-(oxetan-3-yl)-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-7-(morpholin-4-yl)-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-7-(1,1-dioxo-1λ 6 -thiomorpholin-4-yl)-1-methyl-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, (rac)-7-bromo-1-methyl-2-oxo-4-[4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carboxamide, 7-bromo-1-methyl-2-oxo-4-[(4S)-4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carboxamide, 7-bromo-1-methyl-2-oxo-4-[(4S)-4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carboxamide, 4-[4-ethyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-4-[4-ethyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-methoxypyridin-3-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(6-methylpyridin-3-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(pyridin-3-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-N,1-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-N,N,1-trimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(1-methyl-1H-benzimidazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(3-propyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(pyrazin-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-hydroxy-4-[3-(trifluoromethyl)phenyl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-fluoro-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-8-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-8-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-8-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-4-[4-(5,6-difluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-8-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-8-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3,8-dicarbonitrile, 8-(Methylsulfonyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-6-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-6-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3,6-dicarbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3,6-dicarbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3,6-dicarbonitrile, 6-cyclopropyl-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(Methylsulfonyl)-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-6-(oxetane-3-yl)-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(3,6-dihydro-2H-pyran-4-yl)-4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-6-phenyl-1,2-dihydroquinoline-3-carbonitrile, 6-(Methylsulfonyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-[4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-[4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-chloro-1-methyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-{4-methyl-4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-2-oxo-4-{4-[5-(propan-2-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carboxamide, 4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)azepan-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)azepan-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-6-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3,6-dicarbonitrile, 6-cyano-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(3,3-difluorocyclobutyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-cyclopropyl-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(Butan-2-yl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(methoxymethyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(methoxymethyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1,6-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-fluoro-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-6-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,7-dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,7-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-ethylpiperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-bromo-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-1,6-dimethyl-4-[4-methyl-4-(6-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-chloro-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-8-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-chloro-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-1-methyl-4-{4-methyl-4-[5-methyl-4-(trifluoromethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[(2S,4S)-2-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-fluoro-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(1-hydroxycyclopropyl)methoxy]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxetan-3-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-hydroxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(cyclopropyloxy)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-8-(oxetane-3-yl)-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(cyclobutyloxy)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-methoxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3,7-dicarbonitrile, 7-cyclopropyl-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(1-cyanocyclopropyl)methoxy]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(3,3-difluorocyclobutyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-8-[(oxetan-3-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5,6-difluoro-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,7-dimethyl-2-oxo-4-(4-phenylpiperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 7-methoxy-1-methyl-2-oxo-4-(4-phenylpiperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-propoxy-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-chloro-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-methoxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-(oxetane-3-yl)-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-(cyclopropyloxy)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,8-dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(cyclopropyloxy)-1-methyl-2-oxo-4-(4-phenylpiperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[4-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(2S)-butan-2-yl]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-[(oxetan-3-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-[(1-cyanocyclopropyl)methoxy]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-propoxy-1,2-dihydroquinoline-3-carbonitrile, 8-hydroxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-cyclopropyl-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-8-propoxy-1,2-dihydroquinoline-3-carbonitrile, 6-(cyclopropyloxy)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3,7-dicarbonitrile, 4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-6-cyclopropyl-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(cyclobutyloxy)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-6-propoxy-1,2-dihydroquinoline-3-carbonitrile, 6-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(dimethylphosphoryl)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[5-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[6-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxetan-3-yl)methyl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-[(oxetan-3-yl)methyl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[5-(oxetan-3-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carbonitrile, 7-hydroxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-bromo-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[5-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-6-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-6-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-fluoro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-8-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-8-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,7-dimethyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1,7-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1,7-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[4-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[6-(2-methoxyethyl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(2-oxopyrrolidin-1-yl)-1,2-dihydroquinoline-3-carboxamide, 8-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(4,5-dimethyl-1,3-thiazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(quinoxalin-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(1H-pyrazol-3-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(1-methyl-1H-pyrazol-4-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3,4-dimethoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-chlorophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[(2S,4S)-2-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)-1-piperidinyl]-2-oxo-quinoline-3-carbonitrile, 4-[4-(3-cyanophenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-fluoro-1-methyl-2-oxo-4-[(4S)-4-phenylazepan-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[rac-(2R,3S)-2-methyl-3-phenylpyrrolidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[1-(3-cyano-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)piperidin-4-yl]benzamide, 4-[4-hydroxy-4-(2-methoxyphenyl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-1-ethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-chlorophenyl)piperidin-1-yl]-1-ethyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[5-(2-oxopyrrolidin-1-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-acetylphenyl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3-chlorophenyl)-4-methoxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(dimethylphosphoryl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(dimethylphosphoryl)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(Methylsulfonyl)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1-benzothiophen-2-yl)-4-hydroxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1-benzothiophen-2-yl)-4-methoxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1-benzothiophen-2-yl)-4-methylpiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-methoxynaphthalen-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-[1-(3-cyano-1-methyl-2-oxo-1,2-dihydroquinoline-4-yl)piperidin-4-yl]-2-methylquinoline-4-carbonitrile, 1-methyl-4-[4-(2-methyl-1,3-benzoxazol-5-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(2-methyl-1,3-benzothiazol-5-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-[4-(3-methyl-2-oxo-2,3-dihydro-1H-indol-5-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[5-(3-chlorophenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[5-(3-chlorophenyl)-1,3,4-oxadiazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(3,3-dimethyl-2,3-dihydro-1H-indol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[(2R)-2-methyl-2,3-dihydro-1-benzofuran-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(1,3,3-trimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(2-hydroxy-2,3-dihydro-1H-inden-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(2,2-dimethyl-2H-1,3-benzodioxol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-[4-(2'-oxo-1',2'-dihydrospiro[cyclobutane-1,3'-indole]-5'-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-methyl-4-(4-methylquinolin-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(4-fluoro-1-methyl-1H-indol-6-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[1-(3-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[1-(3-chlorophenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[1-(4-chlorophenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-{4-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(2-methylquinolin-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[4-(3-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[4-(2-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[4-(4-methylphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-dimethyl-1H-indazol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(2-methyl-1,3-benzoxazol-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(2-methyl-1,3-benzothiazol-6-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[3-(difluoromethyl)quinolin-7-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxan-4-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(2-methoxyethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{[oxiran-2-yl]methoxy}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxetan-3-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-methoxy-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-2-oxo-4-(4-{5-[(oxolan-2-yl)methoxy]-1,3-benzoxazol-2-yl}piperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-{4-[6-(oxetan-3-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-fluoropiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)-4-methoxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[5-(methoxymethyl)-1,3-benzoxazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-{4-[6-(methoxymethyl)-1,3-benzoxazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-fluoro-4-(5-methoxy-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(5-cyclopropyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(6-cyclopropyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 8-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[methyl(oxetan-3-yl)amino]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(2-hydroxyethyl)(methyl)amino]-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[methyl(oxolan-3-yl)amino]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(Cyanomethyl)(methyl)amino]-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3,6-dicarbonitrile, 3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-6-carboxamide, 6-ethoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(2,2-difluoropropoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(2,2-difluoroethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-(cyclopropylmethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-cyclobutyl-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-[2,2-dimethylcyclobutyl]-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-6-(3,3,3-trifluoroprop-1-en-2-yl)-1,2-dihydroquinoline-3-carbonitrile, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-6-[1-(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carbonitrile, 2-({3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinolin-7-yl}oxy)acetamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{[oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, tert-Butyl (rac)-({3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinolin-7-yl}oxy)acetate, ({3-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinolin-7-yl}oxy)acetic acid, (rac)-4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-(tetrahydrofuran-3-yloxy)-1,2-dihydroquinoline-3-carbonitrile, 7-(cyclopropylamino)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-methoxy-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-nitro-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-7-hydroxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-7-hydroxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[tetrahydrofuran-3-yloxy]-1,2-dihydroquinoline-3,6-dicarbonitrile, 7-hydroxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3,6-dicarbonitrile, (rac)-6-ethoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[tetrahydrofuran-3-yloxy]-1,2-dihydroquinoline-3-carbonitrile, 7-hydroxy-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[tetrahydrofuran-3-yloxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-(2,2-difluoroethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[tetrahydrofuran-3-yloxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-methoxy-1-methyl-2-oxo-7-[tetrahydrofuran-3-yloxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3,6-dicarbonitrile, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-6-(3,3,3-trifluoroprop-1-en-2-yl)-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-6-[1-(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-2-oxo-4-(4-{5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl}piperidin-1-yl)-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-2-oxo-4-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-2-oxo-4-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-1-methyl-4-{4-[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-hydroxy-1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-7-hydroxy-1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-7-{[oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-N,1-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, N,1-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-N,1-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-2-oxo-4-{4-[5-(2-oxopyrrolidin-1-yl)-1,3-benzoxazol-2-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carboxamide, 4-[4-(3-chlorophenyl)-4-methoxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(dimethylphosphoryl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(dimethylphosphoryl)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(Methylsulfonyl)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1-benzothiophen-2-yl)-4-methoxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1-benzothiophen-2-yl)-4-hydroxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(6-methoxynaphthalen-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[5-(3-chlorophenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[5-(3-chlorophenyl)-1,3,4-oxadiazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[2-methyl-2,3-dihydro-1-benzofuran-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(2-hydroxy-2,3-dihydro-1H-inden-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(2,2-dimethyl-2H-1,3-benzodioxol-5-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-2-oxo-4-[4-(2'-oxo-1',2'-dihydrospiro[cyclobutane-1,3'-indole]-5'-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-methyl-4-(4-methylquinolin-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(4-fluoro-1-methyl-1H-indol-6-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[1-(3-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[1-(3-chlorophenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-2-oxo-4-{4-[3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carboxamide, 4-{4-[4-(3-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[4-(2-methoxyphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[4-(4-methylphenyl)-1,3-thiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxan-4-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-(2-methoxyethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{[oxiran-2-yl]methoxy}-2-oxo-1,2-dihydroquinoline-3-carboxamide, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, (-)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo -7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, (+)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxetan-3-yl)oxy]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(5-methoxy-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-2-oxo-4-(4-{5-[(oxolan-2-yl)methoxy]-1,3-benzoxazol-2-yl}piperidin-1-yl)-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-fluoropiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-(1,3-benzoxazol-2-yl)-4-methoxypiperidin-1-yl]-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[5-(methoxymethyl)-1,3-benzoxazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-{4-[6-(methoxymethyl)-1,3-benzoxazol-2-yl]-4-methylpiperidin-1-yl}-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 8-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[methyl(oxetan-3-yl)amino]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-[(2-hydroxyethyl)(methyl)amino]-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{methyl[(3R)-oxolan-3-yl]amino}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-{methyl[(3S)-oxolan-3-yl]amino}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3,6-dicarboxamide, 7-[(Cyanomethyl)(methyl)amino]-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-ethoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(2,2-difluoropropoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(2,2-difluoroethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-(cyclopropylmethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-cyclobutyl-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-6-[1-(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carboxamide, 7-(2-amino-2-oxoethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1-methyl-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-nitro-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-7-hydroxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-7-hydroxy-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, (rac)-6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, (rac)-6-cyano-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, (rac)-6-(2,2-difluoroethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, (rac)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-6-[1-(trifluoromethyl)cyclopropyl]-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-2-oxo-4-(4-{5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl}piperidin-1-yl)-1,2-dihydroquinoline-3-carboxamide, 6-methoxy-1-methyl-4-{4-[3-(3-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-methoxy-1-methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide, 6-methoxy-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-2-oxo-4-[4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-2-oxo-4-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)piperidin-1-yl]-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-1-methyl-4-{4-[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-7-{[(3R)-oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-7-{[(3S)-oxan-3-yl]oxy}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-7-hydroxy-1-methyl-4-{4-[5-(2-methylphenyl)-1,3,4-oxadiazol-2-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-bromo-7-methoxy-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-7-hydroxy-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-bromo-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-bromo-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, (rac)-6-cyano-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, (-)-6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 6-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, 6-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, (rac)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 7-[(2-methoxyethyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-(3-hydroxyazetidin-1-yl)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-[(oxetan-3-yl)amino]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(2-hydroxyethyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(2-hydroxyethyl)(methyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(2-methoxyethyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 7-(3-hydroxyazetidin-1-yl)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, (rac)-1,6-dimethyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carbonitrile, 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 1,6-dimethyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 7-[(2-hydroxyethyl)amino]-1,6-dimethyl-4-{4-[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-1,6-dimethyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 7-[(2-hydroxyethyl)amino]-1,6-dimethyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-bromo-7-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, 6-cyano-7-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carboxamide, (rac)-6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(oxolan-3-yl)methyl]amino}-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-({[(3R)-oxolan-3-yl]methyl}amino)-1,2-dihydroquinoline-3-carboxamide, 6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-({[(3S)-oxolan-3-yl]methyl}amino)-1,2-dihydroquinoline-3-carboxamide, 6-chloro-7-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, 6-chloro-7-hydroxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carboxamide, 6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, 6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]oxy}-1,2-dihydroquinoline-3-carboxamide, (rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)methoxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(oxolan-3-yl)methoxy]-1,2-dihydroquinoline-3-carboxamide, 6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3R)-oxolan-3-yl]methoxy}-1,2-dihydroquinoline-3-carboxamide, 6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-{[(3S)-oxolan-3-yl]methoxy}-1,2-dihydroquinoline-3-carboxamide, (rac)-6-bromo-1-methyl-2-oxo-7-[(oxolan-3-yl)oxy]-4-{4-[2-(pyridin-3-yl)-2H-1,2,3-triazol-4-yl]piperidin-1-yl}-1,2-dihydroquinoline-3-carbonitrile, (rac)-6-bromo-1-methyl-4-{4-[1-(2-methylphenyl)-1H-1,2,3-triazol-4-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, (rac)-1,6-dimethyl-4-{4-[1-(2-methylphenyl)-1H-1,2,3-triazol-4-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, 7-bromo-1,6-dimethyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-4-yl]piperidin-1-yl}-2-oxo-1,2-dihydroquinoline-3-carbonitrile, and (rac)-1,6-dimethyl-4-{4-[1-(2-methylphenyl)-1H-pyrazol-4-yl]piperidin-1-yl}-2-oxo-7-[(oxolan-3-yl)oxy]-1,2-dihydroquinoline-3-carbonitrile, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof; as well as A DGKζ inhibitor compound of general formula (II) selected from: rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methoxy-2-methyl-anilino)propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(dimethylamino)anilino]propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-isopropoxy-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2,4,6-trifluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-bromo-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(6-methylpyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(2-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-cyano-anilino)propionamide, rac-2-(N-[4-amino-5-[4-chloro-3-(trifluoromethyl)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(3-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(dimethylamino)anilino]propionamide, rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5-carbonyl]-N-methyl-benzamide, rac-2-(N-[4-amino-5-(3-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-methoxy-anilino)propionamide, rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-methoxy-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methylsulfonylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-imidazol-1-ylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-cyano-3-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-cyano-3-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-cyano-3-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-cyano-2-fluoro-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(2-fluoro-4-methoxy-benzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(trifluoromethoxy)anilino]propionamide, rac-2-(N-[4-amino-5-(3,4-difluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(3,4-dichlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propionamide, (R)-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propionamide, (S)-2-[N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(trifluoromethyl)anilino]propionamide, rac-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-2-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(dihydroindane-5-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-cyanobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3,4-dichloro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-2-methyl-propionic acid ethyl ester, rac-2-(N-[4-amino-5-[4-(trifluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(trifluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(trifluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(trifluoromethyl)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-(trifluoromethyl)anilino]propionamide, (R)-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-(trifluoromethyl)anilino]propionamide, (S)-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-(trifluoromethyl)anilino]propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, 2-(N-[4-amino-5-[4-[2-amino-1-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]anilino)propionamide (mixture of stereoisomers), (2R)-(N-[4-amino-5-[4-[2-amino-(1R)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]anilino)propionamide, (2R)-(N-[4-amino-5-[4-[2-amino-(1S)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]anilino)propionamide, (2S)-(N-[4-amino-5-[4-[2-amino-(1R)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]anilino)propionamide, (2S)-(N-[4-amino-5-[4-[2-amino-(1S)-methyl-2-oxo-ethoxy]benzoyl]thiazol-2-yl]anilino)propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-2-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-2-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-2-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[6-(trifluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[5-[4-(difluoromethoxy)benzoyl]-4-methyl-thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-chloro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propionamide, (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propionamide, (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-fluorobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2,4-difluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methoxy-anilino)propionamide, rac-2-[(4-amino-5-benzoyl-1,3-thiazol-2-yl)(phenyl)amino]butanamide, rac-2-[(4-amino-5-benzoyl-1,3-thiazol-2-yl)(4-fluorophenyl)amino]butanamide, 2-(N-[4-amino-5-[4-(2-amino-1-methyl-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (mixture of stereoisomers), rac-2-{[4-amino-5-(4-methoxybenzoyl)-1,3-thiazol-2-yl](4-fluorophenyl)amino}butanamide, 2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-anilino)acetamide, 2-(N-[4-amino-5-(4-methylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)acetamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methyl-anilino)propionamide, (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methyl-anilino)propionamide, (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-methyl-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propionamide, (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propionamide, (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propionamide, (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propionamide, (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-methyl-anilino)propionamide, (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-methyl-anilino)propionamide, (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-methyl-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-methyl-anilino)propionamide, (R)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-methyl-anilino)propionamide, (S)-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-2-methyl-anilino)propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1-methylpyrazol-4-yl)amino]propionamide, (R)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1-methylpyrazol-4-yl)amino]propionamide, (S)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1-methylpyrazol-4-yl)amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propionamide, (R)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propionamide, (S)-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(3-pyridyl)amino]propionamide, rac-2-(N-[4-amino-5-(4-bromobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetic acid ethyl ester, (R)-ethyl 2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetate, (S)-ethyl 2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetate, rac-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(m-tolylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(o-tolylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(3-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(4-methylpiperazin-1-yl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(3-methylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(2-morpholino-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-oxo-2-[2-(1-piperidinyl)ethylamino]ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(4-benzyl-1-piperidinyl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(2-methoxyethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(4-cyanoanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[methyl(prop-2-ynyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(2-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(3-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(2-fluorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(4-fluorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(1H-benzimidazol-2-ylmethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-oxo-2-(2,2,2-trifluoroethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[methyl(2-pyridinyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[methyl-(1-methyl-4-piperidinyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(methoxyamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(ethylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(4-methylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(cyclohexylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-3-[[2-[4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]acetyl]amino]benzamide, rac-2-(N-[4-amino-5-[4-[2-oxo-2-(6-quinolinylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-4-[[2-[4-[4-amino-2-(N-[2-amino-1-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]acetyl]amino]benzamide, (2S)-1-[2-[4-[4-amino-2-(N-[2-amino-(1RS)-methyl-2-oxo-ethyl]-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]acetyl]pyrrolidine-2-carboxamide (a mixture of two diastereomers), rac-2-(N-[4-amino-5-[4-[2-[ethyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(3-methylisoxazol-5-yl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[3-(dimethylamino)propyl-methyl-amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[5-[4-[2-(4-acetylpiperazin-1-yl)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-oxo-2-(3-pyridylmethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, 2-(N-[4-amino-5-[4-[2-(2,3-dihydroxypropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (mixture of stereoisomers), rac-2-(N-[4-amino-5-[4-[2-(4-methoxyanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[benzyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(4-chloroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(2-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(4-chlorophenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(4-fluoroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(azepan-1-yl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[(4-methoxyphenyl)methylamino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, 2-(N-[4-amino-5-[4-[2-oxo-2-(1-phenylethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (mixture of stereoisomers), rac-2-(N-[4-amino-5-[4-[2-oxo-2-(p-tolylmethylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[methyl(2-phenylethyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, 2-(N-[4-amino-5-[4-[2-(3-methyl-1-piperidinyl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (mixture of stereoisomers), rac-2-(N-[4-amino-5-[4-[2-(4-methyl-1-piperidinyl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[5-[4-[2-(4-acetamidoanilino)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-oxo-2-(1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(cyclopentylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(2-isoindolin-2-yl-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[2-furylmethyl(methyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[4-(dimethylamino)-1-piperidinyl]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-[methyl(3-pyridylmethyl)amino]-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(N,2-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(N,4-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(N,3-dimethylanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-[2-(2,2-dimethylpropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, 2-(N-[5-[4-[2-(1-adamantylamino)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4-fluoro-anilino)propionamide (single stereoisomer), 2-(N-[5-[4-[2-(1-adamantylmethylamino)-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4-fluoro-anilino)propionamide (single stereoisomer), 2-(N-[5-[4-[2-[2-(1-adamantyl)ethylamino]-2-oxo-ethoxy]benzoyl]-4-amino-thiazol-2-yl]-4-fluoro-anilino)propionamide (single stereoisomer), 2-(N-[4-amino-5-[4-[2-(4-chloroanilino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (single stereoisomer), 4-[[2-[4-[4-amino-2-(4-fluoro-N-[2-amino-1-methyl-2-oxo-ethyl]anilino)thiazole-5-carbonyl]phenoxy]acetyl]amino]benzamide (single stereoisomer), 2-(N-[4-amino-5-[4-[2-((2RS),3-dihydroxypropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (mixture of two diastereomers), 2-(N-[4-amino-5-[4-[2-oxo-2-[2-(1-piperidinyl)ethylamino]ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (single stereoisomer), 2-(N-[4-amino-5-[4-(2-amino-2-oxo-ethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide (single stereoisomer), (R)-2-(N-[4-amino-5-[4-[2-(methylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-[2-(methylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-[2-(isopropylamino)-2-oxo-ethoxy]benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-N-isopropyl-2-methyl-propionamide, rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-2-methyl-propionamide, rac-2-(N-(5-benzoyl-4-methyl-thiazol-2-yl)-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(difluoromethyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, rac-N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5-carbonyl]phenyl]carbamic acid benzyl ester, (R)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate, (S)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-3,4-difluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate, rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]ethyl acetate, rac-N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]carbamic acid benzyl ester, (R)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate, (S)-benzyl N-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]carbamate, rac-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-benzyloxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-iodobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(6-methoxypyridine-3-carbonyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-phenoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-methoxy-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-methoxy-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-methoxy-anilino)propionamide, rac-2-(N-[4-amino-5-(4-nitrobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propionamide, (R)-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propionamide, (S)-2-(4-fluoro-N-[5-(4-methoxybenzoyl)-4-methyl-thiazol-2-yl]anilino)propionamide, rac-4-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenyl]cyclopropanecarboxamide, rac-2-(N-[4-amino-5-(4-morpholinobenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(pyrazol-1-ylmethyl)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(dimethylamino)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(4-pyrrolidin-1-ylbenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-benzyloxy-anilino)propionamide, (R)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-benzyloxy-anilino)propionamide, (S)-2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-benzyloxy-anilino)propionamide, rac-2-(N-[4-amino-5-[3-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(pyridine-3-carbonyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, rac-2-(N-[5-(4-acetamidobenzoyl)-4-amino-thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(2-chloropyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(2-methylpyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[2-(difluoromethyl)pyridine-4-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(4-pyridinyl)amino]propionamide, rac-2-(N-[4-amino-5-(2-methoxypyridine-4-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-3-fluoro-4-methoxy-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-cyano-3-fluoro-anilino)propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-bromo-anilino)propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-ethoxy-anilino)propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(difluoromethoxy)-3-fluoro-anilino]propionamide, rac-2-(N-(4-amino-5-benzoyl-thiazol-2-yl)-4-benzyloxy-anilino)propionamide, rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide, rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide, rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide, rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide, rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-(difluoromethoxy)-3-fluoro-anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-(2,2-difluoro-1,3-benzodioxol-5-yl)amino]propionamide, rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3-fluoro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-3-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methoxy-3-pyridinyl)amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(trifluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(difluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(trifluoromethyl)-3-pyridinyl]amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-[6-(difluoromethyl)-3-pyridinyl]amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-chloro-3-pyridinyl)amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-fluoro-3-pyridinyl)amino]propionamide, rac-2-[(4-amino-5-benzoyl-thiazol-2-yl)-(6-methyl-3-pyridinyl)amino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-fluoro-3-(trifluoromethoxy)anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-(trifluoromethoxy)anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-3-(difluoromethoxy)-4-fluoro-anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-chloro-3-(difluoromethoxy)anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-fluoro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-(trifluoromethoxy)anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-4-(difluoromethoxy)-2-fluoro-anilino]propionamide, rac-2-[N-(4-amino-5-benzoyl-thiazol-2-yl)-2-chloro-4-(difluoromethoxy)anilino]propionamide, rac-2-[N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-(difluoromethyl)anilino]propionamide, rac-2-[N-[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-4-(difluoromethyl)anilino]propionamide, rac-2-[N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-(difluoromethyl)anilino]propionamide, rac-2-[N-[4-amino-5-(pyridine-4-carbonyl)thiazol-2-yl]-4-(difluoromethyl)anilino]propionamide, rac-2-[N-[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-4-(difluoromethyl)anilino]propionamide, rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-[6-(trifluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-[6-(trifluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-[6-(trifluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-[6-(trifluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-[6-(difluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-(4-chlorobenzoyl)thiazol-2-yl]-[6-(difluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-[6-(difluoromethoxy)-3-pyridinyl]amino]propionamide, rac-2-[[4-amino-5-[6-(difluoromethoxy)pyridine-3-carbonyl]thiazol-2-yl]-[6-(difluoromethoxy)-3-pyridinyl]amino]propionamide, rac-N-[5-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-2-pyridinyl]carbamic acid benzyl ester, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]benzoic acid ethyl ester, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]benzoic acid ethyl ester, rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-2-methyl-propionic acid ethyl ester, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-cyclohexyl-benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-isopropyl-benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-benzyl-benzamide, 4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-[(2S)-2-hydroxypropyl]benzamide (mixture of stereoisomers), rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-(2-methoxyethyl)benzamide, 4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-[(2R)-2-hydroxypropyl]benzamide (mixture of stereoisomers), rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-cyclopropyl-benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]-N-cyclopentyl-benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-(2-phenoxyethyl)benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-[2-(trifluoromethoxy)ethyl]benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-[2-(difluoromethoxy)ethyl]benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-(2-tert-butoxyethyl)benzamide, rac-4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-chloro-3-fluoro-anilino)thiazole-5-carbonyl]-N-(2-methoxyethyl)benzamide, rac-2-[4-[4-amino-2-(N-(2-amino-1-methyl-2-oxo-ethyl)-4-fluoro-anilino)thiazole-5-carbonyl]phenoxy]-N-[(4-chlorophenyl)methyl]-2-methyl-propionamide, rac-2-(N-[4-amino-5-(6-bromopyridine-3-carbonyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-[4-(trifluoromethyl)-1-piperidinyl]pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-[4-(oxetan-3-yl)-1-piperidinyl]pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(dimethylamino)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(4,4-dimethyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(3-azabicyclo[3.2.1]octane-3-yl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(3,5-dimethyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(3-azabicyclo[3.1.0]hexane-3-yl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(4,4-difluoro-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, rac-2-(N-[4-amino-5-[6-(4-cyano-4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (R)-2-(N-[4-amino-5-[6-(4-cyano-4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-[6-(4-cyano-4-methyl-1-piperidinyl)pyridine-3-carbonyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, 2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide (single enantiomer), (R)-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, (S)-2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-3,4-difluoro-anilino)propionamide, 2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide (enantiomer 1), 2-(N-[4-amino-5-(4-hydroxybenzoyl)thiazol-2-yl]-4-chloro-3-fluoro-anilino)propionamide (enantiomer 2), 2-(N-[4-amino-5-[4-(difluoromethoxy)benzoyl]thiazol-2-yl]-4-hydroxy-anilino)propionamide (single enantiomer), and rac-2-(N-[4-amino-5-[4-(2-hydroxyethoxy)benzoyl]thiazol-2-yl]-4-fluoro-anilino)propionamide, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

7. A combination according to any one of claims 1 to 6, wherein the DGKα inhibitor compound has the formula: or a tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, as well as wherein the DGKζ inhibitor compound has the following formula: or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

8. The combination according to any one of claims 1 to 7, wherein the DGKα inhibitor compound has the formula: as well as wherein the DGKζ inhibitor compound has the following formula:

9. The combination according to any one of claims 1 to 8, for use in treating or preventing a condition with a dysregulated immune response in a mammal, in particular cancer, or viral infection or other conditions associated with abnormal DGKα and / or DGKζ signalling.

10. The combination of claim 9, wherein the mammal is a human.

11. A method for treating or preventing a disease in a patient, preferably a mammalian condition with a dysregulated immune response, particularly cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling, comprising administering a combination according to any one of claims 1 to 8.

12. The method of claim 11, wherein the mammal is a human.

13. Use of the combination according to any one of claims 1 to 8 for the preparation of a medicament for treating or preventing a condition with a dysregulated immune response in a mammal, in particular cancer, or viral infection or other conditions associated with abnormal DGKα and / or DGKζ signaling.

14. The use according to claim 13, wherein the mammal is a human.

15. A kit comprising: - A DGKα inhibitor compound as defined in any one of claims 3 to 8; - A DGKζ inhibitor compound as defined in any one of claims 3 to 8.

16. The kit of claim 15, wherein optionally both or either of the DGKα inhibitor compound and the DGKζ inhibitor compound are in the form of a pharmaceutical composition ready for simultaneous, concurrent, separate or sequential administration.

17. The kit of claim 15, wherein the DGKα inhibitor compound and the DGKζ inhibitor compound are each in the form of a pharmaceutical composition, and wherein the DGKα inhibitor compound is administered before the DGKζ inhibitor compound.

18. A pharmaceutical composition comprising a combination as defined in any one of claims 1 to 8 and one or more pharmaceutically acceptable excipients.

19. The pharmaceutical composition of claim 18, wherein the DGKα inhibitor compound and the DGKζ inhibitor compound are present in a combined preparation.

20. The pharmaceutical composition of claim 19, wherein the DGKα inhibitor compound and the DGKζ inhibitor compound are present in different formulations.

21. A DGKα inhibitor for use in a method for treating or preventing a disease, wherein the disease is preferably a condition with a dysregulated immune response, particularly cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling, characterized in that The methods comprise administering at least one DGKze inhibitor.

22. A DGKζ inhibitor for use in a method for treating or preventing a disease, preferably a condition with a dysregulated immune response, particularly cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling, characterized in that The method comprises administering at least one DGKa inhibitor.

23. A DGK inhibitor according to any one of claims 21 or 22, for use in a method for treating or preventing a disease, wherein the disease is preferably a condition with a dysregulated immune response, in particular cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling. a. wherein the DGKα inhibitor is as defined in any one of claims 3 to 8, and / or b. wherein the DGKζ inhibitor is as defined in any one of claims 3 to 8.

24. A DGK inhibitor according to any one of claims 21 to 23, for use in a method for treating or preventing a disease, preferably a condition with a dysregulated immune response, in particular cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling. a. wherein the DGKα inhibitor is DGKα inhibitor A, or a tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, and / or b. wherein the DGKζ inhibitor is DGKζ inhibitor A', or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

25. A DGK inhibitor according to any one of claims 21 to 24, for use in a method for treating or preventing a disease, preferably a condition with a dysregulated immune response, in particular cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling. a. wherein the DGKα inhibitor is DGKα inhibitor A, and / or b. wherein the DGKζ inhibitor is DGKζ inhibitor A'.

26. The DGK inhibitor according to any one of claims 21 to 25, for use in a method for treating or preventing a disease, preferably a condition with a dysregulated immune response, in particular cancer, or a viral infection or other condition associated with abnormal DGKα and / or DGKζ signaling, wherein the disease is cancer.

27. The DGK inhibitor for use in a method of treating cancer according to claim 26, wherein the cancer is selected from non-small cell lung cancer (NSCLC), triple negative breast cancer (TNBC), head and neck squamous cell carcinoma (HNSCC), melanoma, skin cancer other than melanoma, gastric cancer, renal cell carcinoma, MSI-high colorectal cancer, or gastroesophageal junction adenocarcinoma.

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