Substituted aminothiazoles as DGKZETA inhibitors for immune activation

Abstract

The present invention relates to aminothiazole compounds of general formula (I), to processes for preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and conjugates comprising said compounds, and the use of said compounds as a sole agent or in combination with other active ingredients for the preparation of a pharmaceutical composition for the treatment and / or prophylaxis of a disease, in particular a diacylglycerol kinase zeta (DGK zeta) modulated condition: # imgabs0 # wherein R1, R2, R3 and R4 are as defined herein, as well as the use of said compounds as a sole agent or in combination with other active ingredients for the treatment and / or prophylaxis of a disease, in particular a diacylglycerol kinase zeta (DGK zeta) modulated condition.

Description

[0001] This application is a divisional application of the Chinese invention patent application with application number 202180043311.4, filed on April 20, 2021, and with the invention name “Substituted aminothiazoles as DGKZETA inhibitors for immune activation”. Technical Field

[0002] The present invention relates to substituted aminothiazole compounds of general formula (I) as described and defined herein, processes for the preparation of said compounds, intermediate compounds useful for the preparation of said compounds, pharmaceutical compositions and conjugates comprising said compounds, and the use of said compounds as a single agent or in combination with other active ingredients for the preparation of pharmaceutical compositions for the treatment or prevention of diseases, in particular diseases regulated by diacylglycerol kinase ζ (DGKzeta, DGKζ).

[0003] The compounds of general formula (I) inhibit DGKζ and thereby enhance T cell-mediated immune responses. This is a new strategy that utilizes the patient's own immune system to overcome the immune escape strategies used by many neoplastic diseases (respectively cancer) and thereby enhance anti-tumor immunity. In addition, the compounds are particularly useful for treating diseases such as viral infections or conditions associated with dysregulated immune responses or other diseases associated with abnormal DGKζ signaling.

[0004] The present invention also relates to the use of the compound of general formula (I) in preparing a pharmaceutical composition for enhancing T cell-mediated immune response.

[0005] The present invention also relates to the use of the compound of general formula (I) in preparing a pharmaceutical composition for treating cancer.

[0006] The present invention also relates to the use of the compound of general formula (I) in the preparation of a pharmaceutical composition for treating or preventing viral infection, lymphoproliferative disease, asthma, eye disease and type 2 diabetes / insulin resistance. Background Art

[0007] Diacylglycerol kinase (DGK) represents a family of enzymes that catalyze the phosphorylation of membrane lipid sn-1,2 diacylglycerol (DAG) to form phosphatidic acid (PA) (TOEichmann and A. Lass, Cell. Mol. Life Sci. 2015, 72, 3931-3952). In T cells, DAG is formed downstream of the T cell receptor (TCR) after activation of the γ1 isomer of phospholipase C (PLCγ1) and cleavage of phosphatidylinositol 4,5-bisphosphate (PIP2) into DAG and another second messenger inositol 1,4,5-triphosphate (IP3) (S. Krishna and X.-P. Zhong, Front. Immunol. 2013, 4, 178). However, IP3 is important in promoting calcium release from the endoplasmic reticulum, and DAG interacts with other proteins important in TCR signal transduction, such as protein kinase Cθ (EJ Quann et al., Nat. Immunol. 2011, 12 (7), 647-654) and Ras activation protein RasGRP1 (S. Krishna and X.-P. Zhong, Front. Immunol. 2013, 4, 178). Although three isomers of DGK are known to exist in T cells [DGKα (DGKalpha), DGKδ (DGKdelta) and DGKζ (DGKzeta)], only two (DGKα and DGKζ) are considered to play an important role in promoting DAG metabolism downstream of TCR (RP Joshi and GA Koretzky, Int. J. Mol. Sci. 2013, 14 (4), 6649-6673).

[0008] Targeting the activity of DGKζ in T cells by germline deletion or using 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 (ERK1 / 2) and NFκB (X.-P.-Zhong et al., Nat. Immunol. 2003, 4, 882-890; B.A. Olechock et al., Nat. Immunol. 2006, 7(11), 1174-1181; M.J. Riese et al., J. Biol. Chem. 2011, 286, 5254-5265; E.M. Wesley et al., Immuno Horizons 2018, 2(4), 107-118).

[0009] Deletion of DGKζ in T cells leads to enhanced production of effector cytokines (e.g. IL2, IFNγ) and increased proliferation (X.-P. Zhong et al., Nat. Immunol. 2003, 4, 882-890; BAO Lenchock et al., Nat. Immunol. 2006, 7(11), 1174-1181; E.M. Riese et al., J. Biol. Chem. 2011, 286, 5254-5264).

[0010] Compared with the control, adoptive transfer of T cells lacking DGKζ after inoculation of C1498.SIY leukemia cells can reduce the leukemia burden. In addition, T cells lacking DGKζ at least partially resist PD1-mediated inhibitory signals (W. Jing et al., Cancer Res. 2017, 77 (20), 5676-5686). In addition, after orthotopic tumor injection of pancreatic tumor model, mice lacking DGKζ had reduced tumor size compared with controls (EM Wesley et al., Immuno Horizons, 2018, 2 (4), 107-118). In addition, S. Wee et al. inoculated C57BL / 6 mice with a variety of homologous tumor cell lines-MC38 colon cancer, B16F1 melanoma and C1498 leukemia-and analyzed the survival rate and tumor growth between mice lacking DGKζ in the presence or absence of anti-PD1 treatment. DGKζ- / - mice inhibited the growth of subcutaneously implanted tumor cells in three model systems, and the combination of DGKζ-deficiency and anti-PD1 played an additive role 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).

[0011] These findings suggest that DGKζ may serve as a useful target for enhancing the antitumor activity of T cells.

[0012] In addition, adoptively transferred DGKζ-deficient CAR (chimeric antigen receptor)-T cells showed increased efficacy in treating mouse mesothelioma (MJ Riese et al., Cancer Res. 2013, 73(12), 3566-3577) and glioblastoma xenograft mouse models combined with DGKα knockout (I.-Y. Jung et al., Cancer Res. 2018, 78(16), 4692-4703) compared to wild-type CAR T cells.

[0013] Furthermore, DGKζ-deficient mice mount a more robust immune response to lymphocytic choriomeningitis virus infection than wild-type mice (X.-P. Zhong et al., Nat. Immunol. 2003, 4, 882-890).

[0014] DGKζ is also associated with natural killer (NK) cells. After stimulation by multiple activating receptors, NK cells from mice lacking DGKζ showed increased cytokine production and degranulation in an ERK-dependent manner. In addition, they had improved cytotoxic function against tumor cell lines. (E. Yang et al. J. Immunol. 2016, 197 (3), 934-41.)

[0015] In addition to immune cell regulation, DGKζ also plays a role in cancer, mediating many aspects of cancer cell progression including proliferation, apoptosis, survival, invasion, and tumorigenicity, such as in osteosarcoma, colon cancer, breast cancer, prostate cancer, glioma, and leukemia models (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).

[0016] In addition, DGKζ knockout reduced airway inflammation and airway hyperresponsiveness in mice, and also reduced bronchoconstriction in in vitro human airway samples by blocking T helper 2 (TH2) differentiation (BASingh et al., Sci. Signal. 2019, 12:eaax3332).

[0017] Taken together, the results of these studies suggest that inhibition of DGKζ activity in T cells and tumor cells may prove valuable in generating more robust immune responses against pathogens and tumors and in ameliorating Th2-driven (auto)immune diseases (rebalancing the immune-system).

[0018] In addition, inhibition of DGKα has the potential to reverse the life-threatening Epstein-Barr virus (EBV)-related immunopathology that occurs in patients with X-linked lymphoproliferative disease (XLP-1) (E. Ruffo et al., Sci. Transl. Med. 2016, 8:(321):321ra7; S. Velnati et al., Eur. J. Med. Chem. 2019, 164, 378-390). Based on the potential mode of action, it can be assumed that inhibition of DGKζ will have a similar effect.

[0019] DGKα-inhibitor II (R59949) can inhibit retinal neovascularization and protect retinal astrocytes in an oxygen-induced retinopathy model (L. Yang et al., J. Mol. Neurosci. 2015, 56, 78-88). In addition, based on the potential mode of action, it can be assumed that inhibition of DGKζ will produce similar effects.

[0020] In DGKζ knockout mice, it was shown that DGKζ deficiency increased protection against insulin resistance (B. Benziane et al., J. Lipid Res. 2017, 58(12), 2324-2333).

[0021] In summary, inhibition of DGKζ activity has therapeutic potential in directly targeting tumors as well as addressing viral infections, lymphoproliferative disorders, asthma, ocular diseases, and type 2 diabetes / insulin resistance.

[0022] Prior art

[0023] WO2020 / 006016 and WO2020 / 006018 describe naphthyridinone compounds as T cell activators that inhibit the activity of DGKα and / or DGKζ for treating viral infections and proliferative diseases, such as cancer. WO2021 / 041588 describes pyridopyrimidinonyl compounds as T cell activators that inhibit the activity of DGKα and / or DGKζ for treating viral infections and proliferative disorders, such as cancer.

[0024] 2,4,5-Trisubstituted triazole derivatives featuring a substituted amino group attached to C-2 of the thiazole core have been disclosed in published patent applications in various technical contexts, but not in the context of DGK inhibition.

[0025] WO 2014 / 181287 discloses heterocyclic compounds as inhibitors of interleukin 17 and tumor necrosis factor alpha.

[0026] WO 2014 / 173904 discloses compounds having antibacterial activity.

[0027] WO 2009 / 149054 discloses small molecule inhibitors for treating or preventing dengue infection.

[0028] WO 2007 / 130075 discloses aminothiazole derivatives as inhibitors of human stearoyl-CoA desaturase.

[0029] WO 2012 / 064715 discloses compositions and methods related to heat shock transcription factor activating compounds and their targets.

[0030] WO 2005 / 103022 discloses substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators.

[0031] CN 106109467 discloses the medical use of aromatic compounds (including thiazoles) in the treatment of pyrazinamide-resistant tuberculosis.

[0032] WO 2015 / 199206 discloses compounds derived from six-membered rings as TRPV4 inhibitors.

[0033] WO 2015 / 046193 discloses aromatic heterocyclic amine derivatives as TRPV4 inhibitors.

[0034] CN 103159695 discloses thiazole compounds that can inhibit the replication of human immunodeficiency virus (HIV) and are effective against drug-resistant HIV strains.

[0035] WO 2013 / 056684 discloses thiazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors.

[0036] WO 2013 / 033037 discloses various chemical types of compounds, in particular thiazole derivatives, as antiprion compounds.

[0037] WO 2012 / 075393 discloses compounds of various chemical types, in particular thiazole derivatives, as activators of proteasomal degradation.

[0038] JP 2011032254 discloses various chemical types of compounds, especially thiazole derivatives, as pest control agents.

[0039] WO 2009 / 041790 discloses 2,4,5-trisubstituted thiazole derivatives as inhibitors of sphingosine phosphorylcholine (SPC) receptors for the treatment of inflammatory diseases.

[0040] WO 2008 / 090382 discloses thiazole and oxazole derivatives for the treatment of prion diseases, cancer and central nervous system conditions and for the regulation of stem cells.

[0041] WO 2007 / 022415 discloses substituted 2-aminothiazoles for the treatment of neurodegenerative diseases.

[0042] WO 2006 / 122011 discloses thiazole compounds and methods for treating viral infections, particularly hepatitis C virus infections.

[0043] WO 2006 / 078287 discloses various 5-membered heteroarene derivatives, in particular thiazoles, as inhibitors of phosphodiesterase 4B.

[0044] WO 2005 / 102318, WO 2005 / 102325, WO 2005 / 102326, WO 2005 / 102346, WO 2005 / 102455, WO 2005 / 112920, WO 2005 / 115304, WO 2005 / 115385 all relate to c-Kit inhibitors of various chemical types (including 2-aminothiazole derivatives), and various uses thereof.

[0045] EP 1543824 and US 2005 / 0137239 disclose thiazole derivatives for counterglycation.

[0046] WO 2004 / 014884 discloses thiazole derivatives as neuropeptide Y receptor ligands.

[0047] WO 2019 / 133445 discloses aminothiazole derivatives as inhibitors of Vanin-1.

[0048] WO 2021 / 043966 discloses substituted five-membered nitrogen-containing heteroaryl compounds as inhibitors of NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3).

[0049] 2,4,5-Trisubstituted triazole derivatives which are structurally related to the compounds of the present invention, but structurally distinct, have also been disclosed in several scientific publications.

[0050] D. Kikelj and U. Urleb, Science of Synthesis (2002), 11, 627-833, is a review of the synthesis of thiazole compounds. Most of the specific compounds disclosed so far, except for the common thiazole core with the compounds of the present invention, are structurally different from these compounds. Several individual compounds disclosed therein, namely those disclosed on pages 651, 681-683 and 719, and including {4-methyl-2-[methyl(phenyl)amino]-1,3-thiazol-5-yl}(phenyl)methanone, are structurally related to the compounds of the present invention, but are structurally different.

[0051] Structurally related to the compounds according to the invention, but structurally distinct 2,4,5-trisubstituted triazole derivatives have also been disclosed in several journal articles.

[0052] None of the journal articles listed below, which also disclose compounds that are somewhat related in structure to the compounds of the present invention but structurally distinct, disclose therapeutic uses of the compounds disclosed therein for pharmaceutical purposes.

[0053] S. Titus et al., Tetrahedron Lett. 2014, 55, 5465-5467, disclose a four-component synthesis of 4-hydrazinothiazole derivatives.

[0054] TN Birkinshaw et al., J. Chem. Soc. Perkin Trans. 1, 1988, 2209-2212, disclose spectroscopic and chemical studies of 5-acyl and 5-nitroso-2-(N,N-disubstituted amino)thiazoles.

[0055] RA Funnell et al., J. Chem. Soc. Perkin Trans. 1, 1987, 2311-2315 disclose a study on the formation of isomeric 2-(N,N-disubstituted amino)thiazol-5-yl ketones.

[0056] JC Brindley et al., J. Chem. Soc. Perkin Trans. 1, 1987, 1153-1158, disclose the conversion of N'-substituted N-acyl and N-imidoyl thioureas into 2-(N,N-disubstituted amino)thiazol-5-yl ketones.

[0057] DMeakins et al., J. Chem. Soc. Chem. Comm. 1984, 837-838, disclose a chemical reaction which unexpectedly produces 5-benzoyl-4-methyl-2-(N-methyl-N-phenylamino)thiazole.

[0058] K. Akiba et al., Tetrahedron Lett. 1975, 7, 459-462, disclose the synthesis of certain 2-arylaminothiazoles by the 1,3-cycloaddition of 4-aryl-3-arylimino-5-imino-1,2-4-thiadiazolidine (also known as Hector's base) and acetylene.

[0059] Finally, the Chemical Abstracts Database (CAS ) discloses three structures that are somewhat related to the compounds of the present invention but have different structures, all of which have no references and no technical applications, and have CAS registration numbers 1349635-19-3, 1349215-57-1 and 1348293-02-6.

[0060] However, the prior art does not record:

[0061] The specific substituted aminothiazole compounds of the general formula (I) of the present invention as described and defined herein, ie compounds having a 2-aminothiazole core with:

[0062] an optionally substituted benzoyl or 6-membered heteroaroyl group attached to C-5,

[0063] -NH connected to C-4 2 or methyl,

[0064] and (i) optionally substituted phenyl or 5- or 6-membered heteroaryl and (ii) a -S(=O) group 2 -NH 2 or especially -C(=O)-NH 2 The side-substituted alkyl groups, (i) and (ii) both attached to the nitrogen atom attached to C-2, are essential for effective inhibition of DGKζ, as shown in the comparative experiments below.

[0065] or its stereoisomers, tautomers, N-oxides, hydrates, solvates, salts or mixtures thereof, as described and defined herein and hereinafter referred to as "compounds of formula (I)" or "compounds of the present invention",

[0066] or their pharmacological activities.

[0067] WO 2021 / 028382, relating to different chemical forms ([1,2,4]triazolo[1.5-c]quinazolin-5-amine compounds) according to formula (I) and abstract, discloses a single compound named N 2 -(4-amino-5-benzoyl-1,3-thiazol-2-yl)-N 2 -(3-methylphenyl)alaninamide, no synthetic protocol is provided, nor are there any biological data related to the compound name.

[0068] It would be desirable to provide new compounds having prophylactic and therapeutic properties. Summary of the invention

[0069] Therefore, the object of the present invention is to provide compounds for the prevention and treatment of DGKζ regulated disorders in a T cell immunostimulatory or immunomodifying manner and pharmaceutical compositions comprising these compounds. DGKζ regulated disorders include disorders with dysregulated immune responses, particularly in immunosuppressive tumor microenvironments in cancer, autoimmune diseases, viral infections, and other disorders associated with abnormal DGKζ signaling. The compounds can be used as a single agent or in combination with other active ingredients.

[0070] It has now been found that the compounds of the invention have unexpected and advantageous properties and this forms the basis of the present invention.

[0071] In particular, it has been unexpectedly found that the compounds of the present invention effectively inhibit DGKζ protein and thereby enhance T cell mediated immunity. Therefore, they provide new structures for treating diseases, especially cancer, in mammals (including humans) and are therefore useful for treating or preventing hyperproliferative diseases, such as cancer. BRIEF DESCRIPTION OF THE DRAWINGS

[0072] Figure 1 : DGKz_hu_1 encodes human DGKζM1 to V928 plus an N-terminal Flag-tag, as described in SEQ ID No.1.

[0073] Figure 2 : SIINFEKL amino acid sequence as described in SEQ ID No.2.

[0074] Figure 3 : OVA-30 peptide sequence, as described in SEQ ID No.3.

[0075] Figure 4 : FLAG-tag, as described in SEQ ID No.4.

[0076] Figure 5 : Kozak sequence for translation initiation, as described in SEQ ID No.5.

[0077] Figure 6 : Example 49.2, 50% thermal ellipsoid of molecule 1. F171 and F151 represent two refined positions with 180° disorder on the C13-C16 axis.

[0078] Figure 7 : Example 59.1, 50% thermal ellipsoid of molecule 1.

[0079] Figure 8 : Example 61.2, 50% thermal ellipsoid of molecule 1.

[0080] Fig. 9 : Example 62.2, 50% thermal ellipsoid of molecule 1. DETAILED DESCRIPTION

[0081] According to a first aspect, the present invention covers compounds of general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof:

[0082]

[0083] in:

[0084] R 1 represents phenyl 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, C 1 -C 6 -alkyl, (phenyl)-(C 1 -C 3 -alkyl)-, C 1 -C 6 -haloalkyl, C 1 -C 6 -alkoxy, (phenyl)-(C 1 -C 3 -alkoxy)-, C 1 -C 6 -haloalkoxy, -N(R 5 )(R 6 ),

[0085] wherein the (phenyl)-(C 1 -C 3 -alkyl)- and (phenyl)-(C 1 -C 3 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0086] or two substituents connected to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-(CH 2 ) 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O-, -O-CF 2 -O-, -O-CH 2 -CF 2 -O- and -O-CF 2 -CF 2 -O- divalent group,

[0087] or

[0088] 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 the following: cyano, C 1 -C 3 -alkyl and C 1 -C 3 - alkoxy;

[0089] R 2 Representative Group

[0090] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0091] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0092] R 4 represents phenyl 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: cyano, nitro, C 1 -C 6 -alkyl, (phenyl)-(C 1 -C 3 -alkyl)-, (5- or 6-membered heteroaryl)-(C 1 -C 3 -alkyl)-, (C 3 -C 7 -cycloalkyl)-(C 1 -C 3 -alkyl)-, ((R 9 )O)-(C 1 -C 6 -alkyl)-, C 1 -C 6 -haloalkyl, C 3 -C 7 -cycloalkyl, -OR 9 、-N(R 10 )(R 11 )、((R 10 )(R 11 )N)-(C 1 -C 3 -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, which itself is optionally substituted by one or two substituents selected from halogen atoms and methyl,

[0093] or two substituents connected to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-(CH 2 ) 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O-, -O-CF 2 -O-, -O-CH 2 -CF 2 -O- and -O-CF 2 -CF 2 -O- divalent group;

[0094] R 5 and R 6 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -cycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[0095] or

[0096] 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 the following: oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4- alkoxy;

[0097] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0098] R 8 represents a group selected from the following: -C(=O)-NH 2 and -S(=O) 2 -NH 2 ;

[0099] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, (5- or 6-membered heteroaryl)-(C 1 -C 3 -alkyl)-, (phenyl)-(C 1 -C 3 -alkyl)-, C 1 -C 6 -haloalkyl, C 2 -C 4 -Hydroxyalkyl, (C 1 -C 3 -alkoxy)-C 2 -C 3 -alkyl-, ((C 1 -C 3 -alkyl)-C(=O)-O)-C 2 -C 3 -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,

[0100] wherein the (phenyl)-(C 1 -C 3 -alkyl)- and the phenyl itself, and the (5- or 6-membered heteroaryl)-(C 1 -C 3 -alkyl)-, and the 5- or 6-membered heteroaryl group itself is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy;

[0101] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -Hydroxyalkyl, (C 1 -C 3 -alkoxy)-C 2 -C 3 -alkyl-, ((R 22 )(R 23 )N)-C 2 -C 3 -alkyl, (C 3 -C 7 -cycloalkyl)-(C 1 -C 3 -alkyl)-, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 7 -cycloalkyl, (C 3 -C 7 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 3 -alkyl)-, (phenyl)-(C 1 -C 3 -alkyl)-C(=O)-, (phenyl)-(C 1 -C 3 -alkyl)-OC(═O)-, phenyl and 5- or 6-membered heteroaryl,

[0102] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 7 -cycloalkyl)-(C 1 -C 3 -alkyl)- and (C 3 -C 7 -cycloalkyl)-C(=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from the following: cyano, C 1 -C 2 -alkyl and C 1 -C 2 - haloalkyl,

[0103] and wherein the phenyl group and the 5- or 6-membered heteroaryl group and the (phenyl)-(C 1 -C 3 -alkyl)-, (phenyl)-(C 1 -C 3 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 3 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0104] or

[0105] 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 or a bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl, which are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 7 -Cycloalkyl, C 1 -C 4 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl;

[0106] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 4 -haloalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3-C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[0107] Among them C 3 -C 7 -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 the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4 - alkoxy,

[0108] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 3 -alkyl)-, the phenyl group in the group consisting of -alkyl)- is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0109] or

[0110] 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 the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4 - alkoxy;

[0111] R 14 represents a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 - haloalkyl and phenyl,

[0112] 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 cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy;

[0113] R 17 Represents C 1 -C 4 -alkyl;

[0114] R 18 and R 19 Each of them independently represents a hydrogen atom or a C 1 -C 4 -alkyl;

[0115] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 11-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[0116] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - 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 optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0117] And among them C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl and bicyclic 5 to 11 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4 - alkoxy,

[0118] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[0119] R 21 Represents hydrogen atom or C 1 -C 4 -alkyl,

[0120] or

[0121] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, (phenyl)-(C 1 -C 3 -alkyl)-, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 4 -alkoxy, C1 -C 3 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[0122] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0123] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 4 -alkyl, and

[0124] n represents an integer of 0, 1 or 2.

[0125] definition

[0126] The term "substituted" means that one or more hydrogen atoms on the designated atom or group is replaced with a group selected from the designated group, provided that the normal valence of the designated atom in the existing situation is not exceeded. Combinations of substituents and / or variables are permitted.

[0127] The term "optionally substituted" means that the number of substituents may be equal to or different from zero. Unless otherwise indicated, an optionally substituted group may be substituted with as many optional substituents as can be accommodated by replacing hydrogen atoms with non-hydrogen substituents on any available carbon or nitrogen atom. Typically, the number of optional substituents (when present) may be 1, 2, 3 or 4, particularly 1, 2 or 3.

[0128] When the group in the compound of the present invention is substituted, unless otherwise indicated, the group may be monosubstituted or polysubstituted by a substituent. Within the scope of the present invention, the meanings of all repeated groups are independent of each other. The group in the compound of the present invention may be substituted by one, two or three identical or different substituents, in particular by one substituent.

[0129] As used herein, an oxo substituent represents an oxygen atom double-bonded to a carbon atom or a sulfur atom.

[0130] If a composite substituent consists of more than one part, for example (C 1 -C 2 -alkoxy) (C 1 -C6 -alkyl)-, the given moiety may be attached at any suitable position of the composite substituent, for example C 1 -C 2 -alkoxy moiety may be attached to said (C 1 -C 2 Alkoxy) (C 1 -C 6 Alkyl)-group C 1 -C 6 -Any suitable carbon atom of the alkyl moiety. A hyphen at the beginning or end of such a composite substituent indicates the point of attachment of the composite substituent to the rest of the molecule. If a ring comprising carbon atoms and optionally one or more heteroatoms (e.g. nitrogen, oxygen or sulfur atoms) is substituted with a substituent, the substituent may be incorporated at any suitable position of the ring, being bonded to a suitable carbon atom and / or a suitable heteroatom.

[0131] When used in the specification, the term "comprising" includes "consisting of".

[0132] If any item is referred to herein as "as referred to herein", it means that it can be referred to anywhere in the text.

[0133] The terms used in this document have the following meanings:

[0134] The term "halogen atom" refers to a fluorine, chlorine, bromine or iodine atom, in particular a fluorine, chlorine or bromine atom.

[0135] The term "C 1 -C 6 "-alkyl" means a straight-chain or branched saturated monovalent hydrocarbon radical 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 radical has 1, 2, 3 or 4 carbon atoms ("C 1 -C 4 -alkyl”), for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl or tert-butyl, more particularly 1, 2 or 3 carbon atoms (“C 1 -C 3 alkyl), for example methyl, ethyl, n-propyl or isopropyl, more particularly 1 or 2 carbon atoms ("C 1-C 2 -alkyl"), such as methyl or ethyl.

[0136] The term "C 1 -C 4 -hydroxyalkyl" refers to a linear or branched saturated monovalent hydrocarbon group, wherein the term "C 1 -C 4 "-alkyl" is as defined above, and wherein 1 or 2 hydrogen atoms are substituted by hydroxy, for example hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxypropyl-2-yl, 2-hydroxypropyl-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxypropyl-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.

[0137] The term "C 1 -C 6 -haloalkyl" refers to a straight or branched saturated monovalent hydrocarbon group, wherein the term "C 1 -C 6 -alkyl" is as defined above, and wherein one or more hydrogen atoms are replaced identically or differently by halogen atoms. In particular, the halogen atoms are fluorine atoms. The C 1 -C 6 -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.

[0138] The term "C 1 -C 6 "-alkoxy" refers to the formula (C 1 -C 6 -alkyl)-O-, wherein the term "C 1 -C 6 "-alkyl" is as defined above, for example methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy, tert-butoxy, pentyloxy, isopentyloxy or n-hexyloxy, or isomers thereof.

[0139] The term "C 1 -C 6 "-Haloalkoxy" refers to a straight-chain or branched saturated monovalent C 1 -C 6 -alkoxy, as defined above, wherein one or more hydrogen atoms are replaced by halogen atoms, identically or differently. In particular, the halogen atoms are fluorine atoms. 1 -C 6-Haloalkoxy is, for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy.

[0140] The term "C 3 -C 4 "-Alkenyl" refers to a straight or branched monovalent hydrocarbon radical 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.

[0141] The term "C 3 -C 4 "-alkynyl" refers to a straight or branched monovalent hydrocarbon radical containing one triple bond and 3 or 4 carbon atoms. 3 -C 4 -Alkynyl is, for example, prop-1-ynyl, prop-2-ynyl (or "propargyl"), but-1-ynyl, but-2-ynyl or but-3-ynyl.

[0142] The term "C 3 -C 7 "-Cycloalkyl" refers to a saturated monovalent monocyclic hydrocarbon ring containing 3, 4, 5, 6 or 7 carbon ring atoms ("C 3 -C 7 -cycloalkyl"). 3 -C 6 -Cycloalkyl is, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl.

[0143] The term "bicyclic C 6 -C 11 "Cycloalkyl" means a spirocycloalkyl group as defined below, a fused C 6 -C 10 Cycloalkyl or bridged C 7 -C 10 Cycloalkyl:

[0144] The term "spirocycloalkyl" refers to a bicyclic, saturated, monovalent C 5 -C 11 Hydrocarbyl, wherein the 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 spirocycloalkyl can be connected to the rest of the molecule through any one carbon atom other than the spiro carbon atom. The spirocycloalkyl is spiro[2.6]nonyl, spiro[3.3]heptyl, spiro[3.4]octyl, spiro[3.5]nonyl, spiro[3.6]decyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[4.6]undecyl or spiro[5.5]undecyl.

[0145] The term "fused C6 -C 10 "Cycloalkyl" means a bicyclic, saturated monovalent hydrocarbon radical in which the two rings share two adjacent ring atoms, for example, bicyclo[4.2.0]octyl, octahydropentenyl or decalinyl.

[0146] The term "bridged C 7 -C 10 "Cycloalkyl" means 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).

[0147] The term "bicyclic C 5 -C 11 "Cycloalkyl" means a spirocycloalkyl group as defined below, a fused C 5 -C 10 Cycloalkyl or bridged C 5 -C 10 Cycloalkyl:

[0148] The term "spirocycloalkyl" refers to a bicyclic, saturated, monovalent C 5 -C 11 Hydrocarbyl, wherein the two rings share a common ring carbon atom, and wherein the bicyclic hydrocarbyl contains 5, 6, 7, 8, 9, 10 or 11 carbon atoms, and the spirocycloalkyl may be attached to the remainder of the molecule via any one carbon atom other than the spiro carbon atom. The spirocycloalkyl is spiro[2.6]nonyl, spiro[3.3]heptyl, spiro[3.4]octyl, spiro[3.5]nonyl, spiro[3.6]decyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[4.6]undecyl or spiro[5.5]undecyl.

[0149] The term "fused C 5 -C 10 "Cycloalkyl" means a bicyclic, saturated monovalent hydrocarbon radical in which the two rings share two adjacent ring atoms, for example, bicyclo[4.2.0]octyl, octahydropentadienyl or decalinyl.

[0150] The term "bridged C 5 -C 10 "Cycloalkyl" means a bicyclic, saturated, monovalent hydrocarbon radical in which the two rings share two non-adjacent common ring atoms, for example, bicyclo[1.1.1]pentyl or bicyclo[2.2.1]heptyl (also known as norbornyl).

[0151] The term "monocyclic 4- to 7-membered heterocycloalkyl" means a monocyclic saturated heterocycle having a total of 4, 5, 6 or 7 ring atoms, containing one or two identical or different ring heteroatoms from the N, O and S series.

[0152] The monocyclic heterocycloalkyl group may 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-dioxythiolanyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl or 1,3-thiazolidinyl; or a 6-membered ring, such as tetrahydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, dithienyl, 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.

[0153] The term "monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl" means a monocyclic saturated heterocycle having a total of 4, 5, 6 or 7 ring atoms, containing one ring nitrogen atom and optionally one further ring heteroatom from the N, O and S series.

[0154] The monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl group may be 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.

[0155] The term "optionally benzo-fused monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl" means a monocyclic saturated heterocycle having a total of 4, 5, 6 or 7 ring atoms, which contains one ring nitrogen atom and optionally one other ring heteroatom from the series of N, O and S, wherein two adjacent ring carbon atoms in the heterocycloalkyl can be shared with an optionally fused benzene ring, and the group is one of the above-mentioned monocyclic nitrogen-containing 4- to 7-membered heterocycloalkyl, such as pyrrolidinyl, piperidinyl, etc., or a benzo condensation group, such as 3,4-dihydroquinolin-1(2H)-yl, 3,4-dihydroisoquinolin-2(1H)-yl, 1,3-dihydro-2H-isoindol-2-yl or 2,3-dihydro-1H-indol-1-yl.

[0156] The term "bicyclic 6 to 11 membered heterocycloalkyl" means a 6 to 11 membered heterospirocycloalkyl, a 6 to 10 membered fused heterocycloalkyl or a 7 to 10 membered bridged heterocycloalkyl as defined below:

[0157] The term "6- to 11-membered heterospirocycloalkyl" means a bicyclic saturated heterocycle having a total of 6, 7, 8, 9, 10 or 11 ring atoms, wherein the two rings share a common ring carbon atom, wherein the "heterospirocycloalkyl" contains one or two identical or different ring heteroatoms from the series: N, O, S; the heterospirocycloalkyl may be attached to the rest of the molecule via any carbon atom other than the spiro carbon atom or via the nitrogen atom (if present).

[0158] The heterospirocycloalkyl group is, for example, azaspiro[2.3]hexyl, azaspiro[3.3]heptyl, oxazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, oxazaspiro[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 homologous scaffolds 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]-.

[0159] The term "6- to 10-membered fused heterocycloalkyl" means a bicyclic saturated heterocycle having a total of 6, 7, 8, 9 or 10 ring atoms, wherein the two rings share two adjacent ring atoms, wherein the "fused heterocycloalkyl" contains one or two identical or different ring heteroatoms from the series: N, O, S; said fused heterocycloalkyl may be attached to the rest of the molecule via any one carbon atom or nitrogen atom (if present).

[0160] The fused heterocycloalkyl group 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.

[0161] The term "7- to 10-membered bridged heterocycloalkyl" means a bicyclic saturated heterocycle having a total of 7, 8, 9 or 10 ring atoms, wherein the two rings share two non-adjacent common ring atoms, wherein the "bridged heterocycloalkyl" contains one or two identical or different ring heteroatoms from the series: N, O, S; said bridged heterocycloalkyl may be attached to the rest of the molecule via any one carbon atom other than the spiro carbon atom or via the nitrogen atom (if present), if present.

[0162] 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[3.2.1]octyl,

[0063] heterobicyclo[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.

[0163] The term "bicyclic nitrogen-containing 6- to 11-membered heterocycloalkyl" means a 6- to 11-membered heterospirocycloalkyl, a 6- to 10-membered fused heterocycloalkyl or a 7- to 10-membered bridged heterocycloalkyl as defined above, but containing one ring nitrogen atom and optionally one or two further ring heteroatoms from the series N, O and S; said bicyclic nitrogen-containing 6- to 11-membered heterocycloalkyl may be attached to the rest of the molecule via the nitrogen atom or any one carbon atom other than the spiro carbon atom.

[0164] The term "bicyclic 5- to 11-membered heterocycloalkyl" means a 5- to 11-membered heterospirocycloalkyl, a 5- to 11-membered fused heterocycloalkyl or a 5- to 11-membered bridged heterocycloalkyl as defined below:

[0165] 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 a common ring carbon atom, wherein the "heterospirocycloalkyl" contains one or two identical or different ring heteroatoms from the series: N, O, S; the heterospirocycloalkyl may be attached to the rest of the molecule via any carbon atom other than the spiro carbon atom or via the nitrogen atom (if present).

[0166] The heterospirocycloalkyl group is, for example, azaspiro[2.2]pentyl, azaspiro[2.3]hexyl, azaspiro[3.3]heptyl, oxazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, oxazaspiro[3.3]heptyl, oxazaspiro[5.3]nonyl, oxazaspiro[4.3]octyl, azaspiro[4,5]decyl, oxazaspiro[5.5]undecyl, diazaspiro[5.5]undecyl, Heterospiro[3.3]heptyl, thiazaspiro[3.3]heptyl, thiazaspiro[4.3]octyl, azaspiro[5.5]undecyl or one of the other homologous scaffolds 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]-.

[0167] The term "5- to 11-membered fused heterocycloalkyl" means 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, wherein the "fused heterocycloalkyl" contains one or two identical or different ring heteroatoms from the series: N, O, S; said fused heterocycloalkyl may be attached to the rest of the molecule via any one carbon atom or nitrogen atom (if present).

[0168] 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.

[0169] The term "5- to 11-membered bridged heterocycloalkyl" means 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, wherein the "bridged heterocycloalkyl" contains one or two identical or different ring heteroatoms from the series: N, O, S; said bridged heterocycloalkyl may be attached to the rest of the molecule via any one carbon atom other than the spiro carbon atom or the nitrogen atom (if present).

[0170] 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[3.2.1]octyl,

[0063] heterobicyclo[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.

[0171] The term "bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl" means a 5- to 11-membered heterospirocycloalkyl, a 5- to 11-membered fused heterocycloalkyl or a 5- to 11-membered bridged heterocycloalkyl as defined above, but containing one ring nitrogen atom and optionally one or two further ring heteroatoms from the series N, O and S; said bicyclic nitrogen-containing 5- to 11-membered heterocycloalkyl may be linked to the rest of the molecule via the nitrogen atom or any one carbon atom other than the spiro carbon atom.

[0172] The term "heteroaryl" refers to a monovalent monocyclic or bicyclic aromatic ring having 5, 6, 8, 9 or 10 ring atoms (a "5- to 10-membered heteroaryl" group), which contains at least one ring heteroatom and optionally one, two or three further ring heteroatoms selected from N, O and / or S, and which is bonded via a ring carbon atom or, if valence permits, for example in pyrrol-1-yl, a nitrogen atom.

[0173] The heteroaryl group may 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 pyridinyl (also referred to herein 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 quinolyl, quinazolinyl, isoquinolyl, cinnolinyl, phthalazinyl, quinoxalinyl or pteridinyl.

[0174] Generally, unless otherwise indicated, a heteroaryl or heteroarylene includes all possible isomeric forms thereof, for example, tautomers and positional isomers with respect to the point of attachment to the rest of the molecule. Thus, for some illustrative, non-limiting examples, the term pyridyl includes pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl; or the term thienyl includes thien-2-yl and thien-3-yl.

[0175] As used herein, for example in "C 1 -C 6 -alkyl", "C 1 -C 6 -haloalkyl", "C 1 -C 6 -Hydroxyalkyl", "C 1 -C 6 -alkoxy" or "C 1 -C 6 -haloalkoxy”, the term “C 1 -C 6 ” refers to an alkyl group having a finite number of carbon atoms from 1 to 6, i.e., 1, 2, 3, 4, 5 or 6 carbon atoms.

[0176] In addition, the term "C 3 -C 7 ", as used herein, for example in "C 3 -C 7 In the context of the definition of "-cycloalkyl", it is intended that the cycloalkyl group has a limited number of carbon atoms of 3 to 7, i.e. 3, 4, 5, 6 or 7 carbon atoms.

[0177] When a numerical range is given, that range includes every value and sub-range within that range.

[0178] For example:

[0179] “C1 -C 6 ” including C 1 、C 2 、C 3 、C 4 、C 5 、C 6 、C 1 -C 6 、C 1 -C 5 、C 1 -C 4 、C 1 -C 3 、C 1 -C 2 、C 2 -C 6 、C 2 -C 5 、C 2 -C 4 、C 2 -C 3 、C 3 -C 6 、C 3 -C 5 、C 3 -C 4 、C 4 -C 6 、C 4 -C 5 and C 5 -C 6 ;

[0180] "C" 2 -C 6 ” including C 2 、C 3 、C 4 、C 5 、C 6 、C 2 -C 6 、C 2 -C 5 、C 2 -C 4 、C 2 -C 3 、C 3 -C 6 、C 3 -C 5 、C 3 -C 4 、C 4 -C 6 、C 4 -C 5 and C 5 -C 6;

[0181] “C 3 -C 6 "Including C 3 , C 4 , C 5 , C 6 , C 3 -C 6 , C 3 -C 5 , C 3 -C 4 , C 4 -C 6 , C 4 -C 5 and C 5 -C 6 .

[0182] As used herein, the term "leaving group" refers to an atom or group of atoms that is displaced as a stable species in a chemical reaction, taking away a bonding electron. In particular, such leaving groups are selected from: a halogen atom, in particular a fluorine atom, a chlorine atom, a bromine atom or an iodine atom, substituted as a halide, in particular a fluoride, a chloride, a bromide or an iodide; (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.

[0183] As used herein, the term "dipolar aprotic solvent" means a solvent selected from the following: acetone, acetonitrile, propionitrile, dimethyl sulfoxide, diethyl sulfoxide, N,N-dimethylformamide, N,N-dimethylacetamide, N,N-diethylformamide, N,N-diethylacetamide, 1-methyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, 1-methyl-2-piperidone and 1-ethyl-2-piperidone, or a mixture thereof. Specifically, the dipolar aprotic solvent is acetonitrile, dimethyl sulfoxide, N,N-dimethylformamide, N,N-dimethylacetamide or 1-methyl-2-pyrrolidone.

[0184] As used herein, the term "room temperature" means a temperature in the range of 15°C to 25°C.

[0185] The compounds of general formula (I) may exist as isotopic variations. Therefore, the present invention includes one or more isotopic variations of the compounds of general formula (I), in particular deuterated compounds of general formula (I).

[0186] The term "isotopic variation" of a compound or agent is defined as a compound that exhibits an unnatural ratio of one or more isotopes that constitute the compound.

[0187] The term "isotopic variation of a compound of formula (I)" is defined as a compound of formula (I) which exhibits an unnatural ratio of one or more isotopes constituting the compound.

[0188] The expression "unnatural proportion" refers to a proportion of this isotope that is higher than its natural abundance. The natural abundance of the isotopes used in this case is described in "Isotopic Compositions of the Elements 1997", Pure Appl. Chem., 70 (1), 217-235, 1998.

[0189] Examples of such isotopes include stable and radioactive isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorus, sulfur, fluorine, chlorine, bromine and iodine, for example 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. 125 I. 129 I and 131 I.

[0190] For the treatment and / or prevention of the diseases specified herein, isotopic variations of the compounds of formula (I) preferably contain deuterium ("deuterated compounds of formula (I)"). Isotopic variations of the compounds of formula (I) (in which one or more radioactive isotopes are incorporated, e.g. 3 H or 14 C) are useful, for example, in drug and / or substrate tissue distribution studies. These isotopes are particularly preferred because they are easy to bind and easy to detect. Positron emitting isotopes such as 18 F or11 C can be incorporated into the compounds of formula (I). These isotopic variants of the compounds of formula (I) can be used for in vivo imaging applications. 13 Compound C can be used for mass spectrometry analysis in preclinical or clinical research settings.

[0191] Isotopic variations of compounds of formula (I) can generally be prepared by methods known to those skilled in the art, such as those described in the schemes and / or in the examples herein, by substituting an isotopic variation of the reagent, preferably a deuterated reagent. Depending on the desired site of deuteration, in some cases, the isotopic variation from D 2 The deuterium of O can be directly incorporated into the compound or incorporated into a reagent that can be used to synthesize such compounds. Deuterium gas is also a useful reagent for incorporating deuterium into molecules. Catalytic deuteration of olefinic and acetylenic bonds is a fast way to bind deuterium. Metal catalysts (i.e., Pd, Pt, and Rh) in the presence of deuterium gas can be used to directly exchange deuterium for hydrogen in hydrocarbon-containing functional groups. Various deuterated reagents and synthetic building blocks are commercially available from the following companies, such as C / D / N Isotopes, Quebec, Canada; Cambridge Isotope Laboratories Inc., Andover, MA, USA; and CombiPhos Catalysts, Inc., Princeton, NJ, USA.

[0192] The term "deuterated compound of formula (I)" is defined as a compound of formula (I) wherein one or more hydrogen atoms are replaced by one or more deuterium atoms, and wherein the deuterium abundance at each deuterated position of the compound of formula (I) is higher than the natural abundance of deuterium, which is about 0.015%. In particular, in the deuterated compound of formula (I), the deuterium abundance at each deuterated position of the compound of formula (I) is higher than 10%, 20%, 30%, 40%, 50%, 60%, 70% or 80% at the position, preferably higher than 90%, 95%, 96% or 97%, even more preferably higher than 98% or 99%. It should be understood that the deuterium abundance at each deuterated position is independent of the deuterium abundance at other deuterated positions.

[0193] Selective incorporation of one or more deuterium atoms into compounds of general formula (I) may alter the physicochemical properties (e.g. acidity [CL Perrin et al., J. Am. Chem. Soc., 2007, 129, 4490], basicity [CL Perrin et al., J. Am. Chem. Soc., 2005, 127, 9641], lipophilicity [B. Testa et al., Int. J. Pharm., 1984, 19 (3), 271]) and / or the metabolic characteristics of the molecule and may result in a change in the ratio of the parent compound to the metabolite or in the amount of the metabolite formed. Such changes may confer certain therapeutic advantages and may therefore be preferred in certain circumstances. It has been reported that in the case of a change in the ratio of metabolites, the rate of metabolism and metabolic conversion is reduced (AEMutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). Exposure to these changes in the parent drug and metabolites may have an important impact on the pharmacodynamics, tolerability and efficacy of the deuterated compounds of general formula (I). In some cases, deuterium substitution reduces or eliminates the formation of undesirable or toxic metabolites and enhances the formation of desired metabolites (e.g., Nevirapine: AM Sharma et al., Chem. Res. Toxicol., 2013, 26, 410; Efavirenz: AEMutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). In other cases, the main effect of deuteration is to reduce systemic clearance. Therefore, the biological half-life of the compound is increased. Potential clinical benefits will include the ability to maintain similar systemic exposure with reduced peak levels and increased trough levels. This may lead to reduced side effects and improved efficacy according to the pharmacokinetic / pharmacodynamic relationship of a specific compound. ML-337 (CJ Wenthur et al., J. Med. Chem., 2013, 56, 5208) and Odanacatib (K. Kassahun et al., WO 2012 / 112363) are examples of this deuterium effect. Other cases have also been reported where reduced metabolic rates lead to increased drug exposure without changing systemic clearance (e.g. Rofecoxib: F. Schneider et al., Arzneim. Forsch. / Drug. Res., 2006, 56, 295; Telaprevir: F. Maltais et al., J. Med. Chem., 2009, 52, 7993). Deuterated drugs that exhibit this effect may require reduced doses (e.g., less doses or lower doses to achieve the desired effect) and / or may produce lower metabolite loads.

[0194] The compound of general formula (I) can have multiple potential attack sites of metabolism. In order to optimize the above-mentioned impact on physicochemical properties and metabolic characteristics, the deuterated compound of the general formula (I) with one or more deuterium-hydrogen exchanges of a specific pattern can be selected. Especially, the deuterium atom of the deuterated compound of general formula (I) is connected to carbon atom and / or is positioned at those positions of general formula (I) compound, which is a metabolic enzyme, for example the attack site of cytochrome P450.

[0195] In a further embodiment of the invention, it relates to deuterium compounds of the general formula (I) having 1, 2, 3 or 4 deuterium atoms, in particular having 1, 2 or 3 deuterium atoms.

[0196] When the plural form of the word compounds, salts, polymorphs, hydrates, solvates and the like is used herein, this also refers to a single compound, salt, polymorph, isomer, hydrate, solvate and the like.

[0197] By "stable compound" or "stable structure" is meant a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.

[0198] The compounds of the present invention optionally contain one or more asymmetric centers, depending on the position and properties of the various substituents required. One or more asymmetric carbon atoms may be present in the (R) or (S) configuration, which may produce a racemic mixture in the case of a single asymmetric center and a diastereomeric mixture in the case of multiple asymmetric centers. In some cases, asymmetry may also exist due to restricted rotation around a given bond (e.g., a central bond adjacent to two substituted aromatic rings of a particular compound). Preferred isomers are those that produce more desirable biological activity. Separated, pure or partially purified isomers or racemic mixtures of these compounds of the present invention are also included within the scope of the present invention. The purification and separation of these materials can be accomplished by standard techniques known in the art.

[0199] Optical isomers can be obtained by resolving racemic mixtures according to conventional methods, for example, by forming diastereomeric salts using optically active acids or bases or by forming covalent diastereomers. Examples of suitable acids are tartaric acid, diacetyltartaric acid, ditoluoyltartaric acid and camphorsulfonic acid. A mixture of diastereoisomers can be separated into their respective diastereomers based on their physical and / or chemical differences by methods known in the art (e.g., by chromatography or fractional crystallization). The optically active base or acid is then released from the separated diastereomeric salts. Different methods for separating optical isomers involve the use of chiral chromatography (e.g., using a HPLC column of a chiral phase), with or without conventional derivatization, optimally selected to maximize the separation of enantiomers. Suitable HPLC columns using chiral phases are commercially available, such as those manufactured by Daicel, such as Chiracel OD and Chiracel OJ, and many others, which are all conventionally selectable. Enzymatic separations, with or without derivatization, are also useful. The optically active compounds of the present invention can also be obtained by chiral synthesis using optically active starting materials.

[0200] In order to distinguish different types of isomers from each other, please refer to IUPAC Rules Section E (Pure Appl Chem 45, 11 30, 1976).

[0201] The present invention includes all possible stereoisomers of the compounds of the present invention as single stereoisomers, or as any mixture of said stereoisomers (e.g., (R) or (S) isomers in any ratio). Separation of single stereoisomers (e.g., single enantiomers or single diastereomers) of the compounds of the present invention can be achieved by any suitable prior art method, such as chromatography, especially chiral chromatography.

[0202] In addition, some compounds of the present invention may exist as tautomers. For example, a compound of the present invention may contain a pyridone moiety and may exist as a pyridone, or a hydroxypyridine, or even a mixture of two tautomers in any amount, i.e.:

[0203]

[0204] The present invention includes all possible tautomers of the compounds of the present invention as single tautomers, or as any mixture of said tautomers in any ratio.

[0205] Additionally, the compounds of the present invention may exist as N-oxides, which are defined as at least one nitrogen of the compounds of the present invention is oxidized. The present invention includes all such possible N-oxides.

[0206] The present invention also encompasses useful forms of the compounds of the present invention, such as metabolites, hydrates, solvates, prodrugs, salts (particularly pharmaceutically acceptable salts) and / or coprecipitates.

[0207] The compounds of the invention may exist as hydrates or solvates, wherein the compounds of the invention contain polar solvents, in particular water, methanol or ethanol, for example as structural elements of the compound lattice. The amount of polar solvents (in particular water) may be present in a stoichiometric or non-stoichiometric ratio. In the case of stoichiometric solvates (e.g. hydrates), hemi-, (semi-), mono-, one-and-a-half-, two-, three-, four-, five- etc. solvates or hydrates are possible, respectively. The present invention includes all these hydrates or solvates.

[0208] In addition, the compounds of the present invention may exist in free form, for example as a free base, or as a free acid, or as a zwitterion, or in the form of a salt. The salt may be any salt, an organic or inorganic addition salt, in particular any pharmaceutically acceptable organic or inorganic addition salt, which is conventionally used in pharmacy, or for example for isolating or purifying the compounds of the present invention.

[0209] The term "pharmaceutically acceptable salt" refers to an inorganic or organic acid addition salt of a compound of the present invention. For example, see SM Berge et al. "Pharmaceutical Salts," J. Pharm. Sci. 1977, 66, 1-19.

[0210] Suitable pharmaceutically acceptable salts of the compounds of the invention may be acid addition salts of compounds of the invention carrying nitrogen atoms in the chain or ring, for example, which have sufficient basicity, such as acid addition salts with, for example, the following inorganic acids or "mineral acids": hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, aminosulfonic acid, disulfuric acid, phosphoric acid or nitric acid; or with, for example, the following organic acids: formic acid, acetic acid, acetoacetic acid, pyruvic acid, trifluoroacetic acid, propionic acid, butyric acid, hexanoic acid, heptanoic acid, undecanoic acid, lauric acid, benzoic acid, salicylic acid, 2-(4-hydroxybenzoyl)-benzoic acid, camphoric acid, carnitine acid, Cinnamic acid, cyclopentanepropionic acid, digluconic acid, 3-hydroxy-2-naphthoic acid, nicotinic acid, pamoic acid, pectic acid, 3-phenylpropionic acid, pivalic acid, 2-hydroxyethanesulfonic acid, itaconic acid, trifluoromethanesulfonic acid, dodecylsulfuric acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, methanesulfonic acid, 2-naphthalenesulfonic acid, naphthalenedisulfonic acid, camphorsulfonic acid, citric acid, tartaric acid, stearic acid, lactic acid, oxalic acid, malonic acid, succinic acid, malic acid, adipic acid, alginic acid, maleic acid, fumaric acid, D-gluconic acid, mandelic acid, ascorbic acid, glucoheptonic acid, glycerophosphoric acid, aspartic acid, sulfosalicylic acid, or thiocyanic acid.

[0211] In addition, another suitable pharmaceutically acceptable salt with sufficient acidity of the compounds of the present invention is an alkali metal salt, such as a sodium salt or a potassium salt, an alkaline earth metal salt, such as a calcium salt, a magnesium salt or a strontium salt, or an aluminum salt or a zinc salt, or a salt derived from ammonia or from an organic primary, secondary or tertiary amine having 1 to 20 carbon atoms, such as ethylamine, diethylamine, triethylamine, ethyldiisopropylamine, monoethanolamine, diethanolamine, triethanolamine, dicyclohexylamine, dimethylaminoethanol, diethylaminoethanol, tris(hydroxymethyl)aminomethane, procaine, dibenzylamine, N-methylmorpholine, arginine ammonium salts of 1- to 20-carbon-atoms quaternary ammonium ions, such as tetramethylammonium, tetraethylammonium, tetra(n-propyl)ammonium, tetra(n-butyl)ammonium, N-benzyl-N,N,N-trimethylammonium, choline or benzalkonium chloride.

[0212] Those skilled in the art will further recognize that the acid addition salts of the claimed compounds can be prepared by any of a variety of known methods by reacting the compounds with a suitable inorganic or organic acid. Alternatively, alkali metal salts and alkaline earth metal salts of the acidic compounds of the present invention are prepared by reacting the compounds of the present invention with a suitable base by various known methods.

[0213] The present invention includes all possible salts of the compounds according to the invention as a single salt, or as any mixture of said salts in any ratio.

[0214] In the text (especially in the "Experimental Part"), for the synthesis of the intermediates and examples of the present invention, when the compounds are mentioned as salt forms with the corresponding bases or acids, the exact stoichiometric composition of said salt forms obtained by the corresponding preparation and / or purification processes is in most cases unknown.

[0215] Unless otherwise indicated, suffixes such as "hydrochloride", "trifluoroacetate", "sodium salt" or "×HCl", "×CF 3 COOH", "×Na + ” etc. denotes a salt form, the stoichiometry of which is unspecified.

[0216] This applies analogously to the case where synthetic intermediates or example compounds or salts thereof have been obtained by the described preparation and / or purification processes as solvates (eg hydrates) of (if defined) unknown stoichiometric composition.

[0217] Furthermore, the present invention includes all possible crystalline forms or polymorphs of the compounds of the present invention, either as a single polymorph or as a mixture of more than one polymorph in any ratio.

[0218] Furthermore, the present invention also includes prodrugs of the compounds of the present invention. The term "prodrug" here means a compound which itself may be biologically active or inactive, but which can be converted (eg metabolized or hydrolyzed) into a compound of the present invention during its residence time in the body.

[0219] The present invention further includes all possible cyclodextrin inclusion complexes, namely α-, β- or γ-cyclodextrin, hydroxypropyl-β-cyclodextrin, methyl-β-cyclodextrin.

[0220] According to a second embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0221] R 1 represents phenyl or pyridyl, 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, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0222] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0223] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 -O- divalent group,

[0224] or

[0225] R 1 represents a pyrazolyl group, which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl and C 1 -C 2 - alkoxy;

[0226] R 2 Representative Group

[0227] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0228] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0229] R 4 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (5-membered heteroaryl)-(C 1 -C 2 -alkyl)-, (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)-, ((R 9 )O)-(C 1 -C 4 -alkyl)-, C 1 -C 4 -haloalkyl, C 3 -C 7 -cycloalkyl, -OR 9 、-N(R 10 )(R11 )、((R 10 )(R 11 )N)-(C 1 -C 3 -alkyl)-, -C(=O)-N(R 12 )(R 13 )、S(=O) n -R 14 、-C(=O)R 14 、-C(=O)-OR 17 and a 5-membered heteroaryl group which itself is optionally substituted with one or two methyl groups,

[0230] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 -O- divalent group;

[0231] R 5 and R 6 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0232] or

[0233] 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 optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0234] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0235] R 8 represents -C(=O)-NH 2 ;

[0236] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -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,

[0237] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, and the phenyl group itself is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from cyano groups, methyl groups, trifluoromethyl groups and methoxy groups;

[0238] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((R 22 )(R 23 )N)-C 2 -alkyl, (C 3 -C7 -cycloalkyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 7 -cycloalkyl, (C 3 -C 7 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[0239] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)- and (C 3 -C 7 -cycloalkyl)-C(=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a cyano group, a C 1 -C 2 -alkyl and C 1 -C 2 - haloalkyl,

[0240] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[0241] or

[0242] 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, or a bicyclic nitrogen-containing 5- to 10-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 the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 1 -C 2 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl;

[0243] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 4 -haloalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[0244] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from halogen atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0245] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1-C 3 -alkyl)-, the phenyl group in the group consisting of -(-alkyl)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from cyano groups, methyl groups, trifluoromethyl groups and methoxy groups,

[0246] or

[0247] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0248] R 14 represents a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 - haloalkyl and phenyl,

[0249] wherein the phenyl group is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy;

[0250] R 17 Represents C 1 -C 4 -alkyl;

[0251] R 18 and R 19 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl;

[0252] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[0253] Wherein C1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 5 to 10 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 fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[0254] And among them C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 5 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0255] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[0256] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[0257] or

[0258] R20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[0259] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0260] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl, and

[0261] n represents an integer of 0, 1 or 2.

[0262] According to a third embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0263] R 1 represents a phenyl group or a 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 from a hydroxyl group, a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R 5 )(R 6 ),

[0264] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 -O- divalent group,

[0265] or

[0266] R 1 represents pyrazolyl, which is optionally substituted by one methyl group;

[0267] R 2 Representative Group

[0268] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0269] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0270] R 4 represents phenyl or pyridyl, 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: cyano, C 1 -C 3 -alkyl, ((R 9 )O)-(C 1 -C 3 -alkyl)-, C 1 -C 3 -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 ,

[0271] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3-、-O-CH 2 -O- and -O-CF 2 -O- divalent group;

[0272] R 5 and R 6 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl,

[0273] or

[0274] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group and C 1 -C 2 -alkyl;

[0275] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0276] R 8 represents -C(=O)-NH 2 ;

[0277] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -Fluoroalkyl, C 2 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -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,

[0278] 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 from cyano groups and methyl groups;

[0279] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-(C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 7 -Cycloalkyl, C 3 -C 7 -cycloalkyl-(C=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[0280] Among them C 3 -C 7 -cycloalkyl, said (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- 3 -C 5 -cycloalkyl and the C 3 -C 7 -Cycloalkyl-(C=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a cyano group, a C 1 -C 2 -alkyl and C 1 -C 2 -fluoroalkyl,

[0281] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2-alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0282] or

[0283] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or selected from cyano, oxo, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0284] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -Fluoroalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[0285] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0286] and wherein the (phenoxy)-C 2 -C 3-alkyl- and the (phenyl)-(C 1 -C 2 -alkyl)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0287] or

[0288] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0289] R 14 represents a group selected from the group consisting of: methyl and trifluoromethyl;

[0290] R 17 Represents C 1 -C 2 -alkyl;

[0291] R 18 and R 19 Each independently represents a hydrogen atom or a methyl group when it occurs;

[0292] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[0293] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[0294] And wherein the C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0295] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ), R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[0296] or

[0297] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[0298] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0299] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl, and

[0300] n represents the integer 2.

[0301] According to a fourth embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0302] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0303] Or the two substituents connected to the adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group -O-CF 2 -O-;

[0304] R 2 Representative Group

[0305] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0306] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0307] R 4 represents phenyl or pyridyl, which is optionally substituted once or twice, each substituent being independently selected from halogen atoms or from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R13 ) and -C(=O)-OR 17 ;

[0308] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0309] R 8 represents -C(=O)-NH 2 ;

[0310] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ) and phenyl,

[0311] 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 from cyano groups and methyl groups;

[0312] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[0313] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 5 -cycloalkyl)-(C 1-C 2 -alkyl)- 3 -C 5 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from cyano, methyl and C 1 -fluoroalkyl,

[0314] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0315] or

[0316] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from cyano, methyl and C 1 -fluoroalkyl;

[0317] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[0318] Among them C 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a methyl group,

[0319] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C1 -C 2 -alkyl)-, the phenyl group is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy;

[0320] R 17 Represents C 1 -C 2 -alkyl;

[0321] R 18 and R 19 Each independently represents a hydrogen atom or a methyl group when it occurs;

[0322] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 3 - alkyl and phenyl,

[0323] Wherein C 1 -C 3 -alkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group, C 1 -C 3 - alkoxy and phenyl, said phenyl itself optionally being substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[0324] and wherein the phenyl group is optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms and chlorine atoms or from methyl, trifluoromethyl, methoxy and trifluoromethoxy, and

[0325] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl.

[0326] According to a fifth embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0327] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0328] Or the two substituents connected to the adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group -O-CF 2 -O-;

[0329] R 2 Representative Group

[0330] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0331] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0332] R 4 represents phenyl or pyridyl, which is optionally substituted once or twice, each substituent being independently selected from halogen atoms or from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR 17 ;

[0333] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0334] R 8 represents -C(=O)-NH 2 ;

[0335] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ) and phenyl,

[0336] 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 from cyano groups and methyl groups;

[0337] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[0338] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- 3 -C 5 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from cyano, methyl and C 1 -fluoroalkyl,

[0339] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0340] or

[0341] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from cyano, methyl and C 1 -fluoroalkyl;

[0342] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3-alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[0343] Among them C 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a methyl group,

[0344] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 2 -alkyl)-, the phenyl group is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy;

[0345] R 17 Represents C 1 -C 2 -alkyl;

[0346] R 18 and R 19 Each independently represents a hydrogen atom or a methyl group when it occurs;

[0347] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 3 - alkyl and phenyl,

[0348] Wherein C 1 -C 3 -alkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group, C 1 -C 3 - alkoxy and phenyl, said phenyl itself optionally being substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[0349] and wherein the phenyl group is optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms and chlorine atoms or from methyl, trifluoromethyl, methoxy and trifluoromethoxy, and

[0350] R 21 Represents hydrogen atom or C 1 -C2 -alkyl.

[0351] According to a sixth embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0352] R 1 Representative Group

[0353] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0354] R 2 Representative Group

[0355] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0356] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0357] R 4 Representative Group

[0358] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0359] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0360] R 8 represents -C(=O)-NH 2 ;

[0361] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21)、-C(=O)-N(R 20 )(R 21 ) and phenyl,

[0362] 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 from cyano groups and methyl groups;

[0363] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 3 -C 7 -cycloalkyl and (benzyl)-OC(=O)-,

[0364] Among them C 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from methyl and trifluoromethyl,

[0365] and wherein the phenyl group in the (benzyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0366] or

[0367] 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 from cyano, methyl and trifluoromethyl;

[0368] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[0369] wherein the (phenoxy)-C2-alkyl- and the (phenyl)-(C 1 -C 2 -alkyl)-, the phenyl group is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy;

[0370] R 17 Represents C 1 -C 2 -alkyl;

[0371] R 18 and R 19 Each independently represents a hydrogen atom or a methyl group when it occurs;

[0372] R 20 represents a group selected from the group consisting of benzyl and phenyl,

[0373] wherein the phenyl group and the phenyl group in the benzyl group are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0374] R 21 represents a hydrogen atom or a methyl group,

[0375] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0376] Y 2 represents -C(H)= or -N=;

[0377] Y 3 Represents -C(R 27 )=or-N=,

[0378] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0379] R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or is selected from methyl, difluoromethyl, trifluoromethyl, methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy, and

[0380] R 27 represents a halogen atom or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR 17 .

[0381] According to a seventh embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0382] R 1 Representative Group

[0383] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0384] R 2 Representative Group

[0385] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0386] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0387] R 4 Representative Group

[0388] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0389] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0390] R 8 represents -C(=O)-NH 2 ;

[0391] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 - fluoroalkyl and phenyl,

[0392] 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 from cyano groups and methyl groups;

[0393] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (benzyl)-OC(=O)-,

[0394] and wherein the phenyl group in the (benzyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0395] or

[0396] 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 from cyano, methyl and trifluoromethyl;

[0397] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, (C 1 -C 4 -alkoxy)-C 2 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-;

[0398] Y 1 represents -C(H)=, -C(F)=, -C(Cl)= or -N=;

[0399] Y 2 represents -C(H)= or -N=;

[0400] Y 3 Represents -C(R 27 )=or-N=,

[0401] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0402] R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or is selected from difluoromethyl, methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy, and

[0403] R 27 represents a halogen atom or is selected from -OR 9 、-N(R 10 )(R 11 ) and -C(=O)-N(R 12 )(R 13 ).

[0404] According to an eighth embodiment of the first aspect, the present invention covers compounds of general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof:

[0405] in:

[0406] R 1 represents phenyl or 6-membered heteroaryl, optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, nitro, C 1 -C 6 -alkyl, (phenyl)-(C 1 -C 3 -alkyl)-, C 1 -C 6 -haloalkyl, C 1 -C 6 -alkoxy, (phenyl)-(C 1 -C 3 -alkoxy)-, C 1 -C 6 -haloalkoxy, -N(R 5 )(R 6 ),

[0407] wherein the (phenyl)-(C 1 -C 3 -alkyl)- and (phenyl)-(C 1 -C 3 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0408] or two substituents connected to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-(CH 2 ) 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O-, -O-CF 2 -O-, -O-CH 2 -CF 2 -O- and -O-CF 2 -CF 2 -O- divalent group,

[0409] or

[0410] 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 the following: cyano, C 1 -C 3 -alkyl and C 1 -C 3 - alkoxy;

[0411] R 2 Representative Group

[0412] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0413] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0414] R 4 represents phenyl or 6-membered heteroaryl, optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, nitro, C 1 -C 6 -alkyl, (phenyl)-(C 1 -C 3 -alkyl)-, (5-membered heteroaryl)-(C 1 -C 3 -alkyl)-, C 1 -C 6 -Hydroxyalkyl, C 1 -C 6 -haloalkyl, -OR 9 、-N(R 10 )(R11 )、-C(=O)-N(R 12 )(R 13 )、S(=O) n -R 14 and a 5-membered heteroaryl group which itself is optionally substituted with one or two methyl groups,

[0415] or two substituents connected to adjacent carbon atoms of the phenyl or 6-membered heteroaryl group together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-(CH 2 ) 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O-, -O-CF 2 -O-, -O-CH 2 -CF 2 -O- and -O-CF 2 -CF 2 -O- divalent group;

[0416] R 5 and R 6 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -cycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[0417] or

[0418] 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 optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or selected from oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4-alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4 - alkoxy;

[0419] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0420] R 8 represents a group selected from the following: -C(=O)-NH 2 and -S(=O) 2 -NH 2 ;

[0421] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, (phenyl)-(C 1 -C 3 -alkyl)-, C 1 -C 6 -haloalkyl, C 2 -C 4 -Hydroxyalkyl, (C 1 -C 3 -alkoxy)-C 2 -C 3 -alkyl-, ((C 1 -C 3 -alkyl)-C(=O)-O)-C 2 -C 3 -alkyl-, -C(R 18 )(R 19 )-C(=O)-OR 17 ,-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ) and phenyl,

[0422] wherein the (phenyl)-(C 1 -C 3 -alkyl)-, and the phenyl group itself is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy;

[0423] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C4 -alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -Hydroxyalkyl, (C 1 -C 3 -alkoxy)-C 2 -C 3 -alkyl-, ((R 22 )(R 23 )N)-C 2 -C 3 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 7 -cycloalkyl, (C 3 -C 7 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 3 -alkyl)-, (phenyl)-(C 1 -C 3 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 3 -alkyl)-OC(=O)-,

[0424] wherein the (phenyl)-(C 1 -C 3 -alkyl)-, (phenyl)-(C 1 -C 3 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 3 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0425] or

[0426] 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, or a bicyclic nitrogen-containing 6- to 11-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 the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, (C 1 -C 4-alkyl)-C(=O)-, C 3 -C 7 -Cycloalkyl, C 1 -C 4 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl;

[0427] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 3 -alkoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[0428] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from halogen atoms or selected from oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4 - alkoxy,

[0429] or

[0430] 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, twice or three times, each substituent being independently selected from a halogen atom or selected from oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4- alkoxy;

[0431] R 14 represents a group selected from the following: C 1 -C 4 -alkyl and C 1 -C 4 - haloalkyl;

[0432] R 17 Represents C 1 -C 4 -alkyl;

[0433] R 18 and R 19 Each of them independently represents a hydrogen atom or a C 1 -C 4 -alkyl;

[0434] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 11-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[0435] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 11-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, said phenyl and 5- to 10-membered heteroaryl substituents themselves optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the group consisting of cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, dimethylamino and trifluoromethoxy,

[0436] Among them C3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl and bicyclic 6 to 11 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl and C 1 -C 4 - alkoxy,

[0437] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[0438] R 21 Represents hydrogen atom or C 1 -C 4 -alkyl,

[0439] or

[0440] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, (phenyl)-(C 1 -C 3 -alkyl)-, (C 1 -C 4 -alkyl)-C(=O)-, C 3 -C4 -Cycloalkyl, C 1 -C 4 -alkoxy, C 1 -C 3 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[0441] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0442] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 4 -alkyl, and

[0443] n represents an integer of 0, 1 or 2.

[0444] According to a ninth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0445] R 1 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0446] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0447] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 -O- divalent group,

[0448] or

[0449] R 1 represents a pyrazolyl group, which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl and C 1 -C 2 - alkoxy;

[0450] R 2 Representative Group

[0451] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0452] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0453] R 4 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (5-membered heteroaryl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -Hydroxyalkyl, C1 -C 4 -haloalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 )、S(=O) n -R 14 and a 5-membered heteroaryl group which itself is optionally substituted with one or two methyl groups,

[0454] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 -O- divalent group;

[0455] R 5 and R 6 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0456] or

[0457] 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 optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0458] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0459] R 8represents -C(=O)-NH 2 ;

[0460] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-OR 17 ,-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ) and phenyl,

[0461] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, and the phenyl group itself is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy;

[0462] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((R 22 )(R 23 )N)-C 2 -alkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 5 -cycloalkyl, (C 3 -C 5-cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[0463] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[0464] or

[0465] 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, or a bicyclic nitrogen-containing 6- to 10-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 the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 1 -C 2 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl;

[0466] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -C 3 -alkyl-, C 3 -C7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[0467] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from halogen atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0468] or

[0469] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0470] R 14 represents a group selected from the following: C 1 -C 2 -alkyl and C 1 -C 2 - haloalkyl;

[0471] R 17 Represents C 1 -C 4 -alkyl;

[0472] R 18 and R 19 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl;

[0473] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[0474] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-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 fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[0475] Among them C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 6 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0476] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[0477] R 21Represents hydrogen atom or C 1 -C 2 -alkyl,

[0478] or

[0479] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[0480] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0481] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl, and

[0482] n represents an integer of 0, 1 or 2.

[0483] According to the tenth embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0484] R 1represents a phenyl group or a 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 from a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0485] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 -O- divalent group,

[0486] or

[0487] R 1 represents a pyrazolyl group, which is optionally substituted by one methyl group,

[0488] R 2 Representative Group

[0489] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0490] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0491] R 4 represents a phenyl group or a 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 from a cyano group, a C 1 -C 3 -alkyl, C 1 -C 3 -Hydroxyalkyl, C 1 -C 3 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and S(=O) n -R 14 ,

[0492] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 -O- divalent group;

[0493] R 5 and R 6 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl,

[0494] or

[0495] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group and C 1 -C 2 -alkyl;

[0496] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0497] R 8 represents -C(=O)-NH 2 ;

[0498] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-OR 17 ,-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ) and phenyl,

[0499] 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, a chlorine atom and a methyl group;

[0500] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[0501] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[0502] or

[0503] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from oxo, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0504] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -Fluoroalkyl, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[0505] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0506] or

[0507] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0508] R 14 represents a group selected from the group consisting of: methyl and trifluoromethyl;

[0509] R 17 Represents C 1 -C 2 -alkyl;

[0510] R 18 and R 19 Each independently represents a hydrogen atom or a methyl group when it occurs;

[0511] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[0512] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6- 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[0513] Wherein C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[0514] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[0515] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[0516] or

[0517] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[0518] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[0519] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl, and

[0520] n represents the integer 2.

[0521] According to the eleventh embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0522] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a cyano group, a C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -Fluoroalkoxy;

[0523] R 2 Representative Group

[0524] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0525] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0526] R 4 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a C 1-C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 ;

[0527] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0528] R 8 represents -C(=O)-NH 2 ,as well as

[0529] R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl,

[0530] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[0531] According to the twelfth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0532] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a cyano group, a C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -Fluoroalkoxy;

[0533] R 2 Representative Group

[0534] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0535] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0536] R 4represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 ;

[0537] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0538] R 8 represents -C(=O)-NH 2 ,as well as

[0539] R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl,

[0540] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[0541] According to the thirteenth embodiment of the first aspect, the present invention covers compounds of the above general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0542] R 1 Representative Group

[0543] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0544] R 2 Representative Group

[0545] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0546] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0547] R 4 Representative Group

[0548] wherein "#" represents the point of attachment of the carbonyl group linked to R 4 ;

[0549] R 7 represents a hydrogen atom or C 1 -C 2 -alkyl;

[0550] R 8 represents -C(=O)-NH 2 ;

[0551] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0552] Y 2 represents -C(H)= and -N=;

[0553] Y 3 represents -C(R 27 )= and -N=,

[0554] provided that if Y 2 represents -N=, Y 3 represents -C(R 27 )=, and if Y 3 represents -N=, Y 2 represents -C(H)=;

[0555] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, C 1 -C 2 -alkoxy and C 1 -C 2 -fluoroalkoxy, and

[0556] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy and C 1 -C 2 -fluoroalkoxy.

[0557] According to the fourteenth embodiment of the first aspect, the present invention encompasses compounds of the above general formula (I), and their stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0558] R 1 represents the group

[0559] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0560] R 2 Representative Group

[0561] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0562] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0563] R 4 Representative Group

[0564] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0565] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0566] R 8 represents -C(=O)-NH 2 ;

[0567] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0568] Y 2 represents -C(H)= or -N=;

[0569] Y 3 Represents -C(R 27 )=or-N=,

[0570] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0571] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy and C 1 -C2 -fluoroalkoxy, and

[0572] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy, and C 1 -C 2 -fluoroalkoxy.

[0573] According to the fifteenth embodiment of the first aspect, the present invention encompasses compounds of the above general formula (I), and their stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, as well as mixtures thereof, wherein:

[0574] R 1 represents the group

[0575] wherein "**" represents the point of attachment of the nitrogen atom connected to R 1 ;

[0576] R 2 represents the group

[0577] wherein "*" represents the point of attachment of the nitrogen atom connected to R 2 ;

[0578] R 3 represents a group selected from: methyl and -NH 2 ;

[0579] R 4 represents the group

[0580] wherein "#" represents the point of attachment of the carbonyl group connected to R 4 ;

[0581] R 7 represents a hydrogen atom or C 1 -C 2 -alkyl;

[0582] R 8 represents -C(=O)-NH 2 ;

[0583] Y 1 represents -C(H)=, -C(F)=, or -N=;

[0584] Y 2 represents -C(H)= and -N=;

[0585] Y 3 represents -C(R 27 )= and -N=,

[0586] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0587] R 26 represents a fluorine atom, a chlorine atom, or is selected from methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy, and

[0588] R 27 represents a chlorine atom or is selected from a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group.

[0589] According to the sixteenth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0590] R 1 Representative Group

[0591] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0592] R 2 Representative Group

[0593] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0594] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0595] R 4 Representative Group

[0596] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0597] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0598] R 8 represents -C(=O)-NH 2 ;

[0599] Y 1 represents -C(H)=, -C(F)= or -N=;

[0600] Y 2 represents -C(H)= or -N=;

[0601] Y 3 Represents -C(R 27 )=or-N=,

[0602] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0603] R 26 represents a fluorine atom, a chlorine atom, or is selected from methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy, and

[0604] R 27 represents a chlorine atom or is selected from a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group.

[0605] According to the seventeenth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0606] R 1 Representative Group

[0607] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0608] R 2 Representative Group

[0609] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0610] R 3 Representative-NH 2；

[0611] R 4 Representative Group

[0612] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0613] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0614] R 8 represents -C(=O)-NH 2 ;

[0615] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0616] Y 2 represents -C(H)= and -N=;

[0617] Y 3 represents -C(R 27 )= and -N=,

[0618] provided that if Y 2 represents -N=, Y 3 represents -C(R 27 )=, and if Y 3 represents -N=, Y 2 represents -C(H)=;

[0619] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, C 1 -C 2 -alkoxy and C 1 -C 2 -fluoroalkoxy, and

[0620] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy and C 1 -C 2 -fluoroalkoxy.

[0621] According to the eighteenth embodiment of the first aspect, the present invention encompasses the compounds of the above general formula (I), and their stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0622] R 1 represents the group

[0623] wherein "**" represents the point of attachment of the nitrogen atom connected to R 1 ;

[0624] R 2 represents the group

[0625] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0626] R 3 Representative-NH 2；

[0627] R 4 Representative Group

[0628] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0629] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0630] R 8 represents -C(=O)-NH 2 ;

[0631] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0632] Y 2 represents -C(H)= or -N=;

[0633] Y 3 Represents -C(R 27 )=or-N=,

[0634] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0635] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy and C 1 -C 2 -fluoroalkoxy, and

[0636] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy and C 1 -C 2 -fluoroalkoxy.

[0637] According to the nineteenth embodiment of the first aspect, the present invention encompasses compounds of the above general formula (I), and their stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, as well as mixtures thereof, wherein:

[0638] R 1 represents a group

[0639] wherein "**" represents the point of attachment of the nitrogen atom connected to R 1 ;

[0640] R 2 represents a group

[0641] wherein "*" represents the point of attachment of the nitrogen atom connected to R 2 ;

[0642] R 3 represents -NH 2 ;

[0643] R 4 represents a group

[0644] wherein "#" represents the point of attachment of the carbonyl group connected to R 4 ;

[0645] R 7 represents a hydrogen atom or C 1 -C 2 -alkyl;

[0646] R 8 represents -C(=O)-NH 2 ;

[0647] Y 1 represents -C(H)=, -C(F)= or -N=;

[0648] Y 2 represents -C(H)= and -N=;

[0649] Y 3 represents -C(R 27 )= and -N=,

[0650] provided that if Y 2 represents -N=, Y 3 represents -C(R 27 )=, and if Y 3 represents -N=, Y 2 represents -C(H)=;

[0651] R 26represents a fluorine atom, a chlorine atom, or is selected from methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy, and

[0652] R 27 represents a chlorine atom, or a group selected from methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy.

[0653] According to the twentieth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0654] R 1 Representative Group

[0655] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0656] R 2 Representative Group

[0657] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0658] R 3 Representative-NH 2 ;

[0659] R 4 Representative Group

[0660] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0661] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0662] R 8 represents -C(=O)-NH 2 ;

[0663] Y 1 represents -C(H)=, -C(F)= or -N=;

[0664] Y 2 represents -C(H)= or -N=;

[0665] Y 3 Represents -C(R 27 )=or-N=,

[0666] The condition is that if Y 2 Represents -N=,Y3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[0667] R 26 represents a fluorine atom, a chlorine atom, or is selected from methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy, and

[0668] R 27 represents a chlorine atom, or a group selected from methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy.

[0669] According to the twenty-first embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0670] R 1 Representative Group

[0671] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom,

[0672] or

[0673] R 1 Representative Group

[0674] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0675] R 2 Representative Group

[0676] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0677] R 3 represents a group selected from the group consisting of methyl and -NH 2 ;

[0678] R 4 represents a group selected from the following:

[0679]

[0680] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0681] R 7 represents methyl;

[0682] R 8 represents -C(=O)-NH 2 ;

[0683] Y 1 represents -C(H)= or -C(F)=;

[0684] R 26 represents a fluorine atom, a chlorine atom, or is selected from difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy;

[0685] R 28 represents a group selected from the group consisting of methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy.

[0686] According to the twenty-second embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0687] R 1 Representative Group

[0688] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom,

[0689] or

[0690] R 1 Representative Group

[0691] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0692] R 2 Representative Group

[0693] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0694] R 3 Representative-NH 2 ;

[0695] R 4 represents a group selected from the following:

[0696]

[0697]

[0698] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0699] R 7 represents methyl;

[0700] R 8 represents -C(=O)-NH 2 ;

[0701] Y 1 represents -C(H)= or -C(F)=;

[0702] R 26 represents a fluorine atom, a chlorine atom, or is selected from difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy;

[0703] R 28 represents a group selected from the group consisting of methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy.

[0704] According to the twenty-third embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0705] R 1 Representative Group

[0706] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom,

[0707] or

[0708] R 1 Representative Group

[0709] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0710] R 2 Representative Group

[0711] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0712] R 3 represents methyl;

[0713] R 4 represents a group selected from the following:

[0714]

[0715] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0716] R 7 represents methyl;

[0717] R 8 represents -C(=O)-NH 2 ;

[0718] Y 1 represents -C(H)= or -C(F)=;

[0719] R 26 represents a fluorine atom, a chlorine atom, or is selected from difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy;

[0720] R 28 represents a group selected from the group consisting of methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy.

[0721] According to the twenty-fourth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0722] R 1 represents a group selected from the following:

[0723]

[0724]

[0725] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0726] R 2 Representative Group

[0727] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0728] R 3 Representative-NH 2 ;

[0729] R 4 represents a group selected from the following:

[0730]

[0731]

[0732] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0733] R 7represents methyl;

[0734] R 8 represents -C(=O)-NH 2 .

[0735] According to the twenty-fifth embodiment of the first aspect, the present invention covers compounds of the above-mentioned general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0736] R 1 represents a group selected from the following:

[0737]

[0738] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0739] R 2 Representative Group

[0740] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0741] R 3 represents methyl;

[0742] R 4 represents a group selected from the following:

[0743]

[0744] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[0745] R 7 represents methyl;

[0746] R 8 represents -C(=O)-NH 2 .

[0747] Other embodiments of the first aspect of the present invention

[0748] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0749] R 1 represents phenyl or pyridyl, 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, C 1 -C4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0750] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0751] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 -O- divalent group,

[0752] or

[0753] R 1 represents a pyrazolyl group, which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl and C 1 -C 2 -alkoxy.

[0754] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0755] R 1 represents phenyl or pyridyl, 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, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0756] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0757] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0758] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0759] R 1represents phenyl or pyridyl, 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, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0760] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0761] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0762] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0763] R 1 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0764] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0765] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 -O- divalent group,

[0766] or

[0767] R 1 represents a pyrazolyl group, which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl and C 1 -C 2 -alkoxy.

[0768] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0769] R1 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0770] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0771] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 )4-、-(CH 2 )2-O-、-(CH 2 )3-O-、-CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0772] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0773] R 1 represents phenyl or pyridyl, 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: cyano, nitro, (phenyl)-(C 1 -C 2 -alkyl)-, C1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 4 -haloalkoxy, -N(R 5 )(R 6 ),

[0774] wherein the (phenyl)-(C 1 -C 2 -alkyl)- and (phenyl)-(C 1 -C 2 -alkoxy)-, the phenyl group in the group consisting of -alkoxy)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy,

[0775] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 )4-、-(CH 2 )2-O-、-(CH 2 )3-O-、-CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0776] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0777] R 1 represents a phenyl group or a 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 from a hydroxyl group, a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R5 )(R 6 ),

[0778] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 -O- divalent group,

[0779] or

[0780] R 1 represents pyrazolyl, which is optionally substituted by one methyl group.

[0781] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0782] R 1 represents a phenyl group or a 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 from a hydroxyl group, a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R 5 )(R 6 ),

[0783] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0784] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0785] R 1 represents a phenyl group or a 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 from a hydroxyl group, a cyano group, a C1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R 5 )(R 6 ),

[0786] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0787] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0788] R 1 represents a phenyl group which is optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from hydroxyl groups, cyano groups, C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R 5 )(R 6 ),

[0789] or two substituents connected to adjacent carbon atoms of the phenyl group together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0790] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0791] R 1represents a phenyl group which is optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from hydroxyl groups, cyano groups, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R 5 )(R 6 ),

[0792] or two substituents connected to adjacent carbon atoms of the phenyl group together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0793] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0794] R 1 represents a 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 selected from a hydroxyl group, a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, (phenyl)-(C 1 -C 2 -alkoxy)-, C 1 -C 2 -fluoroalkoxy and -N(R 5 )(R 6 ),

[0795] or two substituents connected to adjacent carbon atoms of the pyridyl group together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0796] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0797] R 1 represents a phenyl group or a 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 from a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0798] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 -O- divalent group,

[0799] or

[0800] R 1 represents pyrazolyl, which is optionally substituted by one methyl group.

[0801] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0802] R 1 represents a phenyl group or a 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 from a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0803] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 )3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0804] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0805] R 1 represents a phenyl group or a 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 from a cyano group, a C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0806] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0807] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0808] R 1 represents a phenyl 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 from a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0809] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2-O- and -O-CF 2 A divalent group of -O-.

[0810] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0811] R 1 represents a phenyl 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 from a cyano group, a C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0812] or two substituents connected to adjacent carbon atoms of the phenyl group together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0813] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0814] R 1 represents a 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 selected from a cyano group, a C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 5 )(R 6 ),

[0815] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[0816] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0817] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0818] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0819] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0820] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0821] R 1 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or from cyano, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0822] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0823] R 1 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0824] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0825] R 1 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or from cyano, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0826] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0827] R 1 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0828] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0829] R 1represents a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy.

[0830] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0831] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0832] Or the two substituents connected to the adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group -O-CF 2 -O-.

[0833] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0834] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0835] Or the two substituents connected to the adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group -O-CF 2 -O-.

[0836] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0837] R 1 represents a phenyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0838] Or the two substituents connected to the adjacent carbon atoms of the phenyl group together form a divalent group -O-CF 2 -O-.

[0839] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0840] R 1 represents a phenyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0841] Or the two substituents connected to the adjacent carbon atoms of the phenyl group together form a divalent group -O-CF 2 -O-.

[0842] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0843] R 1 represents a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a cyano group, a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0844] Or the two substituents connected to the adjacent carbon atoms of the pyridyl group together form a divalent group -O-CF 2 -O-.

[0845] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0846] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0847] Or the two substituents connected to the adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group -O-CF 2 -O-.

[0848] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0849] R 1 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or selected from a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0850] Or the two substituents connected to the adjacent carbon atoms of the phenyl or pyridyl group together form a divalent group -O-CF 2 -O-.

[0851] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0852] R 1 represents a phenyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0853] Or the two substituents connected to the adjacent carbon atoms of the phenyl group together form a divalent group -O-CF 2 -O-.

[0854] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0855] R 1 represents a phenyl group which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0856] Or the two substituents connected to the adjacent carbon atoms of the phenyl group together form a divalent group -O-CF 2 -O-.

[0857] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0858] R 1represents a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a bromine atom, or from a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group,

[0859] Or the two substituents connected to the adjacent carbon atoms of the pyridyl group together form a divalent group -O-CF 2 -O-.

[0860] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0861] R 1 Representative Group

[0862] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom.

[0863] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0864] R 1 Representative Group

[0865] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0866] Y 1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0867] R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or is selected from a methyl group, a difluoromethyl group, a trifluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group.

[0868] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0869] R 1 Representative Group

[0870] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0871] Y1 represents -C(H)=, -C(F)=, -C(Cl)=, -C(CN)= or -N=;

[0872] R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or is selected from difluoromethyl, trifluoromethyl, methoxy, benzyloxy, difluoromethoxy and trifluoromethoxy.

[0873] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0874] R 1 Representative Group

[0875] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0876] Y 1 represents -C(H)=, -C(F)= or -N=;

[0877] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy and C 1 -C 2 -fluoroalkoxy.

[0878] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0879] R 1 Representative Group

[0880] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0881] Y 1 represents -C(H)=, -C(F)= or -N=;

[0882] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy and C1 -C 2 -fluoroalkoxy.

[0883] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0884] R 1 Representative Group

[0885] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0886] Y 1 represents -C(H)=, -C(F)=, -C(Cl)= or -N=;

[0887] R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or is selected from a difluoromethyl group, a methoxy group, a benzyloxy group, a difluoromethoxy group and a trifluoromethoxy group.

[0888] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0889] R 1 Representative Group

[0890] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom;

[0891] Y 1 represents -C(H)= or -C(F)=, and

[0892] R 26 represents a fluorine atom, a chlorine atom, or is selected from difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy.

[0893] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0894] R 1 Representative Group

[0895] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom; and

[0896] R28 represents a group selected from the group consisting of methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy.

[0897] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0898] R 1 represents a group selected from the following:

[0899]

[0900]

[0901] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom.

[0902] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0903] R 1 represents a group selected from the following:

[0904]

[0905] Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom.

[0906] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0907] R 2 Representative Group

[0908] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0909] R 7 Represents hydrogen atom or C 1 -C 2 -alkyl;

[0910] R 8 represents -C(=O)-NH 2 .

[0911] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0912] R 2 Representative Group

[0913] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0914] R 7 Represents C 1 -C 2 -alkyl;

[0915] R 8 represents -C(=O)-NH 2 .

[0916] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0917] R 2 Representative Group

[0918] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0919] R 7 Represents C 1 -C 2 -alkyl;

[0920] R 8 represents -C(=O)-NH 2 .

[0921] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0922] R 2 Representative Group

[0923] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0924] R 7 Represents C 1 -C 2 -alkyl;

[0925] R 8 represents -C(=O)-NH 2 .

[0926] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0927] R 2 Representative Group In a ratio of about 99:1 and higher, preferably

[0928] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0929] R 7 Represents C 1 -C 2 -alkyl;

[0930] R 8 represents -C(=O)-NH 2 .

[0931] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0932] R 2 Representative Group At a ratio of about 98:2 and higher, preferably

[0933] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0934] R 7 Represents C 1 -C 2 -alkyl;

[0935] R 8 represents -C(=O)-NH 2 .

[0936] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0937] R 2 Representative Group At a ratio of about 95:5 and higher, preferably

[0938] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0939] R 7 Represents C 1 -C 2 -alkyl;

[0940] R 8 represents -C(=O)-NH 2 .

[0941] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0942] R 2 Representative Group At a ratio of about 90:10 and higher, preferably

[0943] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0944] R 7 Represents C 1 -C 2 -alkyl;

[0945] R 8 represents -C(=O)-NH 2 .

[0946] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0947] R 2 Representative Group At a ratio of about 80:20 and higher, preferably

[0948] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0949] R 7 Represents C 1 -C 2 -alkyl;

[0950] R 8 represents -C(=O)-NH 2 .

[0951] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0952] R 2 Representative Group in a ratio of about 50:50, ie, a racemic mixture in the case where the compound is not characterized by an additional chiral element,

[0953] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0954] R 7 Represents C 1 -C 2 -alkyl;

[0955] R 8 represents -C(=O)-NH 2 .

[0956] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0957] R 2 Representative Group

[0958] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0959] R 7 represents methyl;

[0960] R 8 represents -C(=O)-NH 2 .

[0961] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0962] R 2 Representative Group

[0963] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0964] R 7 represents methyl;

[0965] R8 represents -C(=O)-NH 2 .

[0966] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0967] R 2 Representative Group

[0968] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0969] R 7 represents methyl;

[0970] R 8 represents -C(=O)-NH 2 .

[0971] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0972] R 2 Representative Group At a ratio of about 99:1 and higher, preferably

[0973] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0974] R 7 represents methyl;

[0975] R 8 represents -C(=O)-NH 2 .

[0976] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0977] R 2 Representative Group At a ratio of about 98:2 and higher, preferably

[0978] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0979] R 7represents methyl;

[0980] R 8 represents -C(=O)-NH 2 .

[0981] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0982] R 2 Representative Group At a ratio of about 95:5 and higher, preferably

[0983] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0984] R 7 represents methyl;

[0985] R 8 represents -C(=O)-NH 2 .

[0986] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0987] R 2 Representative Group At a ratio of about 90:10 and higher, preferably

[0988] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0989] R 7 represents methyl;

[0990] R 8 represents -C(=O)-NH 2 .

[0991] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0992] R 2 Representative Group At a ratio of about 80:20 and higher, preferably

[0993] The “*” indicates the same as R2 The point of attachment of the attached nitrogen atom;

[0994] R 7 represents methyl;

[0995] R 8 represents -C(=O)-NH 2 .

[0996] In another embodiment of the first aspect, the present invention encompasses isomeric mixtures of compounds of formula (I) above, and tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[0997] R 2 Representative Group in a ratio of about 50:50, ie, a racemic mixture in the case where the compound is not characterized by an additional chiral element,

[0998] The “*” indicates the same as R 2 The point of attachment of the attached nitrogen atom;

[0999] R 7 represents methyl;

[1000] R 8 represents -C(=O)-NH 2 .

[1001] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1002] R 3 represents a group selected from the group consisting of methyl and -NH 2 .

[1003] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1004] R 3 Representative-NH 2 .

[1005] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1006] R 3 Represents methyl.

[1007] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1008] R 4 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (5-membered heteroaryl)-(C 1 -C 2 -alkyl)-, (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)-, ((R 9 )O)-(C 1 -C 4 -alkyl)-, C 1 -C 4 -haloalkyl, C 3 -C 7 -cycloalkyl, -OR 9 、-N(R 10 )(R 11 )、((R 10 )(R 11 )N)-(C 1 -C 3 -alkyl)-, -C(=O)-N(R 12 )(R 13 )、S(=O) n -R 14 、-C(=O)R 14 、-C(=O)-OR 17 and a 5-membered heteroaryl group which itself is optionally substituted with one or two methyl groups,

[1009] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2-O-, -O-CH 2 -CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1010] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1011] R 4 represents phenyl or pyridyl, 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: cyano, nitro, C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (5-membered heteroaryl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -Hydroxyalkyl, C 1 -C 4 -haloalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 )、S(=O) n -R 14 and a 5-membered heteroaryl group which itself is optionally substituted with one or two methyl groups,

[1012] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-, -CH 2 -O-CH 2 -、-O-CH 2 -O-, -O-CH 2 -CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1013] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1014] R 4 represents phenyl or pyridyl, 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: cyano, C 1 -C 3 -alkyl, ((R 9 )O)-(C 1 -C 3 -alkyl)-, C 1 -C 3 -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 ,

[1015] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1016] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1017] R 4 represents a phenyl 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: cyano, C 1 -C 3 -alkyl, ((R 9 )O)-(C 1 -C 3 -alkyl)-, C 1 -C 3 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 )、S(=O) n -R14 and -C(=O)-OR 17 ,

[1018] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1019] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1020] R 4 represents a pyridyl group optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 3 -alkyl, ((R 9 )O)-(C 1 -C 3 -alkyl)-, C 1 -C 3 -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 ,

[1021] or two substituents connected to adjacent carbon atoms of the phenyl or pyridyl radical together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1022] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1023] R 4 represents a phenyl 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 from a cyano group, a C 1 -C 3 -alkyl, C1 -C 3 -Hydroxyalkyl C 1 -C 3 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and S(=O) n -R 14 ,

[1024] or two substituents connected to adjacent carbon atoms of the phenyl group together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1025] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1026] R 4 represents a 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 selected from a cyano group, a C 1 -C 3 -alkyl, C 1 -C 3 -Hydroxyalkyl, C 1 -C 3 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and S(=O) n -R 14 , or two substituents connected to adjacent carbon atoms of the pyridyl group together form a group selected from -(CH 2 ) 3 -、-O-CH 2 -O- and -O-CF 2 A divalent group of -O-.

[1027] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1028] R 4represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 ;

[1029] R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl,

[1030] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1031] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1032] R 4 represents phenyl or pyridyl, which is optionally substituted once or twice, each substituent being independently selected from halogen atoms or from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR 17 .

[1033] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1034] R 4 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR 17 .

[1035] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1036] R 4 represents a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a halogen atom or from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR 17 .

[1037] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1038] R 4 represents a phenyl group or a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom and a chlorine atom, or from a C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 .

[1039] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1040] R 4 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 ;

[1041] R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl,

[1042] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1043] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1044] R 4 represents a phenyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 .

[1045] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1046] R 4 represents a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 ;

[1047] R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl,

[1048] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1049] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1050] R 4 represents a pyridyl group, which is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 .

[1051] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1052] R 4 Representative Group

[1053] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[1054] Y 2 represents -C(H)= or -N=;

[1055] Y 3 Represents -C(R 27 )=or-N=,

[1056] The condition is that if Y 2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[1057] R 27 represents a halogen atom or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, -OR 9 、-N(R 10 )(R 11 )、-C(=O)-N(R 12 )(R 13 ) and -C(=O)-OR17 。

[1058] In another embodiment of the first aspect, the present invention encompasses the compounds of formula (I) above, and their stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1059] R 4 represents a group

[1060] wherein "#" represents the point of attachment of the carbonyl group linked to R 4 ;

[1061] Y 2 represents -C(H)= or -N=;

[1062] Y 3 represents -C(R 27 )= or -N=,

[1063] provided that if Y 2 represents -N=, Y 3 represents -C(R 27 )=, and if Y 3 represents -N=, Y 2 represents -C(H)=;

[1064] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy,

[1065] benzyloxy and C 1 -C 2 -fluoroalkoxy.

[1066] In another embodiment of the first aspect, the present invention encompasses the compounds of formula (I) above, and their stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1067] R 4 represents a group

[1068] wherein "#" represents the point of attachment of the carbonyl group linked to R 4 ;

[1069] Y 2 represents -C(H)= and -N=;

[1070] Y 3 represents -C(R 27 )= and -N=,

[1071] provided that if Y2 Represents -N=,Y 3 Represents -C(R 27 )=, and if Y 3 Represents -N=,Y 2 represents -C(H)=;

[1072] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy and C 1 -C 2 -fluoroalkoxy.

[1073] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1074] R 4 Representative Group

[1075] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[1076] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy and C 1 -C 2 -fluoroalkoxy.

[1077] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1078] R 4 Representative Group

[1079] The “#” indicates the same as R 4 the point of attachment of the attached carbonyl group;

[1080] R 27 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkoxy, benzyloxy and C 1 -C 2 -fluoroalkoxy.

[1081] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1082] R 4 Representative genes selected from the following:

[1083]

[1084]

[1085] The “#” indicates the same as R 4 The point of attachment of the attached carbonyl group.

[1086] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1087] R 4 Representative genes selected from the following:

[1088]

[1089] The “#” indicates the same as R 4 The point of attachment of the attached carbonyl group.

[1090] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1091] R 5 and R 6 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1092] or

[1093] 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 optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1094] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1095] R 5 and R 6 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1096] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1097] 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 optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1098] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1099] R 5 and R 6 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl,

[1100] or

[1101] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group and C 1 -C 2 -alkyl.

[1102] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1103] R 5 and R 6 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1104] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1105] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group and C 1 -C 2 -alkyl.

[1106] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1107] R 7 Represents a hydrogen atom.

[1108] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1109] R 7 Represents methyl.

[1110] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1111] R 7 Represents ethyl.

[1112] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1113] R7 Represents hydrogen atom or C 1 -C 2 -alkyl.

[1114] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1115] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2 -alkyl)-, C 1 -C 4 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -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,

[1116] wherein the (phenyl)-(C 1 -C 2 The phenyl group in the (A)-alkyl)- group and the phenyl group itself are optionally substituted once or twice, each substituent being independently selected from fluorine, chlorine and bromine atoms, or selected from cyano, methyl, trifluoromethyl and methoxy.

[1117] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1118] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, (phenyl)-(C 1 -C 2-alkyl)-, C 1 -C 4 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-OR 17 ,-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ) and phenyl,

[1119] wherein the (phenyl)-(C 1 -C 2 The phenyl group in the (A)-alkyl)- group and the phenyl group itself are optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy groups.

[1120] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1121] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -Fluoroalkyl, C 2 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -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,

[1122] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from fluorine atoms and chlorine atoms, or selected from cyano groups and methyl groups.

[1123] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1124] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-OR 17 ,-C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ) and phenyl,

[1125] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1126] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1127] R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl,

[1128] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1129] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1130] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((C 1 -C 2 -alkyl)-C(=O)-O)-C 2 -alkyl-, -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 )、-C(=O)-N(R 20 )(R 21 ) and phenyl,

[1131] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from fluorine atoms and chlorine atoms, or selected from cyano groups and methyl groups.

[1132] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1133] R 9 represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 - fluoroalkyl and phenyl,

[1134] The phenyl group in the benzyl group and the phenyl group itself are optionally substituted once or twice, and each substituent is independently selected from fluorine atoms and chlorine atoms, or selected from cyano groups and methyl groups.

[1135] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1136] R 10 and R 11Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((R 22 )(R 23 )N)-C 2 -alkyl, (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 7 -cycloalkyl, (C 3 -C 7 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1137] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)- and (C 3 -C 7 -cycloalkyl)-C(=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a cyano group, a C 1 -C 2 -alkyl and C 1 -C 2 - haloalkyl,

[1138] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1139] or

[1140] 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, or a bicyclic nitrogen-containing 5- to 10-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 the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 1 -C 2 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl.

[1141] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1142] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((R 22 )(R 23 )N)-C 2 -alkyl, (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 7 -cycloalkyl, (C3 -C 7 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1143] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 7 -cycloalkyl)-(C 1 -C 2 -alkyl)- and (C 3 -C 7 -cycloalkyl)-C(=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a cyano group, a C 1 -C 2 -alkyl and C 1 -C 2 - haloalkyl,

[1144] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 The phenyl group in the (=O)-alkyl)-OC(=O)- is optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a bromine atom, or selected from a methyl group, a trifluoromethyl group and a methoxy group.

[1145] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1146] 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, or a bicyclic nitrogen-containing 5- to 10-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 the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1-C 2 -haloalkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 1 -C 2 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl.

[1147] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1148] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((R 22 )(R 23 )N)-C 2 -alkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 5 -cycloalkyl, (C 3 -C 5 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1149] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2-alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1150] or

[1151] 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, or a bicyclic nitrogen-containing 6- to 10-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 the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 1 -C 2 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl.

[1152] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1153] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 2 -C 3 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl-, ((R 22 )(R 23 )N)-C 2 -alkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 5 -cycloalkyl, (C 3 -C 5 -cycloalkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1154] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 The phenyl group in the (=O)-alkyl)-OC(=O)- is optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a bromine atom, or selected from a methyl group, a trifluoromethyl group and a methoxy group.

[1155] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1156] 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, or a bicyclic nitrogen-containing 6- to 10-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 the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (C 1 -C 2 -alkyl)-C(=O)-, C 1 -C 2 -alkoxy, -N(R 22 )(R 23 ) and monocyclic 4 to 7 membered heterocycloalkyl.

[1157] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1158] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, (C 3 -C 5-cycloalkyl)-(C 1 -C 2 -alkyl)-(C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 7 -Cycloalkyl, C 3 -C 7 -cycloalkyl-(C=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1159] Among them C 3 -C 7 -cycloalkyl, said (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- 3 -C 5 -cycloalkyl and the C 3 -C 7 -Cycloalkyl-(C=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a cyano group, a C 1 -C 2 -alkyl and C 1 -C 2 -fluoroalkyl,

[1160] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1161] or

[1162] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or selected from cyano, oxo, C 1-C 2 -alkyl, C 1 -C 2 -fluoroalkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1163] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1164] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-(C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 7 -Cycloalkyl, C 3 -C 7 -cycloalkyl-(C=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1165] Among them C 3 -C 7 -cycloalkyl, said (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- 3 -C 5 -cycloalkyl and the C 3 -C 7 -Cycloalkyl-(C=O)- 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a cyano group, a C 1 -C 2 -alkyl and C 1 -C2 -fluoroalkyl,

[1166] And wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 The phenyl group in the -alkyl)-OC(=O)- is optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1167] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1168] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or selected from cyano, oxo, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1169] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1170] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1171] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1172] or

[1173] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from oxo, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1174] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1175] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, (C 1 -C 2 -alkyl)-C(=O)-, (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1176] wherein the (phenyl)-(C 1 -C 2 -alkyl)-, (phenyl)-(C 1 -C 2 -alkyl)-C(═O)- and (phenyl)-(C 1 -C 2The phenyl group in the -alkyl)-OC(=O)- is optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1177] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1178] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from oxo, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1179] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1180] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1181] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- 3 -C 5 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from cyano, methyl and C 1 -fluoroalkyl,

[1182] And wherein the (phenyl)-(C1 -C 2 -alkyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1183] or

[1184] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from cyano, methyl and C 1 -fluoroalkyl.

[1185] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1186] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-OC(=O)-,

[1187] Among them C 3 -C 7 -cycloalkyl and said (C 3 -C 5 -cycloalkyl)-(C 1 -C 2 -alkyl)- 3 -C 5 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from cyano, methyl and C 1 -fluoroalkyl,

[1188] And wherein the (phenyl)-(C 1 -C 2 The phenyl group in the -alkyl)-OC(=O)- is optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1189] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1190] 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from cyano, methyl and C 1 -fluoroalkyl.

[1191] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1192] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, C 3 -C 7 -cycloalkyl and (benzyl)-OC(=O)-,

[1193] Among them C 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from methyl and trifluoromethyl,

[1194] and wherein the phenyl group in the (benzyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1195] or

[1196] 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 from cyano, methyl and trifluoromethyl.

[1197] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1198] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2-alkyl, C 3 -C 7 -cycloalkyl and (benzyl)-OC(=O)-,

[1199] Among them C 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from fluorine atoms or from methyl and trifluoromethyl,

[1200] And wherein the phenyl group in the (benzyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1201] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1202] 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 from cyano, methyl and trifluoromethyl.

[1203] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1204] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (benzyl)-OC(=O)-,

[1205] and wherein the phenyl group in the (benzyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1206] or

[1207] 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 from cyano, methyl and trifluoromethyl.

[1208] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1209] R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (benzyl)-OC(=O)-,

[1210] And wherein the phenyl group in the (benzyl)-OC(=O)- is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a chlorine atom and a methyl group.

[1211] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1212] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 4 -haloalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[1213] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from halogen atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2-alkyl)-C(═O)-,

[1214] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 3 -alkyl)-, the phenyl group in the group consisting of -(-alkyl)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from cyano groups, methyl groups, trifluoromethyl groups and methoxy groups,

[1215] or

[1216] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1217] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1218] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 4 -haloalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[1219] Among them C 3 -C7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from halogen atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1220] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 3 The phenyl group in the (-alkyl)- group is optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a bromine atom, or selected from a cyano group, a methyl group, a trifluoromethyl group and a methoxy group.

[1221] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1222] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1223] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1224] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C1 -C 3 -alkyl)-,

[1225] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from halogen atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1226] or

[1227] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1228] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1229] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 2 -alkoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 3 -alkyl)-,

[1230] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from halogen atoms or selected from oxo, C 1 -C 2-alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1231] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1232] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1233] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1234] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -Fluoroalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[1235] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from fluorine atoms or selected from oxo, C 1-C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1236] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 2 -alkyl)- is optionally substituted once or twice, each substituent being independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy,

[1237] or

[1238] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1239] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1240] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -Fluoroalkyl, C 1 -C 4 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[1241] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1242] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 2 The phenyl group in the (-alkyl)- group is optionally substituted once or twice, and each substituent is independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy groups.

[1243] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1244] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -Fluoroalkyl, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[1245] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1246] or

[1247] 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 oxo, C 1 -C 2-alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1248] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1249] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 4 -Fluoroalkyl, C 3 -C 7 -cycloalkyl, monocyclic 4- to 7-membered heterocycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[1250] Among them C 3 -C 7 -cycloalkyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1251] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1252] 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 oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(=O)-.

[1253] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1254] R 12 and R 13Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -C 3 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -C 3 -alkyl-, (phenoxy)-C 2 -C 3 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[1255] Among them C 3 -C 7 -cycloalkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a methyl group,

[1256] and wherein the (phenoxy)-C 2 -C 3 -alkyl- and the (phenyl)-(C 1 -C 2 The phenyl group in the (-alkyl)- group is optionally substituted once or twice, and each substituent is independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy groups.

[1257] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1258] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 4 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -Hydroxyalkyl, (C 1 -C 4 -alkoxy)-C 2 -alkyl-, (C 1 -C 2-fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-,

[1259] wherein the (phenoxy)-C 2 -alkyl- and the (phenyl)-(C 1 -C 2 The phenyl group in the (-alkyl)- group is optionally substituted once or twice, and each substituent is independently selected from fluorine atoms and chlorine atoms, or selected from methyl, trifluoromethyl and methoxy groups.

[1260] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1261] R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl, (C 1 -C 4 -alkoxy)-C 2 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 3 -C 7 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-.

[1262] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1263] R 14 represents a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 - haloalkyl and phenyl,

[1264] Wherein the phenyl group is optionally substituted once or twice, each substituent is independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy groups.

[1265] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1266] R 14 represents a group selected from the following: C 1 -C 2 -alkyl, C 1 -C 2 - haloalkyl and phenyl,

[1267] Wherein the phenyl group is optionally substituted once or twice, each substituent is independently selected from fluorine atoms, chlorine atoms and bromine atoms, or selected from methyl, trifluoromethyl and methoxy groups.

[1268] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1269] R 14 Representatives selected from C 1 -C 2 -alkyl and C 1 -C 2 -haloalkyl.

[1270] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1271] R 14 represents a group selected from the group consisting of methyl and trifluoromethyl.

[1272] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1273] R 14 Represents methyl.

[1274] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1275] R 17 Represents C 1 -C 4 -alkyl.

[1276] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1277] R 17 Represents C 1 -C 3 -alkyl.

[1278] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1279] R 17 Represents C 1 -C 2 -alkyl.

[1280] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1281] R 17 Represents methyl.

[1282] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1283] R 17 Represents ethyl.

[1284] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1285] R 18 and R 19 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1286] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1287] R 18 and R 19Each occurrence independently represents a hydrogen atom or a methyl group.

[1288] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1289] R 18 and R 19 Both represent methyl.

[1290] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1291] R 18 and R 19 Both represent hydrogen atoms.

[1292] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1293] R 18 represents a hydrogen atom and R 19 Represents methyl.

[1294] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1295] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1296] Wherein C 1 -C 6-alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -cycloalkyl, bicyclic C6-C11-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, the 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 bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1297] Among them C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 6 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1298] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1299] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1300] or

[1301] R 20 and R 21, together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[1302] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[1303] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1304] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1305] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1306] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -cycloalkyl, bicyclic C6-C11-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, the 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 bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1307] Among them C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 6 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1308] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1309] R 21 Represents hydrogen atom or C1 -C 2 -alkyl,

[1310] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[1311] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1312] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1313] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[1314] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2-alkyl)-C(═O)-;

[1315] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1316] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1317] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1318] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 5 to 10 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 fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1319] And among them C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11-cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 5 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1320] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),as well as

[1321] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1322] or

[1323] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23) and -C(=O)-N(R 24 )(R 25 ).

[1324] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1325] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 5- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1326] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 - cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 5 to 10 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 fluorine atoms, chlorine atoms and bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1327] And among them C 3 -C 7 -Cycloalkyl, bicyclic C 5 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 5 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2-alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1328] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),as well as

[1329] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl.

[1330] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1331] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1332] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23), C 3 -C 7 -cycloalkyl, bicyclic C6-C11-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, the 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 bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1333] Among them C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 6 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1334] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1335] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1336] or

[1337] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ).

[1338] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1339] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 6 -alkyl, C 3 -C 4 -Alkenyl, C 3 -C 4 -Alkynyl, C 1 -C 3 -alkoxy, C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl, naphthyl and 5- to 10-membered heteroaryl,

[1340] Wherein C 1 -C 6 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 7-cycloalkyl, bicyclic C6-C11-cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, bicyclic 6- to 10-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl, the 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 bromine atoms, or from methyl, trifluoromethyl and methoxy,

[1341] Among them C 3 -C 7 -Cycloalkyl, bicyclic C 6 -C 11 -cycloalkyl, adamantyl, monocyclic 4 to 7 membered heterocycloalkyl, bicyclic 6 to 10 membered heterocycloalkyl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1342] and wherein the phenyl, naphthyl and 5 to 10 membered heteroaryl are optionally substituted once, twice or three times, each substituent being independently selected from a halogen atom or a group selected from the following: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1343] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl.

[1344] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1345] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C1 -C 2 -alkyl, C 1 -C 2 -haloalkyl, (phenyl)-(C 1 -C 2 -alkyl)-, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ).

[1346] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1347] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1348] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1349] Wherein C 3 -C 6-cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1350] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1351] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1352] or

[1353] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[1354] R 22and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[1355] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1356] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1357] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1358] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1359] Wherein C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1360] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1361] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1362] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[1363] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1364] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1365] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 );

[1366] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-;

[1367] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1368] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1369] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1370] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1371] Wherein C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1372] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1373] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1374] or

[1375] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25).

[1376] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1377] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1378] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1379] Wherein C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1380] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1381] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl.

[1382] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1383] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -haloalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ).

[1384] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1385] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1386] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1387] And wherein the C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1388] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1389] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl,

[1390] or

[1391] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ).

[1392] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1393] R 20 represents a hydrogen atom or is selected from optionally substituted C 1 -C 3 -alkyl, unsubstituted C 4 -C 6 -alkyl, prop-2-ynyl, methoxy, C 3 -C 6 - cycloalkyl, adamantyl, monocyclic 4- to 7-membered heterocycloalkyl, phenyl and 5- to 10-membered heteroaryl,

[1394] Wherein C 1 -C 3 -alkyl 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, C 1 -C 3 -alkoxy, -N(R 22 )(R 23 ), C 3 -C 6 - 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 once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1395] And wherein the C 3 -C 6 -cycloalkyl, adamantyl and monocyclic 4 to 7 membered heterocycloalkyl are optionally substituted once or twice or three times, each substituent being independently selected from fluorine atoms or selected from oxo, C 1 -C2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-,

[1396] 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, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ),

[1397] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl.

[1398] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1399] R 20 and R 21 , together with the nitrogen atom to which they are attached, represent an optionally benzo-condensed 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 a group selected from the following: cyano, oxo, hydroxyl, C 1 -C 2 -alkyl, C 1 -C 2 -fluoroalkyl, benzyl, (C 1 -C 2 -alkyl)-C(=O)-, C 3 -C 4 -Cycloalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ).

[1400] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1401] R 20 represents a hydrogen atom or a group selected from the following: C 1 -C 3 - alkyl and phenyl,

[1402] Wherein C 1 -C 3 -alkyl is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or from a hydroxyl group, C 1 -C 3 - alkoxy and phenyl, said phenyl itself optionally being substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms and methyl,

[1403] and wherein the phenyl group is optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms and chlorine atoms or from methyl, trifluoromethyl, methoxy and trifluoromethoxy;

[1404] R 21 Represents hydrogen atom or C 1 -C 2 -alkyl.

[1405] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1406] R 20 represents a group selected from the group consisting of benzyl and phenyl,

[1407] wherein the phenyl group and the phenyl group in the benzyl group are optionally substituted once or twice, and each substituent is independently selected from a fluorine atom, a chlorine atom and a methyl group,

[1408] R 21 Represents a hydrogen atom or a methyl group.

[1409] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1410] R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1-C 2 -alkyl)-C(=O)-.

[1411] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1412] R 22 and R 23 Each occurrence independently represents a hydrogen atom or is selected from methyl and (CH 3 )-C(=O)-.

[1413] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1414] R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl.

[1415] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1416] R 24 and R 25 Each occurrence independently represents a hydrogen atom or a methyl group.

[1417] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein:

[1418] R 26 represents a fluorine atom, a chlorine atom, or is selected from C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy and C 1 -C 2 -fluoroalkoxy.

[1419] In another embodiment of the first aspect, the present invention encompasses compounds of formula (I) above, and stereoisomers, tautomers, N-oxides, hydrates, solvates and salt...

Claims

1. A pharmaceutical composition comprising a compound of general formula (I), or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients: in: R 1 Representative Group Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom; R 2 Representative Group Where "*" indicates the same as R 2 The point of attachment of the attached nitrogen atom; R 3 Representative-NH 2 Group; R 4 Representative Group The "#" indicates the same as R 4 the point of attachment of the attached carbonyl group; R 7 represents methyl; R 8 represents -C(=O)-NH 2 ; R 9 Represents -C(R 18 )(R 19 )-C(=O)-N(R 20 )(R 21 ) group, R 18 and R 19 Each represents a hydrogen atom; R 20 represents a group selected from the following: substituted C 1 -C 3 -alkyl, C 3 -C 6 - cycloalkyl, adamantyl and phenyl, wherein the substituted C 1 -C 3 -The alkyl group is selected from C 3 -C 6 - cycloalkyl, adamantyl and phenyl substituents substituted once, said phenyl substituents themselves optionally being substituted once or twice, each substituent being independently selected from fluorine atoms, chlorine atoms, methyl and methoxy groups, and wherein the phenyl group is optionally substituted once, twice or three times, each substituent being independently selected from fluorine atoms and chlorine atoms or from the following groups: cyano, C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl, C 1 -C 2 -alkoxy, C 1 -C 2 -fluoroalkoxy, -N(R 22 )(R 23 ) and -C(=O)-N(R 24 )(R 25 ), R 21 Represents hydrogen atom or C 1 -C 2 -alkyl, R 22 and R 23 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (C 1 -C 2 -alkyl)-C(═O)-; R 24 and R 25 Each of them independently represents a hydrogen atom or a C 1 -C 2 -alkyl, Y 1 represents -C(H)=; Y 2 represents -C(H)=; Y 3 Represents -C(R 27 )=, R 26 represents a fluorine atom or a chlorine atom, and R 27 Representative-OR 9 Group.

2. A pharmaceutical composition comprising a compound of general formula (I), or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients: in: R 1 Representative Group Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom; R 2 Representative Group Where "*" indicates the same as R 2 The point of attachment of the attached nitrogen atom; R 3 Representative-NH 2 Group; R 4 represents phenyl, which is optionally substituted once or twice, each substituent being independently selected from the following groups: C 1 -C 2 -alkyl, C 1 -C 2 -Fluoroalkyl and -OR 9 ; R 7 represents methyl; R 8 represents -C(=O)-NH 2 ; R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, (C 1 -C 2 -alkoxy)-C 2 -alkyl- and phenyl, Y 1 represents -C(H)=, -C(F)= or -C(Cl)=, and R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or a group selected from the group consisting of a difluoromethyl group and a trifluoromethyl group.

3. A pharmaceutical composition comprising a compound of general formula (I), or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients: in: R 1 Representative Group Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom; R 2 Representative Group Where "*" indicates the same as R 2 The point of attachment of the attached nitrogen atom; R 3 represents a group selected from the group consisting of methyl and -NH 2 ; R 4 Representative Group The "#" indicates the same as R 4 the point of attachment of the attached carbonyl group; R 7 represents methyl; R 8 represents -C(=O)-NH 2 ; R 9 represents a group selected from the following: C 1 -C 2 -alkyl, benzyl, C 1 -C 2 - fluoroalkyl and phenyl; R 10 and R 11 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 1 -C 2 -alkyl and (benzyl)-OC(=O)-, 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 optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from cyano, methyl and trifluoromethyl; Y 1 represents -C(H)=, -C(F)= or -C(Cl)=; Y 2 represents -C(H)=; Y 3 Represents -C(R 27 )=; R 26 represents a fluorine atom, a chlorine atom or a bromine atom, or a group selected from the group consisting of a difluoromethyl group, a benzyloxy group and a difluoromethoxy group, and R 27 represents a halogen atom or is selected from -OR 9 and -N(R 10 )(R 11 ) group.

4. A pharmaceutical composition comprising a compound of general formula (I), or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients: in: R 1 Representative Group Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom; R 2 Representative Group Where "*" indicates the same as R 2 The point of attachment of the attached nitrogen atom; R 3 Representative-NH 2 Group; R 4 Representative Group The "#" indicates the same as R 4 the point of attachment of the attached carbonyl group; R 7 represents methyl; R 8 represents -C(=O)-NH 2 ; R 9 Represents C 1 -C 2 -fluoroalkyl; R 10 and R 11 Each occurrence independently represents a hydrogen atom or (benzyl)-OC(=O)-, 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 or a bicyclic nitrogen-containing 5- to 10-membered heterocycloalkyl which is optionally substituted once or twice, each substituent being independently selected from a fluorine atom or a group selected from cyano, methyl and trifluoromethyl; Y 1 represents -C(H)=, -C(F)=, -C(Cl)= or -N=; Y 2 Represents -N=; Y 3 Represents -C(R 27 )=; R 26 represents a fluorine atom or a chlorine atom, or a group selected from the group consisting of difluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy, and R 27 represents a group selected from trifluoromethyl, -OR 9 and -N(R 10 )(R 11 ) group.

5. A pharmaceutical composition comprising a compound of general formula (I), or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients: in: R 1 Representative Group Where "**" indicates the same as R 1 The point of attachment of the attached nitrogen atom; R 2 Representative Group Where "*" indicates the same as R 2 The point of attachment of the attached nitrogen atom; R 3 Representative-NH 2 Group; R 4 Representative Group The "#" indicates the same as R 4 the point of attachment of the attached carbonyl group; R 7 represents methyl; R 8 represents -C(=O)-NH 2 ; R 12 and R 13 Each occurrence independently represents a hydrogen atom or a group selected from the following: C 4 -alkoxy-C 2 -alkyl-, (C 1 -C 2 -fluoroalkoxy)-C 2 -alkyl-, (phenoxy)-C 2 -alkyl-, C 5 -C 6 -cycloalkyl and (phenyl)-(C 1 -C 2 -alkyl)-; Y 1 represents -C(H)=, -C(F)= or -C(Cl)=; Y 2 represents -C(H)=; Y 3 Represents -C(R 27 )=; R 26 represents a fluorine atom or a chlorine atom, and R 27 represents -C(=O)-N(R 12 )(R 13 ).

6. A pharmaceutical composition comprising a compound of general formula (I), or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients: in: R 1 represents a phenyl group that is substituted twice, The two substituents attached to adjacent carbon atoms of the phenyl group together form -O-CF 2 -O- divalent group; R 2 Representative Group Where "*" indicates the same as R 2 The point of attachment of the attached nitrogen atom; R 3 Representative-NH 2 Group; R 4 Representative Group The "#" indicates the same as R 4 the point of attachment of the attached carbonyl group; R 7 represents methyl; R 8 represents -C(=O)-NH 2 ; R 9 represents a group selected from the following: C 1 -C 2 -alkyl and C 1 -C 2 -fluoroalkyl; Y 2 represents -C(H)= or -N=; Y 3 Represents -C(R 27 )=, and R 27 Represents a halogen atom or -OR 9 Group.

7. A pharmaceutical composition comprising a compound having the following chemical structure, or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients:

8. A pharmaceutical composition comprising a compound which is rac-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide or (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propionamide, or a salt thereof, or a mixture thereof, and one or more pharmaceutically acceptable excipients.

9. A pharmaceutical composition comprising a compound which is (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients.

10. A pharmaceutical composition comprising a compound which is (R)-2-(N-[4-amino-5-(4-methoxybenzoyl)thiazol-2-yl]-4-fluoro-anilino)propanamide, and one or more pharmaceutically acceptable excipients.

Images