Azine-based compounds as par-2 inhibitors and therapeutic uses thereof

Abstract

The present invention provides novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds of formula (I) can act as PAR-2 inhibitors / antagonists, which renders these compounds highly advantageous for use in therapy, particularly in the treatment or prevention of pain, an autoimmune disorder, an autoinflammatory disorder, an inflammatory disorder, a central nervous system disorder, spinal cord injury, a metabolic disorder, a gastrointestinal disorder, a cardiovascular disorder, a fibrotic disorder, a respiratory disorder, a skin disorder, an allergic disorder, or cancer.

Description

[0001] Azine-based compounds as PAR-2 inhibitors and therapeutic uses thereof

[0002] The present application claims the benefit of priority of European patent application EP24305402.0 filed on March 15, 2024, which is incorporated herein by reference in its entirety.

[0003] The present invention provides novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds of formula (I) can act as PAR-2 inhibitors / antagonists, which renders these compounds highly advantageous for use in therapy, particularly in the treatment or prevention of pain, an autoimmune disorder, an autoinfl ammatory disorder, an inflammatory disorder, a central nervous system disorder, spinal cord injury, a metabolic disorder, a gastrointestinal disorder, a cardiovascular disorder, a fibrotic disorder, a respiratory disorder, a skin disorder, an allergic disorder, or cancer.

[0004] The protease-activated receptors (PARs) family

[0005] G Protein-Coupled Receptors (GPCRs) form the largest family of human membrane proteins (~ 800 members) and are involved in many physiological processes. Compounds targeting GPCRs also represent approximately 27% of the global market for therapeutic drugs (Hauser et al., Nat. Rev. Drug Discov., 2017, 16(12):829-842).

[0006] 2% of the human genome code for proteases (also called proteinases) which suggests their importance in the correct functioning of the body (Hollenberg et al., Br. J. Pharmacol., 2014, 171 (5): 1180-94). Indeed, it has been shown that certain soluble and membrane-bound proteinases can regulate cell function by cleaving GPCRs at the cell surface to activate or inactivate receptors such as the Protease-Activated Receptors (PARs). The PARs family is composed of four members (PAR-1 , PAR-2, PAR-3 and PAR-4) and belongs to the class A GPCR-receptor sub-family (Marcfarlane et al., Pharmacological Reviews, 2001 , 475(7357):519-23). They are expressed in widely diverse cells such as platelets, immune cells, endothelial cells, myocytes, astrocytes, neurons, epithelial cells and fibroblasts and involved in a large set of physiological and pathophysiological functions (Ossovskaya et al., Physiol. Rev., 2004, 84(2):579- 621).

[0007] PAR-2: mechanism of action

[0008] Activation of PARs involves the cleavage of the extracellular N-terminal part of the receptor by proteases at a specific site. This unmasks an amino-acid sequence in the amino terminus that folds back to act as a "tethered ligand” (TL): it binds to a conserved region in the second extracellular loop of the cleaved receptor and triggers intra-cellular signalling (Ossovskaya et al., Physiol. Rev., 2004, 84(2):579-621 ; Hollenberg et al., Br. J. Pharmacol., 2014, 171 (5): 1180-94).

[0009] PAR-2 is activated by several host and pathogen-derived serine proteases such as trypsin, mast cell tryptase, kallikreins and members of the coagulation cascade TF-FVIla and FVa-FXa. These proteases cleave at R34J,S35LIGKV and unmask the tethered ligand SLIGKV in humans. Artificially, in vitro, synthetic peptides corresponding to the TL (SLIGKV) can activate the receptor without cleavage.

[0010] Activation of PAR-2 induces several signalling cascades involving a number of G proteins such as Gq, G, and G12 / 13. The pathway best described so far involves its interaction with Gqand the mobilization of intracellular calcium that influences the function of several cell types. After repeated activations, PAR2 is rapidly desensitized via its endocytosis by a p-arrestin-dependent mechanism and its targeting to the lysosomes (Ossovskaya et al., Physiol. Rev., 2004, 84(2):579-621 ).

[0011] PAR-2 in physiological conditions

[0012] PAR-2 has been shown to have a key function in multiple organs (Ossovskaya et al., Physiol. Rev., 2004, 84(2):579- 621). PAR-2 is expressed in the brain within neurons and glial cells. It is also found in the periphery in spinal afferent neurons and nociceptive DRG neurons. PAR-2 signalling has been involved in the survival, sensitization of these cells and their signal transmission, thereby controlling neuronal damage, inflammation and pain.

[0013] PAR-2 is involved in the function of the cardiovascular system. Indeed, its activation can induce the relaxation or contraction of some vessels such as pulmonary arteries, coronary and intramyocardial arteries, therefore regulating the blood flow. It also controls inflammation and repair of the endothelium which influences vascular permeability.

[0014] PAR-2 expression has been detected within the gastrointestinal system in the small intestine, colon, liver, pancreas and stomach. Its activation has been involved in the regulation of ion transport from the intestinal mucosa, contraction of gastric longitudinal muscle, pancreatic, salivary and gastric secretions, excitation of myenteric neurons, intestinal barrier integrity, release of prostaglandins from enterocytes. PAR-2 therefore plays a key role in controlling fluid secretion, intestinal inflammation, and gastro-intestinal hyperalgesia.

[0015] PAR-2 is involved in airways function since it is expressed by epithelial and endothelial cells in the lungs. Its activation has been shown to regulate bronchodilatation or bronchoconstriction (depending on the experimental system used), ion transport in the airway epithelium, proliferation and activation of airway smooth muscle cells and lung fibroblasts. PAR-2 can thus regulate airway resistance, lung inflammation and lung fibrosis.

[0016] In the skin, PAR-2 expression has been detected in keratinocytes, microvasculature and immune cells. Its activation has been involved in skin pigmentation, skin inflammation, and wound healing.

[0017] Finally, PAR-2 expression has been detected in immune cells such as macrophages where it influences cell maturation and cytokine secretion, thereby regulating inflammation.

[0018] PAR-2 in pathological conditions

[0019] Since PAR-2 regulates numerous and diverse biological processes, it is not surprising that its dysfunction is involved in as many pathological conditions.

[0020] PAR-2 is expressed in the brain, dorsal root ganglia, spinal afferent neurons and nociceptive DRG neurons. Its activation by proteases such as the tryptase released by mast cells leads to calcium and cAMP signalling (Steinhoff et al., Nat Med, 2000, 6(2): 151 -8; Zhao et al., J Biol Chem., 2015, 290(22): 13875-87). This promotes inflammation and hyperalgesia through the release of CGRP (calcitonine gene-related peptide) and SP (substance P) from spinal afferent neurons and the sensitization of Transient Receptors Potential Vanilloid (TRPV) TRPV1 and TRPV4 in sensory neurons (Vergnolle et al., Nat Med, 2001 , 6(2):151-8; Steinhoff et al., Nat Med, 2000, 6(2):151-8; Amadesi et al., J Neurosci, 2004, 24(18):4300-12; Grant et al., J Physiol, 2007, 578 (Pt 3), 715-33; Jimenez Vargas et al., Proc Natl Acad Sci USA, 2018, 115(31 ): E7438-E7447). This is supported by the large amount of in vivo data available in the literature demonstrating that inhibition of PAR-2 reduces inflammatory pain, neuropathic pain, cancer pain and treatment-induced pain in animal models (Bao et al., Expert Opin Ther Targets, 2014; 18(1):15-27; Chen et al., Neuroscience, 2011 , 193, 440-51). PAR-2 is therefore clearly involved in the generation and the transmission of the pain signal, neurogenic inflammation and nociception. The expression of PAR-2 and proteases is elevated in the spinal cord after a contusion-compression injury (Radulovic et al., Neurobiol Dis, 2015, 83, 75-89; Li et al, Physiol. Res., 2019, 68(2):305-316). Its activation can result in cAMP signalling in oligodendrocytes (Yoon et al., Glia, 2017, 65(12):2070-2086). Experiments in vitro and in vivo in rodents have shown that the inhibition of PAR-2 signalling during experimental spinal cord injury reduces inflammation, scar formation and mechanical and thermal hyperalgesia and improves remyelination of oligodendrocytes and locomotor recovery (Radulovic et al., Neurobiol Dis, 2015, 83, 75-89; Li et al, Physiol. Res., 2019, 68(2):305-316; Yoon et al., Glia, 2017, 65(12):2070-2086; Li et al, Physiol. Res., 2019, 68(2):305-316 ; Wei et al, Physiol. Res., 2016, 65(1 ): 145- 53). PAR-2 inhibitors can thus improve recovery from spinal cord injuries.

[0021] Disorders of the immune system are at the basis of numerous diseases. In all cases, the immune system attacks the normal constituents of the organism considering them as foreign. It becomes pathogenic and induces lesions on a specific organ (e.g., type 1 diabetes in the pancreas or multiple sclerosis in the brain) or systemically (e.g., rheumatoid arthritis or systemic lupus erythematosus, SLE).

[0022] Cytokines are small proteins involved in cell signalling that orchestrate the immune response. Their dysregulation is at the basis of the pathogenesis of autoinflammatory diseases. These conditions are characterized by immune activation, infiltration and abnormal cytokine production. They include conditions such as: rheumatologic inflammatory diseases, skin inflammatory diseases, lung inflammatory diseases, muscle inflammatory diseases, bowel inflammatory diseases, brain inflammatory diseases and autoimmune diseases.

[0023] While autoinflammatory diseases evolve chronically, some conditions can lead to an acute immune disorder. Indeed, a sudden excessive and uncontrolled release of pro-inflammatory cytokines, also called cytokine storm, has been observed in graft-versus-host disease, multiple sclerosis, pancreatitis, multiple organ dysfunction syndrome, viral diseases, bacterial infections, hemophagocytic lymphohistiocytosis, and sepsis (Gerlach H, F1000Res, 2016, 5, 2909; Tisoncik JR et al., Microbiol Mol Biol Rev, 2012, 76(1):16-32). In these conditions, a dysregulated immune response and subsequent hyperinflammation may lead to multiple organ failure that can be fatal.

[0024] Because PAR-2 influences the production of inflammatory cytokines and the function of diverse organs, numerous studies have demonstrated that it is a promising therapeutic target for various autoinflammatory diseases.

[0025] The expression of proteinases and PAR-2 is significantly increased in organs directly involved in autoinflammatory diseases such as the coronary arteries of atherosclerotic patients (Jones et al., Arterioscler Thromb Vase Biol, 2018, 38(6): 1271 -1282), the skin of atopic dermatitis and psoriasis patients (Nattkemper et al., Journal of Investigative Dermatology, 2018, 138:1311-1317), the joints of rheumatoid arthritis and osteoarthritis patients (Tindell et al., Rheum Int, 2012, 32(10):3077-86), the colon of inflammatory bowel disease patients (Christerson et al., J Crohns Colitis, 2009, 3(1):15-24; Kim et al., Inflamm Bowel Dis., 2003, 9(4):224-9), the lungs of idiopathic pulmonary fibrosis patients (Bardou et al., Am J Respir Crit Care Med, 2016, 193(8):847-60), the liver of non-alcoholic steatohepatitis patients (Rana et al., Mol Metab, 2019, 29:99-113), the area of active demyelination in the brain of multiple sclerosis patients (Noorbakhsh et al., J Exp Med, 2006, 203(2):425-35).

[0026] There, PAR-2 activation leads to calcium signalling in several cells such as osteoblasts, fibroblasts, monocytes, keratinocytes (Abraham et al, Bone, 2000, 26(1 ):7-14; Lin et al., J. Cell. Mol. Med., 2015, 19(6): 1346-56; Johansson et al., J leukoc Biol, 2005, 78(4):967-75; Joo et al., Bio Mol Ther, 2016, 24(5):529-535). This signalling is associated with cell maturation and / or migration, activation as well as the secretion of inflammatory cytokines such as IL-8, IL-6, TN Fa and IL-113 in various cell types such as vascular smooth muscle cells, synovial cells, monocytes, keratinocytes, astrocytes, chondrocytes, adipocytes and fibroblasts (Demetz et al., Atherosclerosis, 2010, 212:466-471 ; Kelso et al., Arthritis Rheum, 2007, 56(3):765-71 ; Johansson et al., J Leukoc Biol, 2005, 78(4):967-75; Steven et al., Innate Immun, 2013, 19(6):663-72; Kim et al., Bio Mol Ther, 2012, 20(5):463-9; Radulovic et al., Neurobiol Dis, 2015, 83, 75-89; Lin et al., J. Cell. Mol. Med., 2015, 19(6): 1346-56; Bagher et al., Cell Communi and Signal, 2018, 16(1), 59; Huang et al, Aging, 2019, 11 (24): 12532- 12545; Bandeanlou et al., Nat. Med, 2011 , 17: 1490-1497). PAR-2 signalling also influences tissue remodelling through its role in the survival of key cells such as neurons and chondrocytes in central nervous system disorders and rheumatologic inflammatory diseases respectively (Afkhami-Goli et al., J Immunol, 2007, 179(8):5493-503; Huang et al., Aging, 2019, 11 (24): 12532-12545), as well as the secretion of growth factors (e.g. CTGF) and extracellular components (e.g. collagen) (Lin et al., Mol. Med, 2015, 21 (1):576-83; Chung et al., J Biol Chem, 2013, 288(52):37319-31 ). It is important to note that other signalling pathways such as cyclic AMP in alveolar macrophages and Gi in hepatocytes seem important to regulate cytokine secretion and steatosis respectively (Rayees et al., Cell Rep, 2019, 27(3):793-805.e4; Rana et al., Mol Metab, 2019, 29, 99-113).

[0027] In vivo, it has clearly been shown that the inhibition of PAR-2 signaling, either pharmacologically or by genetic modification, significantly reduced the symptoms of atherosclerosis, idiopathic pulmonary fibrosis, atopic dermatitis, multiple sclerosis, arthritis, non-alcoholic steatohepatitis and inflammatory bowel disease in mouse models (Jones et al., Arterioscler Thromb Vase Biol, 2018, 38(6): 1271 -1282; Borensztajn et al., Am J Pathol, 2010, 177(6):2753-64; Moniaga et al., Am J Pathol, 2013, 182: 841e851 ; Noorbakhsh et al., J Exp Med, 2006, 203(2):425-35, Ferrell et al., J Clin Invest, 2003, 111 (1):35-41 ; Rana et al., Mol Metab, 2019, 29:99-113; Hyun et al., Gut, 2008, 57(9): 1222-9). PAR-2 therefore plays a key role in the molecular and cellular mechanisms underlying the pathogenesis of autoinfl ammatory diseases.

[0028] PAR-2-dependent inflammation can also impair cellular metabolism and promote insulin resistance which then leads to the pathogenesis of diabetes, obesity and metabolic syndrome. Indeed, PAR-2 expression in adipocyte tissues has been correlated with the increasing BMI of volunteer people and the inhibition of PAR-2 signaling attenuates the symptoms of metabolic disorders in mice (Lim et al., FASEB Journal, 2013, 27(12):4757-4767; Badeanlou et al., Nat. Med, 2011 , 17(11): 1490-1497).

[0029] Many airborne allergens from house dust mite and cockroach allergens contain protease activity. This protease activity can activate PAR-2 expressed on human airway epithelial cells, endothelial cells as well as immune cells and induce calcium signalling. This ultimately leads to the release of inflammatory cytokines and angiogenic response at the basis of the pathogenesis of cockroach allergy and allergic asthma (Do et al., Allergy, 2016, 71 (4):463-74; Asosingh et al., J Clin Invest, 2018, 128(7):3116-3128). In vivo, functional blockade of PAR-2 in the airways during allergen challenge improves allergen-induced inflammation and airway hyperresponsiveness in mice (Asaduzzaman et al., Clin Exp Allergy, 2015, 45(12): 1844-55).

[0030] The expression of PAR-2 and proteases is also significantly increased in many cancer types such as cervical squamous cell carcinoma, endocervical adenocarcinoma, colon adenocarcinoma, esophageal carcinoma, glioblastoma multiforme, acute myeloid leukemia, lung adenocarcinoma, lung squamous cell carcinoma, ovarian serous cystadenocarcinoma, pancreatic adenocarcinoma, prostate adenocarcinoma, rectum adenocarcinoma, stomach adenocarcinoma, testicular germ cell tumors, uterine corpus endometrial carcinoma, uterine carcinosarcoma, hepatocellular carcinoma, and breast cancer, which can be associated to poor prognosis (Kaufmann et al., Carcinogenesis, 2009, 30(9): 1487-96; Su et al., Oncogene, 2009, 28(34):3047-57; Arakaki et al., Int. J. Mol. Sci. 2018, 19, 1886). The activation of this receptor in cancer cells can lead to several signalling cascades such as calcium, p-arrestin and Gi signalling (Kaufmann et al., J Cancer Res Clin Oncol, 2011 , 137 (6): 965-73; Wu et al, Mol Med Rep, 2014, 10(6):3021 -6; Ge et al., J Biol Chem, 2004, 279(53):55419-24). This ultimately controls cancer cell migration, proliferation, survival, and expression of inflammatory cytokines (Jiang et al., J Pharmacol Exp Ther, 2018, 364(2):246-257; Darmoul et al., British J Cancer, 2001 , 85(5):772-9; Quan et al., Oncol Res., 2019, 27(7):779-788). The expression of PAR-2 on other cells of the tumor microenvironment, such as immune cells, fibroblasts, endothelial cells and DRG neurons, can also control the immune response to cancer cells, fibrosis, as well as angiogenesis and cancer-induced pain (Mubbach et al., Mol cancer, 2016, 15(1):54; Uusitalo-Jarvinen et al., Arieriocler Thromb Vase Biol, 2007, 27(6): 1456-62; D’Andrea et al, Am J Pathol, 2001 , 158(6):2031-41 ; Graf et al, Sci Immunol, 2019, 4(39):eaaw8405; Qian at al., Oncol Lett, 2018, 16(2): 1513-20; Tu et al, J Neurosci, 2021 , 41 (1): 193-210). In vivo, the inhibition of PAR-2 has been shown to be an efficient way of reducing tumor growth and increasing survival in mouse models of different cancers such as breast cancer, liver cancer and colon cancer (Versteeg et al., Cancer Res, 2008, 68(17)7219-27; Sun et al., World J Gastroenterol, 2018, 24(10): 1120-1133; Quan et al., Oncol Res., 2019, 27(7)779- 788). Importantly, inhibition of PAR2 or one of its ligands led to reduced infiltration of immune-supressive Tumor Associated Macrophages and regulatory T cells while increasing cytotoxic T cells in the tumor as well as increasing antigen presenting cells in the draining lymph nodes in several syngeneic mouse models; this unleashed the anti- tumoral immune response and increased the potency of immune-checkpoint inhibitors currently used in the clinic (Graf et al, Sci Immunol, 2019, 4(39):eaaw8405). PAR-2 therefore constitutes a promising therapeutic target in oncology and immune-oncology.

[0031] Considering the role of PAR-2 in several pathophysiological conditions, inhibitors of this receptor can have therapeutic applications in a wide variety of human diseases. This has drawn a great interest from pharmaceutical industry to develop such compounds. Various PAR-2 inhibitors and therapeutic uses thereof have been proposed, for example, in: Yau et al., Expert Opin Ther Pat, 2016, 26(4):471-83; Jiang et al., J Pharmacol Exp Ther, 2018, 364(2):246-57; WO 2004 / 002418; WO 2005 / 030773; WO 2012 / 012843; WO 2012 / 026765; WO 2012 / 026766; WO 2012 / 101453; WO 2015 / 048245; WO 2016 / 154075; WO 2017 / 194716; WO 2017 / 197463; WO 2018 / 043461 (EP 3508 487); WO 2018 / 057588; WO 2019 / 124567; WO 2019 / 163956 (EP 3 760 631); WO 2019 / 199800; JP 2020 / 007262; WO 2021 / 106864; WO 2022 / 117882; WO 2022 / 255408; and WO 2023 / 233033. However, despite the efforts made, no PAR-2 inhibitor has reached the market yet (Yau et al., Expert Opin Ther Pat., 2016, 26 (4): 471-83). There is therefore still an unmet need for novel and / or improved PAR-2 inhibitors with high potency, selectivity and bioavailability.

[0032] The present invention addresses this need and solves the problem of providing novel and highly potent PAR-2 inhibitors / antagonists. In particular, it has surprisingly been found that the compounds of formula (I) as provided herein are potent and selective inhibitors of PAR-2 signalling, which renders these compounds advantageous for use in therapy, including in particular in the treatment or prevention of pain, an autoimmune disorder, an autoinflammatory disorder, an inflammatory disorder, a central nervous system disorder, spinal cord injury, a metabolic disorder, a gastrointestinal disorder, a cardiovascular disorder, a fibrotic disorder, a respiratory disorder, a skin disorder, an allergic disorder, or cancer. Accordingly, the present invention provides a compound of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof.

[0033] In formula (I), the ring atom X is N or C(-R5).

[0034] R1is a group R11, and R2is a group -L2-R21; or alternatively, R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24.

[0035] R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -CO(Ci-5 alkyl).

[0036] L2is selected from a bond, C1-8 alkylene, C2-8 alkenylene, and C2-8 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups R22, and wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -CO-, -O-, -S-, -SO-, -SO2-, -NH- and -N(CI-5 alkyl)-.

[0037] R21is selected from carbocyclyl, heterocyclyl, C1-8 alkyl, and C1-8 haloalkyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23, and wherein one or more -CH2- units comprised in said alkyl or in said haloalkyl are each optionally replaced by -O-.

[0038] Each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -ON, -SF5, -OHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5 alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), - SO2-N(CI.5 alkyl)(Ci.5 alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups RCyc.

[0039] Each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci_5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-0(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups F .

[0040] Each R24is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups Rc c.

[0041] R3is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein said alkyl, said alkenyl, said alkynyl, the alkylene group in said -(C0-5 alkylene)-carbocyclyl, and the alkylene group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R31, and wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32.

[0042] Each R31is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5 alkyl), -NH-OH, -N(Ci_5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci_5alkyl), -Si(Ci.5alkyl)(Ci_5alkyl)(Ci_5alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -CHO, -C0-(Ci-5 alkyl), -COOH, -CO-O-(Ci-5 alkyl), -O-CO-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI-5alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci_5alkyl), -NH-COO(CI-5alkyl), -N(CI.5alkyl)-COO(Ci_5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups RCyc.

[0043] Each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci_5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc.

[0044] R4and R5are each independently selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups F .

[0045] RAand RBare each independently selected from hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, -(Co-8 alkylene)-OH, -(Co-8 alkylene)-O(Ci-5 alkyl), -(Co-8 alkylene)-SH, -(Co-8 alkylene)-S(Ci-5 alkyl), -(C1-8 alkylene)-NH2, -(C1-8 alkylene)-NH(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-halogen, -(C1-8 alkylene)-Ci-5 haloalkyl, -(Co-8 alkylene)-O-(Ci-8 haloalkyl), -(Co-8 alkylene)-CN, -(Co-8 alkylene)-SF5, -(Co-8 alkylene)-CHO, -(Co-8 alkylene)-CO-(Ci-5 alkyl), -(Co-8 alkylene)-COOH, -(Co-8 alkylene)-CO-O-(Ci-5 alkyl), -(Co-8 alkylene)-O-CO-(Ci-5 alkyl), -(Co-8 alkylene)-CO-NH2, -(Co-8 alkylene)-CO-NH(Ci-5 alkyl), -(Co-8 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-NH-CO-(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C1-8 alkylene)-NH-COO(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(Co-8 alkylene)-O-CO-NH(Ci-5 alkyl), -(Co-8 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(Co-8 alkylene)-SO2-NH2, -(Co-8 alkylene)-SO2-NH(Ci-5 alkyl), -(Co-8 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-NH-SO2-(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(Co-8 alkylene)-SO-(Ci-5 alkyl), -(Co-8 alkylene)-SO2-(Ci-5 alkyl), -(Co-8 alkylene)-carbocyclyl, -(Co-8 alkylene)-heterocyclyl, and -Lz-Rz, wherein one or more -CH2- units comprised in said C1-8 alkyl, said C2-8 alkenyl, said C2-8 alkynyl, and in any of the aforementioned Co-s alkylene and C1-8 alkylene groups are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-, wherein the carbocyclyl group in said -(Co-s alkylene)-carbocyclyl and the heterocyclyl group in said -(Co-s alkylene)-heterocyclyl are each optionally substituted with one or more groups R°yc, and wherein at least one of the groups RAand RBis not hydrogen; or alternatively, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc.

[0046] Each Rcis independently selected from C1.5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alky lene)-0 H, -(C0-3 alky lene)-0 (C 1-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups F .

[0047] Each R°rcis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5alkyl), -(C0-3 alkylene)-P(=O)(-OH)(-OH), -(C0-3 alkylene)-P(=O)(-OH)(-O-Ci.5alkyl), -(C0-3 alkylene)-P(=O)(-O-Ci-5 alkyl)(-O-Ci-5 alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz.

[0048] Each Lzis independently selected from a covalent bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), and -N(CI-5 alkyl)(Ci-5 alkyl), and further wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-.

[0049] Each Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -CN, -SP5, -CHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI-5alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci-5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI-5alkyl)(Ci-5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI-5 alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5 alkyl), -S0-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(CI.5 alkyl)(Ci.5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5 alkyl), -N(CI_5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), and -SO2-(Ci-5 alkyl).

[0050] For the compounds of formula (I), the following provisos apply:

[0051] If X is N, if R1is a group R11, and if R11is hydrogen, then R3is not a group -(C1-5 alkylene)-phenyl, wherein the alkylene group in said -(C1-5 alkylene)-phenyl is optionally substituted with one or more groups R31and wherein the phenyl group in said -(C1-5 alkylene)-phenyl is optionally substituted with one or more groups R32.

[0052] If X is N, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, and if RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a bicyclic fused heterocyclyl which is optionally substituted with one or more groups Rc, then the heterocyclyl formed from R1and R2is not a spirocyclic group which comprises a piperidine ring and is attached via the nitrogen ring atom of said piperidine ring.

[0053] If X is N, if one of RAand RBis hydrogen, and if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, then said heterocyclyl is not decahydroquinoxalin-1-yl or octahydro-1 H-cyclopenta[b]pyrazin-1-yl.

[0054] If X is N and if one of RAand RBis hydrogen, then R3is not phenyl which is optionally substituted with one or more groups R32.

[0055] If X is C(-R5), if one of RAand RBis hydrogen, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is piperazin-1 -yl and which is optionally substituted with one or more groups R24, then said piperazin-1 -yl is not substituted with 1 H-quinoxalin-2-on- 7-ylmethyl, wherein the 1 H-quinoxalin-2-on-7-yl group in said 1 H-quinoxalin-2-on-7-ylmethyl is optionally substituted with one or more groups RCyc.

[0056] If R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups R24, if R3is C1-8 alkyl which is optionally substituted with one or more halogen atoms, and if one of RAand RBis hydrogen, then the other one of RAand RBis not methyl.

[0057] If X is N and if R3is phenyl which is substituted with one or more halogen atoms, then R1and R2are not mutually joined to form, together with the nitrogen atom that they are attached to, a group which is pyrrolidin- 1-yl or piperidin-1-yl.

[0058] If X is N, if R11is C1-5 alkyl, and if R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said C1-8 alkyl are each optionally replaced by -O-, then R3is not a cyclic group selected from phenyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, and azepanyl, wherein said cyclic group is optionally substituted with one or more halogen atoms.

[0059] If X is N and if R21is Cvs alkyl, wherein one or more -CH2- units comprised in said C1-8 alkyl are each optionally replaced by -O-, then R3is not a heterocycloalkyl comprising one or two nitrogen ring atoms, wherein all remaining ring atoms in said heterocycloalkyl are carbon atoms, and wherein said heterocycloalkyl is substituted with one or more groups R32.

[0060] If R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is imidazol-1-yl or 1 ,2,4-triazol-1-yl and which is optionally substituted with one or more groups R24, then R3is not C1-6 alkyl or -CF3.

[0061] If X is C(-R5) and if one of RAand RBis hydrogen, then the other one of RAand RBis not -NH-carbocyclyl or -NH-heterocyclyl, wherein the carbocyclyl in said -NH-carbocyclyl and the heterocyclyl in said -NH- heterocyclyl are each optionally substituted with one or more groups Rc c.

[0062] If R1is a group R11and R11is hydrogen, then R2is not -CO-NH-(1 ,2,3,4-tetrahydronaphthalen-1-yl), -CO- NH-(3',4'-dihydro-2'H-spiro[cyclopropane-1 , 1'-naphthalene]-4'-yl), -CO-NH-(3’,4’-dihydro-2’H- spiro[cyclobutane-1 ,1'-naphthalene]-4'-yl), -CO-NH-(3,4-dihydro-2H-spiro[naphthalene-1,3'-oxetane]-4-yl), - CO-NH-(3,4-dihydro-2H-spiro[naphthalene-1 ,2'-oxetane]-4-yl) or -CO-NH-(3',4'-dihydro-2'H-spiro[azetidine- 3,1'-naphthalene]-4'-yl), wherein the 1 ,2,3,4-tetrahydronaphthalen-1-yl in said -CO-NH-(1 ,2,3,4- tetrahydronaphthalen-1-yl), the 3',4'-dihydro-2’H-spiro[cyclopropane-1 ,1’-naphthalene]-4’-yl in said -CO-NH- (3',4'-dihydro-2'H-spiro[cyclopropane-1 , 1'-naphthalene]-4'-yl), the 3',4'-dihydro-2'H-spiro[cyclobutane-1 , T- naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[cyclobutane-1 , 1'-naphthalene]-4'-yl), the 3,4- dihy d ro-2 H-spiro[naphth alene-1 , 3'-oxetane]-4-y I in said -CO-N H-(3,4-dihy d ro-2H-spi ro[naphthalene-1 , 3’- oxetane]-4-yl), the 3,4-dihydro-2H-spiro[naphthalene-1 ,2'-oxetane]-4-yl in said -CO-NH-(3,4-dihydro-2H- spiro[naphthalene-1,2'-oxetane]-4-yl) and the 3',4'-dihydro-2'H-spiro[azetidine-3, 1'-naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[azetidine-3, 1'-naphthalene]-4'-yl) are each optionally substituted with one or more groups R23.

[0063] If R1is a group R11and if R11is hydrogen, then R2is not -CO-O-CH2-CCI3, -CO-O-phenyl, -CO-O-(4- methlyphenyl), -CO-O-(imidazol-l-yl), -CO-O-(pyrrolidin-2,5-dion-1-yl).

[0064] The present invention also relates to a pharmaceutical composition comprising a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, in combination with a pharmaceutically acceptable excipient. Accordingly, the invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising any of the aforementioned entities and a pharmaceutically acceptable excipient, for use as a medicament.

[0065] The invention further relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising any of the aforementioned entities and a pharmaceutically acceptable excipient, for use in the treatment or prevention of a PAR-2 mediated disease or disorder. Thus, the invention in particular provides a pharmaceutical composition comprising, as an active ingredient, a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, together with a pharmaceutically acceptable excipient, for use in the treatment or prevention of a PAR-2 mediated disease or disorder. Moreover, the present invention relates to the use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof in the preparation of a medicament for the treatment or prevention of a PAR-2 mediated disease or disorder.

[0066] The invention likewise relates to a method of treating or preventing a PAR-2 mediated disease or disorder, the method comprising administering a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising any of the aforementioned entities in combination with a pharmaceutically acceptable excipient, to a subject (preferably a human) in need thereof. It will be understood that a therapeutically effective amount of the compound of formula (I) or the pharmaceutically acceptable salt or solvate thereof (or of the pharmaceutical composition) is to be administered in accordance with this method.

[0067] As explained above, the disease or disorder to be treated or prevented with a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof (or a corresponding pharmaceutical composition) in accordance with the present invention includes any PAR-2 mediated disease or disorder. It is preferred that the disease / disorder to be treated or prevented in accordance with the invention is pain (e.g., chronic pain), an autoimmune disorder, an autoinfl ammatory disorder, an inflammatory disorder (e.g., a rheumatologic inflammatory disorder, a skin inflammatory disorder, a lung inflammatory disorder, a muscle inflammatory disorder, a bowel inflammatory disorder, or a brain inflammatory disorder), a central nervous system disorder, spinal cord injury, a metabolic disorder, a gastrointestinal disorder, a cardiovascular disorder, a fibrotic disorder, a respiratory disorder, a skin disorder, an allergic disorder, or cancer. More preferably, the disease / disorder to be treated or prevented in accordance with the present invention is selected from neuropathic pain, inflammatory pain, cancer pain, post-operative incision pain, fracture pain, osteoporotic fracture pain, gout joint pain, chronic pain, spinal cord injury, atopic dermatitis, contact dermatitis, dry skin dermatitis, seborrhoeic dermatitis, arthritis, rheumatoid arthritis, osteoarthritis, psoriasis, psoriatic arthritis, multiple sclerosis, non-alcoholic steatohepatitis (NASH), obesity (e.g., diet-induced obesity), diabetes (e.g., type 1 diabetes or type 2 diabetes), adipose inflammation, pancreatitis, metabolic syndrome, PAR-2 associated metabolic dysfunction, periodontitis, gingivitis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, peptic ulcer disease (e.g., gastric ulcer or duodenal ulcer), infectious enteritis, irritable bowel syndrome, atherosclerosis, asthma, interstitial lung disease, pulmonary fibrosis (e.g., idiopathic pulmonary fibrosis), rheumatoid arthritis- associated interstitial lung disease, liver fibrosis, cystic fibrosis, renal fibrosis, peritoneal fibrosis, pancreatic fibrosis, intestinal fibrosis, cardiac fibrosis, skin fibrosis, systemic lupus erythematosus (SLE), scleroderma, skin eczema, acne, rosacea, post-inflammatory hyperpigmentation, lichen planus, pruritus, polymyositis, vasculitis, Wegener's granulomatosis (or granulomatosis with polyangiitis), Netherton syndrome, dermatomyositis, uveitis, liver cirrhosis, Alzheimer's disease, Parkinson's disease, dust mite allergy (e.g., house dust mite allergy), cockroach allergy, allergic asthma, colorectal cancer (e.g., colorectal carcinoma), colon cancer (e.g., colon adenocarcinoma), gastrointestinal cancer, gastric cancer (or stomach cancer; e.g., stomach adenocarcinoma), rectal cancer (e.g., rectum adenocarcinoma), anal cancer, liver cancer (e.g., hepatocellular carcinoma), breast cancer (e.g., triple-negative breast cancer, including in particular COX-2 expressing triple-negative breast cancer, or breast cancer having a BRCA1 and / or BRCA2 gene mutation), pancreatic cancer (e.g., pancreatic adenocarcinoma or pancreatic ductal adenocarcinoma), cervical cancer (e.g., cervical squamous cell carcinoma or endocervical adenocarcinoma), prostate cancer (e.g., prostate adenocarcinoma or hormone-refractory prostate cancer), ovarian cancer (e.g., ovarian carcinoma or ovarian serous cystadenocarcinoma), endometrial cancer (e.g., uterine corpus endometrial carcinoma), vaginal cancer, vulvar cancer, uterine cancer (e.g., uterine corpus cancer, uterine sarcoma, or uterine carcinosarcoma), testicular cancer, germ cell cancer (e.g., testicular germ cell cancer), esophageal cancer, laryngeal cancer, mouth cancer, hematological cancer, leukemia (e.g., acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, or chronic lymphocytic leukemia), lymphoma (e.g., Hodgkin lymphoma or non-Hodgkin lymphoma, such as, e.g., follicular lymphoma, diffuse large B-cell lymphoma, or lymphoid neoplasm diffuse large B- cell lymphoma), multiple myeloma, lung cancer (e.g., non-small cell lung cancer (including, e.g., lung adenocarcinoma or lung squamous cell carcinoma), small cell lung cancer, large cell lung carcinoma, lung carcinoid tumor, adenoid cystic carcinoma of the lung, pulmonary lymphoma, or pulmonary sarcoma), adrenal gland cancer (e.g., adrenocortical carcinoma), biliary tract cancer, bile duct cancer (e.g., cholangiocarcinoma), hepatobiliary cancer, genitourinary cancer, urothelial cancer (e.g., urothelial carcinoma), bladder cancer (e.g., bladder urothelial carcinoma), gallbladder cancer (e.g., gallbladder carcinoma), head and / or neck cancer (e.g., head and neck cancer, or head and neck squamous cell carcinoma), kidney cancer (e.g., kidney chromophobe, kidney renal cell carcinoma, kidney renal clear cell carcinoma, or kidney renal papillary cell carcinoma), mesothelioma, sarcoma, skin cancer, melanoma (e.g., skin cutaneous melanoma, or uveal melanoma), Merkel-cell cancer (e.g., Merkel-cell carcinoma), epidermoid cancer, thyroid cancer (e.g., papillary thyroid cancer, follicular thyroid cancer, medullary thyroid cancer, anaplastic thyroid cancer, or thyroid carcinoma), thymus cancer (or thymic cancer; e.g., thymoma), squamous cell cancer (or squamous cell carcinoma; including, e.g., oral squamous cell carcinoma / squamous-cell mouth carcinoma, squamous-cell skin cancer, squamous-cell lung carcinoma, squamous-cell thyroid carcinoma, squamous-cell esophageal carcinoma, or squamous-cell vaginal carcinoma), goblet cell cancer (e.g., goblet cell carcinoid), spleen cancer, bone cancer (e.g., osteosarcoma or osteogenic sarcoma), fibrosarcoma, Ewing's sarcoma, Kaposi's sarcoma, neuroendocrine cancer (e.g., neuroendocrine carcinoma), neuroblastoma, or brain cancer (e.g., glioblastoma). The cancer to be treated may further be a carcinoma or a sarcoma. The cancer to be treated or prevented (including any one of the aforementioned specific types of cancer) may also be a relapsed or refractory cancer. Moreover, the cancer to be treated or prevented (including any one of the aforementioned specific types of cancer) may also be a metastatic cancer.

[0068] The treatment can be used as first, second or third line therapy against cancer. When used as first line therapy in resectable solid tumors, it can be administered in a neoadjuvant or adjuvant setting or both.

[0069] As explained above, the cancer to be treated in accordance with the present invention may also be a hematological cancer (e.g., a lymphoma or a leukemia). Thus, for example, the hematological cancer may be selected from: Hodgkin's lymphoma, including, e.g., nodular sclerosing subtype of Hodgkin's lymphoma, mixed-cellularity subtype of Hodgkin's lymphoma, lymphocyte-rich subtype of Hodgkin's lymphoma, or lymphocyte-depleted subtype of Hodgkin's lymphoma; non-Hodgkin's lymphoma, including, e.g., follicular non-Hodgkin's lymphoma, mantle cell lymphoma, or diffuse non-Hodgkin's lymphoma (e.g., diffuse large B-cell lymphoma or Burkitt's lymphoma); nodular lymphocyte predominant Hodgkin's lymphoma; peripheral / cutaneous T-cell lymphoma, including, e.g., mycosis fungoides, Sezary syndrome, T-zone lymphoma, lymphoepithelioid lymphoma (e.g., Lennert's lymphoma), or peripheral T-cell lymphoma; lymphosarcoma; a malignant immunoproliferative disorder, including, e.g., Waldenstrom's macroglobulinemia, alpha heavy chain disease, gamma heavy chain disease (e.g., Franklin's disease), or an immunoproliferative small intestinal disease (e.g., Mediterranean disease); multiple myeloma, including, e.g., Kahler's disease, or myelomatosis; plasma cell leukemia; lymphoid leukemia, including, e.g., acute lymphoblastic leukemia, chronic lymphocytic leukemia, subacute lymphocytic leukemia, prolymphocytic leukemia, hairy-cell leukemia (e.g., leukemic reticuloendotheliosis), or adult T-cell leukemia; myeloid leukemia, including, e.g., acute myeloid leukemia, chronic myeloid leukemia, subacute myeloid leukemia, myeloid sarcoma (e.g., chloroma, or granulocytic sarcoma), acute promyelocytic leukemia, or acute myelomonocytic leukemia; a myeloproliferative neoplastic disorder, including, e.g., polycythemia vera, essential thrombocythemia, or idiopathic myelofibrosis; monocytic leukemia; acute erythraemia or erythroleukemia, including, e.g., acute erythraemic myelosis, or Di Guglielmo's disease; chronic erythraemia, including, e.g., Heilmeyer-Schdner disease; acute megakaryoblastic leukemia; mast cell leukemia; acute panmyelosis; acute myelofibrosis; and Letterer-Siwe disease.

[0070] In particular, the disease / disorder to be treated or prevented in accordance with the present invention may be selected from neuropathic pain, inflammatory pain, cancer pain, post-operative incision pain, fracture pain, osteoporotic fracture pain, gout joint pain, chronic pain, spinal cord injury, atopic dermatitis, contact dermatitis, dry skin dermatitis, seborrhoeic dermatitis, arthritis, rheumatoid arthritis, osteoarthritis, psoriasis, psoriatic arthritis, multiple sclerosis, non-alcoholic steatohepatitis (NASH), obesity (e.g., diet-induced obesity), diabetes (e.g., type 1 diabetes or type 2 diabetes), adipose inflammation, pancreatitis, metabolic syndrome, PAR-2 associated metabolic dysfunction, periodontitis, gingivitis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, peptic ulcer disease (e.g., gastric ulcer or duodenal ulcer), infectious enteritis, irritable bowel syndrome, atherosclerosis, asthma, interstitial lung disease, pulmonary fibrosis (e.g., idiopathic pulmonary fibrosis), rheumatoid arthritis-associated interstitial lung disease, liver fibrosis, cystic fibrosis, renal fibrosis, peritoneal fibrosis, pancreatic fibrosis, intestinal fibrosis, cardiac fibrosis, skin fibrosis, systemic lupus erythematosus (SLE), scleroderma, skin eczema, acne, rosacea, post- inflammatory hyperpigmentation, lichen planus, pruritus, polymyositis, vasculitis, Wegener's granulomatosis (or granulomatosis with polyangiitis), Netherton syndrome, dermatomyositis, uveitis, liver cirrhosis, Alzheimer's disease, Parkinson's disease, dust mite allergy (e.g., house dust mite allergy), cockroach allergy, allergic asthma, colorectal cancer, colon cancer (e.g., colon adenocarcinoma), gastric cancer (e.g., stomach adenocarcinoma), rectal cancer (e.g., rectum adenocarcinoma), liver cancer (e.g., hepatocellular carcinoma), breast cancer, pancreatic cancer (e.g., pancreatic adenocarcinoma or pancreatic ductal adenocarcinoma), cervical cancer (e.g., cervical squamous cell carcinoma or endocervical adenocarcinoma), prostate cancer (e.g., prostate adenocarcinoma), ovarian cancer (e.g., ovarian serous cystadenocarcinoma), endometrial cancer (e.g., uterine corpus endometrial carcinoma), uterine sarcoma (e.g., uterine carcinosarcoma), germ cell cancer (e.g., testicular germ cell cancer), esophageal cancer, leukemia (e.g., acute myeloid leukemia), lung cancer (e.g., non-small cell lung cancer (including, e.g., lung adenocarcinoma or lung squamous cell carcinoma), small cell lung cancer, large cell lung carcinoma, lung carcinoid tumor, adenoid cystic carcinoma of the lung, pulmonary lymphoma, or pulmonary sarcoma), adrenal gland cancer (e.g., adrenocortical carcinoma), bile duct cancer (e.g., cholangiocarcinoma), bladder cancer (e.g., bladder urothelial carcinoma), head and neck cancer, kidney cancer (e.g., kidney chromophobe, kidney renal cell carcinoma, kidney renal clear cell carcinoma, or kidney renal papillary cell carcinoma), lymphoma (e.g., lymphoid neoplasm diffuse large B-cell lymphoma), mesothelioma, sarcoma, melanoma (e.g., skin cutaneous melanoma, or uveal melanoma), thyroid carcinoma, thymus cancer (e.g., thymoma), or glioblastoma.

[0071] Accordingly, the present invention particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising any of the aforementioned entities and a pharmaceutically acceptable excipient, for use in the treatment or prevention of neuropathic pain, inflammatory pain, cancer pain, post-operative incision pain, fracture pain, osteoporotic fracture pain, gout joint pain, chronic pain, spinal cord injury, atopic dermatitis, contact dermatitis, dry skin dermatitis, seborrhoeic dermatitis, arthritis, rheumatoid arthritis, osteoarthritis, psoriasis, psoriatic arthritis, multiple sclerosis, non-alcoholic steatohepatitis (NASH), obesity (e.g., diet-induced obesity), diabetes (e.g., type 1 diabetes or type 2 diabetes), adipose inflammation, pancreatitis, metabolic syndrome, PAR-2 associated metabolic dysfunction, periodontitis, gingivitis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, peptic ulcer disease (e.g., gastric ulcer or duodenal ulcer), infectious enteritis, irritable bowel syndrome, atherosclerosis, asthma, interstitial lung disease, pulmonary fibrosis (e.g., idiopathic pulmonary fibrosis), rheumatoid arthritis-associated interstitial lung disease, liver fibrosis, cystic fibrosis, renal fibrosis, peritoneal fibrosis, pancreatic fibrosis, intestinal fibrosis, cardiac fibrosis, skin fibrosis, systemic lupus erythematosus (SLE), scleroderma, skin eczema, acne, rosacea, post-inflammatory hyperpigmentation, lichen planus, pruritus, polymyositis, vasculitis, Wegener's granulomatosis (or granulomatosis with polyangiitis), Netherton syndrome, dermatomyositis, uveitis, liver cirrhosis, Alzheimer's disease, Parkinson's disease, dust mite allergy (e.g., house dust mite allergy), cockroach allergy, allergic asthma, colorectal cancer (e.g., colorectal carcinoma), colon cancer (e.g., colon adenocarcinoma), gastrointestinal cancer, gastric cancer (or stomach cancer; e.g., stomach adenocarcinoma), rectal cancer (e.g., rectum adenocarcinoma), anal cancer, liver cancer (e.g., hepatocellular carcinoma), breast cancer (e.g., triple-negative breast cancer, including in particular COX-2 expressing triple-negative breast cancer, or breast cancer having a BRCA1 and / or BRCA2 gene mutation), pancreatic cancer (e.g., pancreatic adenocarcinoma or pancreatic ductal adenocarcinoma), cervical cancer (e.g., cervical squamous cell carcinoma or endocervical adenocarcinoma), prostate cancer (e.g., prostate adenocarcinoma or hormone-refractory prostate cancer), ovarian cancer (e.g., ovarian carcinoma or ovarian serous cystadenocarcinoma), endometrial cancer (e.g., uterine corpus endometrial carcinoma), vaginal cancer, vulvar cancer, uterine cancer (e.g., uterine corpus cancer, uterine sarcoma, or uterine carcinosarcoma), testicular cancer, germ cell cancer (e.g., testicular germ cell cancer), esophageal cancer, laryngeal cancer, mouth cancer, hematological cancer, leukemia (e.g., acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, or chronic lymphocytic leukemia), lymphoma (e.g., Hodgkin lymphoma or nonHodgkin lymphoma, such as, e.g., follicular lymphoma, diffuse large B-cell lymphoma, or lymphoid neoplasm diffuse large B-cell lymphoma), multiple myeloma, lung cancer (e.g., non-small cell lung cancer (including, e.g., lung adenocarcinoma or lung squamous cell carcinoma), small cell lung cancer, large cell lung carcinoma, lung carcinoid tumor, adenoid cystic carcinoma of the lung, pulmonary lymphoma, or pulmonary sarcoma), adrenal gland cancer (e.g., adrenocortical carcinoma), biliary tract cancer, bile duct cancer (e.g., cholangiocarcinoma), hepatobiliary cancer, genitourinary cancer, urothelial cancer (e.g., urothelial carcinoma), bladder cancer (e.g., bladder urothelial carcinoma), gallbladder cancer (e.g., gallbladder carcinoma), head and / or neck cancer (e.g., head and neck cancer, or head and neck squamous cell carcinoma), kidney cancer (e.g., kidney chromophobe, kidney renal cell carcinoma, kidney renal clear cell carcinoma, or kidney renal papillary cell carcinoma), mesothelioma, sarcoma, skin cancer, melanoma (e.g., skin cutaneous melanoma, or uveal melanoma), Merkel-cell cancer (e.g., Merkel-cell carcinoma), epidermoid cancer, thyroid cancer (e.g., papillary thyroid cancer, follicular thyroid cancer, medullary thyroid cancer, anaplastic thyroid cancer, or thyroid carcinoma), thymus cancer (or thymic cancer; e.g., thymoma), squamous cell cancer (or squamous cell carcinoma; including, e.g., oral squamous cell carcinoma / squamous-cell mouth carcinoma, squamous-cell skin cancer, squamous-cell lung carcinoma, squamous-cell thyroid carcinoma, squamous-cell esophageal carcinoma, or squamous-cell vaginal carcinoma), goblet cell cancer (e.g., goblet cell carcinoid), spleen cancer, bone cancer (e.g., osteosarcoma or osteogenic sarcoma), fibrosarcoma, Ewing's sarcoma, Kaposi's sarcoma, neuroendocrine cancer (e.g., neuroendocrine carcinoma), neuroblastoma, or brain cancer (e.g., glioblastoma).

[0072] The present invention further relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising any of the aforementioned entities and a pharmaceutically acceptable excipient, for use in the treatment or prevention of neuropathic pain, inflammatory pain, cancer pain, postoperative incision pain, fracture pain, osteoporotic fracture pain, gout joint pain, chronic pain, spinal cord injury, atopic dermatitis, contact dermatitis, dry skin dermatitis, seborrhoeic dermatitis, arthritis, rheumatoid arthritis, osteoarthritis, psoriasis, psoriatic arthritis, multiple sclerosis, non-alcoholic steatohepatitis (NASH), obesity (e.g., diet-induced obesity), diabetes, adipose inflammation, pancreatitis, metabolic syndrome, PAR-2 associated metabolic dysfunction, periodontitis, gingivitis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, peptic ulcer disease (e.g., gastric ulcer or duodenal ulcer), infectious enteritis, irritable bowel syndrome, atherosclerosis, asthma, interstitial lung disease, pulmonary fibrosis (e.g., idiopathic pulmonary fibrosis), rheumatoid arthritis-associated interstitial lung disease, liver fibrosis, cystic fibrosis, renal fibrosis, peritoneal fibrosis, pancreatic fibrosis, intestinal fibrosis, cardiac fibrosis, skin fibrosis, systemic lupus erythematosus (SLE), scleroderma, skin eczema, acne, rosacea, post- inflammatory hyperpigmentation, lichen planus, pruritus, polymyositis, vasculitis, Wegener's granulomatosis (or granulomatosis with polyangiitis), Netherton syndrome, dermatomyositis, uveitis, liver cirrhosis, Alzheimer's disease, Parkinson's disease, dust mite allergy (e.g., house dust mite allergy), cockroach allergy, allergic asthma, or cancer (e.g., colorectal cancer, colon cancer (e.g., colon adenocarcinoma), gastric cancer (e.g., stomach adenocarcinoma), rectal cancer (e.g., rectum adenocarcinoma), liver cancer (e.g., hepatocellular carcinoma), breast cancer, pancreatic cancer (e.g., pancreatic adenocarcinoma or pancreatic ductal adenocarcinoma), cervical cancer (e.g., cervical squamous cell carcinoma or endocervical adenocarcinoma), prostate cancer (e.g., prostate adenocarcinoma), ovarian cancer (e.g., ovarian serous cystadenocarcinoma), endometrial cancer (e.g., uterine corpus endometrial carcinoma), uterine sarcoma (e.g., uterine carcinosarcoma), germ cell cancer (e.g., testicular germ cell cancer), esophageal cancer, leukemia (e.g., acute myeloid leukemia), lung cancer (e.g., lung adenocarcinoma or lung squamous cell carcinoma), adrenal gland cancer (e.g., adrenocortical carcinoma), bile duct cancer (e.g., cholangio carcinoma), bladder cancer (e.g., bladder urothelial carcinoma), head and neck cancer, kidney cancer (e.g., kidney chromophobe, kidney renal cell carcinoma, kidney renal clear cell carcinoma, or kidney renal papillary cell carcinoma), lymphoma (e.g., lymphoid neoplasm diffuse large B-cell lymphoma), mesothelioma, sarcoma, melanoma (e.g., skin cutaneous melanoma, or uveal melanoma), thyroid carcinoma, thymus cancer (e.g., thymoma), or glioblastoma.

[0073] The present invention also relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein said compound is conjugated via a linker to a membrane anchor. The corresponding conjugate can be employed in place of the compound of formula (I) for any use or purpose described in the present specification, e.g., for use in the treatment or prevention of a PAR-2 mediated disease or disorder, including any of the diseases / disorders mentioned herein above. Such conjugates are advantageous in that they allow to tether the conjugated compound of formula (I) to a cell membrane in the proximity of PAR-2 and, thus, to facilitate its interaction with PAR-2. The membrane anchor may be any moiety that is capable of inserting / partitioning into a lipid membrane (preferably a cell membrane), particularly a hydrophobic moiety or a lipid moiety; the conjugated compound of formula (I) is thereby "anchored” to the corresponding lipid membrane. For example, the membrane anchor may be a C12-20 alkanoyl group (e.g., a hexadecanoyl group, -CO-(CH2)i4-CH3), cholesterol, cholestanol, a sphingolipid, or glycophosphatidylinositol (GPI). The membrane anchor may also be, e.g., a moiety of formula (II), (III), (VI), (VII), (VIII), (IX), (X), (XI), (XII), (XIII), (XIV) or (XV) as described and defined in WO 2017 / 197463, particularly on pages 10 to 15 of WO 2017 / 197463 which is incorporated herein by reference. The membrane anchor may further be, e.g., a raftophile A or A', or a moiety of any one of the formulae 2, 200a to 200m, 3, 300a to 300g, 4a, 400aa to 400ap, 4b, 400ba, 5a, 500aa to 500ae, 5b, 500ba, 6, 600, 7, 700, 700a to 700c, 8a, 800a, 8b, 9, 900, 10, 1000, 11 , 1100a, 1100b, 12, 1200a, 1200b, 13a, 1300aa to 1300ac, 13b, 1300b, 14a, 1400aa to 1400ae, 14b, 1400b, 14c, 15, 1500a, 16, 1600a, 18a, 1800a to 1800d, 18b, 19a, 1900a, 19b or 1900b, as described and defined in WO 2005 / 097199 which is incorporated herein by reference.

[0074] The linker is covalently bound to the membrane anchor and to the compound of formula (I) (or the pharmaceutically acceptable salt or solvate thereof). While the linker is not particularly limited, it preferably has a length of about 1 nm to about 50 nm, and / or it preferably provides a distance of at least 8 atoms between the compound of formula (I) and the membrane anchor. For example, the linker may comprise (or consist of) one or more polyethylene glycol (PEG) units, or may comprise (or consist of) a peptide (which may be composed of, e.g., 2 to 200 amino acid residues). The linker may also be, e.g., a moiety of formula (IV), (XX), (XXI) or (XXII) as described and defined in WO 2017 / 197463, particularly on pages 15 to 18 of WO 2017 / 197463 which is incorporated herein by reference. The linker may further be, e.g., a linker B or B', or a moiety of any one of the formulae 20, 2000, 2001 , 21 , 2100, 2101 , 22, 23, 28 or 28a, as described and defined in WO 2005 / 097199 which is incorporated herein by reference. It will be understood that the linker may be attached to the membrane anchor via any suitable chemical linkage, e.g. via an amide linkage or via an ester linkage. Likewise, the linker may be attached to the compound of formula (I) (or the pharmaceutically acceptable salt or solvate thereof) via any suitable chemical linkage, e.g. via an amide linkage or via an ester linkage. While the linker may be attached at any position (or to any functional group) of the compound of formula (I) or the pharmaceutically acceptable salt or solvate thereof, it is preferred that the linker is attached to the moiety -N(-RA)-RB, particularly to one of the groups RAor RB, to the heterocyclyl formed from RAor RB, or to a substituent Rc.

[0075] Moreover, the linker and the membrane anchor may together form, e.g., any one of the moieties described to be attached to a PAR-2 inhibitor in WO 2017 / 197463 (which is incorporated herein by reference), or to a PAR-2 modulating compound in WO 2017 / 173347 (which is incorporated herein by reference), or to a pharmacophore in WO 2005 / 097199 (which is incorporated herein by reference). Suitable protocols for the preparation of corresponding linkers and membrane anchors are also described in these documents.

[0076] In particular, the invention provides a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein said compound is conjugated via a linker to a membrane anchor, wherein the membrane anchor is a C12-20 alkanoyl group (e.g., a hexadecanoyl group, -CO-(CH2)i4-CH3). A corresponding exemplary conjugate may be prepared, e.g., by coupling a compound of formula (I) having a carboxylic acid group (wherein said a carboxylic acid group preferably forms part of the moiety -N(-RA)-RB), or a pharmaceutically acceptable salt or solvate thereof, with the compound N-(1-amino-26-methyl-12,25-dioxo- 3,6,9,16, 19,22-hexaoxa-13,26-diazaoctacosan-28-yl)-N-methylpalmitamide (e.g., analogously as described in Example 227 of WO 2022 / 117882 or in Example 261 of WO 2023 / 233033, both of which are incorporated herein by reference). The present invention thus provides a compound of formula (I) having a carboxylic acid group (preferably a carboxylic acid group which forms part of the moiety -N(-RA)-RB) (including, e.g., any one of the specific compounds of formula (I) having a carboxylic acid group which are described in the examples section herein below), or a pharmaceutically acceptable salt or solvate thereof, wherein the carboxylic acid group (-COOH) is replaced by the following group:

[0077] The present invention furthermore relates to the use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof as an inhibitor of protease-activated receptor 2 (PAR-2) in research, particularly as a research tool compound for inhibiting PAR-2. Accordingly, the invention refers to the in vitro use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof as a PAR-2 inhibitor and, in particular, to the in vitro use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof as a research tool compound acting as a PAR-2 inhibitor. The invention likewise relates to a method, particularly an in vitro method, of inhibiting PAR-2, the method comprising the application of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof. The invention further relates to a method of inhibiting PAR-2, the method comprising applying a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof to a test sample (e.g., a biological sample) or a test animal (i.e., a non-human test animal). The invention also refers to a method, particularly an in vitro method, of inhibiting PAR-2 in a sample (e.g., a biological sample), the method comprising applying a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof to said sample. The present invention further provides a method of inhibiting PAR-2, the method comprising contacting a test sample (e.g., a biological sample) or a test animal (i.e., a non-human test animal) with a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof. The terms "sample”, "test sample” and "biological sample” include, without being limited thereto: a cell, a cell culture or a cellular or subcellular extract; biopsied material obtained from an animal (e.g., a human), or an extract thereof; or blood, serum, plasma, saliva, urine, feces, or any other body fluid, or an extract thereof. It is to be understood that the term “in vitro" is used in this specific context in the sense of "outside a living human or animal body”, which includes, in particular, experiments performed with cells, cellular or subcellular extracts, and / or biological molecules in an artificial environment such as an aqueous solution or a culture medium which may be provided, e.g., in a flask, a test tube, a Petri dish, a microtiter plate, etc.

[0078] The compounds of formula (I) as well as the pharmaceutically acceptable salts and solvates thereof will be described in more detail in the following.

[0079] In formula (I), the ring atom X is N or C(-R5).

[0080] Preferably, X is N.

[0081] R1is a group R11, and R2is a group -L2-R21; or alternatively, R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more (e.g., one, two, or three) groups R24.

[0082] Preferably, R1is a group R11, and R2is a group -L2-R21.

[0083] R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -CO(Ci-5 alkyl).

[0084] Preferably, R11is selected from hydrogen, C1-5 alkyl, and C1-5 haloalkyl (e.g., -CF3).

[0085] More preferably, R11is hydrogen or C1-5 alkyl (e.g., methyl or ethyl).

[0086] Even more preferably, R11is hydrogen.

[0087] L2is selected from a bond, C1-8 alkylene, C2-8 alkenylene, and C2-8 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more (e.g., one, two, or three) groups R22, and wherein one or more (e.g., one, two, or three) -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -CO-, -O-, -S-, -SO-, -SO2-, -NH- and -N(CI-5 alkyl)-

[0088] Preferably, L2is a bond or C1-8 alkylene, wherein said alkylene is optionally substituted with one or more groups R22, and wherein one or more -CH2- units comprised in said alkylene are each optionally replaced by a group independently selected from -CO-, -O-, -S-, -SO-, -SO2-, -NH- and -N(CI-5 alkyl)-. Corresponding preferred examples of L2include a bond, -CH2-, -CH(CI-5 alkyl)- (e.g., -CH(-CH3)-), -C(Ci-3 alkyl)(Ci-3 alkyl)-, -COO-(Co-5 alkylene)- (which is preferably attached to R21via the C0-5 alkylene group in said -COO-(Co-5 alkylene)-) (e.g., -COO- which is attached to R21via the -0- in said -COO-; or -COO-CH2- which is preferably attached to R21via the -CH2- group in said -COO- CH2-), or -CO-(Co-5 alkylene)- (which is preferably attached to R21via the C0-5 alkylene group in said -CO-(Co-5 alkylene)-) (e.g., -CO-, or -CO-CH2- which is preferably attached to R21via the -CH2- group in said -CO-CH2-). More preferably, L2is a bond or C1-5 alkylene, wherein said alkylene is optionally substituted with one or more (e.g., one or two) groups R22, and wherein one or more (e.g., one or two) -CH2- units comprised in said alkylene are each optionally replaced by a group independently selected from -CO-, -O-, -S-, -SO-, -SO2-, -NH- and -N(CI-5 alkyl)-. Even more preferably, L2is a bond or C1-5 alkylene (e.g., -CH2-).

[0089] Yet even more preferably, L2is a bond or -CH2-.

[0090] R21is selected from carbocyclyl, heterocyclyl, C1-8 alkyl, and C1-8 haloalkyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more (e.g., one, two, three, or four) groups R23, and wherein one or more (e.g., one or two) -CH2- units comprised in said alkyl or in said haloalkyl are each optionally replaced by -O-.

[0091] Preferably, R21is selected from carbocyclyl, heterocyclyl, and C1-8 alkyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more (e.g., one, two, three, or four) groups R23, and wherein one or more (e.g., one or two) -CH2- units comprised in said alkyl are each optionally replaced by -O-.

[0092] More preferably, R21is selected from carbocyclyl, heterocyclyl, C1-8 alkyl, and -(Ci.palkylene)-O-(Ci-qalkyl), wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23, wherein p and q are each independently an integer from 2 to 5 (I ,e. , 2, 3, 4 or 5), and wherein the sum of p and q is 7. Said carbocyclyl may be, e.g., an aryl, a cycloalkyl or a cycloalkenyl. Said heterocyclyl may be, e.g., a heteroaryl, a heterocycloalkyl or a heterocycloalkenyl. Said C1-8 alkyl may be, e.g., ethyl, n-butyl, isobutyl, neopentyl, isopentyl, or 3,3-dimethylbutyl. Said -(Ci-Palkylene)-O-(Ci-qalkyl) may be, e.g., -(C1-2 alkylene)-O-(Ci-5 alkyl), -(C1-4 alkylene)-O-(Ci-3 alkyl), or -(C1-5 alkylene)-O-(Ci.2 alkyl), such as e.g. -(CH2)3-O-CH3or -CH2CH(-CH3)-O-CH3.

[0093] Even more preferably, R21is selected from carbocyclyl, heterocyclyl, C1-8 alkyl, and -(C1-4 alkylene)-O-(Ci-4 alkyl), wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23.

[0094] Even more preferably, R21is selected from carbocyclyl, heterocyclyl, and C1-8 alkyl (e.g., isobutyl or isopentyl), wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23.

[0095] Even more preferably, R21is selected from carbocyclyl and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23.

[0096] Yet even more preferably, R21is selected from aryl, cycloalkyl, heteroaryl, and heterocycloalkyl, wherein each of the aforementioned groups is optionally substituted with one or more groups R23.

[0097] If R21is cycloalkyl which is optionally substituted with one or more groups R23, corresponding preferred examples of said cycloalkyl include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or bicyclo[1.1.1]pentanyl (e.g., bicyclo[1 .1 .1]pentan-1-yl), particularly cyclopentyl or cyclohexyl.

[0098] If R21is heterocycloalkyl which is optionally substituted with one or more groups R23, corresponding preferred examples of said heterocycloalkyl include tetrahydrofuranyl (e.g., tetrahydrofuran-3-yl), tetrahydropyranyl (e.g., tetrahydropyran-4-yl), pyrrolidinyl (e.g., pyrrolidin-1-yl), oxopyrrolidinyl (e.g., 2-oxopyrrolidin-1-yl), piperidinyl (e.g., piperidin-1-yl or piperidin-4-yl), morpholinyl (e.g., morpholin-4-yl), or 1 ,4-dioxanyl (e.g., 1 ,4-dioxan-2-yl).

[0099] If R21is aryl which is optionally substituted with one or more groups R23, corresponding preferred examples of said aryl include phenyl, naphthyl (e.g., naphthalen-1-yl or naphthalen-2-yl) or 2,3-dihydro-1 H-indenyl (e.g., 2,3-dihydro- 1 H-inden-1-yl or 2,3-dihydro-1 H-inden-2-yl), particularly phenyl. If R21is heteroaryl which is optionally substituted with one or more groups R23, corresponding preferred examples of said heteroaryl include a monocyclic 5- or 6-membered heteroaryl or a bicyclic 9- or 10-membered heteroaryl, particularly pyrrolyl (e.g., 1 H-pyrrol-1-yl, 1 H-pyrrol-2-yl.or 1 H-pyrrol-3-yl), pyrazolyl (e.g., pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, or pyrazol-5-yl), imidazolyl (e.g., imidazol-1-yl, imidazol-2-yl, or imidazol-4-yl), triazolyl (e.g., 1 H-1,2,3- triazolyl, 2H-1 ,2,3-triazolyl, 1 H-1 ,2,4-triazolyl, or 4H-1 ,2,4-triazolyl; such as, e.g., 1 H-1,2,3-triazol-1-yl, 1 H-1 ,2,3- triazol-4-yl, 1 H-1,2,3-triazol-5-yl, 1 H-1,2,4-triazol-1-yl, 1 H-1,2,4-triazol-3-yl, or 1 H-1,2,4-triazol-5-yl), furanyl (e.g., furan-2-yl or furan-3-yl), thiophenyl (e.g., thiophen-2-yl or thiophen-3-yl), oxazolyl (e.g., oxazol-2-yl, oxazol-4-yl, or oxazol-5-yl), isoxazolyl (e.g., isoxazol-3-yl, isoxazol-4-yl, or isoxazol-5-yl), thiazolyl (e.g., thiazol-2-yl), isothiazolyl, pyridinyl (e.g., pyridin-2-yl, pyridin-3-yl, or pyridin-4-yl), pyridazinyl, pyrimidinyl, pyrazinyl (e.g., pyrazin-2-yl), 1 H- indolyl, 2H-isoindolyl, indolizinyl (e.g., indolizin-1-yl or indolizin-2-yl), 1 H-indazolyl, benzimidazolyl, benzofuranyl (e.g., benzofuran-2-yl, benzofuran-3-yl, benzofuran-4-yl, benzofuran-5-yl, benzofuran-6-yl, or benzofuran-7-yl), isobenzofuranyl, benzo[b]thiophenyl (e.g., benzo[b]thiophen-2-yl, benzo[b]thiophen-3-yl, benzo[b]thiophen-4-yl, benzo[b]thiophen-5-yl, benzo[b]thiophen-6-yl, or benzo[b]thiophen-7-yl), benzo[c]thiophenyl, quinolinyl, isoquinolinyl, quinoxalinyl, phthalazinyl, quinazolinyl, cinnolinyl, 2,3-dihydrobenzofuranyl (e.g., 2,3-dihydrobenzofuran-2-yl, 2,3- dihydrobenzofuran-3-yl, 2,3-dihydrobenzofuran-4-yl, 2,3-dihydrobenzofuran-5-yl, 2,3-dihydrobenzofuran-6-yl, or 2,3- dihydrobenzofuran-7-yl), 1 ,3-dihydroisobenzofuranyl (e.g., 1 ,3-dihydroisobenzofuran-1-yl, 1 ,3-dihydroisobenzofuran- 4-yl, or 1 ,3-dihydroisobenzofuran-5-yl), chromanyl (e.g., chroman-2-yl, chroman-3-yl, or chroman-4-yl), or 2,3- dihydrobenzo[b][1 ,4]dioxinyl (e.g., 2,3-dihydrobenzo[b][1 ,4]dioxin-2-yl).

[0100] It is particularly preferred that R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl, preferably cyclopentyl) or phenyl, wherein said cycloalkyl or said phenyl is optionally substituted with one or more (e.g., one, two, or three) groups R23.

[0101] In accordance with the above definitions of L2and R21, it is particularly preferred that R2is -CFh-cyclopentyl, -CH2- cyclohexyl, or phenyl, wherein the cyclopentyl in said -CFh-cyclopentyl, the cyclohexyl in said -CF -cyclohexyl, and said phenyl are each optionally substituted with one or more (e.g., one, two, or three) groups R23. Even more preferably, R2is -CFh-cyclopentyl, -CH2-cyclohexyl, or phenyl, wherein said phenyl is optionally substituted with one or more (e.g., one, two, or three) groups R23. If said phenyl is optionally substituted with one group R23, it is preferred that said group R23is attached in meta or para position on the phenyl (preferably in para position), i.e. , that R2is 3- R23-phenyl or 4-R23-phenyl (preferably 4-R23-phenyl). If said phenyl is optionally substituted with two groups R23, it is preferred that the two groups R23are attached in meta and para position, i.e., that R2is 3-R23-4-R23-phenyl. If said phenyl is optionally substituted with three groups R23, it is preferred that two of the three groups R23are attached in meta position and one group R23is attached in para position, i.e., that R2is 3-R23-4-R23-5-R23-phenyl. It is furthermore preferred that said phenyl is substituted with two or three (particularly with two) groups R23.

[0102] As explained above, R2may be phenyl which is optionally substituted with one or more groups R23. In this case, it is particularly preferred that R2is 3-R23-4-R23-phenyl or 3-R23-4-R23-5-R23-phenyl, wherein each R23is independently selected from halogen (e.g., -F, -Cl, -Br, or -I), C1-5 haloalkyl (e.g., -CF3), -SF5, and C1-5 alkyl (e.g., -CH3), even more preferably wherein each R23is independently selected from -F, -Cl, -CF3, and -CH3. Corresponding preferred examples of R2include 4-chloro-3-fluoro-phenyl, 3,4-dichloro-phenyl, 3,4-difluoro-phenyl, 3-chloro-4-fluoro-phenyl, 3- fluoro-4-trifluoromethyl-phenyl, 3-chloro-4-trifluoromethyl-phenyl, 3-fluoro-4-methyl-phenyl, 3-chloro-4-methyl- phenyl, 3,4,5-trifluoro-phenyl, or 4-chloro-3,5-difluoro-phenyl. Corresponding particularly preferred examples of R2are 4-chloro-3-fluoro-phenyl or 3,4-difluoro-phenyl. Yet even more preferably, R2is -CH2-cyclopentyl or -CH2-cyclohexyl. Still more preferably, R2is -CF cyclopentyl. Further examples of R2include any of the specific groups R2comprised in the compounds of formula (I) described in the examples section herein below.

[0103] As explained above, R1and R2may also be mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24. It will be understood that said heterocyclyl contains at least one nitrogen ring atom, namely the nitrogen atom that carries R1and R2, and that the heterocyclyl is attached to the remainder of the compound of formula (I) via this nitrogen ring atom.

[0104] If R1and R2are mutually joined (as described above), it is preferred that the heterocyclyl formed from R1and R2is a monocyclic heterocycloalkyl, a bicyclic heterocycloalkyl, or a bicyclic heteroaryl, wherein said monocyclic heterocycloalkyl, said bicyclic heterocycloalkyl and said bicyclic heteroaryl are each optionally substituted with one or more groups R24. Accordingly, in that case, it is preferred that R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a monocyclic heterocycloalkyl, a bicyclic heterocycloalkyl, or a bicyclic heteroaryl, wherein said monocyclic heterocycloalkyl, said bicyclic heterocycloalkyl and said bicyclic heteroaryl are each optionally substituted with one or more groups R24.

[0105] Said monocyclic heterocycloalkyl may be, e.g., a monocyclic 5, 6 or 7-membered heterocycloalkyl comprising one nitrogen ring atom (i.e., the nitrogen atom that carries R1and R2) and optionally one further ring heteroatom selected from nitrogen, oxygen and sulfur, wherein all remaining ring atoms are carbon atoms; corresponding examples include, in particular, pyrrolidin-1-yl, piperidin-1-yl, or azepan-1-yl.

[0106] Said bicyclic heteroaryl may be, e.g., a bicyclic fused ring system consisting of a heterocycloalkyl (e.g., a monocyclic 5, 6 or 7-membered heterocycloalkyl) fused to an aryl (e.g., phenyl) or to a heteroaryl (e.g., pyridinyl), preferably to a phenyl, wherein said heterocycloalkyl comprises at least one nitrogen ring atom (i.e., the nitrogen atom that carries R1and R2); corresponding examples include, in particular, isoindolin-2-yl, indolin-1-yl, 1 ,2,3,4-tetrahydroisoquinolin- 2-yl, 1 ,2,3,4-tetrahydroquinolin-1-yl, benzo[b]azepan-1-yl, benzo[c]azepan-2-yl, or benzo[d]azepan-3-yl.

[0107] In accordance with the above, if R1and R2are mutually joined (as described herein), it is preferred that the heterocyclyl formed from R1and R2is not spirocyclic (i.e., is not a spirocyclic heterocyclyl). Moreover, if R1and R2are mutually joined, it is preferred that the heterocyclyl formed from R1and R2is not a fused-ring heterocycloalkyl containing two or more nitrogen ring atoms (i.e., the heterocyclyl is not a polycyclic fused heterocycloalkyl containing two or more nitrogen ring atoms).

[0108] Each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci_5alkylene)-S(Ci_5alkyl), -NH2, -NH(Ci.5alkyl), -N(Ci_5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci_5haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5 alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(Ci_5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci.5 alkyl), -NH-SO2-(Ci.5alkyl), -N(CI.5alkyl)-SO2-(Ci_5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more (e.g., one, two or three) groups Rc c. Preferably, each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alky lene)-0 H, -O(Ci-5 al ky lene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(Ci.5alkyl), -N(Ci.5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci_5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5 alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(Ci.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(Ci.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(Ci.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), and -SO2-(Ci-5 alkyl).

[0109] More preferably, each R22is independently selected from -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(CI-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), and -ON.

[0110] Each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two or three) groups RCyc.

[0111] Preferably, each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(OI.5alkyl), -N(Ci.5alkyl)(Ci.5alkyl), -NH-OH, -N(Ci.5alkyl)-OH, -NH-O(Ci.5alkyl), -N(Ci.5alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -CHO, -CO-(Ci-5 alkyl), -COOH, -CO-O-(Ci-5 alkyl), -O-CO-(Ci.5 alkyl), -CO-NH2, -CO-NH(Ci.5alkyl), -CO-N(Ci.5alkyl)(Ci.5alkyl), -NH-CO-(Ci.5alkyl), -N(Ci.5alkyl)-CO-(Ci.5 alkyl), -NH-COO(Ci.5alkyl), -N(Ci.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(Ci.5alkyl), -O-CO-N(Ci.5alkyl)(Ci-5alkyl), -SO2-NH2, -SO2-NH(Ci-5 alkyl), -SO2-N(Ci-5 alkyl)(Ci.5alkyl), -NH-SO2-(Ci-5 alkyl), -N(Ci.5alkyl)-SO2-(Ci-5 alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups R0''0.

[0112] More preferably, each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), and -CN.

[0113] Even more preferably, each R23is independently selected from C1-5 alkyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, and -SF5.

[0114] Yet even more preferably, each R23is independently selected from halogen (e.g., -F, -Cl, -Br, or -I), C1-5 haloalkyl (e.g., -CF3), -SF5, and C1-5 alkyl (e.g., methyl).

[0115] Still more preferably, each R23is independently halogen (particularly -F or -Cl) or C1-5 haloalkyl (particularly -CF3).

[0116] Each R24is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci_5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two or three) groups Rc c.

[0117] Preferably, each R24is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -CHO, -C0-(Ci-5 alkyl), -COCH, -C0-0-(Ci-5 alkyl), -0-C0-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci-5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci-5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci-5 alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups Rc c.

[0118] More preferably, each R24is independently selected from C1-5 alkyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(0I-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -(C0-3 alkylene)-aryl, and -(C0-3 alkylene)-heteroaryl, wherein the aryl group in said -(C0-3 alkylene)-aryl and the heteroaryl group in said -(C0-3 alky lene)-heteroary I are each optionally substituted with one or more groups F .

[0119] If R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl (e.g., a heterocycloalkyl) which is optionally substituted with one or more groups R24, it is particularly preferred that said heterocyclyl is substituted with one group R24which is -(C0-3 al ky lene)-ary I or -(C0-3 alkylene)-heteroaryl, wherein the aryl group in said -(C0-3 alkylene)-aryl and the heteroaryl group in said -(C0-3 alkylene)-heteroaryl are each optionally substituted with one or more groups Rc c, and that said heterocyclyl is optionally further substituted with one or two groups R24which is / are selected independently from C1-5 alkyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci.5 alkyl), -SH, -S(Ci_5alkyl), -S(Ci_5alkylene)-SH, -S(Ci.5alkylene)-S(Ci_5alkyl), -NH2, -NH(CI.5alkyl), -N(CI-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -SF5, and -ON.

[0120] Moreover, if R1and R2are mutually joined (as described above), it is even more preferred that the heterocyclyl (which is formed from R1and R2) is substituted with -(C0-3 al ky lene)-pheny I (e.g., phenyl or -CH2-pheny I), wherein the phenyl group in said -(C0-3 alkylene)-phenyl is optionally substituted with one or more groups RCyc.

[0121] R3is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein said alkyl, said alkenyl, said alkynyl, the alkylene group in said -(C0-5 alkylene)-carbocyclyl, and the alkylene group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups R31, and wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups R32.

[0122] Preferably, R3is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein said alkyl, said alkenyl, said alkynyl, the alkylene group in said -(C0-5 alkylene)-carbocyclyl, and the alkylene group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups R31, and further wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups R32. Thus, for example, R3may be C1-6 alkyl substituted with one or more (e.g., one or two) groups -O(Ci-5 alkyl); a corresponding example of R3is -CH(-CH3)-O-CH3. R3may also be, for example, C2-6 alkynyl (e.g., ethynyl) which is optionally substituted with one or more groups R31; corresponding examples of R3include ethynyl, cyclobutylethynyl or (trimethylsilyl)ethynyl.

[0123] More preferably, R3is selected from C1-6 alkyl, -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein said alkyl is optionally substituted with one or more groups R31, and wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32.

[0124] Even more preferably, R3is selected from C1-6 alkyl, -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32.

[0125] Even more preferably, R3is selected from C2-5 alkyl (e.g., ethyl, propyl, butyl or pentyl; including, in particular, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, or tert-butyl), -(C0-5 alkylene)-carbocyclyl (e.g., carbocyclyl, -CH2-carbocyclyl or -CH2CH2-carbocyclyl; preferably carbocyclyl or -C H2-carbocycly I), and -(C0-5 al ky lene)-heterocycly I (e.g., heterocyclyl, -CH2-heterocyclyl or -CH2CH2-heterocyclyl; preferably heterocyclyl or -CFh-heterocyclyl), wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32.

[0126] The carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl may be, e.g., a cycloalkyl, cycloalkenyl, or aryl, preferably cycloalkyl or aryl. Said cycloalkyl is preferably a monocyclic cycloalkyl, more preferably a C3-7 cycloalkyl (e.g., cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl); particularly preferred examples of said cycloalkyl are cyclobutyl or cyclopentyl. Said cycloalkenyl is preferably a monocyclic cycloalkenyl, more preferably a C4-7 cycloalkenyl (e.g., cyclobutenyl, cyclopentenyl, cyclohexenyl, or cyclohepentyl); particularly preferred examples of said cycloalkenyl are cyclobutenyl, cyclopentenyl, or cyclohexenyl (e.g., cyclohex-1 -en-1-yl). Said aryl is preferably phenyl.

[0127] The heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl may be, e.g., a heterocycloalkyl, heterocycloalkenyl, or heteroaryl, preferably heterocycloalkyl or heteroaryl. Said heterocycloalkyl is preferably a monocyclic heterocycloalkyl, more preferably a 3- to 7-membered heterocycloalkyl (e.g., containing one or two ring heteroatoms selected independently from oxygen, sulfur and nitrogen, wherein all remaining ring atoms are carbon atoms), even more preferably a 4- to 7-membered heterocycloalkyl having one ring heteroatom selected from oxygen, sulfur and nitrogen (wherein all other ring atoms are carbon atoms); corresponding examples of said heterocycloalkyl include tetrahydrofuranyl (e.g., tetrahydrofuran-3-yl), tetrahydropyranyl (e.g., tetrahydropyran-4-yl), tetrahydrothiophenyl (e.g., tetrahydrothiophene-3-yl), thianyl (e.g., thian-4-yl), pyrrolidinyl (e.g., pyrrolidin-3-yl), piperidinyl (e.g., piperidin- 4-yl), or morpholinyl (e.g., morpholin-4-yl); a particularly preferred example of said heterocycloalkyl is tetrahydrofuranyl (e.g., tetrahydrofuran-3-yl). Said heterocycloalkenyl is preferably a monocyclic heterocycloalkenyl, more preferably a 4- to 7-membered heterocycloalkenyl (e.g., containing one or two ring heteroatoms selected independently from oxygen, sulfur and nitrogen, wherein all remaining ring atoms are carbon atoms), even more preferably a 4- to 7-membered heterocycloalkenyl having one ring heteroatom selected from oxygen, sulfur and nitrogen (wherein all other ring atoms are carbon atoms). Said heteroaryl is preferably a monocyclic 5- or 6-membered heteroaryl (e.g., containing one or two ring heteroatoms selected independently from oxygen, sulfur and nitrogen, wherein all remaining ring atoms are carbon atoms).

[0128] Even more preferably, R3is selected from C3-5 alkyl, -(C0-5 alkylene)-cycloalkyl (e.g., cycloalkyl, -CF cycloalkyl, or - CH2CH2-cycloalkyl), -(C0-5 alkylene)-heterocycloalkyl (e.g., heterocycloalkyl, -CF heterocycloalkyl, or -CH2CH2- heterocycloalkyl), -(C0-5 alkylene)-aryl (e.g., aryl, -CF aryl, or -CH2CH2-aryl), and -(C0-5 alkylene)-heteroaryl (e.g., heteroaryl, -CF heteroaryl, or -CH2CH2-heteroaryl), wherein the cycloalkyl group in said -(C0-5 alkylene)-cycloalkyl, the heterocycloalkyl group in said -(C0-5 alkylene)-heterocycloalkyl, the aryl group in said -(C0-5 alkylene)-aryl, and the heteroaryl group in said -(C0-5 alkylene)-heteroaryl are each optionally substituted with one or more groups R32.

[0129] Yet even more preferably, R3is selected from C3-5 alkyl, -(C0-3 al ky lene)-cycloalky I [e.g., cyclopropyl, -CF cyclopropyl, -CH2CH2-cyclopropyl, cyclobutyl, -CF cyclobutyl, -CH2CH2-cyclobutyl, cyclopentyl, -CF cyclopentyl, or -CH2CH2- cyclopentyl], -(C0-3 alkylene)-heterocycloalkyl [e.g., oxetanyl (such as oxetan-2-yl or oxetan-3-yl), -CH2-oxetanyl (such as oxetan-2-y I methyl or oxetan-3-ylmethyl), -CH2CH2-oxetanyl (such as oxetan-2-ylethyl or oxetan-3-ylethyl), tetrahydrofuranyl (such as tetrahydrofuran-3-yl), -CFh-tetrahydrofuranyl (such as tetrahydrofuran-3-ylmethyl), -CH2CH2-tetrahydrofuranyl (such as tetrahydrofuran-3-ylethyl), tetrahydropyranyl (such as tetrahydropyran-4-yl), -CH2-tetrahydropyranyl (such as tetrahydropyran-4-ylmethyl), or -CH2CH2-tetrahydropyranyl (such as tetrahydropyran-4-ylethyl)], -(C0-3 alkylene)-aryl [e.g., phenyl, -CF phenyl, or -CH2CH2-phenyl], and -(C0-3 alkylene)-heteroaryl [e.g., oxazolyl (such as oxazol-2-yl, oxazol-4-yl, or oxazol-5-yl), -CH2-oxazolyl (such as oxazol- 2-ylmethyl, oxazol-4-ylmethyl, or oxazol-5-ylmethyl), -CH2CH2-oxazolyl (such as oxazol-2-ylethyl, oxazol-4-ylethyl, or oxazol-5-ylethyl), pyridinyl (such as pyridin-2-yl, pyridin-3-yl, or pyridin-4-yl), -CFh-pyridinyl (such as pyridin-2- ylmethyl, pyridin-3-ylmethyl, or pyridin-4-ylmethyl), -CFhCFk-pyridinyl (such as pyridin-2-ylethyl, pyridin-3-ylethyl, or pyridin-4-ylethyl),-C(-CH3)(-CH3)-pyridinyl (such as -C(-CH3)(-CH3)-(pyridin-2-yl)), -CH2C(-CH3)(-CH3)-pyridinyl (such as -CH2C(-CH3)(-CH3)-(pyridin-2-yl)), pyrimidinyl (such as pyrimidin-2-yl), -CFh-pyrimidinyl (such as pyrimidin-2- ylmethyl), -CH2CH2-pyrimidinyl (such as pyrimidin-2-ylethyl), pyrazinyl (such as pyrazin-2-yl), -CFh-pyrazinyl (such as pyrazin-2-ylmethyl), or -CH2CH2-pyrazinyl (such as pyrazin-2-ylethyl)], wherein the cycloalkyl group in said -(C0-3 alkylene)-cycloalkyl, the heterocycloalkyl group in said -(C0-3 alkylene)-heterocycloalkyl, the aryl group in said -(C0-3 alkylene)-aryl, and the heteroaryl group in said -(C0-3 alkylene)-heteroaryl are each optionally substituted with one or more groups R32. A corresponding preferred example of R3is -CH2-phenyl, wherein the phenyl group in said -CH2- phenyl is optionally substituted with one or more groups R32.

[0130] Still more preferably, R3is selected from C3-5 alkyl, cycloalkyl, -CH2-cycloalkyl, heterocycloalkyl, and -CH2- heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CH2-cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CFh-heterocycloalkyl are each optionally substituted with one or more groups R32. Corresponding particularly preferred examples of R3include propyl (particularly n-propyl or isopropyl), butyl (particularly n-butyl, isobutyl, sec-butyl, or tert-butyl), pentyl (particularly pentan-1 -yl, pentan-2-yl, pentan-3-yl, 3- methylbutan-1-yl, 1 ,1-dimethylpropan-1-yl, 2,2-dimethylpropan-1-yl, or 2-methylbutan-1-yl), cyclopropyl, cyclobutyl, cyclopentyl, tetrahydrofuranyl (particularly tetrahydrofuran-3-yl), -CH2-cyclopropyl, -CH2-cyclobutyl, -CH2-cyclopentyl, or -CH2-tetrahydrofuranyl (e.g., -CH2-(tetrahydrofuran-3-yl)), wherein said cyclopropyl, said cyclobutyl, said cyclopentyl, said tetrahydrofuranyl, the cyclopropyl in said -CH2-cyclopropyl, the cyclobutyl in said -CH2-cyclobutyl, the cyclopentyl in said -CH2-cyclopentyl, and the tetrahydrofuranyl in said -CH2-tetrahydrofuranyl are each optionally substituted with one or more groups R32. Even more preferred examples of R3include propyl (particularly isopropyl), butyl, pentyl, cyclopropyl, cyclobutyl, cyclopentyl, -CH2-cyclopropyl, -CH2-cyclobutyl, or -CF cyclopentyl. Yet even more preferred examples of R3are isopropyl or -CH2-cyclobutyl.

[0131] Further examples of R3include any of the specific groups R3comprised in the compounds of formula (I) described in the examples section, including in any one of Examples 1 to 275 described herein below.

[0132] Each R31is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci_5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci_5alkyl), -Si(Ci.5alkyl)(Ci_5alkyl)(Ci.5alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -CHO, -C0-(Ci-5 alkyl), -COOH, -C0-0-(Ci-5 alkyl), -0-C0-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5 alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups RCyc.

[0133] Preferably, each R31is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alky lene)-0 H, -O(Ci-5 al ky lene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5 alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci_5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -CN, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI-5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(Ci.5alkyl)-CO-(Ci_5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci-5alkyl), -O-CO-NH(Ci.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci-5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups Rc c.

[0134] More preferably, each R31is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(Ci.5alkyl), -N(CI.5 alkyl)(Ci.5alkyl), -NH-OH, -N(Ci.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -CN, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI-5 alkyl), -N(Ci.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(Ci-5 alkyl)(Ci.5alkyl), -NH-SO2-(Ci-5 alkyl), -N(CI.5alkyl)-SO2-(Ci-5 alkyl), -SO-(Ci-5 alkyl), and -SO2-(Ci-5 alkyl).

[0135] Even more preferably, each R31is independently selected from -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(CI-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), and -CN.

[0136] Each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups Rc c.

[0137] Preferably, each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(0i-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(Ci.5alkyl)-OH, -NH-O(Ci.5alkyl), -N(Ci.5alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -CHO, -C0-(Ci-5 alkyl), -COOH, -C0-0-(Ci-5 alkyl), -0-C0-(Ci.5 alkyl), -CO-NH2, -CO-NH(Ci.5alkyl), -CO-N(Ci.5alkyl)(Ci.5alkyl), -NH-CO-(Ci.5alkyl), -N(Ci.5 alkyl)-CO-(Ci-5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci_5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci-5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci-5 alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups F .

[0138] More preferably, each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), and -CN.

[0139] Even more preferably, each R32is independently selected from C1-5 alkyl (e.g., methyl), halogen (e.g., -F, -Cl, -Br, or -I), C1-5 haloalkyl (e.g., -CF3), -O-(Ci-5 haloalkyl) (e.g., -OCF3), -CN, and -SF5.

[0140] R4and R5(if present) are each independently selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci.5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two or three) groups RCyc.

[0141] Preferably, R4is selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -CHO, -CO-(Ci-5 alkyl), -COCH, -CO-O-(Ci-5 alkyl), -O-CO-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5 alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci-5 alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups R0''0. More preferably, R4is selected from hydrogen, C1-5 alkyl, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(CI-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -(C0-3 alkylene)-cycloalkyl (e.g., cyclopropyl), and -(C0-3 alkylene)-heterocycloalkyl, wherein the cycloalkyl group in said -(C0-3 alkylene)-cycloalkyl and the heterocycloalkyl group in said -(C0-3 alkylene)-heterocycloalkyl are each optionally substituted with one or more groups RCyc.

[0142] Even more preferably, R4is selected from hydrogen, C1-5 alkyl, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(0I-5 alkyl)(Ci-5 alkyl), halogen (e.g., fluoro), C1-5 haloalkyl, -O-(Ci-5 haloalkyl), and -ON. For example, R4may be hydrogen or fluoro.

[0143] Yet even more preferably, R4is hydrogen.

[0144] Preferably, R5(if present) is selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -S(0i-5 alkylene)-SH, -S(0i-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(Ci.5alkyl)(Ci.5alkyl), -NH-OH, -N(Ci.5alkyl)-OH, -NH-O(Ci.5alkyl), -N(Ci.5alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -OHO, -C0-(Ci-5 alkyl), -COOH, -C0-0-(Ci-5 alkyl), -0-C0-(Ci.5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(Ci.5alkyl)-CO-(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(Ci.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5 alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(Ci.5alkyl)-SO2-(Ci-5 alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc.

[0145] More preferably, R5is selected from hydrogen, C1-5 alkyl, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(0I-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -(C0-3 alkylene)-cycloalkyl (e.g., cyclopropyl), and -(C0-3 alkylene)-heterocycloalkyl, wherein the cycloalkyl group in said -(C0-3 alkylene)-cycloalkyl and the heterocycloalkyl group in said -(C0-3 alkylene)-heterocycloalkyl are each optionally substituted with one or more groups RCyc.

[0146] Even more preferably, R5is selected from hydrogen, C1-5 alkyl, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(0I-5 alkyl)(Ci-5 alkyl), halogen (e.g., fluoro), C1-5 haloalkyl, -O-(Ci-5 haloalkyl), and -ON. For example, R5may be hydrogen or fluoro.

[0147] Yet even more preferably, R5is hydrogen.

[0148] It will be understood that the aforementioned meanings of R5apply only if this group is present in the compound of formula (I), i.e., only if the ring atom X is C(-R5).

[0149] RAand RBare each independently selected from hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, -(Co-8 alkylene)-OH, -(Co-8 alkylene)-O(Ci-5 alkyl), -(Co-8 alkylene)-SH, -(Co-8 alkylene)-S(Ci-5 alkyl), -(C1-8 alkylene)-NH2, -(C1-8 alkylene)-NH(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-halogen, -(C1-8 alkylene)-Ci-5 haloalkyl, -(Co-8 alkylene)-O-(Ci-8 haloalkyl), -(Co-8 alkylene)-CN, -(Co-8 alkylene)-SF5, -(Co-8 alkylene)-CHO, -(Co-8 alkylene)-CO-(Ci-5 alkyl), -(Co-8 alkylene)-COOH, -(Co-8 alkylene)-CO-O-(Ci-5 alkyl), -(Co-8 alkylene)-O-CO-(Ci-5 alkyl), -(Co-8 alkylene)-CO-NH2, -(Co-8 alkylene)-CO-NH(Ci-5 alkyl), -(Co-8 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-NH-CO-(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C1-8 alkylene)-NH-COO(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(Co-8 alkylene)-O-CO-NH(Ci-5 alkyl), -(Co-8 alkylene)-0-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(Co-8 alkylene)-SO2-NH2, -(Co-8 alkylene)-SO2-NH(Ci-5 alkyl), -(Co-8 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.8 alkylene)-NH-SO2-(Ci-5 alkyl), -(C1.8 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(Co-8 alkylene)-S0-(Ci-5 alkyl), -(Co-8 alkylene)-SO2-(Ci-5 alkyl), -(Co-8 alkylene)-carbocyclyl, -(Co-8 alkylene)-heterocyclyl, and -Lz-Rz, wherein one or more -CH2- units comprised in said C1-8 alkyl, said C2-8 alkenyl, said C2-8 alkynyl, and in any of the aforementioned Co-s alkylene and C1-8 alkylene groups are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-, wherein the carbocyclyl group in said -(Co-s alkylene)-carbocyclyl and the heterocyclyl group in said -(Co-s alkylene)-heterocyclyl are each optionally substituted with one or more groups R°yc, and wherein at least one of the groups RAand RBis not hydrogen; or alternatively, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc.

[0150] Preferably, RAand RBare each independently selected from hydrogen, C1.5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-5 alkylene)-OH, -(C0-5 alkylene)-O(Ci-5 alkyl), -(C0-5 alkylene)-SH, -(C0-5 alkylene)-S(Ci-5 alkyl), -(C1.5 alkylene)-NH2, -(C1.5 alkylene)-NH(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.5 alkylene)-halogen, -(C1.5 alkylene)-Ci-5 haloalkyl, -(C0-5 alkylene)-O-(Ci-5 haloalkyl), -(C0-5 alkylene)-CN, -(C0-5 alkylenej-SFs, -(C0-5 alkylene)-CHO, -(C0-5 alkylene)-CO-(Ci-5 alkyl), -(C0-5 alkylene)-COOH, -(C0-5 alkylene)-CO-O-(Ci-5 alkyl), -(C0-5 alkylene)-O-CO-(Ci-5 alkyl), -(C0-5 alkylene)-CO-NH2, -(C0-5 alkylene)-CO-NH(Ci-5 alkyl), -(C0-5 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.5 alkylene)-NH-CO-(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C1.5 alkylene)-NH-COO(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-5 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-5 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-5 alkylene)-SO2-NH2, -(C0-5 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-5 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.5 alkylene)-NH-SO2-(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-5 alkylene)-SO-(Ci-5 alkyl), -(C0-5 alkylene)-SO2-(Ci-5 alkyl), -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein one or more (e.g., one, two, or three) -CH2- units comprised in said C1.5 alkyl, said C2-5 alkenyl, said C2-5 alkynyl, and in any of the aforementioned C0-5 alkylene and C1.5 alkylene groups are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2- , wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups R0^, and wherein at least one of the groups RAand RBis not hydrogen; or alternatively, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc.

[0151] More preferably, RBis selected from hydrogen, C1.5 alkyl, and -(C1.5 alkylene)-O(Ci-5 alkyl) [particularly from hydrogen and C1-5 alkyl (e.g., methyl); even more preferably, RBis hydrogen], and RAis selected from C1.5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-5 alkylene)-OH, -(C0-5 alkylene)-O(Ci-5 alkyl), -(C0-5 alkylene)-SH, -(C0-5 alkylene)-S(Ci-5 alkyl), -(C1.5 alkylene)-NH2, -(C1.5 alkylene)-NH(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.5 alkylene)-halogen, -(C1.5 alkylene)-Ci-5 haloalkyl, -(C0-5 alkylene)-O-(Ci-5 haloalkyl), -(C0-5 alkylene)-CN, -(C0-5 alkylenej-SFs, -(C0-5 alkylene)-CHO, -(C0-5 alkylene)-CO-(Ci-5 alkyl), -(C0-5 alkylene)-COOH, -(C0-5 alkylene)-CO-O-(Ci-5 alkyl), -(C0-5 alkylene)-O-CO-(Ci-5 alkyl), -(C0-5 alkylene)-CO-NH2, -(C0-5 alkylene)-CO-NH(Ci-5 alkyl), -(C0-5 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.5 alkylene)-NH-CO-(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C1.5 alkylene)-NH-COO(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-5 alkylene)-O-CO-NH(Ci-5 alkyl), -(Co-5 alkylene)-0-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-5 alkylene)-SO2-NH2, -(C0-5 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-5 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1.5 alkylene)-NH-SO2-(Ci-5 alkyl), -(C1.5 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-5 alkylene)-S0-(Ci-5 alkyl), -(C0-5 alkylene)-SO2-(Ci-5 alkyl), -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein one or more (e.g., one, two, or three) -CH2- units comprised in said C1-5 alkyl, said C2-5 alkenyl, said C2-5 alkynyl, and in any of the aforementioned C0-5 alkylene and C1-5 alkylene groups are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2- , and further wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two, or three) groups F ; or alternatively, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc.

[0152] Corresponding preferred examples of the moiety -N(-RA)-RBinclude -NH-C(-CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy-4,6- dimethyl-pyridin-2-yl), -NH-C(-CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy-pyridin-2-yl), -NH-C(-CH3)(-CH3)-CO-N(-CH3)- CH2-CO-NH2, -NH-C(-CH3)(-CH3)-CO-N(-CH3)(-CH3), -NH-C(-CH3)(-CH3)-CO-NH-CH3, -NH-CH(-CH3)-CH2-COOH, -NH-CH2-CH2-CH(-CH3)-COOH, -NH-CH2-CH2-CH(-CH3)-CH2-COOH, -NH-CH2-CH2-CH(-CH3)-CH2-CO-NH2, -NH- CH2-CH2-CH(-CH3)-CH2-CO-N(-CH3)-CH3, -NH-(1-(aminocarbonyl)cyclopropan-1-yl), -N(CI.5alkyl)-C(-CH3)(-CH3)- CH2-N(-CH3)-(5-carboxy-4,6-dimethyl-pyridin-2-yl), -N(CI-5 alkyl)-C(-CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy-pyridin-2- yl), -N(CI.5 alkyl)-C(-CH3)(-CH3)-CO-N(-CH3)-CH2-CO-NH2, -N(CI.5alkyl)-C(-CH3)(-CH3)-CO-N(-CH3)(-CH3), -N(CI.5alkyl)-C(-CH3)(-CH3)-CO-NH-CH3, -N(CI.5alkyl)-CH(-CH3)-CH2-COOH, -N(CI.5alkyl)-CH2-CH2-CH(-CH3)-COOH, -N(CI-5 alkyl)-CH2-CH2-CH(-CH3)-CH2-COOH, -N(CI.5alkyl)-CH2-CH2-CH(-CH3)-CH2-CO-NH2, -N(CI.5alkyl)-CH2- CH2-CH(-CH3)-CH2-CO-N(-CH3)-CH3, -N(CI-5 alkyl)-(1-(aminocarbonyl)cyclopropan-1-yl), -N[-(CI-5 alkylene)-O(Ci-5 alkyl)]-C(-CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy-4,6-dimethyl-pyridin-2-yl), -N[-(CI.5alkylene)-O(Ci-5 alkyl)]-C(-CH3)(- CH3)-CH2-N(-CH3)-(5-carboxy-pyridin-2-yl), -N[-(CI.5alkylene)-O(Ci-5 alkyl)]-C(-CH3)(-CH3)-CO-N(-CH3)-CH2-CO- NH2, -N[-(CI.5 alkylene)-O(Ci.5 alkyl)]-C(-CH3)(-CH3)-CO-N(-CH3)(-CH3), -N[-(CI.5alkylene)-O(Ci-5 alkyl)]-C(-CH3)(- CH3)-CO-NH-CH3, -N[-(CI.5 alkylene)-O(Ci.5 alkyl)]-CH(-CH3)-CH2-COOH, -N[-(CI.5alkylene)-O(Ci-5 alkyl)]-CH2-CH2- CH(-CH3)-COOH, -N[-(CI.5 alkylene)-O(Ci.5 alkyl)]-CH2-CH2-CH(-CH3)-CH2-COOH, -N[-(CI.5alkylene)-O(Ci-5 alkyl)]- CH2-CH2-CH(-CH3)-CH2-CO-NH2, -N[-(CI.5 alkylene)-O(Ci.5 alkyl)]-CH2-CH2-CH(-CH3)-CH2-CO-N(-CH3)-CH3, or -N[-(CI-5 alkylene)-O(Ci-5 alkyl)]-(1-(aminocarbonyl)cyclopropan-1-yl). Further preferred examples of the moiety -N(-RA)-RB, particularly wherein RAand RBare mutually joined (as defined herein), are described further below and include, in particular, 2,2-dimethyl-piperazin-3-on-1-yl, 2,2-dimethyl-4-(5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin- 1-yl, 2,2-dimethyl-4-(5-carboxy-pyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxymethylpyridin-2-yl)piperazin-1- yl, 2,2-dimethyl-4-(6-carboxy-5-methyl-pyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(4-carboxythiazol-2-yl)piperazin-1- yl, 2,2-dimethyl-4-(5-carboxythiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(4-aminocarbonylthiazol-2-yl)piperazin-1-yl,

[0153] 2.2-dimethyl-4-(5-aminocarbonylthiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(4-aminocarbonyl-5-methyl-thiazol-2- yl)piperazin-1-yl, 2,2-dimethyl-4-(5-aminocarbonyl-4-methyl-thiazol-2-yl)piperazin-1-yl, 3-methoxy-4- (carboxymethyl)piperidin-l-yl, 3-methyl-4-(carboxymethyl)piperidin-1-yl, 3-fluoro-4-(carboxymethyl)piperidin-1-yl,

[0154] 2.2-dimethylpiperidin-1-yl, or 3,3-dimethylmorpholin-4-yl, wherein each of the aforementioned moieties is optionally further substituted with one or more groups Rc.

[0155] Particularly preferred examples of the moiety -N(-RA)-RBinclude -N(-CH3)-C(-CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy- 4,6-dimethyl-pyridin-2-yl), -N(-CH3)-C(-CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy-pyridin-2-yl), -N(-CH2CH2-O-CH3)-C(- CH3)(-CH3)-CH2-N(-CH3)-(5-carboxy-4,6-dimethyl-pyridin-2-yl), -N(-CH2CH2-O-CH3)-C(-CH3)(-CH3)-CH2-N(-CH3)-(5- carboxy-pyridin-2-yl), -N(-CH3)-C(-CH3)(-CH3)-CO-N(-CH3)-CH2-CO-NH2, -N(-CH3)-C(-CH3)(-CH3)-CO-N(-CH3)(- CH3), -N(-CH3)-C(-CH3)(-CH3)-CO-NH-CH3, -N(-CH3)-CH(-CH3)-CH2-COOH, -N(-CH3)-CH2-CH2-CH(-CH3)-COOH, -N(-CH3)-CH2-CH2-CH(-CH3)-CH2-COOH, -N(-CH3)-CH2-CH2-CH(-CH3)-CH2-CO-NH2, -N(-CH3)-CH2-CH2-CH(-CH3)- CH2-CO-N(-CH3)-CH3, -NH-(1-(aminocarbonyl)cyclopropan-1-yl), 2,2-dimethyl-piperazin-3-on-1-yl, 2,2-dimethyl-4- (5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxy-pyridin-2-yl)piperazin-1-yl, 2,2- dimethyl-4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(6-carboxy-5-methyl-pyridin-2-yl)piperazin-1- yl, 2,2-dimethyl-4-(4-carboxythiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxythiazol-2-yl)piperazin-1-yl, 2,2- dimethyl-4-(4-aminocarbonylthiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-aminocarbonylthiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(4-aminocarbonyl-5-methyl-thiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-aminocarbonyl-4-methyl- thiazol-2-yl)piperazin-1-yl, 3-methoxy-4-(carboxymethyl)piperidin-1-yl, 3-methyl-4-(carboxymethyl)piperidin-1-yl, 3- fluoro-4-(carboxymethyl)piperidin-1-yl, 2,2-dimethylpiperidin-1-yl, or 3,3-dimethylmorpholin-4-yl.

[0156] Even more preferably, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc. It will be understood that in this case, the moiety -N(-RA)-RBis a heterocyclyl which is optionally substituted with one or more groups Rc, wherein said heterocyclyl is attached via a ring nitrogen atom (i.e., the nitrogen atom carrying RAand RB) to the remainder of the compound of formula (I), i.e., to the -C(=O)- group in formula (I). Said heterocyclyl may be, e.g., a 5- to 14-membered heterocyclyl. It is preferred that said heterocyclyl is a heterocycloalkyl or a heterocycloalkenyl, particularly a heterocycloalkyl.

[0157] Accordingly, even more preferably, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl or heterocycloalkenyl, wherein said heterocycloalkyl or said heterocycloalkenyl is optionally substituted with one or more groups Rc. Said heterocycloalkyl or said heterocycloalkenyl may be, e.g., a 5- to 14-membered heterocycloalkyl or a 5- to 14-membered heterocycloalkenyl.

[0158] Yet even more preferably, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups Rc. As explained above, said heterocycloalkyl is attached via a ring nitrogen atom (i.e., the nitrogen atom carrying RAand RB) to the -C(=O)- group in formula (I).

[0159] Said heterocycloalkyl is preferably a 5- to 11-membered heterocycloalkyl containing one nitrogen ring atom (through which the heterocycloalkyl is attached to the -C(=O)- group in formula (I)) and optionally containing one or more (e.g., one, two, or three) further ring heteroatoms independently selected from nitrogen, oxygen and sulfur, wherein all remaining ring atoms are carbon atoms, wherein any nitrogen ring atom (if present) and / or any sulfur ring atom (if present) is optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized (i.e., to form an oxo group). More preferably, said heterocycloalkyl is a 5- to 7-membered (even more preferably a 6-membered) monocyclic heterocycloalkyl containing one nitrogen ring atom (through which the heterocycloalkyl is attached to the -C(=0)- group in formula (I)) and optionally containing one or two further ring heteroatoms independently selected from nitrogen, oxygen and sulfur, wherein all remaining ring atoms are carbon atoms, wherein any nitrogen ring atom (if present) and / or any sulfur ring atom (if present) is optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized.

[0160] Moreover, the heterocycloalkyl may contain a lactam function, i.e. the heterocycloalkyl may contain a second nitrogen ring atom (in addition to the first nitrogen ring atom through which the moiety -N(-RA)-RBis attached to the -C(=0)- group in formula (I)) which is adjacent to an oxidized carbon ring atom (C=O). A corresponding preferred example of the moiety -N(-RA)-RBis 3-oxopiperazin-1-yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; a corresponding particularly preferred example of the moiety -N(-RA)-RBis 2,2-dimethy l-piperazin-3- on-1-yl (which may optionally be further substituted with one or more Rc).

[0161] A further preferred example of the moiety -N(-RA)-RBis 4-(5-carboxypyridin-2-yl)piperazin-1-yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; corresponding preferred examples of the moiety -N(-RA)-RBinclude 2,2-dimethyl-4-(5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl or 2,2-dimethyl-4-(5- carboxy-pyridin-2-yl)piperazin-1-yl (each of which may optionally be further substituted with one or more Rc), particularly 2,2-dimethyl-4-(5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl.

[0162] A further preferred example of the moiety -N(-RA)-RBis 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; a corresponding preferred example of the moiety -N(-RA)-RBincludes 2, 2-dimethyl-4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl (which may optionally be further substituted with one or more Rc).

[0163] Further preferred examples of the moiety -N(-RA)-RBare 4-(4-carboxythiazol-2-yl)piperazin-1-yl or 4-(5- carboxythiazol-2-yl)piperazin-1-yl, which are each optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; corresponding preferred examples of the moiety -N(-RA)-RBinclude 2,2-dimethyl-4-(4-carboxythiazol- 2-yl)piperazin-1-yl or 2,2-dimethyl-4-(5-carboxythiazol-2-yl)piperazin-1-yl (each of which may optionally be further substituted with one or more Rc).

[0164] A further preferred example of the moiety -N(-RA)-RBis 4-(carboxymethyl)piperidin-1 -yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; corresponding preferred examples of the moiety -N(-RA)- RBinclude 3-methoxy-4-(carboxymethyl)piperidin-1-yl, 3-methyl-4-(carboxymethyl)piperidin-1-yl, or 3-fluoro-4- (carboxymethyl)piperidin-l -yl (each of which may optionally be further substituted with one or more Rc).

[0165] A further preferred example of the moiety -N(-RA)-RBis 4-(6-carboxypyridin-2-yl)piperazin-1 -yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; a corresponding preferred example of the moiety -N(-RA)-RBis 2,2-dimethyl-4-(6-carboxy-5-methyl-pyridin-2-yl)piperazin-1 -yl (which may optionally be further substituted with one or more Rc).

[0166] Further preferred examples of the moiety -N(-RA)-RBare 4-(4-aminocarbonylthiazol-2-yl)piperazin-1-yl or 4-(5- ami nocarbony lthiazol-2-yl)pi perazi n-1 -yl, which are each optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; corresponding preferred examples of the moiety -N(-RA)-RBinclude 2,2-dimethyl-4-(4- aminocarbonylthiazol-2-yl)piperazin-1-yl or 2,2-dimethyl-4-(5-aminocarbonylthiazol-2-yl)piperazin-1-yl (each of which may optionally be further substituted with one or more Rc), as well as 2,2-dimethyl-4-(4-aminocarbonyl-5-methyl- thiazol-2-yl)piperazin-1-yl or 2,2-dimethyl-4-(5-aminocarbonyl-4-methyl-thiazol-2-yl)piperazin-1-yl.

[0167] A further preferred example of the moiety -N(-RA)-RBis piperidin-1-yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; a corresponding preferred example of the moiety -N(-RA)-RBis 2,2- dimethylpiperidin-1-yl.

[0168] A further preferred example of the moiety -N(-RA)-RBis morpholin-4-yl which is optionally substituted with one or more (e.g., one, two, three, or four) groups Rc; a corresponding preferred example of the moiety -N(-RA)-RBis 3,3- dimethylmorpholin-4-yl.

[0169] Thus, particularly preferred examples of the moiety -N(-RA)-RBinclude 2,2-dimethyl-piperazin-3-on-1 -yl, 2,2-dimethyl- 4-(5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxy-pyridin-2-yl)piperazin-1-yl, 2,2- dimethyl-4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(6-carboxy-5-methyl-pyridin-2-yl)piperazin-1- yl, 2,2-dimethyl-4-(4-carboxythiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxythiazol-2-yl)piperazin-1-yl, 2,2- dimethyl-4-(4-aminocarbonylthiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-aminocarbonylthiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(4-aminocarbonyl-5-methyl-thiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-aminocarbonyl-4-methyl- thiazol-2-yl)piperazin-1-yl, 3-methoxy-4-(carboxymethyl)piperidin-1-yl, 3-methyl-4-(carboxymethyl)piperidin-1-yl, 3- fluoro-4-(carboxymethyl)piperidin-1-yl, 2,2-dimethylpiperidin-1-yl, or 3,3-dimethylmorpholin-4-yl (wherein each of the aforementioned moieties may optionally be further substituted with one or more Rc).

[0170] Further examples of the moiety -N(-RA)-RBinclude any of the specific moieties -N(-RA)-RBcomprised in the compounds of formula (I) described in the examples section, including in any one of Examples 1 to 275 described herein below.

[0171] Each Rcis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alky lene)-0 H, -(C0-3 alky lene)-0 (C 1-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more (e.g., one, two or three) groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more (e.g., one, two or three) groups RCyc.

[0172] Preferably, each Rcis independently selected from C1-5 alkyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alky lene)-C N, -(C0-3 alky lene)-S F5, -(C0-3 alky lene)-C HO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SC>2-(Ci-5 alkyl), -(C0-3 alkylene)-aryl, -(C0-3 alkylene)-cycloalkyl (e.g., cyclopropyl), -(C0-3 alkylene)-heteroaryl (e.g., pyridinyl; such as pyridin-2-yl), and -(C0-3 alkylene)-heterocycloalkyl, wherein the aryl group in said -(C0-3 alkylene)-aryl, the cycloalkyl group in said -(C0-3 alkylene)-cycloalkyl, the heteroaryl group in said -(C0-3 alkylene)-heteroaryl, and the heterocycloalkyl group in said -(C0-3 alkylene)-heterocycloalkyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl (e.g., a C3-7 cycloalkyl, such as cyclopropyl).

[0173] If RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl (including any of the corresponding preferred or exemplary heterocyclyl groups described herein) which is optionally substituted with one or more groups Rc, it is particularly preferred that at least two substituents Rcare present, which are attached to the same carbon ring atom of said heterocyclyl, and which are each independently a C1-5 alkyl group or which are mutually joined to form, together with the carbon ring atom that they are attached to, a C3-7 cycloalkyl group.

[0174] Accordingly, it is particularly preferred that the moiety -N(-RA)-RBis a heterocycloalkyl (including any of the specific heterocycloalkyl groups described herein above) which is attached via a ring nitrogen atom to the -C(=O)- group in formula (I), wherein said heterocycloalkyl is either (i) substituted with two C1-5 alkyl groups which are attached to the same ring carbon atom of said heterocycloalkyl or is (ii) substituted with two substituents Rcwhich are attached to the same ring carbon atom (of said heterocycloalkyl) and are mutually joined to form, together with the ring carbon atom that they are attached to, a C3-7 cycloalkyl group (e.g., a cyclopropyl group), and wherein said heterocycloalkyl is optionally further substituted with one or more groups Rc. Thus, the moiety -N(-RA)-RBmay be, in particular, a heterocycloalkyl (including any of the specific heterocycloalkyl groups described herein above) which is attached via a ring nitrogen atom to the -C(=O)- group in formula (I), wherein said heterocycloalkyl is substituted with two C1-5 alkyl groups which are attached to the same ring carbon atom (of said heterocycloalkyl), and wherein said heterocycloalkyl is optionally further substituted with one or more groups Rc(e.g., with one group Rcwhich is 5-carboxy-4,6-dimethyl- pyridin-2-yl).

[0175] The two C1-5 alkyl groups that are attached to the same ring carbon atom (of said heterocycloalkyl) may be the same or different, and are preferably selected independently from methyl, ethyl, propyl and butyl; more preferably, the two C1-5 alkyl groups that are attached to the same ring carbon atom (of said heterocycloalkyl) are each methyl.

[0176] The C3-7 cycloalkyl group (which is formed from the two mutually joined substituents Rc, as described above) is preferably selected from cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; more preferably, the C3-7 cycloalkyl group is a cyclopropyl group.

[0177] The position (i.e., the specific carbon ring atom of said heterocyclyl or said heterocycloalkyl) at which the two C1-5 alkyl groups or the two mutually joined substituents Rc(which together form a C3-7 cycloalkyl group) are attached is not particularly limited. For example, the two C1-5 alkyl groups or the two mutually joined substituents Rc(which together form a C3-7 cycloalkyl group) may be attached to a carbon ring atom (of said heterocyclyl or said heterocycloalkyl) which is (I) directly adjacent to the nitrogen ring atom through which said heterocyclyl (or said heterocycloalkyl) is attached to the -C(=O)- group in formula (I), or is (II) separated by one ring atom from said nitrogen ring atom (through which said heterocyclyl or said heterocycloalkyl is attached to the -C(=O)- group in formula (I)), or is (iii) separated by two ring atoms from said nitrogen ring atom (through which said heterocyclyl or said heterocycloalkyl is attached to the -C(=O)- group in formula (I)).

[0178] Corresponding preferred examples of the moiety -N(-RA)-RBinclude 2,2-dimethyl-piperazin-l-yl, 3,3-dimethyl- piperazin-1-yl, 2,2-dimethyl-piperazin-3-on-1-yl, 2,2,4-trimethyl-piperazin-3-on-1-yl, 4-ethyl-2,2-dimethyl-piperazin-3- on-1-yl, spiro[piperazin-2,1'-cyclopropane]-1-yl, spiro[piperazin-3,1'-cyclopropane]-1-yl, 2,2-dimethyl-piperidin-l-yl, 3, 3-d i methy l-piperid i n- 1 -yl, 4, 4-d I methy I -pi perid I n- 1 -yl, spi ro [piperidin-2, 1 '-cyclopropane]-1 -yl, spi ro[pi peridi n-3, 1 cyclopropane]-1-yl, or spiro[piperidin-4, 1'-cyclopropane]-1-yl, wherein the piperazinyl moiety, the piperazinonyl moiety or the piperidinyl moiety in each of the aforementioned groups is optionally further substituted with one or more (e.g., one or two) groups Rc(e.g., with one group Rcwhich is selected from 5-carboxypyridin-2-yl, 5-carboxy- 4,6-dimethyl-pyridin-2-yl, 5-carboxymethyl-pyridin-2-yl, 5-carboxymethyl-4,6-dimethyl-pyridin-2-yl, 4-carboxythiazol- 2-yl, and 5-carboxythiazol-2-yl).

[0179] It is particularly preferred that the two C1-5 alkyl groups or the two mutually joined substituents Rc(which together form a C3-7 cycloalkyl group, preferably a cyclopropyl group) are attached to a carbon ring atom which is directly adjacent to the nitrogen ring atom through which the heterocyclyl or the heterocycloalkyl (which is formed from RAand RB) is attached to the -C(=O)- group in formula (I).

[0180] A corresponding particularly preferred example of the moiety -N(-RA)-RBis 2,2-dimethyl-piperazin-1 -yl, wherein the piperazinyl group in said 2,2-dimethyl-piperazin-1-yl is optionally further substituted with one or more groups Rc; accordingly, the moiety -N(-RA)-RBmay be, e.g., 2,2-dimethyl-4-(5-carboxypyridin-2-yl)piperazin-1 -yl, 2,2-dimethyl-4- (5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, 2,2- dimethyl-4-(5-carboxymethyl-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(6-carboxy-5-methyl-pyridin-2- yl)piperazin-1-yl, 2,2-dimethyl-4-(4-carboxythiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-carboxythiazol-2- yl)piperazin-1-yl, 2,2-dimethyl-4-(4-aminocarbonylthiazol-2-yl)piperazin-1-yl, 2,2-dimethyl-4-(5-aminocarbonylthiazol- 2-yl)piperazin-1-yl, 2,2-dimethyl-4-(4-aminocarbonyl-5-methyl-thiazol-2-yl)piperazin-1-yl, or 2,2-dimethyl-4-(5- aminocarbonyl-4-methyl-thiazol-2-yl)piperazin-1-yl. An even more preferred example of the moiety -N(-RA)-RBis 2,2- dimethyl-4-(5-carboxy-4,6-dimethyl-pyridin-2-yl)piperazin-1-yl.

[0181] In accordance with the above, it is particularly preferred that the moiety -N(-RA)-RBis selected from any one of the following groups / moieties:

[0182] An especially preferred example of the moiety -N(-RA)-RBis 2,2-dimethyl-4-(5-carboxy-4,6-dimethyl-pyridin-2- yl)piperazin-1-yl:

[0183] A further especially preferred example of the moiety -N(-RA)-RBis 3-methoxy-4-(carboxymethyl)piperidin-1 -yl:

[0184] A further especially preferred example of the moiety -N(-RA)-RBis 2,2-dimethyl-3-oxo-piperazin-1-yl:

[0185] Each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5alkyl), -(C0-3 alkylene)-P(=O)(-OH)(-OH), -(C0-3 alkylene)-P(=O)(-OH)(-O-Ci.5alkyl), -(C0-3 alkylene)-P(=O)(-O-Ci-5 alkyl)(-O-Ci-5 alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz.

[0186] Preferably, each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -CHO, -CO(Ci-5 alkyl), -COCH, -COO(Ci-5 alkyl), -O-CO(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci-5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci-5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5 alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -P(=O)(-OH)(-OH), -P(=O)(-OH)(-O-CI.5alkyl), -P(=O)(-O- C1-5 alkyl)(-O-Ci-5 alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz.

[0187] More preferably, each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI-5 alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -CHO, -CO(Ci-5 alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO(CI-5 alkyl), -N(CI.5alkyl)-CO(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO- NH(CI-5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz. Even more preferably, each R°rcis independently selected from C1-5 alkyl, -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)- OH, -O(Ci.5 alkylene)-O(Ci.5 alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci_5alkyl), halogen, C1.5 haloalkyl, -O-(Ci-5 haloalkyl), and -ON.

[0188] Each Lzis independently selected from a covalent bond, C1.7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more (e.g., one, two, or three) groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), and -N(CI-5 alkyl)(Ci-5 alkyl), and further wherein one or more (e.g., one, two, or three) -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-.

[0189] Preferably, each Lzis independently selected from a covalent bond, C1-5 alkylene, C2-5 alkenylene, and C2-5 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more (e.g., one, two, or three) groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -OH, -O(Ci.5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), and -N(CI.5alkyl)(Ci.5alkyl), and further wherein one or more (e.g., one, two, or three) -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-.

[0190] More preferably, each Lzis independently a covalent bond or C1-5 alkylene, wherein said alkylene is optionally substituted with one or more (e.g., one, two, or three) groups independently selected from halogen, C1-5 haloalkyl, -0- (C1.5 haloalkyl), -ON, -OH, -O(Ci.5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), and -N(CI.5alkyl)(Ci.5alkyl), and further wherein one or more (e.g., one, two, or three) -CH2- units comprised in said alkylene are each optionally replaced by a group independently selected from -0-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -S02-.

[0191] Each Rzis independently selected from -OH, -0(Ci-5 alkyl), -0(Ci-5 alkylene)-OH, -0(Ci-5 alkylene)-0(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -ON, -SF5, -OHO, -C0(Ci.5alkyl), -COOH, -C00(Ci.5alkyl), -0-C0(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -C0-N(CI-5 alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-C00(Ci.5 alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci.5 alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more (e.g., one, two or three) groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -0-(Ci-5 haloalkyl), -ON, -SF5, -OH, -0(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -OHO, -C0-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -0-C0-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-C0-(Ci.5 alkyl), -NH-COO(Ci.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5 alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci-5 alkyl), -S0-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(Ci_5alkyl)(Ci_5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5 alkyl), -N(Ci_5alkyl)-COO(Ci_5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), and -SO2-(Ci-5 alkyl).

[0192] Preferably, each Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 al ky lene)-OH , -O(Ci-5 al ky lene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci_5alkylene)-S(Ci.5alkyl), -NH2, -NH(Ci_5alkyl), -N(Ci_5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci_5haloalkyl), -CN, -CHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI-5 alkyl)(Ci_5alkyl), -NH-CO(CI.5alkyl), -N(Ci_5alkyl)-CO(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(Ci_5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(Ci.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more (e.g., one, two or three) groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -OH, -O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(Ci_5alkyl), and -N(Ci_5alkyl)(Ci_5alkyl).

[0193] For the compounds of formula (I), the following provisos apply:

[0194] If X is N, if R1is a group R11, and if R11is hydrogen, then R3is not a group -(C1-5 alkylene)-phenyl, wherein the alkylene group in said -(C1-5 alkylene)-phenyl is optionally substituted with one or more groups R31and wherein the phenyl group in said -(C1-5 alkylene)-phenyl is optionally substituted with one or more groups R32.

[0195] If X is N, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, and if RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a bicyclic fused heterocyclyl which is optionally substituted with one or more groups Rc, then the heterocyclyl formed from R1and R2is not a spirocyclic group which comprises a piperidine ring and is attached via the nitrogen ring atom of said piperidine ring.

[0196] If X is N, if one of RAand RBis hydrogen, and if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, then said heterocyclyl is not decahydroquinoxalin-1-yl or octahydro-1 H-cyclopenta[b]pyrazin-1-yl.

[0197] If X is N and if one of RAand RBis hydrogen, then R3is not phenyl which is optionally substituted with one or more groups R32.

[0198] If X is C(-R5), if one of RAand RBis hydrogen, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is piperazin-1 -yl and which is optionally substituted with one or more groups R24, then said piperazin-1 -yl is not substituted with 1 H-quinoxalin-2-on- 7-ylmethyl, wherein the 1 H-quinoxalin-2-on-7-yl group in said 1 H-quinoxalin-2-on-7-ylmethyl is optionally substituted with one or more groups RCyc. If R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups R24, if R3is C1-8 alkyl which is optionally substituted with one or more halogen atoms, and if one of RAand RBis hydrogen, then the other one of RAand RBis not methyl.

[0199] If X is N and if R3is phenyl which is substituted with one or more halogen atoms, then R1and R2are not mutually joined to form, together with the nitrogen atom that they are attached to, a group which is pyrrolidin- 1-yl or piperidin-1-yl.

[0200] If X is N, if R11is C1-5 alkyl, and if R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said C1-8 alkyl are each optionally replaced by -O-, then R3is not a cyclic group selected from phenyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, and azepanyl, wherein said cyclic group is optionally substituted with one or more halogen atoms.

[0201] If X is N and if R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said C1-8 alkyl are each optionally replaced by -O-, then R3is not a heterocycloalkyl comprising one or two nitrogen ring atoms, wherein all remaining ring atoms in said heterocycloalkyl are carbon atoms, and wherein said heterocycloalkyl is substituted with one or more groups R32.

[0202] If R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is imidazol-1-yl or 1 ,2,4-triazol-1-yl and which is optionally substituted with one or more groups R24, then R3is not C1-6 alkyl or -CF3.

[0203] If X is C(-R5) and if one of RAand RBis hydrogen, then the other one of RAand RBis not -NH-carbocyclyl or -NH-heterocyclyl, wherein the carbocyclyl in said -NH-carbocyclyl and the heterocyclyl in said -NH- heterocyclyl are each optionally substituted with one or more groups RCyc.

[0204] If R1is a group R11and R11is hydrogen, then R2is not -CO-NH-(1 ,2,3,4-tetrahydronaphthalen-1-yl), -CO- NH-(3',4'-dihydro-2'H-spiro[cyclopropane-1 , 1'-naphthalene]-4'-yl), -CO-NH-(3’,4’-dihydro-2’H- spiro[cyclobutane-1 ,1'-naphthalene]-4'-yl), -CO-NH-(3,4-dihydro-2H-spiro[naphthalene-1,3'-oxetane]-4-yl), -CO-NH-(3,4-dihydro-2H-spiro[naphthalene-1 , 2'-oxetane]-4-y I) or -CO-N H-(3’ ,4'-di hy d ro-2' H- spiro[azetidine-3,1'-naphthalene]-4'-yl), wherein the 1 ,2,3,4-tetrahydronaphthalen-1-yl in said -CO-NH- (1 ,2,3,4-tetrahydronaphthalen-1-yl), the 3',4'-dihydro-2'H-spiro[cyclopropane-1 ,1'-naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[cyclopropane-1 ,1'-naphthalene]-4'-yl), the 3’,4’-dihydro-2’H- spiro[cyclobutane-1 ,1'-naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[cyclobutane-1 ,T- naphthalene]-4'-yl), the 3,4-dihydro-2H-spiro[naphthalene-1 ,3'-oxetane]-4-yl in said -CO-NH-(3,4-dihydro- 2H-spiro[naphthalene-1 ,3'-oxetane]-4-yl), the 3,4-dihydro-2H-spiro[naphthalene-1 ,2'-oxetane]-4-yl in said -CO-NH-(3,4-dihydro-2H-spiro[naphthalene-1 ,2'-oxetane]-4-yl) and the 3',4'-dihydro-2'H-spiro[azetidine- 3,1'-naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[azetidine-3, 1'-naphthalene]-4'-yl) are each optionally substituted with one or more groups R23.

[0205] If R1is a group R11and if R11is hydrogen, then R2is not -CO-O-CH2-CCI3, -CO-O-phenyl, -CO-O-(4- methlyphenyl), -CO-O-(imidazol-l-yl), -CO-O-(pyrrolidin-2,5-dion-1-yl).

[0206] It is furthermore preferred that if X is N, if R1is a group R11, and if R11is hydrogen, then R3is not a C3-5 cycloalkyl which is substituted in 1 -position with phenyl, wherein said phenyl is optionally substituted with one or more groups RCy0. Moreover, it is preferred that if X is N and if R1is a group R11which is hydrogen or C1-5 alkyl, then R3is not a monocyclic heterocycloalkyl containing one or two nitrogen ring atoms, wherein all remaining ring atoms of said monocyclic heterocycloalkyl are carbon ring atoms, wherein said monocyclic heterocycloalkyl is substituted with -(C1-3 alkylene)- carbocyclyl, -(C1-3 alkylene)-heterocyclyl, -Lz-aryl, -Lz-heteroaryl, -Lz-cycloalkyl or -Lz-heterocycloalkyl, wherein the carbocyclyl in said -(C1-3 alkylene)-carbocyclyl and the heterocyclyl in said -(C1-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups Rc c, wherein the aryl in said -Lz-aryl, the heteroaryl in said -Lz- heteroaryl, the cycloalkyl in said -Lz-cycloal ky I and the heterocycloalkyl in said -Lz-heterocycloalky I are each optionally substituted, and wherein said monocyclic heterocycloalkyl is optionally further substituted with one or more groups R32. More preferably, if X is N and if R1is a group R11which is hydrogen or C1-5 alkyl, then R3is not a monocyclic heterocycloalkyl containing one or two nitrogen ring atoms, wherein all remaining ring atoms of said monocyclic heterocycloalkyl are carbon ring atoms, and wherein said monocyclic heterocycloalkyl is substituted with one or more groups R32. Even more preferably, if X is N, R1is a group R11, and R2is a group -L2-R21, then R3is not a monocyclic heterocycloalkyl containing one or two nitrogen ring atoms, wherein all remaining ring atoms of said monocyclic heterocycloalkyl are carbon ring atoms, and wherein said monocyclic heterocycloalkyl is optionally substituted with one or more groups R32.

[0207] It is further preferred that if X is N, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, and if RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a polycyclic fused heterocyclyl (I . e. , a heterocyclyl having a ring system with two or more fused rings) which is optionally substituted with one or more groups Rc, then the heterocyclyl formed from R1and R2(and from the nitrogen atom that R1and R2are attached to) is not a spirocyclic group.

[0208] It is furthermore preferred that if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups R24, and if one of RAand RBis hydrogen or C1-4 alkyl, then the other one of RAand RBis not hydrogen, C1-4 alkyl or cycloalkyl. Even more preferably, if one of RAand RBis hydrogen or C1-4 alkyl, then the other one of RAand RBis not hydrogen, C1-4 alkyl or cycloalkyl, wherein said cycloalkyl is optionally substituted with one or more groups RCyc.

[0209] It is also preferred that if one of RAand RBis methyl, then the other one of RAand RBis not hydrogen or methyl. Even more preferably, if one of RAand RBis C1-5 alkyl, then the other one of RAand RBis not hydrogen or C1-5 alkyl.

[0210] Moreover, it is preferred that if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is piperidin-1-yl and which is optionally substituted with one or more groups R24, if X is C(-R5), and if R3is C1-6 alkyl which is optionally substituted with one or more halogen atoms, then RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc. Even more preferably, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is piperidin-1-yl and which is optionally substituted with one or more groups R24, and if R3is C1-6 alkyl which is optionally substituted with one or more halogen atoms, then RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc.

[0211] As explained above, if X is N and if R3is phenyl which is substituted with one or more halogen atoms, then R1and R2are not mutually joined to form, together with the nitrogen atom that they are attached to, a group which is pyrrol id i n- 1-yl or piperidin-1-yl. It is furthermore preferred that if X is N, if R3is phenyl which is substituted with one or more halogen atoms, and if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups R24, then said heterocycloalkyl is not pyrrolidin-1-yl or piperidin-1-yl.

[0212] In a 1stspecific embodiment, the compound of formula (I) is a compound of the following formula (la) or a pharmaceutically acceptable salt or solvate thereof: wherein the groups / variables in formula (la) have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0213] In a 2ndspecific embodiment, the compound of formula (I) is a compound of the following formula (la-1) or a pharmaceutically acceptable salt or solvate thereof:

[0214] (la-1) wherein the groups / variables in formula (la-1) have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0215] In a 3rdspecific embodiment, the compound of formula (I) is a compound of the following formula (la-2) or a pharmaceutically acceptable salt or solvate thereof: (la-2) wherein the groups / variables in formula (la-2) have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0216] In a 4thspecific embodiment, the compound of formula (I) is a compound of the following formula (lb) or a pharmaceutically acceptable salt or solvate thereof: wherein the groups / variables in formula (lb) have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0217] In a 5thspecific embodiment, the compound of formula (I) is a compound of the following formula (lb-1) or a pharmaceutically acceptable salt or solvate thereof:

[0218] (lb-1) wherein the groups / variables in formula (lb-1) have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0219] In a 6thspecific embodiment, the compound of formula (I) is a compound of the following formula (lb-2) or a pharmaceutically acceptable salt or solvate thereof:

[0220] (lb-2) wherein the groups / variables in formula (lb-2) have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0221] In a 7thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond or C1-5 alkylene (e.g., -CH2- or -CH2CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) or phenyl, wherein said cycloalkyl or said phenyl is optionally substituted with one or more (e.g., one, two, or three) groups R23, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0222] In an 8thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is phenyl which is optionally substituted with one or more (e.g., one, two, or three) groups R23, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0223] In this specific embodiment, it is particularly preferred that R2is 3-R23-4-R23-phenyl or 3-R23-4-R23-5-R23-phenyl, wherein each R23is independently selected from halogen (e.g., -F, -Cl, -Br, or -I), C1-5 haloalkyl (e.g., -CF3), -SF5, and C1-5 alkyl (e.g., -CH3), even more preferably wherein each R23is independently selected from -F, -Cl, -CF3, and -CH3. Corresponding preferred examples of R2include 4-chloro-3-fluoro-phenyl, 3,4-dichloro-phenyl, 3,4-difluoro-phenyl, 3- chloro-4-fluoro-phenyl, 3-fluoro-4-trifluoromethyl-phenyl, 3-chloro-4-trifluoromethyl-phenyl, 3-fluoro-4-methyl-phenyl, 3-chloro-4-methyl-phenyl, 3,4,5-trifluoro-phenyl, or 4-chloro-3,5-difluoro-phenyl. Particularly preferred examples of R2are 4-chloro-3-fluoro-phenyl or 3,4-difluoro-phenyl.

[0224] In a 9thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is C1-5 alkylene (e.g., -CH2- or -CH2CH2-; preferably -CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) which is optionally substituted with one or more (e.g., one, two, or three) groups R23, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I). In a 10thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is -CH2-, wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0225] In an 11thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is C1-5 alkylene (e.g., -CH2- or -CH2CH2-; preferably -CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) which is optionally substituted with one or more (e.g., one, two, or three) groups R23, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0226] In a 12thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is -CH2-, wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0227] In a 13thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is C1-5 alkylene (e.g., -CH2- or -CH2CH2-; preferably -CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) which is optionally substituted with one or more (e.g., one, two, or three) groups R23, wherein R3is selected from C3-5 alkyl (e.g., isopropyl), cycloalkyl (e.g., cyclopropyl, cyclobutyl, or cyclopentyl), -CFh-cycloalkyl (e.g., -CF cyclopropyl, -CF cyclobutyl, or -CFh-cyclopentyl), heterocycloalkyl, and -CF heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CF cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CFh-heterocycloalkyl are each optionally substituted with one or more groups R32, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0228] In a 14thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is -CH2-, wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl), wherein R3is C3-5 alkyl (preferably isopropyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0229] In a 15thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is -CH2-, wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl), wherein R3is cycloalkyl or -CFh-cycloalkyl (preferably wherein R3is -CFh-cyclobutyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0230] In a 16thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is C1-5 alkylene (e.g., -CH2- or -CH2CH2-; preferably -CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) which is optionally substituted with one or more (e.g., one, two, or three) groups R23, wherein R3is selected from C3-5 alkyl (e.g., isopropyl), cycloalkyl (e.g., cyclopropyl, cyclobutyl, or cyclopentyl), -CFh-cycloalkyl (e.g., -CF cyclopropyl, -CF cyclobutyl, or -CFh-cyclopentyl), heterocycloalkyl, and -CF heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CF cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CFh-heterocycloalkyl are each optionally substituted with one or more groups R32, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0231] In a 17thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is C1-5 alkylene (e.g., -CH2- or -CH2CH2-; preferably -CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) which is optionally substituted with one or more (e.g., one, two, or three) groups R23, wherein R3is C3-5 alkyl (preferably isopropyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0232] In an 18thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is C1-5 alkylene (e.g., -CH2- or -CH2CH2-; preferably -CH2-), wherein R21is cycloalkyl (e.g., cyclopentyl or cyclohexyl; preferably cyclopentyl) which is optionally substituted with one or more (e.g., one, two, or three) groups R23, wherein R3is cycloalkyl or -CFh-cycloalkyl (preferably wherein R3is -CH2- cyclobutyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0233] In a 19thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is C1-8 alkyl (e.g., isobutyl or isopentyl; preferably isopentyl), wherein R3is selected from C3-5 alkyl (e.g., isopropyl), cycloalkyl (e.g., cyclopropyl, cyclobutyl, or cyclopentyl), -CFh-cycloalkyl (e.g., -CF cyclopropyl, -CF cyclobutyl, or -CFh-cyclopentyl), heterocycloalkyl, and -CH2-heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CF cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CFh-heterocycloalkyl are each optionally substituted with one or more groups R32, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0234] In a 20thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is C1-8 alkyl (e.g., isobutyl or isopentyl; preferably isopentyl), wherein R3is C3-5 alkyl (preferably isopropyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0235] In a 21stspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is C1-8 alkyl (e.g., isobutyl or isopentyl; preferably isopentyl), wherein R3is cycloalkyl or -CFh-cycloalkyl (preferably wherein R3is -CFh-cyclobutyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0236] In a 22ndspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is C1-8 alkyl (e.g., isobutyl or isopentyl; preferably isopentyl), wherein R3is selected from C3-5 alkyl (e.g., isopropyl), cycloalkyl (e.g., cyclopropyl, cyclobutyl, or cyclopentyl), -CFh-cycloalkyl (e.g., -CF cyclopropyl, -CF cyclobutyl, or -CFh-cyclopentyl), heterocycloalkyl, and -CH2-heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CF cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CFh-heterocycloalkyl are each optionally substituted with one or more groups R32, and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0237] In a 23rdspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is C1-8 alkyl (e.g., isobutyl or isopentyl; preferably isopentyl), wherein R3is C3-5 alkyl (preferably isopropyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0238] In a 24thspecific embodiment, the compound of formula (I) is a compound of the following formula or a pharmaceutically acceptable salt or solvate thereof: wherein R2is a group -L2-R21, wherein L2is a bond, wherein R21is C1-8 alkyl (e.g., isobutyl or isopentyl; preferably isopentyl), wherein R3is cycloalkyl or -CH2-cycloalkyl (preferably wherein R3is -CH2-cyclobutyl), and wherein all further groups / variables in this formula have the same meanings, including the same preferred meanings, as the corresponding groups / variables described with respect to formula (I).

[0239] In a 25thspecific embodiment, the compound of formula (I) is a compound of the following formula (Ic) or a pharmaceutically acceptable salt or solvate thereof: wherein:

[0240] R1is a group R11, and R2is a group -L2-R21;

[0241] R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -C0(Ci-5 alkyl);

[0242] L2is selected from a bond, C1-8 alkylene, C2-8 alkenylene, and C2-8 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups R22;

[0243] R21is selected from carbocyclyl and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23; each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci_5alkylene)-S(Ci.5alkyl), -NH2, -NH(Ci.5alkyl), -N(Ci_5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci_5haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5 alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(Ci_5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(Ci.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci.5 alkyl), -NH-SO2-(Ci.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups RCyc; each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alky lene)-0 H, -(C0-3 alky lene)-0 (C1-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;

[0244] R3is selected from C1-6 alkyl, -(C0-5 alkylene)-cycloalkyl, and -(C0-5 alkylene)-heterocyclyl, wherein the cycloalkyl group in said -(C0-5 alkylene)-cycloalkyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32; each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alky lene)-0 H, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;

[0245] R4is selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-NH(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-S0-(Ci-5 alkyl), -(C0-3 alkylene)-SC>2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;

[0246] RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc; each Rcis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 al ky lene)-OH , -(C0-3 alky lene)-0 (C1-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups RCyc; each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-C0(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5alkyl), -(C0.3alkylene)-P(=O)(-OH)(-OH), -(C0.3alkylene)-P(=O)(-OH)(-O-Ci.5alkyl), -(C0.3alkylene)-P(=0)(-0-Ci-5 alkyl)(-0-Ci-5 alkyl), -(Co-3alkylene)-cycloalkyl, -(Co-3alkylene)-heterocycloalkyl, and -Lz-Rz; each Lzis independently selected from a covalent bond, C1.7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), and -N(CI-5 alkyl)(Ci-5 alkyl), and further wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-; and each Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -CN, -SF5, -OHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI-5 alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci.5 alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -OHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI-5 alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(0I-5 alkyl)(Ci.5alkyl), -OHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI-5 alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), and -SO2-(Ci-5 alkyl).

[0247] It will be understood that the preferred meanings and exemplary options described for the groups / variables in formula (I) likewise apply to the corresponding groups / variables in formula (Ic), insofar as such preferred meanings and exemplary options are encompassed by the respective groups / variables defined in relation to formula (Ic).

[0248] In a 26thspecific embodiment, the compound of formula (I) is a compound of the following formula (Id) or a pharmaceutically acceptable salt or solvate thereof: wherein:

[0249] R1is a group R11, and R2is a group -L2-R21;

[0250] R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -C0(Ci-5 alkyl);

[0251] L2is a bond;

[0252] R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said alkyl are each optionally replaced by -O-; each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci_5alkylene)-S(Ci_5alkyl), -NH2, -NH(Ci.5alkyl), -N(Ci_5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci_5alkyl), halogen, C1.5 haloalkyl, -O-(Ci_5haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5 alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(Ci_5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5 alkyl), -O-CO-NH(Ci.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5 alkyl)(Ci-5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R°rc; each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alky lene)-0 H, -(C0-3 alky lene)-0 (C1-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups R°rc;

[0253] R3is C1-6 alkyl or -(C0-5 alkylene)-cycloalkyl, wherein the cycloalkyl group in said -(C0-5 alky lene)-cycloal kyl is optionally substituted with one or more groups R32; each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alky lene)-0 H, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-0(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-0(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;

[0254] R4is selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;

[0255] RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc; each Rcis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 al ky lene)-OH , -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFo, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-C0-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(Co-3 alkylene)-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-C0-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-C0-(Ci-5 alkyl), -(C0-3 alkylene)-NH-C00(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-C00(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-NH(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-S0-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups RCyc; each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-C0(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5alkyl), -(C0-3 alkylene)-P(=O)(-OH)(-OH), -(C0-3 alkylene)-P(=O)(-OH)(-O-Ci.5alkyl), -(C0-3 alkylene)-P(=O)(-O-Ci-5 alkyl)(-O-Ci-5 alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz; each Lzis independently selected from a covalent bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), and -N(CI-5 alkyl)(Ci-5 alkyl), and further wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-; and each Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci.5alkyl), -S(Ci.5alkylene)-SH, -S(Ci.5alkylene)-S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI.5alkyl)-O(Ci.5alkyl), halogen, C1.5 haloalkyl, -O-(Ci.5haloalkyl), -CN, -SP5, -CHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI-5alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci-5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI-5alkyl)(Ci-5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(Ci_5alkyl)(Ci.5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5 alkyl), -N(Ci_5alkyl)-COO(Ci_5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), -SO2-(Ci-5 alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -NH2, -NH(CI-5 alkyl), -N(CI-5 alkyl)(Ci_5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5alkyl), -NH-COO(CI-5 alkyl), -N(Ci_5alkyl)-COO(Ci_5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5 alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci-5 alkyl), and -SO2-(Ci-5 alkyl).

[0256] It will be understood that the preferred meanings and exemplary options described for the groups / variables in formula (I) likewise apply to the corresponding groups / variables in formula (Id), insofar as such preferred meanings and exemplary options are encompassed by the respective groups / variables defined in relation to formula (Id).

[0257] It is particularly preferred that the compound of formula (I) is any one of the specific compounds of formula (I) described in the examples section of this specification, including any one of Examples 1 to 275 described further below, either in non-salt form and / or non-solvated form, or as a pharmaceutically acceptable salt or solvate of the respective compound.

[0258] Accordingly, it is particularly preferred that the compound of formula (I) is selected from: 4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpicolinoyl)-3,3-dimethylpiperazin-2-one; 4-(5-((4-chloro-3-fluorophenyl)(methyl)amino)-6-cyclopentylpicolinoyl)-1 ,3,3-trimethylpiperazin-2-one; 4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpicolinoyl)-3,3-dimethylpiperazin-2-one; benzyl (6-(2,2-dimethyl-3-oxopiperazine-1-carbonyl)-2-(prop-1-en-2-yl)pyridin-3-yl)carbamate;

[0259] 1-(4-chloro-3-fluorophenyl)-4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-2- one;

[0260] 4-(5-((4-chloro-3-fluorophenyl)amino)-6-(difluoromethyl)picolinoyl)-3,3-dimethylpiperazin-2-one; 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-2-one; benzyl (6-(2,2-dimethyl-3-oxopiperazine-1-carbonyl)-2-(2-ethoxyvinyl)pyridin-3-yl)carbamate; 4-(5-((4-chloro-3-fluorophenyl)amino)-6-(2-ethoxyethyl)picolinoyl)-3,3-dimethylpiperazin-2-one; methyl 2-(1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)piperidin-4-yl)acetate;

[0261] 2-(1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)piperidin-4-yl)acetic acid; methyl 2-((3R,4S)-1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3-methoxypiperidin-4-yl)acetate; 2-((3R,4S)-1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3-methoxypiperidin-4-yl)acetic acid; methyl 6-(4-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 2-(6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)pyridin-3-yl)acetate; 2-(6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)pyridin-3- yl)acetic acid;

[0262] 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;

[0263] 4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(5-(isoindolin-2-yl)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(3,3-dimethyl-4-(5-((4-(pentafluorosulfanyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-1-yl)-2,4- dimethylnicotinate;

[0264] 6-(3,3-dimethyl-4-(5-((4-(pentafluorosulfanyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0265] 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0266] 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;

[0267] 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;

[0268] 3.3-dimethyl-4-(5-((4-(pentafluorosulfanyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-2-one; 4-(5-((4-chloro-3-fluorophenyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0269] 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0270] 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;

[0271] 3.3-dimethyl-4-(5-((4-(methylsulfonyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-2-one;

[0272] 4-(5-((4-chlorobenzyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;

[0273] 4-(6-benzyl-5-((4-chloro-3-fluorophenyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; 4-(5-((4,4-difluorocyclohexyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(5-(4,4-difluoropiperidin-1-yl)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; tert-butyl 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazine-1- carboxylate; (5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazin-2-yl)(2,2-dimethylpiperazin-1-yl)methanone;

[0274] 1-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)ethan-1-one; ethyl 2-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)acetate;

[0275] 2-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)acetic acid; ethyl 2-(2-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2-azabicyclo[2.2.1]heptan-5- yl)acetate; ethyl 2-(2-((5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carboxamido)methyl)cyclopentyl)acetate; 2-(2-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2-azabicyclo[2.2.1]heptan-5-yl)acetic acid; 2-(2-((5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carboxamido)methyl)cyclopentyl)acetic acid;

[0276] 4-(5-((4-chlorobenzyl)(methyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; tert-butyl 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazine-1- carboxylate;

[0277] 5-((4-chloro-3-fluorophenyl)amino)-6-isopropyl-N-methyl-N-(piperidin-4-yl)pyrazine-2-carboxamide; N-(1-acetylpiperidin-4-yl)-5-((4-chloro-3-fluorophenyl)amino)-6-isopropyl-N-methylpyrazine-2-carboxamide; 4-(5-((4-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((4-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0278] 6-(4-(5-((4-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; 4-(5-(benzylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-(benzylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(benzylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; N-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)-N- methylacetamide; N-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)-2,2,2-trifluoro- N-methylacetamide; 2-((1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)oxy)-N,N- dimethyl acetamide; methyl 6-(4-(5-(3,4-dihydroisoquinolin-2(1 H)-yl)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0279] 6-(4-(5-(3,4-dihydroisoquinolin-2(1 H)-yl)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; N-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)-N- methylmethanesulfonamide; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-(methoxymethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate; 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-(methoxymethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclohexylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; (5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazin-2-yl)(4-(2-(dimethylamino)ethoxy)-2,2-dimethylpiperidin-1- yl)methanone; ethyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-ethylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0280] 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0281] 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(tert-butyl)-5-((4-chloro-3-fluorophenyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-(tert-butyl)-5-((4-chloro-3-fluorophenyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(isopentylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(isopentylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid methyl (S)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; (S)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)phenethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)phenethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclohexylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((2-cyclohexylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl (R)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; (R)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl (R)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate;

[0282] (R)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-cyclobutyl-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid methyl 6-(4-(6-cyclobutyl-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-cyclobutyl-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(isobutylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(isobutylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2,3-dihydro-1 H-inden-2-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0283] 6-(4-(5-((2,3-dihydro-1 H-inden-2-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(tetrahydrofuran-3-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate;

[0284] 6-(4-(6-isopropyl-5-((2-(tetrahydrofuran-3-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopropylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopropylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl (R)-6-(4-(6-isopropyl-5-(((tetrahydrofuran-3-yl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;

[0285] (R)-6-(4-(6-isopropyl-5-(((tetrahydrofuran-3-yl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-methylpiperidin-4-yl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-(((1-methylpiperidin-4-yl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (R)-6-(4-(5-hydroxy-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; (R)-6-(4-(5-((cyclohexylmethyl)amino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (R)-6-(4-(5-(isopentylamino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; (R)-6-(4-(5-(isopentylamino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (R)-6-(4-(5-((4-fluorobenzyl)amino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0286] (R)-6-(4-(5-((4-fluorobenzyl)amino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((3-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((3-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(4-methoxycyclohexyl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-(4-methoxycyclohexyl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(isopentylamino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0287] 6-(4-(5-(isopentylamino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(cyclopropylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-(cyclopropylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl (S)-6-(4-(6-isopropyl-5-((2-phenylpropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0288] (S)-6-(4-(6-isopropyl-5-((2-phenylpropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-fluorobenzyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate; 6-(4-(5-((4-fluorobenzyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-(cyclopropylmethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0289] 6-(4-(5-((cyclohexylmethyl)amino)-6-(cyclopropylmethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;

[0290] 6-(4-(5-((cyclohexylmethyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(cyclobutylmethyl)-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0291] 6-(4-(6-(cyclobutylmethyl)-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(ethylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(ethylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclopropoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((2-cyclopropoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclopropylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((2-cyclopropylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(cyclobutylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-(cyclobutylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-(cyclobutylmethyl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0292] 6-(4-(6-(cyclobutylmethyl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(3-methoxybicyclo[1 .1 .1]pentan-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-(3-methoxybicyclo[1 .1 .1]pentan-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n i c acid; methyl 6-(4-(5-(butylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(butylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((3-methoxycyclobutyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((3-methoxycyclobutyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4,4-difluorobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((4,4-difluorobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0293] 6-(4-(5-((4-chloro-3-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((3,3-difluorocyclobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((3,3-difluorocyclobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2,3-dihydrobenzofuran-3-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0294] 6-(4-(5-((2,3-dihydrobenzofuran-3-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (S)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate;

[0295] (S)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((cyclobutylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0296] 6-(4-(5-((cyclobutylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-methylcyclobutyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0297] 6-(4-(6-isopropyl-5-(((1-methylcyclobutyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(chroman-4-ylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(chroman-4-ylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-cyclopropyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclopropyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(neopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-(neopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclobutyl-2-methoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-

[0298] 2.4-dimethylnicotinate;

[0299] 6-(4-(5-((2-cyclobutyl-2-methoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-cyclopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0300] 6-(4-(6-cyclopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclohexylmethyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((4-methoxybenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((4-methoxybenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2-(1 ,3-dihydroisobenzofuran-5-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-((2-(1 ,3-dihydroisobenzofuran-5-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-

[0301] 2.4-dimethy Inicotinic acid; methyl 6-(4-(5-(((S)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(((S)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((R)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(((R)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((3,3-dimethylbutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((3,3-dimethylbutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(tetrahydro-2H-pyran-4-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-(tetrahydro-2H-pyran-4-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(((2,3-dihydrobenzo[b][1 ,4]dioxin-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-(((2,3-dihydrobenzo[b][1 ,4]dioxin-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n i c acid; methyl 6-(4-(6-isopropyl-5-((pyrazin-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0302] 6-(4-(6-isopropyl-5-((pyrazin-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((3-chlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0303] 6-(4-(6-isopropyl-5-((pyrazin-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2,4-dichlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0304] 6-(4-(5-((2,4-dichlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2-(1 H-pyrazol-1-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0305] 6-(4-(5-((2-(1 H-pyrazol-1-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(1-methyl-1 H-pyrazol-3-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;

[0306] 6-(4-(6-isopropyl-5-((2-(1-methyl-1 H-pyrazol-5-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-(methoxymethyl)cyclopentyl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-(((1-(methoxymethyl)cyclopentyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-

[0307] 2,4-dimethy Inicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0308] 6-(4-(6-isopropyl-5-(((1-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((4-(trifluoromethyl)cyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n ate;

[0309] 6-(4-(6-isopropyl-5-(((4-(trifluoromethyl)cyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-

[0310] 2.4-dimethy Inicotinic acid; methyl 6-(4-(5-(((4,4-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-

[0311] 2.4-dimethylnicotinate; 6-(4-(5-(((4,4-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-morpholinopyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-morpholinopyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(piperidin-1-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-(piperidin-1-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((4-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0312] 6-(4-(6-isopropyl-5-(((4-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(((3,3-difluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate;

[0313] 6-(4-(5-(((3,3-difluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(((3,3-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethylnicotinate;

[0314] 6-(4-(5-(((3,3-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(((1 ,4-dioxan-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0315] 6-(4-(5-(((1 ,4-dioxan-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(2-oxopyrrolidin-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0316] 6-(4-(6-isopropyl-5-((2-(2-oxopyrrolidin-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-morpholinocyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;

[0317] 6-(4-(6-isopropyl-5-(((1-morpholinocyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;

[0318] 4-(6-(cyclohex-1-en-1-yl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(6-(cyclobutylethynyl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(5-(isopentylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;

[0319] 4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;

[0320] 4-(5-((cyclohexylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(6-isopropyl-5-((thiazol-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(6-isopropyl-5-((thiophen-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((thiophen-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((thiophen-3-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((thiophen-3-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-3- methylpicolinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-3-methylpicolinic acid; methyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-5- methylthiazole-4-carboxylate; 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-5-methylthiazole-4- carboxylic acid; ethyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4- methylthiazole-5-carboxylate; 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4-methylthiazole-5- carboxylic acid; methyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)thiazole-4- carboxylate; 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)thiazole-4-carboxylic acid; 4-(5-((cyclopentylmethyl)amino)-6-((trimethylsilyl)ethynyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-4-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-4-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((3-fluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(((3-fluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; 4-(6-isopropyl-5-((2-methoxybenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)thiazole-4- carboxamide; 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-5-methylthiazole-4- carboxamide; methyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4,6- dimethylpyrimidine-5-carboxylate; 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4,6- dimethylpyrimidine-5-carboxylic acid; (5-((cyclopentylmethyl)amino)-6-isopropylpyrazin-2-yl)(2,2-dimethylpiperidin-1-yl)methanone; (5-((cyclopentylmethyl)amino)-6-isopropylpyrazin-2-yl)(3,3-dimethylmorpholino)methanone; 4-(5-((4-chlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;

[0321] 4-(5-((cyclopentylmethyl)amino)-6-ethynylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-3-fluoro-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0322] 6-(4-(5-((cyclopentylmethyl)amino)-3-fluoro-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methoxypicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methoxypicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 5-bromo-6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;

[0323] 5-bromo-6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; 4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-(trifluoromethyl)picolinoyl)-3,3-dimethylpiperazin-2-one; 4-(4-bromo-5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-2-one; or a pharmaceutically acceptable salt or solvate of any one of the above-mentioned compounds.

[0324] The present invention also relates to each of the intermediates described further below in the examples section of this specification, including any one of these intermediates in non-salt form and / or non-solvated form, or in the form of a salt or solvate (e.g., a pharmaceutically acceptable salt or solvate) of the respective compound. Such intermediates can be used, in particular, in the synthesis of the compounds of formula (I).

[0325] For a person skilled in the field of synthetic chemistry, various ways for the preparation of the compounds of general formula (I) and their pharmaceutically acceptable salts and solvates will be readily apparent. For example, the compounds of the invention can be prepared in accordance with, or in analogy to, the synthetic routes described in detail in the examples section. In particular, the compounds of formula (I) can be synthesized in accordance with the methods described in the following general schemes (general disconnections).

[0326] Schematic overview:

[0327] Compounds of formula (I) can be obtained from a precursor (ll)-A according to the general disconnection A:

[0328] With Z1being a hydroxy group (based on the work described in Org. Process Res. Dev. 2004, 8, 62-71 or Tet. Lett., 1992, 33, 1181-1184):

[0329] By a transformation or sequence known to the person skilled in the art of Z1into a hydrogen, a halogen or a pseudo-halogen, followed by a transformation or a sequence described below.

[0330] With Z1being a hydrogen atom (based on the work described in ARKIVOC 2013, 1 , 154-174, ARKIVOC 2001, 1 , 242-268, Synthesis 2011, 20, 3209-3219, Adv. Synth. Catal. 2021, 363, 2-39, Angew. Chem. 2020, 132, 2 - 26, or Chem. Rev. 2017, 117, 9302-9332):

[0331] By N-oxidation followed by a sequence leading to the conversion of Z1into a halogen or a pseudo-halogen, followed by a transformation or a sequence described below.

[0332] By carbon-hydrogen bond activation with a metal leading to the conversion of Z1into a halogen, a pseudohalogen, or an organometallic group, followed by a transformation or a sequence described below.

[0333] By a transformation or sequence known to the person skilled in the art of Z1into a halogen or pseudohalogen, followed by a transformation or a sequence described below.

[0334] With Z1being a halogen or pseudo-halogen (based on the work described in Org. Biomol. Chem., 2013, 11 , 3583- 3602):

[0335] By a nucleophilic aromatic substitution with the appropriate organometallic partner. By a metal catalyzed coupling with the appropriate organometallic or halogenated or pseudo-halogenated partner.

[0336] By halogen-metal exchange followed by the nucleophilic substitution with the appropriate electrophile, or by the metal catalyzed coupling with the appropriate organometallic or halogenated or pseudo-halogenated partner.

[0337] Compounds of formula (I) can be obtained from a precursor (ll)-B according to the general disconnection B:

[0338] With Z2being a hydroxy group (based on the work described in Org. Process Res. Dev. 2004, 8, 62-71 , Comprehensive Heterocyclic Chemistry II, Volume 6, 1996, Pages 233-278, or Tet. Lett., 1992, 33, 1181-1184):

[0339] By a transformation or sequence known to the person skilled in the art of Z2into a hydrogen, a halogen or a pseudo-halogen, followed by a transformation or a sequence described below.

[0340] With Z2being a hydrogen atom (based on the work described in ARKIVOC 2013, 1 , 154-174, ARKIVOC 2001, 1 , 242-268 or Synthesis 2011, 20, 3209-3219):

[0341] By N-oxidation followed by a sequence leading to the conversion of Z2into a halogen or a pseudo-halogen, followed by a transformation or a sequence described below.

[0342] By carbon-hydrogen bond activation with a metal leading to the conversion of Z2into a halogen, a pseudohalogen, or an organometallic group, followed by a transformation or a sequence described below.

[0343] With Z2being a halogen or pseudo-halogen (based on the worked described in Org. Biomol. Chem., 2013, 11, 3583- 3602):

[0344] By a nucleophilic aromatic substitution with the appropriate amine or aniline partner.

[0345] By a metal catalyzed coupling with the appropriate amine or aniline.

[0346] By halogen-metal exchange followed by the nucleophilic substitution with the appropriate electrophile, or by the metal catalyzed coupling with the appropriate amine or aniline.

[0347] Compounds of formula (I) can be obtained from a precursor (ll)-C according to the general disconnection C:

[0348] With a partner containing a carbonyl:

[0349] By a reductive amination reaction or amide synthesis known to the person skilled in the art.

[0350] By a Petasis reaction (based on the works described in Chem. Rev. 2019, 119, 11245-11290, or RSC Adv., 2015, 5, 76337-76341). With a partner containing a halogen or pseudo-halogen, or an organometallic group:

[0351] By a nucleophilic substitution known to the person skilled in the art.

[0352] By a metal catalyzed coupling reaction (based on the works described in Chem. Rev. 2016, 116, 19, 12564— 12649, Chem. See. Rev., 2014, 43, 3525-3550 or Chem. Rev. 2019, 119, 24, 12491-12523).

[0353] Compounds of formula (I) can be obtained from a precursor (ll)-D according to the general disconnection D:

[0354] With Z3being a hydrogen atom (based on the work described in ARKIVOC 2013, 1 , 154-174, ARKIVOC 2001, 1 , 242-268 or Synthesis 2011, 20, 3209-3219):

[0355] By N-oxidation followed by a sequence leading to the carboxylic acid, and subsequent amide synthesis with the appropriate amine.

[0356] By N-oxidation followed by a sequence leading to the conversion of Z3into a halogen or a pseudo-halogen, followed by a transformation or a sequence described below.

[0357] By carbon-hydrogen bond activation with a metal leading to the conversion of Z3into a halogen, a pseudohalogen, or an organometallic group, followed by a transformation or a sequence described below.

[0358] With Z3being a hydroxy group (based on the work described in Org. Process Res. Dev. 2004, 8, 62-71 or Tet. Lett., 1992, 33, 1181-1184):

[0359] By a transformation or sequence known to the person skilled in the art of Z3into a halogen or pseudohalogen, followed by a transformation or a sequence described below.

[0360] With Z3being a halogen or a pseudo-halogen, or an organometallic group (based on the worked described in Org. Biomol. Chem., 2013, 11 , 3583-3602):

[0361] By a direct, metal catalyzed amino-carbonylation reaction with the appropriate amine (based on the work described in RSC Adv., 2014, 4, 10367-10389 or Synthesis, 2008, 311-312).

[0362] By a transformation or a sequence known to the person skilled in the art leading to a carboxylic, followed by amide, synthesis with the appropriate amine (based on the work described in J. Org. Chem., 2008, 73, 3967- 3969).

[0363] Compounds of formula (I) can be obtained from a precursor (ll)-E according to the general disconnection E:

[0364] With the link containing an unsaturation:

[0365] By oxidative cleavage of the double bond.

[0366] By reductive cleavage of the carbon nitrogen bond. With the link containing a carbonyl:

[0367] By oxidation of the ketone to the ester (Baeyer-Villiger oxidation) and subsequent ester cleavage.

[0368] By acidic or basic hydrolysis of the amide generating the amino-acid, potentially followed by a decarboxylation.

[0369] Or the compounds of formula (I) can be obtained by any other disconnection reaction known to the person skilled in the art.

[0370] Using and combining the above-mentioned general disconnections A, B, C, D, E, and available literature, enables the synthesis of compounds of formula (I) from commercially available compounds or from compounds whose synthesis is already described in the literature or compounds which are accessible with a method known in the art.

[0371] The following definitions apply throughout the present specification and the claims, unless specifically indicated otherwise.

[0372] The term "hydrocarbon group” refers to a group consisting of carbon atoms and hydrogen atoms.

[0373] The term "alicyclic” is used in connection with cyclic groups and denotes that the corresponding cyclic group is non-aromatic.

[0374] As used herein, the term "alkyl” refers to a monovalent saturated acyclic (i.e., non-cyclic) hydrocarbon group which may be linear or branched. Accordingly, an "alkyl” group does not comprise any carbon-to-carbon double bond or any carbon-to-carbon triple bond. A“CI-5 alkyl” denotes an alkyl group having 1 to 5 carbon atoms. Preferred exemplary alkyl groups are methyl, ethyl, propyl (e.g., n-propyl or isopropyl), or butyl (e.g., n-butyl, isobutyl, sec-butyl, or tertbutyl). Unless defined otherwise, the term "alkyl” preferably refers to C1-4 alkyl, more preferably to methyl or ethyl, and even more preferably to methyl.

[0375] As used herein, the term "alkenyl” refers to a monovalent unsaturated acyclic hydrocarbon group which may be linear or branched and comprises one or more (e.g., one or two) carbon-to-carbon double bonds while it does not comprise any carbon-to-carbon triple bond. The term "C2-5 alkenyl” denotes an alkenyl group having 2 to 5 carbon atoms. Preferred exemplary alkenyl groups are ethenyl, propenyl (e.g., prop-1 -en-1-yl, prop-1 -en-2-yl, or prop-2-en-1-yl), butenyl, butadienyl (e.g., buta-1 ,3-dien-1-yl or buta-1 ,3-dien-2-yl), pentenyl, or pentadienyl (e.g., isoprenyl). Unless defined otherwise, the term "alkenyl” preferably refers to C2-4 alkenyl.

[0376] As used herein, the term “alky ny I” refers to a monovalent unsaturated acyclic hydrocarbon group which may be linear or branched and comprises one or more (e.g., one or two) carbon-to-carbon triple bonds and optionally one or more (e.g., one or two) carbon-to-carbon double bonds. The term "C2-5 alkynyl” denotes an alkynyl group having 2 to 5 carbon atoms. Preferred exemplary alkynyl groups are ethynyl, propynyl (e.g., propargyl), or butynyl. Unless defined otherwise, the term "alkynyl” preferably refers to C2-4 alkynyl. As used herein, the term "alkylene” refers to an alkanediyl group, i.e. a divalent saturated acyclic hydrocarbon group which may be linear or branched. A “C1-5 alkylene” denotes an alkylene group having 1 to 5 carbon atoms, and the term "C0-3 alkylene” indicates that a covalent bond (corresponding to the option "Co alkylene”) or a C1-3 alkylene is present. Preferred exemplary alkylene groups are methylene (-CH2-), ethylene (e.g., -CH2-CH2- or -CH(-CH3)-), propylene (e.g., -CH2-CH2-CH2-, -CH(-CH2-CH3)-, -CH2-CH(-CH3)-, or -CH(-CH3)-CH2-), or butylene (e.g., -CH2-CH2- CH2-CH2-). Unless defined otherwise, the term "alkylene” preferably refers to C1-4 alkylene (including, in particular, linear C1-4 alkylene), more preferably to methylene or ethylene, and even more preferably to methylene.

[0377] As used herein, the term "alkenylene” refers to an alkenediyl group, i.e. a divalent unsaturated acyclic hydrocarbon group which may be linear or branched and comprises one or more (e.g., one or two) carbon-to-carbon double bonds while it does not comprise any carbon-to-carbon triple bond. A "C2-5 alkenylene” denotes an alkenylene group having 2 to 5 carbon atoms. Unless defined otherwise, the term "alkenylene” preferably refers to C2-4 alkenylene (including, in particular, linear C2-4 alkenylene).

[0378] As used herein, the term "alkynylene” refers to an alkynediyl group, i.e. a divalent unsaturated acyclic hydrocarbon group which may be linear or branched and comprises one or more (e.g., one or two) carbon-to-carbon triple bonds and optionally one or more (e.g., one or two) carbon-to-carbon double bonds. A "C2-5 alkynylene” denotes an alkynylene group having 2 to 5 carbon atoms. Unless defined otherwise, the term "alkynylene” preferably refers to C2-4 alkynylene (including, in particular, linear C2-4 alkynylene).

[0379] As used herein, the term "carbocyclyl” refers to a hydrocarbon ring group, including monocyclic rings as well as bridged ring, spiro ring and / or fused ring systems (which may be composed, e.g., of two or three rings), wherein said ring group may be saturated, partially unsaturated (i.e., unsaturated but not aromatic) or aromatic. Unless defined otherwise, "carbocyclyl” preferably refers to aryl, cycloalkyl or cycloalkenyl.

[0380] As used herein, the term “heterocyclyl” refers to a ring group, including monocyclic rings as well as bridged ring, spiro ring and / or fused ring systems (which may be composed, e.g., of two or three rings), wherein said ring group comprises one or more (such as, e.g., one, two, three, or four) ring heteroatoms independently selected from 0, S and N, and the remaining ring atoms are carbon atoms, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) may optionally be oxidized, wherein one or more carbon ring atoms may optionally be oxidized (i.e., to form an oxo group), and further wherein said ring group may be saturated, partially unsaturated (i.e., unsaturated but not aromatic) or aromatic. For example, each heteroatom-containing ring comprised in said ring group may contain one or two 0 atoms and / or one or two S atoms (which may optionally be oxidized) and / or one, two, three or four N atoms (which may optionally be oxidized), provided that the total number of heteroatoms in the corresponding heteroatom-containing ring is 1 to 4 and that there is at least one carbon ring atom (which may optionally be oxidized) in the corresponding heteroatom-containing ring. Unless defined otherwise, "heterocyclyl” preferably refers to heteroaryl, heterocycloalkyl or heterocycloalkenyl.

[0381] As used herein, the term "aryl” refers to an aromatic hydrocarbon ring group, including monocyclic aromatic rings as well as bridged ring and / or fused ring systems containing at least one aromatic ring (e.g., ring systems composed of two or three fused rings, wherein at least one of these fused rings is aromatic; or bridged ring systems composed of two or three rings, wherein at least one of these bridged rings is aromatic). If the aryl is a bridged and / or fused ring system which contains, besides one or more aromatic rings, at least one non-aromatic ring (e.g., a saturated ring or an unsaturated alicyclic ring), then one or more carbon ring atoms in each non-aromatic ring may optionally be oxidized (i.e., to form an oxo group). "Aryl” may, e.g., refer to phenyl, naphthyl, dialinyl (i.e., 1 ,2-dihydronaphthyl), tetralinyl (i.e., 1 ,2,3,4-tetrahydronaphthyl), indanyl, indenyl (e.g., 1 H-indenyl), anthracenyl, phenanthrenyl, 9H- fluorenyl, or azulenyl. Unless defined otherwise, an "aryl” preferably has 6 to 14 ring atoms, more preferably 6 to 10 ring atoms, even more preferably refers to phenyl or naphthyl, and most preferably refers to phenyl.

[0382] As used herein, the term "heteroaryl” refers to an aromatic ring group, including monocyclic aromatic rings as well as bridged ring and / or fused ring systems containing at least one aromatic ring (e.g., ring systems composed of two or three fused rings, wherein at least one of these fused rings is aromatic; or bridged ring systems composed of two or three rings, wherein at least one of these bridged rings is aromatic), wherein said aromatic ring group comprises one or more (such as, e.g., one, two, three, or four) ring heteroatoms independently selected from 0, S and N, and the remaining ring atoms are carbon atoms, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) may optionally be oxidized, and further wherein one or more carbon ring atoms may optionally be oxidized (i.e., to form an oxo group). For example, each heteroatom-containing ring comprised in said aromatic ring group may contain one or two 0 atoms and / or one or two S atoms (which may optionally be oxidized) and / or one, two, three or four N atoms (which may optionally be oxidized), provided that the total number of heteroatoms in the corresponding heteroatom-containing ring is 1 to 4 and that there is at least one carbon ring atom (which may optionally be oxidized) in the corresponding heteroatom-containing ring. "Heteroaryl” may, e.g., refer to thienyl (i.e., thiophenyl), benzo[b]thienyl, naphtho[2,3-b]thienyl, thianthrenyl, furyl (i.e., furanyl), benzofuranyl, isobenzofuranyl, chromanyl, chromenyl (e.g., 2H-1 -benzopyranyl or 4H-1 -benzopyranyl), isochromenyl (e.g., 1 H-2-benzopyranyl), chromonyl, xanthenyl, phenoxathiinyl, pyrrolyl (e.g., 1 H-pyrrolyl), imidazolyl, pyrazolyl, pyridyl (i.e., pyridinyl; e.g., 2-pyridyl, 3-pyridyl, or 4-pyridyl), pyrazinyl, pyrimidinyl, pyridazinyl, indolyl (e.g., 1 H-indolyl), isoindolyl, indazolyl, indolizinyl, purinyl, quinolyl, isoquinolyl, phthalazinyl, naphthyridinyl, quinoxalinyl, cinnolinyl, pteridinyl, carbazolyl, p-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl (e.g., [1 ,10]phenanthrolinyl, [1,7]phenanthrolinyl, or [4,7]phenanthrolinyl), phenazinyl, thiazolyl, isothiazolyl, phenothiazinyl, oxazolyl, isoxazolyl, oxadiazolyl (e.g.,

[0383] 1.2.4-oxadiazolyl, 1 ,2,5-oxadiazolyl (i.e., furazanyl), or 1 ,3,4-oxadiazolyl), thiadiazolyl (e.g., 1 ,2,4-thiadiazolyl, 1,2,5- thiadiazolyl, or 1 ,3,4-thiadiazolyl), phenoxazinyl, pyrazolo[1,5-a]pyrimidinyl (e.g., pyrazolo[1 ,5-a]pyrimidin-3-yl), 1 ,2-benzoisoxazol-3-yl, benzothiazolyl, benzothiadiazolyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzo[b]thiophenyl (i.e., benzothienyl), triazolyl (e.g., 1 H-1,2,3-triazolyl, 2H-1 ,2,3-triazolyl, 1 H-1 ,2,4-triazolyl, or 4H-

[0384] 1.2.4-triazolyl), benzotriazolyl, 1 H-tetrazolyl, 2H-tetrazolyl, triazinyl (e.g., 1 ,2,3-triazinyl, 1 ,2,4-triazinyl, or 1,3,5- triazinyl), furo[2,3-c]pyridinyl, dihydrofuropyridinyl (e.g., 2,3-dihydrofuro[2,3-c]pyridinyl or 1 ,3-dihydrofuro[3,4- c]pyridinyl), imidazopyridinyl (e.g., imidazo[1 ,2-a]pyridinyl or imidazo[3,2-a]pyridinyl), quinazolinyl, thienopyridinyl, tetrahydrothienopyridinyl (e.g., 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl), dibenzofuranyl, 1 ,3-benzodioxolyl, benzodioxanyl (e.g., 1,3-benzodioxanyl or 1 ,4-benzodioxanyl), or coumarinyl. Unless defined otherwise, the term "heteroaryl” preferably refers to a 5 to 14 membered (more preferably 5 to 10 membered) monocyclic ring or fused ring system comprising one or more (e.g., one, two, three or four) ring heteroatoms independently selected from 0, S and N, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) are optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized; even more preferably, a "heteroaryl” refers to a 5 or 6 membered monocyclic ring comprising one or more (e.g., one, two or three) ring heteroatoms independently selected from 0, S and N, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) are optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized. Moreover, unless defined otherwise, particularly preferred examples of a "heteroaryl” include pyridinyl (e.g., 2-pyridyl, 3-pyridyl, or 4-pyridyl), imidazolyl, thiazolyl, 1 H-tetrazolyl, 2H-tetrazolyl, thienyl (i.e., thiophenyl), or pyrimidinyl.

[0385] As used herein, the term “cycloalky I” refers to a saturated hydrocarbon ring group, including monocyclic rings as well as bridged ring, spiro ring and / or fused ring systems (which may be composed, e.g., of two or three rings; such as, e.g., a fused ring system composed of two or three fused rings). "Cycloalkyl” may, e.g., refer to cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, decalinyl (i.e., decahydronaphthyl), or adamantyl. Unless defined otherwise, "cycloalkyl” preferably refers to a C3-11 cycloalkyl, and more preferably refers to a C3-7 cycloalkyl. A particularly preferred "cycloalkyl” is a monocyclic saturated hydrocarbon ring having 3 to 7 ring members. Moreover, unless defined otherwise, particularly preferred examples of a "cycloalkyl” include cyclohexyl or cyclopropyl, particularly cyclohexyl.

[0386] As used herein, the term “heterocycloalkyl” refers to a saturated ring group, including monocyclic rings as well as bridged ring, spiro ring and / or fused ring systems (which may be composed, e.g., of two or three rings; such as, e.g., a fused ring system composed of two or three fused rings), wherein said ring group contains one or more (such as, e.g., one, two, three, or four) ring heteroatoms independently selected from 0, S and N, and the remaining ring atoms are carbon atoms, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) may optionally be oxidized, and further wherein one or more carbon ring atoms may optionally be oxidized (i.e., to form an oxo group). For example, each heteroatom-containing ring comprised in said saturated ring group may contain one or two 0 atoms and / or one or two S atoms (which may optionally be oxidized) and / or one, two, three or four N atoms (which may optionally be oxidized), provided that the total number of heteroatoms in the corresponding heteroatomcontaining ring is 1 to 4 and that there is at least one carbon ring atom (which may optionally be oxidized) in the corresponding heteroatom-containing ring. "Heterocycloalkyl” may, e.g., refer to aziridinyl, azetidinyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, piperidinyl, piperazinyl, piperazinonyl (e.g., piperazin-2-on-1-yl or piperazin-3-on-1-yl), azepanyl, diazepanyl (e.g., 1 ,4-diazepanyl), oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, morpholinyl (e.g., morpholin-4-yl), thiomorpholinyl (e.g., thiomorpholin-4-yl), oxazepanyl, oxiranyl, oxetanyl, tetrahydrofuranyl,

[0387] 1.3-dioxolanyl, tetrahydropyranyl, 1 ,4-dioxanyl, oxepanyl, thiiranyl, thietanyl, tetrahydrothiophenyl (i.e., thiolanyl),

[0388] 1.3-dithiolanyl, thianyl, thiepanyl, decahydroquinolinyl, decahydroisoquinolinyl, or 2-oxa-5-aza-bicyclo[2.2.1]hept-5- yl. Unless defined otherwise, "heterocycloalkyl” preferably refers to a 3 to 11 membered saturated ring group, which is a monocyclic ring or a fused ring system (e.g., a fused ring system composed of two fused rings), wherein said ring group contains one or more (e.g., one, two, three, or four) ring heteroatoms independently selected from 0, S and N, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) are optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized; more preferably, "heterocycloalkyl” refers to a 5 to 7 membered saturated monocyclic ring group containing one or more (e.g., one, two, or three) ring heteroatoms independently selected from 0, S and N, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) are optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized. Moreover, unless defined otherwise, particularly preferred examples of a “heterocycloalky I” include tetrahydropyranyl, piperidinyl, piperazinyl, piperazinonyl, morpholinyl, pyrrolidinyl, or tetrahydrofuranyl.

[0389] As used herein, the term “cycloalkenyl” refers to an unsaturated alicyclic (non-aromatic) hydrocarbon ring group, including monocyclic rings as well as bridged ring, spiro ring and / or fused ring systems (which may be composed, e.g., of two or three rings; such as, e.g., a fused ring system composed of two or three fused rings), wherein said hydrocarbon ring group comprises one or more (e.g., one or two) carbon-to-carbon double bonds and does not comprise any carbon-to-carbon triple bond. "Cycloalkenyl” may, e.g., refer to cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclohexenyl, cyclohexadienyl, cycloheptenyl, or cycloheptadienyl. Unless defined otherwise, "cycloalkenyl” preferably refers to a C3-11 cycloalkenyl, and more preferably refers to a C3-7 cycloalkenyl. A particularly preferred "cycloalkenyl” is a monocyclic unsaturated alicyclic hydrocarbon ring having 3 to 7 ring members and containing one or more (e.g., one or two; preferably one) carbon-to-carbon double bonds.

[0390] As used herein, the term "heterocycloal keny I” refers to an unsaturated alicyclic (non-aromatic) ring group, including monocyclic rings as well as bridged ring, spiro ring and / or fused ring systems (which may be composed, e.g., of two or three rings; such as, e.g., a fused ring system composed of two or three fused rings), wherein said ring group contains one or more (such as, e.g., one, two, three, or four) ring heteroatoms independently selected from 0, S and N, and the remaining ring atoms are carbon atoms, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) may optionally be oxidized, wherein one or more carbon ring atoms may optionally be oxidized (i.e., to form an oxo group), and further wherein said ring group comprises at least one double bond between adjacent ring atoms and does not comprise any triple bond between adjacent ring atoms. For example, each heteroatom-containing ring comprised in said unsaturated alicyclic ring group may contain one or two 0 atoms and / or one or two S atoms (which may optionally be oxidized) and / or one, two, three or four N atoms (which may optionally be oxidized), provided that the total number of heteroatoms in the corresponding heteroatom-containing ring is 1 to 4 and that there is at least one carbon ring atom (which may optionally be oxidized) in the corresponding heteroatomcontaining ring. "Heterocycloalkenyl” may, e.g., refer to imidazolinyl (e.g., 2-imidazolinyl (i.e., 4,5-dihydro-1 H- imidazolyl), 3-imidazolinyl, or 4-imidazolinyl), tetrahydropyridinyl (e.g., 1 ,2,3,6-tetrahydropyridinyl), dihydropyridinyl (e.g., 1 ,2-dihydropyridinyl or 2,3-dihydropyridinyl), pyranyl (e.g., 2H-pyranyl or 4H-pyranyl), thiopyranyl (e.g., 2H-thiopyranyl or 4H-thiopyranyl), dihydropyranyl, dihydrofuranyl, dihydropyrazolyl, dihydropyrazinyl, dihydroisoindolyl, octahydroquinolinyl (e.g., 1 ,2,3,4,4a,5,6,7-octahydroquinolinyl), or octahydroisoquinolinyl (e.g., 1 ,2,3,4,5,6,7,8-octahydroisoquinolinyl). Unless defined otherwise, "heterocycloalkenyl” preferably refers to a 3 to 11 membered unsaturated alicyclic ring group, which is a monocyclic ring or a fused ring system (e.g., a fused ring system composed of two fused rings), wherein said ring group contains one or more (e.g., one, two, three, or four) ring heteroatoms independently selected from 0, S and N, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) are optionally oxidized, wherein one or more carbon ring atoms are optionally oxidized, and wherein said ring group comprises at least one double bond between adjacent ring atoms and does not comprise any triple bond between adjacent ring atoms; more preferably, "heterocycloalkenyl” refers to a 5 to 7 membered monocyclic unsaturated non-aromatic ring group containing one or more (e.g., one, two, or three) ring heteroatoms independently selected from 0, S and N, wherein one or more S ring atoms (if present) and / or one or more N ring atoms (if present) are optionally oxidized, wherein one or more carbon ring atoms are optionally oxidized, and wherein said ring group comprises at least one double bond between adjacent ring atoms and does not comprise any triple bond between adjacent ring atoms.

[0391] As used herein, the term "halogen” refers to fluoro (-F), chloro (-CI), bromo (-Br), or iodo (-I).

[0392] As used herein, the term "haloalkyl” refers to an alkyl group substituted with one or more (preferably 1 to 6, more preferably 1 to 3) halogen atoms which are selected independently from fluoro, chloro, bromo and iodo, and are preferably all fluoro atoms. It will be understood that the maximum number of halogen atoms is limited by the number of available attachment sites and, thus, depends on the number of carbon atoms comprised in the alkyl moiety of the haloalkyl group. "Haloalkyl” may, e.g, refer to -CF3, -CHF2, -CH2F, -CF2-CH3, -CH2-CF3, -CH2-CHF2, -CH2-CF2-CH3, -CH2-CF2-CF3, or -CH(CF3)2. A preferred "haloalkyl” group is fluoroalkyl. A particularly preferred "haloalkyl” group is -CF3.

[0393] As used herein, the term “fluoroalky I” refers to an alkyl group substituted with one or more (preferably 1 to 6, more preferably 1 to 3) fluoro atoms (-F). It will be understood that the maximum number of fluoro atoms is limited by the number of available attachment sites and, thus, depends on the number of carbon atoms comprised in the alkyl moiety of the fluoroalkyl group. “ Fluoroalky I” may, e.g., refer to -CF3, -CHF2, -CH2F, -CF2-CH3, -CH2-CF3, -CH2-CHF2, -CH2-CF2-CH3, -CH2-CF2-CF3, or -CH(CF3)2. A particularly preferred “fluoroalkyl” group is -CF3.

[0394] The terms "bond” and "covalent bond” are used herein synonymously, unless explicitly indicated otherwise or contradicted by context.

[0395] As used herein, the terms "optional”, "optionally” and "may” denote that the indicated feature may be present but can also be absent. Whenever the term "optional”, "optionally” or "may” is used, the present invention specifically relates to both possibilities, i.e, that the corresponding feature is present or, alternatively, that the corresponding feature is absent. For example, the expression "X is optionally substituted with Y” (or "X may be substituted with Y”) means that X is either substituted with Y or is unsubstituted. Likewise, if a component of a composition is indicated to be "optional”, the invention specifically relates to both possibilities, i.e., that the corresponding component is present (contained in the composition) or that the corresponding component is absent from the composition.

[0396] Various groups are referred to as being "optionally substituted” in this specification. Generally, these groups may carry one or more substituents, such as, e.g., one, two, three or four substituents. It will be understood that the maximum number of substituents is limited by the number of attachment sites available on the substituted moiety. Unless defined otherwise, the "optionally substituted” groups referred to in this specification carry preferably not more than two substituents and may, in particular, carry only one substituent. Moreover, unless defined otherwise, it is preferred that the optional substituents are absent, i.e. that the corresponding groups are unsubstituted.

[0397] A skilled person will appreciate that the substituent groups comprised in the compounds of the present invention may be attached to the remainder of the respective compound via a number of different positions of the corresponding specific substituent group. Unless defined otherwise, the preferred attachment positions for the various specific substituent groups are as illustrated in the examples.

[0398] As used herein, unless explicitly indicated otherwise or contradicted by context, the terms "a”, "an” and "the” are used interchangeably with "one or more” and "at least one”. Thus, for example, a composition comprising "a” compound of formula (I) can be interpreted as referring to a composition comprising "one or more” compounds of formula (I).

[0399] It is to be understood that wherever numerical ranges are provided / disclosed herein, all values and subranges encompassed by the respective numerical range are meant to be encompassed within the scope of the invention. Accordingly, the present invention specifically and individually relates to each value that falls within a numerical range disclosed herein, as well as each subrange encompassed by a numerical range disclosed herein.

[0400] As used herein, the term "about” preferably refers to ±10% of the indicated numerical value, more preferably to ±5% of the indicated numerical value, and in particular to the exact numerical value indicated. If the term "about” is used in connection with the endpoints of a range, it preferably refers to the range from the lower endpoint -10% of its indicated numerical value to the upper endpoint +10% of its indicated numerical value, more preferably to the range from of the lower endpoint -5% to the upper endpoint +5%, and even more preferably to the range defined by the exact numerical values of the lower endpoint and the upper endpoint.

[0401] As used herein, the term "comprising” (or "comprise”, "comprises”, "contain”, "contains”, or "containing”), unless explicitly indicated otherwise or contradicted by context, has the meaning of "containing, inter alia”, i.e., "containing, among further optional elements, ...”. In addition thereto, this term also includes the narrower meanings of "consisting essentially of' and "consisting of”. For example, the term "A comprising B and C” has the meaning of "A containing, inter alia, B and C”, wherein A may contain further optional elements (e.g., "A containing B, C and D” would also be encompassed), but this term also includes the meaning of "A consisting essentially of B and C” and the meaning of "A consisting of B and C” (i.e., no other components than B and C are comprised in A).

[0402] The scope of the invention embraces all pharmaceutically acceptable salt forms of the compounds of formula (I) which may be formed, e.g., by protonation of an atom carrying an electron lone pair which is susceptible to protonation, such as an amino group, with an inorganic or organic acid, or as a salt of an acid group (such as a carboxylic acid group) with a physiologically acceptable cation. Exemplary base addition salts comprise, for example: alkali metal salts such as sodium or potassium salts; alkaline earth metal salts such as calcium or magnesium salts; zinc salts; ammonium salts; aliphatic amine salts such as trimethylamine, triethylamine, dicyclohexylamine, ethanolamine, diethanolamine, triethanolamine, procaine salts, meglumine salts, ethylenediamine salts, or choline salts; aralkyl amine salts such as N, N-dibenzylethylenediamine salts, benzathine salts, benethamine salts; heterocyclic aromatic amine salts such as pyridine salts, picoline salts, quinoline salts or isoquinoline salts; quaternary ammonium salts such as tetramethylammonium salts, tetraethylammonium salts, benzyltrimethylammonium salts, benzyltriethylammonium salts, benzyltributylammonium salts, methyltrioctylammonium salts or tetrabutylammonium salts; and basic amino acid salts such as arginine salts, lysine salts, or histidine salts. Exemplary acid addition salts comprise, for example: mineral acid salts such as hydrochloride, hydrobromide, hydroiodide, sulfate salts (such as, e.g., sulfate or hydrogensulfate salts), nitrate salts, phosphate salts (such as, e.g., phosphate, hydrogenphosphate, or dihydrogenphosphate salts), carbonate salts, hydrogencarbonate salts, perchlorate salts, borate salts, or thiocyanate salts; organic acid salts such as acetate, propionate, butyrate, pentanoate, hexanoate, heptanoate, octanoate, cyclopentanepropionate, decanoate, undecanoate, oleate, stearate, lactate, maleate, oxalate, fumarate, tartrate, malate, citrate, succinate, adipate, gluconate, glycolate, nicotinate, benzoate, salicylate, ascorbate, pamoate (embonate), camphorate, glucoheptanoate, or pivalate salts; sulfonate salts such as methanesulfonate (mesylate), ethanesulfonate (esylate), 2-hydroxyethanesulfonate (isethionate), benzenesulfonate (besylate), p-toluenesulfonate (tosylate), 2-naphthalenesulfonate (napsylate), 3-phenylsulfonate, or camphorsulfonate salts; glycerophosphate salts; and acidic amino acid salts such as aspartate or glutamate salts. Further pharmaceutically acceptable salts are described in the literature, e.g., in Stahl PH & Wermuth CG (eds.), "Handbook of Pharmaceutical Salts: Properties, Selection, and Use”, Wiley-VCH, 2002 and in the references cited therein. Preferred pharmaceutically acceptable salts of the compounds of formula (I) include a hydrochloride salt, a hydrobromide salt, a mesylate salt, a sulfate salt, a tartrate salt, a fumarate salt, an acetate salt, a citrate salt, and a phosphate salt. A particularly preferred pharmaceutically acceptable salt of the compound of formula (I) is a hydrochloride salt. Accordingly, it is preferred that the compound of formula (I), including any one of the specific compounds of formula (I) described herein, is in the form of a hydrochloride salt, a hydrobromide salt, a mesylate salt, a sulfate salt, a tartrate salt, a fumarate salt, an acetate salt, a citrate salt, or a phosphate salt, and it is particularly preferred that the compound of formula (I) is in the form of a hydrochloride salt.

[0403] The present invention also specifically relates to the compound of formula (I), including any one of the specific compounds of formula (I) described herein, in non-salt form.

[0404] Moreover, the scope of the invention embraces the compounds of formula (I) in any solvated form, including, e.g., solvates with water (I ,e. , as a hydrate) or solvates with organic solvents such as, e.g., methanol, ethanol, isopropanol, acetic acid, ethyl acetate, ethanolamine, DMSO, or acetonitrile. All physical forms, including any amorphous or crystalline forms (i.e., polymorphs), of the compounds of formula (I) are also encompassed within the scope of the invention. It is to be understood that such solvates and physical forms of pharmaceutically acceptable salts of the compounds of the formula (I) are likewise embraced by the invention.

[0405] Furthermore, the compounds of formula (I) may exist in the form of different isomers, in particular stereoisomers (including, e.g., geometric isomers (or cis / trans isomers), enantiomers and diastereomers) or tautomers (including, in particular, prototropic tautomers, such as keto / enol tautomers or thione / thiol tautomers). All such isomers of the compounds of formula (I) are contemplated as being part of the present invention, either in admixture or in pure or substantially pure form. As for stereoisomers, the invention embraces the isolated optical isomers of the compounds according to the invention as well as any mixtures thereof (including, in particular, racemic mixtures / racemates). The racemates can be resolved by physical methods, such as, e.g., fractional crystallization, separation or crystallization of diastereomeric derivatives, or separation by chiral column chromatography. The individual optical isomers can also be obtained from the racemates via salt formation with an optically active acid followed by crystallization. The present invention further encompasses any tautomers of the compounds of formula (I). It will be understood that some compounds may exhibit tautomerism. In such cases, the formulae provided herein expressly depict only one of the possible tautomeric forms. The formulae and chemical names as provided herein are intended to encompass any tautomeric form of the corresponding compound and not to be limited merely to the specific tautomeric form depicted by the drawing or identified by the name of the compound.

[0406] The scope of the invention also embraces compounds of formula (I), in which one or more atoms are replaced by a specific isotope of the corresponding atom. For example, the invention encompasses compounds of formula (I), in which one or more hydrogen atoms (or, e.g., all hydrogen atoms) are replaced by deuterium atoms (i.e.,2H; also referred to as “D”). Accordingly, the invention also embraces compounds of formula (I) which are enriched in deuterium. Naturally occurring hydrogen is an isotopic mixture comprising about 99.98 mol-% hydrogen-1 (1H) and about 0.0156 mol-% deuterium (2H or D). The content of deuterium in one or more hydrogen positions in the compounds of formula (I) can be increased using deuteration techniques known in the art. For example, a compound of formula (I) or a reactant or precursor to be used in the synthesis of the compound of formula (I) can be subjected to an H / D exchange reaction using, e.g., heavy water (D2O). Further suitable deuteration techniques are described in: Atzrodt J et al., Bioorg Med Chem, 20(18), 5658-5667, 2012; William JS et al., Journal of Labelled Compounds and Radiopharmaceuticals, 53(11-12), 635-644, 2010; Modvig A et al., J Org Chem, 79, 5861-5868, 2014. The content of deuterium can be determined, e.g., using mass spectrometry or NMR spectroscopy. Unless specifically indicated otherwise, it is preferred that the compound of formula (I) is not enriched in deuterium. Accordingly, the presence of naturally occurring hydrogen atoms or1H hydrogen atoms in the compounds of formula (I) is preferred.

[0407] The present invention also embraces compounds of formula (I), in which one or more atoms are replaced by a positron-emitting isotope of the corresponding atom, such as, e.g.,18F,11C,13N,150,76Br,77Br,120l and / or124l. Such compounds can be used as tracers, trackers or imaging probes in positron emission tomography (PET). The invention thus includes (i) compounds of formula (I), in which one or more fluorine atoms (or, e.g., all fluorine atoms) are replaced by18F atoms, (ii) compounds of formula (I), in which one or more carbon atoms (or, e.g., all carbon atoms) are replaced by11C atoms, (iii) compounds of formula (I), in which one or more nitrogen atoms (or, e.g., all nitrogen atoms) are replaced by13N atoms, (iv) compounds of formula (I), in which one or more oxygen atoms (or, e.g., all oxygen atoms) are replaced by15O atoms, (v) compounds of formula (I), in which one or more bromine atoms (or, e.g., all bromine atoms) are replaced by76Br atoms, (vi) compounds of formula (I), in which one or more bromine atoms (or, e.g., all bromine atoms) are replaced by77Br atoms, (vii) compounds of formula (I), in which one or more iodine atoms (or, e.g., all iodine atoms) are replaced by120l atoms, and (viii) compounds of formula (I), in which one or more iodine atoms (or, e.g., all iodine atoms) are replaced by124l atoms. In general, it is preferred that none of the atoms in the compounds of formula (I) are replaced by specific isotopes.

[0408] The compounds provided herein may be administered as compounds perse or may be formulated as medicaments. The medicaments / pharmaceutical compositions may optionally comprise one or more pharmaceutically acceptable excipients, such as carriers, diluents, fillers, disintegrants, lubricating agents, binders, colorants, pigments, stabilizers, preservatives, antioxidants, and / or solubility enhancers.

[0409] The pharmaceutical compositions may comprise one or more solubility enhancers, such as, e.g., polyethylene glycol), including poly (ethylene glycol) having a molecular weight in the range of about 200 to about 5,000 Da (e.g., PEG 200, PEG 300, PEG 400, or PEG 600), ethylene glycol, propylene glycol, glycerol, a non-ionic surfactant, tyloxapol, polysorbate 80, macrogol-15-hydroxystearate (e.g., Kolliphor® HS 15, CAS 70142-34-6), a phospholipid, lecithin, dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine, a cyclodextrin, o-cyclodextrin, p-cyclodextrin, y-cyclodextrin, hydroxyethyl-p-cyclodextrin, hydroxypropyl-p- cyclodextrin, hydroxyethyl-y-cyclodextrin, hydroxypropyl-y-cyclodextrin, dihydroxypropyl-p-cyclodextrin, sulfobutylether-p-cyclodextrin, sulfobutylether-y-cyclodextrin, glucosyl-o-cyclodextrin, glucosyl-p-cyclodextrin, diglucosyl-p-cyclodextrin, maltosyl-o-cyclodextrin, maltosyl-p-cyclodextrin, maltosyl-y-cyclodextrin, maltotriosyl-p- cyclodextrin, maltotriosyl-y-cyclodextrin, dimaltosyl-p-cyclodextrin, methyl-p-cyclodextrin, a carboxyalkyl thioether, hydroxypropyl methylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone, a vinyl acetate copolymer, vinyl pyrrolidone, sodium lauryl sulfate, dioctyl sodium sulfosuccinate, or any combination thereof.

[0410] The pharmaceutical compositions may also comprise one or more preservatives, particularly one or more antimicrobial preservatives, such as, e.g., benzyl alcohol, chlorobutanol, 2-ethoxyethanol, m-cresol, chlorocresol (e.g., 2-chloro-3-methyl-phenol or 4-chloro-3-methy l-phenol), benzalkonium chloride, benzethonium chloride, benzoic acid (or a pharmaceutically acceptable salt thereof), sorbic acid (or a pharmaceutically acceptable salt thereof), chlorhexidine, thimerosal, or any combination thereof.

[0411] The pharmaceutical compositions can be formulated by techniques known to the person skilled in the art, such as the techniques published in "Remington: The Science and Practice of Pharmacy”, Pharmaceutical Press, 22ndedition. The pharmaceutical compositions can be formulated as dosage forms for oral, parenteral, such as intramuscular, intravenous, subcutaneous, intradermal, intraarterial, intracardial, rectal, nasal, topical, aerosol or vaginal administration. Dosage forms for oral administration include coated and uncoated tablets, soft gelatin capsules, hard gelatin capsules, lozenges, troches, solutions, emulsions, suspensions, syrups, elixirs, powders and granules for reconstitution, dispersible powders and granules, medicated gums, chewing tablets and effervescent tablets. Dosage forms for parenteral administration include solutions, emulsions, suspensions, dispersions and powders and granules for reconstitution. Emulsions are a preferred dosage form for parenteral administration. Dosage forms for rectal and vaginal administration include suppositories and ovula. Dosage forms for nasal administration can be administered via inhalation and insufflation, for example by a metered inhaler. Dosage forms for topical administration include creams, gels, ointments, salves, patches and transdermal delivery systems.

[0412] The compounds of formula (I) or the pharmaceutically acceptable salts or solvates thereof, or the above described pharmaceutical compositions comprising any of the aforementioned entities, may be administered to a subject by any convenient route of administration, whether systemically / peri pherally or at the site of desired action, including but not limited to one or more of: oral (e.g., as a tablet, capsule, or as an ingestible solution), topical (e.g., transdermal, intranasal, ocular, buccal, and sublingual), parenteral (e.g., using injection techniques or infusion techniques, and including, for example, by injection, e.g., subcutaneous, intradermal, intramuscular, intravenous, intraarterial, intracardiac, intrathecal, intraspinal, intracapsular, subcapsular, intraorbital, intraperitoneal, intratracheal, subcuticular, intraarticular, subarachnoid, or intrasternal by, e.g., implant of a depot, for example, subcutaneously or intramuscularly), pulmonary (e.g., by inhalation or insufflation therapy using, e.g., an aerosol, e.g., through mouth or nose), gastrointestinal, intrauterine, intraocular, subcutaneous, ophthalmic (including intravitreal or intracameral), rectal, or vaginal administration.

[0413] If said compounds or pharmaceutical compositions are administered parenterally, then examples of such administration include one or more of: intravenously, intraarterially, intraperitoneally, intrathecally, intraventricularly, intraurethrally, intrasternally, intracardially, intracranially, intramuscularly or subcutaneously administering the compounds or pharmaceutical compositions, and / or by using infusion techniques. For parenteral administration, the compounds are best used in the form of a sterile aqueous solution which may contain other substances, for example, enough salts or glucose to make the solution isotonic with blood. The aqueous solutions should be suitably buffered (preferably to a pH of from 3 to 9), if necessary. The preparation of suitable parenteral formulations under sterile conditions is readily accomplished by standard pharmaceutical techniques well known to those skilled in the art.

[0414] Said compounds or pharmaceutical compositions can also be administered orally in the form of tablets, capsules, ovules, elixirs, solutions or suspensions, which may contain flavoring or coloring agents, for immediate-, delayed-, modified-, sustained-, pulsed- or controlled-release applications.

[0415] The tablets may contain excipients such as microcrystalline cellulose, lactose, sodium citrate, calcium carbonate, dibasic calcium phosphate and glycine, disintegrants such as starch (preferably corn, potato or tapioca starch), sodium starch glycolate, croscarmellose sodium and certain complex silicates, and granulation binders such as polyvinylpyrrolidone, hydroxypropylmethylcellulose (HPMC), hydroxypropylcellulose (HPC), sucrose, gelatin and acacia. Additionally, lubricating agents such as magnesium stearate, stearic acid, glyceryl behenate and talc may be included. Solid compositions of a similar type may also be employed as fillers in gelatin capsules. Preferred excipients in this regard include lactose, starch, a cellulose, or high molecular weight polyethylene glycols. For aqueous suspensions and / or elixirs, the agent may be combined with various sweetening or flavoring agents, coloring matter or dyes, with emulsifying and / or suspending agents and with diluents such as water, ethanol, propylene glycol and glycerin, and combinations thereof.

[0416] For oral administration, the compounds or pharmaceutical compositions are preferably administered by oral ingestion, particularly by swallowing. The compounds or pharmaceutical compositions can thus be administered to pass through the mouth into the gastrointestinal tract, which can also be referred to as "oral-gastrointestinal” administration.

[0417] Alternatively, said compounds or pharmaceutical compositions can be administered in the form of a suppository or pessary, or may be applied topically in ...

Claims

CLAIMS1 . A compound of the following formula (I)wherein:X is N or C(-R5);R1is a group R11, and R2is a group -L2-R21; or alternatively, R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24;R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -C0(Ci-5 alkyl);L2is selected from a bond, C1-8 alkylene, C2-8 alkenylene, and C2-8 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups R22, and wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -CO-, -O-, -S- , -SO-, -SO2-, -NH- and -N(CI.5alkyl)-;R21is selected from carbocyclyl, heterocyclyl, C1-8 alkyl, and C1-8 haloalkyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23, and wherein one or more -CH2- units comprised in said alkyl or in said haloalkyl are each optionally replaced by -0- each R22is independently selected from -OH, -0(Ci-5 alkyl), -0(Ci-5 alkylene)-OH, -0(Ci-5 alkylene)-0(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI-5 alkyl)-0(Ci-5 alkyl), halogen, C1-5 haloalkyl, -0-(Ci-5 haloalkyl), -ON, -SF5, -OHO, -C0-(Ci.5alkyl), -COOH, -C0-0-(Ci.5alkyl), -0-C0-(Ci.5alkyl), -CO-NH2, -C0-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci-5alkyl), -NH-COO(Ci.5alkyl), -N(Ci_5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI-5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5 alkyl), -N(Ci_5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups F ; each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci_5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups R°rc; each R24is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5alkyl), -(Co-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-S0-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups F ;R3is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, -(C0-5 alkylene)-carbocyclyl, and -(C0-5 alkylene)-heterocyclyl, wherein said alkyl, said alkenyl, said alkynyl, the alkylene group in said -(C0-5 alkylene)-carbocyclyl, and the alkylene group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R31, and wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32; each R31is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(Ci_5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI-5 alkyl)-O(Ci-5 alkyl), -Si(Ci-5 alkyl)(Ci-5 alkyl)(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci.5haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -0-C0-(Ci.5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI-5 alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO- NH(CI-5 alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(Ci_5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups RCyc; each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3alkylene)-S0-(Ci-5 alkyl), -(C0-3 alkylene)-SC>2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;R4and R5are each independently selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0.3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;RAand RBare each independently selected from hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, -(Co-8 alkylene)-OH, -(Co-8 alkylene)-O(Ci-5 alkyl), -(Co-8 alkylene)-SH, -(Co-8 alkylene)-S(Ci-5 alkyl), -(C1-8 alkylene)-NH2, -(C1-8 alkylene)-NH(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-halogen, -(C1-8 alkylene)-Ci-5 haloalkyl, -(Co-8 alkylene)-O-(Ci-8 haloalkyl), -(Co-8 alkylene)-CN, -(Co-8 alkylene)-SF5, -(Co-8 alkylene)-CHO, -(Co-8 alkylene)-CO-(Ci-5 alkyl), -(Co-8 alkylene)-COOH, -(Co-8 alkylene)-CO-O-(Ci-5 alkyl), -(Co-8 alkylene)-O-CO-(Ci-5 alkyl), -(Co-8 alkylene)-CO-NH2, -(Co-8 alkylene)-CO-NH(Ci-5 alkyl), -(Co-8 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-NH-CO-(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C1-8 alkylene)-NH-COO(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(Co-8 alkylene)-O-CO- NH(CI-5 alkyl), -(Co-8 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(Co-8 alkylene)-SO2-NH2, -(Co-8 alkylene)-SO2-NH(Ci-5 alkyl), -(Co-8 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C1-8 alkylene)-NH-SO2-(Ci-5 alkyl), -(C1-8 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(Co-8 alkylene)-SO-(Ci-5 alkyl), -(Co-8 alkylene)-SO2-(Ci-5 alkyl), -(Co-8 alkylene)-carbocyclyl, -(Co-8 alkylene)-heterocyclyl, and -Lz-Rz, wherein one or more -CH2- units comprised in said C1-8 alkyl, said C2-8 alkenyl, said C2-8 alkynyl, and in any of the aforementioned Co-s alkylene and C1-8 alkylenegroups are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-, wherein the carbocyclyl group in said -(Co-8 al ky lene)-carbocycly I and the heterocyclyl group in said -(Co-8 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc, and wherein at least one of the groups RAand RBis not hydrogen; or alternatively, RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc; each Rcis independently selected from C1.5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0.3 alkylene)-N(Ci.5alkyl)-OH, -(C0.3 alkylene)-NH-O(Ci.5alkyl), -(C0.3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups RCyC; each RCycis independently selected from C1.5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0.3 alkylene)-N(Ci.5alkyl)-OH, -(C0.3 alkylene)-NH-O(Ci.5alkyl), -(C0.3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alky lene)-CO(C 1-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 al ky lene)-O-C0(Ci-5 alkyl), -(C0-3 alkylene)-C0-NH2, -(C0-3 alkylene)-C0-NH(Ci-5 alkyl), -(C0-3 alkylene)-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-C0(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-C0(Ci-5 alkyl), -(C0-3 alkylene)-NH-C00(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-C00(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-NH(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci.5 alkyl), -(C0-3 alkylene)-SO-(Ci.5alkyl), -(C0-3 alkylene)-P(=O)(-OH)(-OH), -(C0-3 alkylene)-P(=0)(-0H)(-0-Ci.5 alkyl), -(C0-3 alkylene)-P(=O)(-O-Ci.5alkyl)(-O-Ci.5alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz; each Lzis independently selected from a covalent bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SP5, -OH, -O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), and -N(CI.5alkyl)(Ci-5 alkyl), and further wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-; and each Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(0i-5 alkylene)-SH, -S(0i-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(0I-5 alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SP5, -CHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci-5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI-5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI-5alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SP5, -OH, -O(Ci.5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI-5 alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -0-C0-(Ci.5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5 alkyl)-CO-(Ci_5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO- NH(CI.5 alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI_5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), and -SO2-(Ci.5alkyl); with the proviso that: if X is N, if R1is a group R11, and if R11is hydrogen, then R3is not a group -(C1-5 alkylene)-phenyl, wherein the alkylene group in said -(C1-5 alkylene)-phenyl is optionally substituted with one or more groups R31and wherein the phenyl group in said -(C1-5 alky lene)-phenyl is optionally substituted with one or more groups R32; if X is N, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, and if RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a bicyclic fused heterocyclyl which is optionally substituted with one or more groups Rc, then the heterocyclyl formed from R1and R2is not a spirocyclic group which comprises a piperidine ring and is attached via the nitrogen ring atom of said piperidine ring; if X is N, if one of RAand RBis hydrogen, and if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups R24, then said heterocyclyl is not decahydroquinoxalin-1-yl or octahydro-1 H-cyclopenta[b]pyrazin-1-yl; if X is N and if one of RAand RBis hydrogen, then R3is not phenyl which is optionally substituted with one or more groups R32; if X is C(-R5), if one of RAand RBis hydrogen, if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is piperazin- 1-yl and which is optionally substituted with one or more groups R24, then said piperazin- 1-yl is not substituted with 1 H-quinoxalin-2-on-7-yl methyl, wherein the 1 H-quinoxalin-2-on- 7-yl group in said 1 H-quinoxalin-2-on-7-y Imethy I is optionally substituted with one or more groups RCyc; if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups R24, if R3is C1-8 alkyl which is optionally substituted with one or more halogen atoms, and if one of RAand RBis hydrogen, then the other one of RAand RBis not methyl; if X is N and if R3is phenyl which is substituted with one or more halogen atoms, then R1and R2are not mutually joined to form, together with the nitrogen atom that they are attached to, a group which is pyrrolidin-1-yl or piperidin-1-yl; if X is N, if R11is C1-5 alkyl, and if R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said C1-8 alkyl are each optionally replaced by -O-, then R3is not a cyclic group selected from phenyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl,thiomorpholiny I , and azepanyl, wherein said cyclic group is optionally substituted with one or more halogen atoms; if X is N and if R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said C1-8 alkyl are each optionally replaced by -O-, then R3is not a heterocycloalkyl comprising one or two nitrogen ring atoms, wherein all remaining ring atoms in said heterocycloalkyl are carbon atoms, and wherein said heterocycloalkyl is substituted with one or more groups R32; if R1and R2are mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is imidazol-1-yl or 1 ,2,4-triazol-1-yl and which is optionally substituted with one or more groups R24, then R3is not C1-6 alkyl or -CF3; if X is C(-R5) and if one of RAand RBis hydrogen, then the other one of RAand RBis not -NH-carbocyclyl or -NH-heterocyclyl, wherein the carbocyclyl in said -NH-carbocyclyl and the heterocyclyl in said -NH-heterocyclyl are each optionally substituted with one or more groups RCyc; if R1is a group R11and R11is hydrogen, then R2is not -CO-NH-(1, 2,3,4- tetrahydronaphthalen-1-yl), -CO-NH-(3',4'-dihydro-2'H-spiro[cyclopropane-1, 1'- naphthalene]-4'-yl), -CO-NH-(3',4'-dihydro-2'H-spiro[cyclobutane-1 ,1'-naphthalene]-4'-yl), -CO-NH-(3,4-dihydro-2H-spiro[naphthalene-1 ,3'-oxetane]-4-yl), -CO-NH-(3,4-dihydro-2H- spiro[naphthalene-1,2'-oxetane]-4-yl) or -CO-NH-(3',4'-dihydro-2'H-spiro[azetidine-3,1'- naphthalene]-4'-yl), wherein the 1 ,2,3,4-tetrahydronaphthalen-1-yl in said -CO-NH- (1 ,2,3,4-tetrahydronaphthalen-1-yl), the 3',4'-dihydro-2'H-spiro[cyclopropane-1 ,1'- naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[cyclopropane-1 ,1'- naphthalene]-4'-yl), the 3',4'-dihydro-2'H-spiro[cyclobutane-1, 1'-naphthalene]-4'-yl in said -CO-NH-(3',4'-dihydro-2'H-spiro[cyclobutane-1 ,1'-naphthalene]-4'-yl), the 3,4-dihydro-2H- spiro[naphthalene-1,3'-oxetane]-4-yl in said -CO-NH-(3,4-dihydro-2H-spiro[naphthalene- 1 ,3'-oxetane]-4-yl), the 3,4-dihydro-2H-spiro[naphthalene-1 ,2'-oxetane]-4-yl in said -CO- NH-(3,4-dihydro-2H-spiro[naphthalene-1 ,2'-oxetane]-4-yl) and the 3',4'-dihydro-2'H- spiro[azetidine-3,1'-naphthalene]-4'-yl in said -CO-NH-(3',4’-dihydro-2’H-spiro[azetidine- 3,1'-naphthalene]-4'-yl) are each optionally substituted with one or more groups R23; if R1is a group R11and if R11is hydrogen, then R2is not -CO-O-CH2-CCI3, -CO-O-phenyl, -CO-O-(4-methlyphenyl), -CO-O-(imidazol-l-yl), -CO-O-(pyrrolidin-2,5-dion-1-yl); or a pharmaceutically acceptable salt or solvate thereof.

2. The compound of claim 1 , wherein X is N.

3. The compound of claim 1 or 2, wherein R1is a group R11, and R2is a group -L2-R21; wherein L2is a bond or C1-5 alkylene; and wherein R21is selected from aryl, cycloalkyl, heteroaryl, and heterocycloalkyl, wherein said aryl, said cycloalkyl, said heteroaryl, and said heterocycloalkyl are each optionally substituted with one or more groups R23.

4. The compound of any one of claims 1 to 3, wherein R2is -(C1-5 alkylenej-cycloalkyl.

5. The compound of claim 4, wherein R2is -CFh-cyclopentyl or -CF cyclohexyl.

6. The compound of any one of claims 1 to 3, wherein R2is phenyl which is optionally substituted with one or more groups R23.

7. The compound of claim 6, wherein R2is phenyl which is substituted with one or more groups independently selected from C1-5 alkyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, and -SF5.

8. The compound of any one of claims 1 to 7, wherein R3is selected from C1-6 alkyl, -(C0-5 alky lene)-carbocycly I, and -(C0-5 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-5 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32.

9. The compound of any one of claims 1 to 8, wherein R3is selected from C3-5 alkyl, cycloalkyl, -CH2-cycloal ky I, heterocycloalkyl, and -CH2-heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CH2-cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CH2-heterocycloalkyl are each optionally substituted with one or more groups R32.

10. The compound of any one of claims 1 to 9, wherein R3is selected from propyl, butyl, pentyl, cyclopropyl, cyclobutyl, cyclopentyl, -CF cyclopropyl, -CF cyclobutyl, and -CH2-cyclopentyl.11 . The compound of any one of claims 1 to 10, wherein R3is isopropyl or -CF cyclobutyl.

12. The compound of any one of claims 1 to 11 , wherein RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc.

13. The compound of any one of claims 1 to 12, wherein RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups Rc, wherein said heterocycloalkyl is a 5- to 7-membered monocyclic heterocycloalkyl containing one nitrogen ring atom, through which the heterocycloalkyl is attached to the -C(=O)- group in formula (I), and optionally containing one or two further ring heteroatoms independently selected from nitrogen, oxygen and sulfur, wherein all remaining ring atoms are carbon atoms, wherein any nitrogen ring atom and / or any sulfur ring atom is optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized.

14. The compound of any one of claims 1 to 13, wherein the moiety -N(-RA)-RBis selected from 4-(5- carboxypyridin-2-yl)piperazin-1-yl, 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, 4-(carboxymethyl)piperidin-l -yl, and 3-oxopiperazin-1-yl, wherein said 4-(5-carboxypyridin-2-yl)piperazin-1 -yl, said 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, said 4-(carboxymethyl)piperidin-1-yl, and said 3- oxopiperazin-1-yl are each optionally substituted with one or more groups Rc.

15. The compound of any one of claims 1 to 14, wherein the moiety -N(-RA)-RBis16. The compound of any one of claims 1 to 15, wherein the moiety -N(-RA)-RBis17. The compound of claim 1 , which is a compound of the following formulawherein:R1is a group R11, and R2is a group -L2-R21;R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -C0(Ci-5 alkyl);L2is selected from a bond, C1-8 alkylene, C2-8 alkenylene, and C2-8 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups R22;R21is selected from carbocyclyl and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups R23;each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(Ci_5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI-5 alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(Ci_5alkyl)-CO-(Ci.5 alkyl), -NH-COO(Ci.5alkyl), -N(Ci_5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5 alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5 alkyl), -N(Ci_5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups RCyc; each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0.3 alkylene)-N(Ci_5alkyl)-OH, -(C0.3 alkylene)-NH-O(Ci.5alkyl), -(C0.3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;R3is selected from C1-6 alkyl, -(C0-5 alkylene)-cycloalkyl, and -(C0-5 alkylene)-heterocyclyl, wherein the cycloalkyl group in said -(C0-5 alkylene)-cycloalkyl and the heterocyclyl group in said -(C0-5 alkylene)-heterocyclyl are each optionally substituted with one or more groups R32; each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0.3 alkylene)-N(Ci_5alkyl)-OH, -(C0.3 alkylene)-NH-O(Ci.5alkyl), -(C0.3 alkylene)-N(Ci-5 alkyl)-0(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;R4is selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 al ky lene)-OH , -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alky lene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO- NH(CI-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc;each Rcis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci_5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups RCyc; each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-C0(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 al ky lene)-O- C0(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci.5 alkyl), -(C0-3 alkylene)-SO-(Ci.5alkyl), -(C0-3 alkylene)-P(=O)(-OH)(-OH), -(C0-3alkylene)-P(=O)(-OH)(-O-Ci-5alkyl), -(C0.3alkylene)-P(=O)(-O-Ci.5alkyl)(-O-Ci_5alkyl), -(C0.3alkylene)-cycloalkyl, -(Co-3alkylene)-heterocycloalkyl, and -Lz-Rz; each Lzis independently selected from a covalent bond, C1.7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), and -N(CI.5alkyl)(Ci-5 alkyl), and further wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-; and each Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(0i-5 alkylene)-SH, -S(0i-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(0I-5 alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI-5 alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -OHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI-5 alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -OHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -0-C0-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5 alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO- NH(CI-5 alkyl), -O-CO-N(CI.5alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), and -SO2-(Ci.5alkyl); or a pharmaceutically acceptable salt or solvate thereof.

18. The compound of claim 17, wherein L2is a bond or C1-5 alkylene, and wherein R21is selected from aryl, cycloalkyl, heteroaryl, and heterocycloalkyl, wherein said aryl, said cycloalkyl, said heteroaryl, and said heterocycloalkyl are each optionally substituted with one or more groups R23.

19. The compound of claim 17 or 18, wherein R2is -(C1-5 alkylenej-cycloalkyl; preferably wherein R2is -CFh-cyclopentyl or -CF cyclohexyl.

20. The compound of claim 17 or 18, wherein R2is phenyl which is optionally substituted with one or more groups R23; preferably wherein R2is phenyl which is substituted with one or more groups independently selected from C1-5 alkyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, and -SF5.

21. The compound of any one of claims 17 to 20, wherein R3is selected from C1-6 alkyl, -(C0-5 alkylene)-cycloalkyl, and -(C0-5 alkylene)-heterocycloalkyl, wherein the cycloalkyl group in said -(C0-5 alkylene)-cycloalkyl and the heterocycloalkyl group in said -(C0-5 alkylene)-heterocycloalkyl are each optionally substituted with one or more groups R32; preferably wherein R3is selected from C3-5 alkyl, cycloalkyl, -CF cycloalkyl, heterocycloalkyl, and -CH2- heterocycloalkyl, wherein said cycloalkyl, the cycloalkyl in said -CF cycloalkyl, said heterocycloalkyl, and the heterocycloalkyl in said -CH2-heterocycloalkyl are each optionally substituted with one or more groups R32.

22. The compound of any one of claims 17 to 21, wherein R3is selected from propyl, butyl, pentyl, cyclopropyl, cyclobutyl, cyclopentyl, -CF cyclopropyl, -CF cyclobutyl, and -CH2-cyclopentyl; preferably wherein R3is isopropyl or -CF cyclobutyl.

23. The compound of any one of claims 17 to 22, wherein RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups Rc, wherein said heterocycloalkyl is a 5- to 7-membered monocyclic heterocycloalkyl containing one nitrogen ring atom, through which the heterocycloalkyl is attached to the -C(=O)- group in formula (I), and optionally containing one or two further ring heteroatoms independently selected from nitrogen, oxygen and sulfur, wherein all remaining ring atoms are carbon atoms, wherein any nitrogen ring atom and / or any sulfur ring atom is optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized.

24. The compound of any one of claims 17 to 23, wherein the moiety -N(-RA)-RBis selected from 4-(5- carboxypyridin-2-yl)piperazin-1-yl, 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, 4-(carboxymethyl)piperidin-l -yl, and 3-oxopiperazin-1-yl, wherein said 4-(5-carboxypyridin-2-yl)piperazin-1 -yl, said 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, said 4-(carboxymethyl)piperidin-1-yl, and said 3- oxopiperazin-1-yl are each optionally substituted with one or more groups Rc; preferably wherein the moiety -N(-RA)-RBis25. The compound of claim 1 , which is a compound of the following formulawherein:R1is a group R11, and R2is a group -L2-R21;R11is selected from hydrogen, C1-5 alkyl, C1-5 haloalkyl, and -C0(Ci-5 alkyl);L2is a bond;R21is C1-8 alkyl, wherein one or more -CH2- units comprised in said alkyl are each optionally replaced by -O-; each R22is independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI_5alkyl)(Ci_5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI-5 alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci.5alkyl), -NH-CO-(CI.5alkyl), -N(CI_5alkyl)-CO-(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI_5alkyl)-COO(Ci_5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5 alkyl)(Ci.5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI_5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl),carbocyclyl, heterocyclyl, and -Lz-Rz, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups F ; each R23is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci_5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc;R3is C1-6 alkyl or -(C0-5 alkylene)-cycloalkyl, wherein the cycloalkyl group in said -(C0-5 alky lene)-cycloalky I is optionally substituted with one or more groups R32; each R32is independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5alkyl), -(Co-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-S0-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups F ;R4is selected from hydrogen, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alky lene)-0 (C1-5 alkyl), -(C0-3 alky lene)-0 (C 1-5 al ky lene)-OH , -(C0-3 alky lene)-0 (C 1-5 al ky lene)-0(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci-5 alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alky lene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylene)-SF5, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO-(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO- NH(CI-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, and -(C0-3 alkylene)-heterocyclyl, wherein the carbocyclyl group in said -(C0-3 alkylene)-carbocyclyl and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups R°rc;RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocyclyl which is optionally substituted with one or more groups Rc; each Rcis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-(Ci-5 haloalkyl), -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-C0-(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-CO-O-(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5alkyl)-C0-(Ci-5 alkyl), -(C0-3 alkylene)-NH-C00(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-C00(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-NH(Ci-5 alkyl), -(C0-3 alkylene)-0-C0-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-S0-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-carbocyclyl, -(C0-3 alkylene)-heterocyclyl, and -Lz-Rz, wherein the carbocyclyl group in said -(C0-3 al ky lene)-carbocycly I and the heterocyclyl group in said -(C0-3 alkylene)-heterocyclyl are each optionally substituted with one or more groups RCyc; and further wherein any two groups Rc, which are attached to the same ring carbon atom of the heterocyclyl formed from RAand RB, may also be mutually joined to form, together with said ring carbon atom that they are attached to, a cycloalkyl or a heterocycloalkyl, wherein said cycloalkyl or said heterocycloalkyl is optionally substituted with one or more groups RCyc; each RCycis independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, -(C0-3 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-O(Ci-5 alkylene)-OH, -(C0-3 alkylene)-O(Ci-5 alkylene)-O(Ci-5 alkyl), -(C0-3 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-S(Ci-5 alkylene)-SH, -(C0-3 alkylene)-S(Ci-5 alkylene)-S(Ci-5 alkyl), -(C0-3 alkylene)-NH2, -(C0-3 alkylene)-NH(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-OH, -(C0-3 alkylene)-N(Ci.5alkyl)-OH, -(C0-3 alkylene)-NH-O(Ci.5alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-O(Ci-5 alkyl), -(C0-3 alkylene)-halogen, -(C0-3 alkylene)-Ci-5 haloalkyl, -(C0-3 alkylene)-O-(Ci-5 haloalkyl), -(C0-3 alkylene)-CN, -(C0-3 alkylenej-SFs, -(C0-3 alkylene)-CHO, -(C0-3 alkylene)-C0(Ci-5 alkyl), -(C0-3 alkylene)-COOH, -(C0-3 alkylene)-COO(Ci-5 alkyl), -(C0-3 al ky lene)-O- C0(Ci-5 alkyl), -(C0-3 alkylene)-CO-NH2, -(C0-3 alkylene)-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-CO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-CO(Ci-5 alkyl), -(C0-3 alkylene)-NH-COO(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-COO(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-NH(Ci-5 alkyl), -(C0-3 alkylene)-O-CO-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-SO2-NH2, -(C0-3 alkylene)-SO2-NH(Ci-5 alkyl), -(C0-3 alkylene)-SO2-N(Ci-5 alkyl)(Ci-5 alkyl), -(C0-3 alkylene)-NH-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-N(Ci-5 alkyl)-SO2-(Ci-5 alkyl), -(C0-3 alkylene)-SO2-(Ci.5 alkyl), -(C0-3 alkylene)-SO-(Ci.5alkyl), -(C0-3 alkylene)-P(=O)(-OH)(-OH), -(C0-3 alkylene)-P(=O)(-OH)(-O-Ci.5 alkyl), -(C0-3 alkylene)-P(=O)(-O-Ci.5alkyl)(-O-Ci.5alkyl), -(C0-3 alkylene)-cycloalkyl, -(C0-3 alkylene)-heterocycloalkyl, and -Lz-Rz; each Lzis independently selected from a covalent bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene, wherein said alkylene, said alkenylene and said alkynylene are each optionally substituted with one or more groups independently selected from halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -CN, -SP5, -OH, -O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), and -N(CI.5alkyl)(Ci-5 alkyl), and further wherein one or more -CH2- units comprised in said alkylene, said alkenylene or said alkynylene are each optionally replaced by a group independently selected from -O-, -NH-, -N(CI-5 alkyl)-, -CO-, -S-, -SO-, and -SO2-; andeach Rzis independently selected from -OH, -O(Ci-5 alkyl), -O(Ci-5 alkylene)-OH, -O(Ci-5 alkylene)-O(Ci-5 alkyl), -SH, -S(Ci-5 alkyl), -S(Ci-5 alkylene)-SH, -S(Ci-5 alkylene)-S(Ci-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -NH-OH, -N(CI.5alkyl)-OH, -NH-O(CI.5alkyl), -N(CI-5 alkyl)-O(Ci-5 alkyl), halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -CHO, -CO(Ci.5alkyl), -COOH, -COO(Ci.5alkyl), -O-CO(Ci.5alkyl), -CO-NH2, -CO-NH(CI.5 alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO(CI.5alkyl), -N(CI.5alkyl)-CO(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI.5 alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, wherein said aryl, said heteroaryl, said cycloalkyl, and said heterocycloalkyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -OH, -O(Ci-5alkyl), -SH, -S(Ci.5alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci.5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -O-CO-(Ci.5alkyl), -CO-NH2, -CO-NH(CI-5 alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5alkyl)-CO-(Ci.5 alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci.5alkyl), -O-CO-NH(CI.5alkyl), -O-CO-N(CI-5 alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci.5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI.5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), -SO2-(Ci.5alkyl), carbocyclyl, and heterocyclyl, wherein said carbocyclyl and said heterocyclyl are each optionally substituted with one or more groups independently selected from C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halogen, C1-5 haloalkyl, -O-(Ci-5 haloalkyl), -ON, -SF5, -OH, -O(Ci-5 alkyl), -SH, -S(0i-5 alkyl), -NH2, -NH(CI.5alkyl), -N(CI.5alkyl)(Ci_5alkyl), -CHO, -CO-(Ci.5alkyl), -COOH, -CO-O-(Ci.5alkyl), -0-C0-(Ci-5 alkyl), -CO-NH2, -CO-NH(CI.5alkyl), -CO-N(CI.5alkyl)(Ci_5alkyl), -NH-CO-(CI.5alkyl), -N(CI.5 alkyl)-CO-(Ci.5alkyl), -NH-COO(CI.5alkyl), -N(CI.5alkyl)-COO(Ci_5alkyl), -O-CO- NH(CI-5 alkyl), -O-CO-N(CI.5alkyl)(Ci_5alkyl), -SO2-NH2, -SO2-NH(CI.5alkyl), -SO2-N(CI.5alkyl)(Ci_5alkyl), -NH-SO2-(CI.5 alkyl), -N(CI_5alkyl)-SO2-(Ci.5alkyl), -SO-(Ci.5alkyl), and -SO2-(Ci.5alkyl); or a pharmaceutically acceptable salt or solvate thereof.

26. The compound of claim 25, wherein R2is C1-8 alkyl; preferably wherein R2is isopentyl.

27. The compound of claim 25 or 26, wherein R3is selected from C3-5 alkyl, cycloalkyl, and -CH2-cycloalkyl, wherein said cycloalkyl and the cycloalkyl in said -CH2-cycloalkyl are each optionally substituted with one or more groups R32; preferably wherein R3is selected from propyl, butyl, pentyl, cyclopropyl, cyclobutyl, cyclopentyl, -CH2- cyclopropyl, -CH2-cyclobutyl, and -CH2-cyclopentyl; more preferably wherein R3is isopropyl or -CH2-cyclobutyl.

28. The compound of any one of claims 25 to 27, wherein RAand RBare mutually joined to form, together with the nitrogen atom that they are attached to, a heterocycloalkyl which is optionally substituted with one or more groups Rc, wherein said heterocycloalkyl is a 5- to 7-membered monocyclic heterocycloalkyl containing one nitrogen ring atom, through which the heterocycloalkyl is attached to the -C(=O)- group in formula (I), and optionally containing one or two further ring heteroatoms independently selected from nitrogen, oxygen and sulfur, wherein all remaining ring atoms are carbon atoms, wherein any nitrogen ring atom and / or any sulfur ring atom is optionally oxidized, and wherein one or more carbon ring atoms are optionally oxidized.

29. The compound of any one of claims 25 to 28, wherein the moiety -N(-RA)-RBis selected from 4-(5- carboxypyridin-2-yl)piperazin-1-yl, 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, 4-(carboxymethyl)piperidin-l -yl, and 3-oxopiperazin-1-yl, wherein said 4-(5-carboxypyridin-2-yl)piperazin-1 -yl, said 4-(5-carboxymethylpyridin-2-yl)piperazin-1-yl, said 4-(carboxymethyl)piperidin-1-yl, and said 3- oxopiperazin-1-yl are each optionally substituted with one or more groups Rc; preferably wherein the moiety -N(-RA)-RBismore preferably wherein the moiety -N(-RA)-RBis30. The compound of claim 1 , wherein said compound is selected from:4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpicolinoyl)-3,3-dimethylpiperazin-2-one;4-(5-((4-chloro-3-fluorophenyl)(methyl)amino)-6-cyclopentylpicolinoyl)-1 ,3,3-trimethylpiperazin-2-one;4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpicolinoyl)-3,3-dimethylpiperazin-2-one; benzyl (6-(2,2-dimethyl-3-oxopiperazine-1-carbonyl)-2-(prop-1-en-2-yl)pyridin-3-yl)carbamate;1-(4-chloro-3-fluorophenyl)-4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3- dimethylpiperazin-2-one;4-(5-((4-chloro-3-fluorophenyl)amino)-6-(difluoromethyl)picolinoyl)-3,3-dimethylpiperazin-2-one;4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-2-one; benzyl (6-(2,2-dimethyl-3-oxopiperazine-1-carbonyl)-2-(2-ethoxyvinyl)pyridin-3-yl)carbamate;4-(5-((4-chloro-3-fluorophenyl)amino)-6-(2-ethoxyethyl)picolinoyl)-3,3-dimethylpiperazin-2-one; methyl 2-(1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)piperidin-4-yl)acetate;2-(1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)piperidin-4-yl)acetic acid; methyl 2-((3R,4S)-1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3-methoxypiperidin-4-yl)acetate; 2-((3R,4S)-1-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3-methoxypiperidin-4-yl)acetic acid; methyl 6-(4-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((3,4-difluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 2-(6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)pyridin-3-yl)acetate;2-(6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpi perazin-1- y l)py ridin-3-y l)acetic acid;4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(5-(isoindolin-2-yl)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(3,3-dimethyl-4-(5-((4-(pentafluorosulfanyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin- 1 -y I )-2, 4-d I methy In I coti n ate;6-(3,3-dimethyl-4-(5-((4-(pentafluorosulfanyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-1-yl)-2.4-dimethy Inicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopentylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;4-(5-((4-chloro-3-fluorophenyl)amino)-6-isobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;3.3-dimethyl-4-(5-((4-(pentafluorosulfanyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-2-one; 4-(5-((4-chloro-3-fluorophenyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;3,3-dimethyl-4-(5-((4-(methylsulfonyl)phenyl)amino)-6-propylpyrazine-2-carbonyl)piperazin-2-one; 4-(5-((4-chlorobenzyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(6-benzyl-5-((4-chloro-3-fluorophenyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;4-(5-((4,4-difluorocyclohexyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; 4-(5-(4,4-difluoropiperidin-1-yl)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; tert-butyl 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazine-1- carboxylate; (5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazin-2-yl)(2,2-dimethylpiperazin-1-yl)methanone; 1-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)ethan-1-one; ethyl 2-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4- yl)acetate;2-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)acetic acid; ethyl 2-(2-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2-azabicyclo[2.2.1]heptan-5- yl)acetate; ethyl 2-(2-((5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2- carboxamido)methyl)cyclopentyl)acetate; 2-(2-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2-azabicyclo[2.2.1]heptan-5- yl)acetic acid; 2-(2-((5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carboxamido)methyl)cyclopentyl)acetic acid;4-(5-((4-chlorobenzyl)(methyl)amino)-6-propylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; tert-butyl 4-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazine-1- carboxylate;5-((4-chloro-3-fluorophenyl)amino)-6-isopropyl-N-methyl-N-(piperidin-4-yl)pyrazine-2-carboxamide; N-(1-acetylpiperidin-4-yl)-5-((4-chloro-3-fluorophenyl)amino)-6-isopropyl-N-methylpyrazine-2-carboxamide; 4-(5-((4-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((4-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((4-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; 4-(5-(benzylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-(benzylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(benzylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; N-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)-N- methylacetamide;N-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)-2,2,2- trifluoro-N-methylacetamide;2-((1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)oxy)- N,N-dimethylacetamide; methyl 6-(4-(5-(3,4-dihydroisoquinolin-2(1 H)-yl)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-(3,4-dihydroisoquinolin-2(1 H)-yl)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;N-(1-(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazine-2-carbonyl)-2,2-dimethylpiperidin-4-yl)-N- methylmethanesulfonamide; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-(methoxymethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-(methoxymethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((cyclohexylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;(5-((4-chloro-3-fluorophenyl)amino)-6-isopropylpyrazin-2-yl)(4-(2-(dimethylamino)ethoxy)-2,2- dimethylpiperidin-1-yl)methanone; ethyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-methylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-ethylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclobutylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorophenyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;methyl 6-(4-(6-(tert-butyl)-5-((4-chloro-3-fluorophenyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate; 6-(4-(6-(tert-butyl)-5-((4-chloro-3-fluorophenyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(isopentylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(isopentylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid methyl (S)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; (S)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)phenethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n ate; 6-(4-(6-isopropyl-5-((4-(trifluoromethyl)phenethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethy Inicotinic acid; methyl 6-(4-(5-((2-cyclohexylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((2-cyclohexylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (R)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;(R)-6-(4-(6-isopropyl-5-((1-phenylethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (R)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; (R)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethy Inicotinic acid; methyl 6-(4-(6-cyclobutyl-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid methyl 6-(4-(6-cyclobutyl-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid;methyl 6-(4-(6-cyclobutyl-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclobutyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(isobutylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(isobutylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2,3-dihydro-1H-inden-2-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((2,3-dihydro-1 H-inden-2-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(tetrahydrofuran-3-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-(tetrahydrofuran-3-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(5-((cyclopropylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((cyclopropylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (R)-6-(4-(6-isopropyl-5-(((tetrahydrofuran-3-yl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; (R)-6-(4-(6-isopropyl-5-(((tetrahydrofuran-3-yl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-methylpiperidin-4-yl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-(((1-methylpiperidin-4-yl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl (R)-6-(4-(5-hydroxy-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; (R)-6-(4-(5-((cyclohexylmethyl)amino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethy Inicotinic acid; methyl (R)-6-(4-(5-(isopentylamino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;(R)-6-(4-(5-(isopentylamino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;methyl (R)-6-(4-(5-((4-fluorobenzyl)amino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n ate;(R)-6-(4-(5-((4-fluorobenzyl)amino)-6-(1-methoxyethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(6-isopropyl-5-((3-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-isopropyl-5-((3-methoxypropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(4-methoxycyclohexyl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-((2-(4-methoxycyclohexyl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(5-(isopentylamino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-(isopentylamino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(cyclopropylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-(cyclopropylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl (S)-6-(4-(6-isopropyl-5-((2-phenylpropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;(S)-6-(4-(6-isopropyl-5-((2-phenylpropyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-fluorobenzyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((4-fluorobenzyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-(cyclopropylmethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n ate;6-(4-(5-((cyclohexylmethyl)amino)-6-(cyclopropylmethyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((cyclohexylmethyl)amino)-6-(tetrahydro-2H-pyran-4-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1 -y I )-2, 4-d i methy In i coti n i c acid; methyl 6-(4-(6-(cyclobutylmethyl)-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(6-(cyclobutylmethyl)-5-((4-fluorobenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;methyl 6-(4-(5-(ethylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(ethylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclopropoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;6-(4-(5-((2-cyclopropoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclopropylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((2-cyclopropylethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(cyclobutylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-(cyclobutylmethyl)-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-(cyclobutylmethyl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n ate;6-(4-(6-(cyclobutylmethyl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethy Inicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(3-methoxybicyclo[1 .1 .1]pentan-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-((2-(3-methoxybicyclo[1 .1 .1]pentan-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(butylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(butylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((3-methoxycyclobutyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;6-(4-(6-isopropyl-5-((3-methoxycyclobutyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4,4-difluorobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((4,4-difluorobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((4-chloro-3-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((4-chloro-3-fluorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((3,3-difluorocyclobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((3,3-difluorocyclobutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2,3-dihydrobenzofuran-3-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n ate;6-(4-(5-((2,3-dihydrobenzofuran-3-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl (S)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;(S)-6-(4-(5-((2,3-dihydro-1 H-inden-1-yl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclobutylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((cyclobutylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-methylcyclobutyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n ate;6-(4-(6-isopropyl-5-(((1-methylcyclobutyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(5-(chroman-4-ylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-(chroman-4-ylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-cyclopropyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-cyclopropyl-5-(isopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(neopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-(neopentylamino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((2-cyclobutyl-2-methoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(5-((2-cyclobutyl-2-methoxyethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(6-cyclopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n ate;6-(4-(6-cyclopropyl-5-((4-(trifluoromethyl)benzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethy Inicotinic acid; methyl 6-(4-(5-((cyclohexylmethyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;6-(4-(5-((cyclohexylmethyl)amino)-6-cyclopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((4-methoxybenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-isopropyl-5-((4-methoxybenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2-(1 ,3-dihydroisobenzofuran-5-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-((2-(1 ,3-dihydroisobenzofuran-5-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((S)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-(((S)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((R)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-(((R)-2,3-dihydro-1 H-inden-1-yl)amino)-6-((R)-1-methoxyethyl)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-((3,3-dimethylbutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((3,3-dimethylbutyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(tetrahydro-2H-pyran-4-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate; 6-(4-(6-isopropyl-5-((2-(tetrahydro-2H-pyran-4-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n I c acid; methyl 6-(4-(5-(((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-(((2,3-dihydrobenzo[b][1 ,4]dioxin-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((pyrazin-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-isopropyl-5-((pyrazin-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((3-chlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-isopropyl-5-((pyrazin-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2,4-dichlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((2,4-dichlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((2-(1 H-pyrazol-1-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-((2-(1 H-pyrazol-1-yl)ethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(1-methyl-1 H-pyrazol-3-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-((2-(1-methyl-1 H-pyrazol-5-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1 -y I )-2, 4-d I methy In I coti n I c acid; methyl 6-(4-(6-isopropyl-5-(((1-(methoxymethyl)cyclopentyl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-(((1-(methoxymethyl)cyclopentyl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n ate;6-(4-(6-isopropyl-5-(((1-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)- 2,4-dimethy Inicotinic acid; methyl 6-(4-(6-isopropyl-5-(((4-(trifluoromethyl)cyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-(((4-(trifluoromethyl)cyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((4,4-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-(((4,4-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-morpholinopyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(6-isopropyl-5-morpholinopyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(piperidin-1-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(6-isopropyl-5-(piperidin-1-yl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-(((4-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n ate;6-(4-(6-isopropyl-5-(((4-methylcyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid; methyl 6-(4-(5-(((3,3-difluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-(((3,3-difluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((3,3-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(5-(((3,3-difluorocyclohexyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid; methyl 6-(4-(5-(((1 ,4-dioxan-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinate;6-(4-(5-(((1 ,4-dioxan-2-yl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((2-(2-oxopyrrolidin-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d I methy In I coti n ate;6-(4-(6-isopropyl-5-((2-(2-oxopyrrolidin-1-yl)ethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethy Inicotinic acid; methyl 6-(4-(6-isopropyl-5-(((1-morpholinocyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3- dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-(((1-morpholinocyclohexyl)methyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)-2,4-dimethylnicotinic acid;4-(6-(cyclohex-1-en-1-yl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(6-(cyclobutylethynyl)-5-((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(5-(isopentylamino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(5-((cyclohexylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(6-isopropyl-5-((thiazol-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(6-isopropyl-5-((thiophen-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2.4-dimethylnicotinate;6-(4-(6-isopropyl-5-((thiophen-2-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(6-isopropyl-5-((thiophen-3-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinate;6-(4-(6-isopropyl-5-((thiophen-3-ylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-3- methylpicolinate;6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-3- methylpicolinic acid;methyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-5- methylthiazole-4-carboxylate;2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-5- methylthiazole-4-carboxylic acid; ethyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4- methylthiazole-5-carboxylate;2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4- methylthiazole-5-carboxylic acid; methyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1- yl)thiazole-4-carboxylate;2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)thiazole-4- carboxylic acid;4-(5-((cyclopentylmethyl)amino)-6-((trimethylsilyl)ethynyl)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2- one; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-4-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-4-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-(((3-fluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin- 1 -y I )-2, 4-d i methy In i coti n ate;6-(4-(5-(((3-fluorocyclopentyl)methyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethy Inicotinic acid;4-(6-isopropyl-5-((2-methoxybenzyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)thiazole-4- carboxamide;2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-5- methylthiazole-4-carboxamide; methyl 2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4,6- dimethylpyrimidine-5-carboxylate;2-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-4,6- dimethylpyrimidine-5-carboxylic acid;(5-((cyclopentylmethyl)amino)-6-isopropylpyrazin-2-yl)(2,2-dimethylpiperidin-1-yl)methanone;(5-((cyclopentylmethyl)amino)-6-isopropylpyrazin-2-yl)(3,3-dimethylmorpholino)methanone;4-(5-((4-chlorobenzyl)amino)-6-isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one;4-(5-((cyclopentylmethyl)amino)-6-ethynylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-2-one; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate;6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid;methyl 6-(4-(5-((cyclopentylmethyl)amino)-3-fluoro-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-3-fluoro-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methoxypicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-methoxypicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; methyl 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid; methyl 5-bromo-6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinate; 5-bromo-6-(4-(5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-1-yl)-2,4- dimethylnicotinic acid; 4-(5-((cyclopentylmethyl)amino)-6-isopropyl-3-(trifluoromethyl)picolinoyl)-3,3-dimethylpiperazin-2-one; 4-(4-bromo-5-((cyclopentylmethyl)amino)-6-isopropylpicolinoyl)-3,3-dimethylpiperazin-2-one; or a pharmaceutically acceptable salt or solvate of any of the aforementioned compounds.

31. The compound of claim 1 or 17, wherein said compound is 6-(4-(5-((cyclohexylmethyl)amino)-6- isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid or a pharmaceutically acceptable salt or solvate thereof.

32. The compound of claim 1 or 25, wherein said compound is 6-(4-(5-(isopentylamino)-6-isopropylpyrazine-2- carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid or a pharmaceutically acceptable salt or solvate thereof.

33. The compound of claim 1 or 17, wherein said compound is 6-(4-(6-(cyclobutylmethyl)-5- ((cyclohexylmethyl)amino)pyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid or a pharmaceutically acceptable salt or solvate thereof.

34. The compound of claim 1 or 17, wherein said compound is 6-(4-(5-((cyclopentylmethyl)amino)-6- isopropylpyrazine-2-carbonyl)-3,3-dimethylpiperazin-1-yl)-2,4-dimethylnicotinic acid or a pharmaceutically acceptable salt or solvate thereof.

35. A compound as defined in any one of claims 1 to 34, wherein said compound is conjugated via a linker to a membrane anchor.

36. A pharmaceutical composition comprising the compound of any one of claims 1 to 35 and a pharmaceutically acceptable excipient.

37. The compound of any one of claims 1 to 35 or the pharmaceutical composition of claim 36 for use in the treatment or prevention of pain, an autoimmune disorder, an autoinflammatory disorder, an inflammatory disorder, a central nervous system disorder, spinal cord injury, a metabolic disorder, a gastrointestinal disorder, a cardiovascular disorder, a fibrotic disorder, a respiratory disorder, a skin disorder, an allergic disorder, or cancer.

38. The compound of any one of claims 1 to 35 or the pharmaceutical composition of claim 36 for use in the treatment or prevention of neuropathic pain, inflammatory pain, cancer pain, post-operative incision pain, fracture pain, osteoporotic fracture pain, gout joint pain, chronic pain, spinal cord injury, atopic dermatitis, contact dermatitis, dry skin dermatitis, seborrhoeic dermatitis, arthritis, rheumatoid arthritis, osteoarthritis, psoriasis, psoriatic arthritis, multiple sclerosis, non-alcoholic steatohepatitis, obesity, diabetes, adipose inflammation, pancreatitis, metabolic syndrome, PAR-2 associated metabolic dysfunction, periodontitis, gingivitis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, peptic ulcer disease, infectious enteritis, irritable bowel syndrome, atherosclerosis, asthma, interstitial lung disease, pulmonary fibrosis, rheumatoid arthritis-associated interstitial lung disease, liver fibrosis, cystic fibrosis, renal fibrosis, peritoneal fibrosis, pancreatic fibrosis, intestinal fibrosis, cardiac fibrosis, skin fibrosis, systemic lupus erythematosus, scleroderma, skin eczema, acne, rosacea, post-inflammatory hyperpigmentation, lichen planus, pruritus, polymyositis, vasculitis, Wegener's granulomatosis, Netherton syndrome, dermatomyositis, uveitis, liver cirrhosis, Alzheimer's disease, Parkinson's disease, dust mite allergy, cockroach allergy, or allergic asthma.

39. The compound of any one of claims 1 to 35 or the pharmaceutical composition of claim 36 for use in the treatment or prevention of cancer.

40. The compound for use according to claim 39 or the pharmaceutical composition for use according to claim 39, wherein said cancer is selected from colorectal cancer, colon cancer, gastrointestinal cancer, gastric cancer, rectal cancer, anal cancer, liver cancer, breast cancer, pancreatic cancer, cervical cancer, prostate cancer, ovarian cancer, endometrial cancer, vaginal cancer, vulvar cancer, uterine cancer, testicular cancer, germ cell cancer, esophageal cancer, laryngeal cancer, mouth cancer, hematological cancer, leukemia, lymphoma, multiple myeloma, lung cancer, adrenal gland cancer, biliary tract cancer, bile duct cancer, hepatobiliary cancer, genitourinary cancer, urothelial cancer, bladder cancer, gallbladder cancer, head and / or neck cancer, kidney cancer, mesothelioma, sarcoma, skin cancer, melanoma, Merkel-cell cancer, epidermoid cancer, thyroid cancer, thymus cancer, squamous cell cancer, goblet cell cancer, spleen cancer, bone cancer, osteosarcoma, fibrosarcoma, Ewing's sarcoma, Kaposi's sarcoma, neuroendocrine cancer, neuroblastoma, brain cancer, and glioblastoma.41 . The compound for use according to claim 39 or 40 or the pharmaceutical composition for use according to claim 39 or 40, wherein said compound or said pharmaceutical composition is to be administered in combination with one or more anticancer drugs.

42. An anticancer drug for use in the treatment or prevention of cancer, wherein said anticancer drug is to be administered in combination with the compound of any one of claims 1 to 35 or the pharmaceutical composition of claim 36.

43. The compound for use according to claim 41 or the pharmaceutical composition for use according to claim 41 or the anticancer drug for use according to claim 42, wherein said anticancer drug(s) is / are selected from immune checkpoint inhibitors.

44. The compound for use according to claim 43 or the pharmaceutical composition for use according to claim 43 or the anticancer drug for use according to claim 43, wherein said immune checkpoint inhibitors are selected from anti-CTLA-4 antibodies, anti-PD-1 antibodies, anti-PD-L1 antibodies, anti-TIGIT antibodies, anti-TIM3 antibodies, anti-VISTA antibodies, anti-BTLA antibodies, anti-CD47 antibodies, anti-LAG3 antibodies, anti-OX40 antibodies, and anti-ICOS antibodies.

45. The compound for use according to claim 43 or 44 or the pharmaceutical composition for use according to claim 43 or 44 or the anticancer drug for use according to claim 43 or 44, wherein said immune checkpoint inhibitors are selected from ipilimumab, tremelimumab, nivolumab, pembrolizumab, cemiplimab, spartalizumab, dostarlimab, camrelizumab, sintilimab, tislelizumab, toripalimab, zimberelimab, pidilizumab, penpulimab, cadonilimab, serplulimab, pucotenlimab, prolgolimab, retifanlimab, sintilimab, AMP-224, AMP- 514, JTX-4014, APE02058, atezolizumab, avelumab, durvalumab, envafolimab, adebrelimab, socazolimab, sugemalimab, CK-301, BMS-936559, MEDI4736, MPDL3280A, MDX-1105, MEDI6469, bintrafusp alfa, tiragolumab, vibostolimab, domvanalimab, etigilimab, BMS-986207, EOS-448, COM902, ASP8374, SEA- TGT, BGB-A1217, IBI-939, M6223, sabatolimab, cobolimab, lomvastomig, BGB-A425, BMS-986258, INCAGN02390, LY3321367, LY3415244, SHR-1702, Sym023, TQB2618, onvatilimab, HMBD-002, KVA12123, W0180, IGN-381 , PMC-309, APX-201 , tifcemalimab, icatolimab, ANB032, HFB200603, magrolimab, lemzoparlimab, ligufalimab, CC-90002, IMM0306, TG-1801 , TI-061 , relatlimab, ieramilimab, encelimab, tebotelimab, REGN3767, FS118, IMP701 , IMP731 , ivuxolimab, MEDI0562, MEDI6383, MEDI6469, INCAGN01949, ABBV-368, BAT6026, BGB-A445, YH-002, BMS 986178, INBRX-106, IBI101 , MOXR0916, alomfilimab, feladilimab, izuralimab, vopratelimab, BMS-986226, and MEDI-570.

46. In vitro use of a compound as defined in any one of claims 1 to 35 as a PAR-2 inhibitor.

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