Pyridone carboxamide derived compounds as soluble epoxide hydrolase inhibitors

Abstract

The invention provides new heterocyclic compounds having the general formula (I) wherein R1, R2, A, X, RA1, RA2, and RA3 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Description

[0001]F. Hoffmann-La Roche AG, CH-4070 Basel, Switzerland Case: 39264 PYRIDONE CARBOXAMIDE DERIVED COMPOUNDS AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS Field of the Invention The present invention relates to organic compounds useful for therapy or prophylaxis in a human, in particular to selected pyridone carboxamide derived compounds as inhibitors of soluble epoxide hydrolase (sEH) for the treatment or prophylaxis of diseases and disorders that are associated with sEH, such as diabetic retinopathy, pain and neurodegenerative diseases. Background of the Invention Diabetic retinopathy is a common and serious complication of diabetes mellitus, affecting the blood vessels in the retina of the eye. It is a leading cause of blindness in adults. The pathogenesis of diabetic retinopathy is complex and involves various molecular and cellular mechanisms. One enzyme that has gained attention in the context of diabetic retinopathy is soluble epoxide hydrolase (sEH). Soluble epoxide hydrolase plays a crucial role in the metabolism of epoxyeicosatrienoic acids (EETs), which are lipid mediators derived from arachidonic acid. EETs have been shown to possess anti-inflammatory, vasodilatory, and angiogenic properties, making them important regulators of vascular function. In the context of diabetic retinopathy, alterations in the EET pathway and increased activity of sEH have been observed in the development and progression of the disease. Several studies have demonstrated that diabetic conditions lead to an upregulation of sEH in the retina. The increased activity of sEH results in the degradation of EETs, leading to a reduction in their beneficial effects. This imbalance in the EET pathway contributes to the vascular dysfunction, inflammation, and oxidative stress observed in diabetic retinopathy. The role of sEH in diabetic retinopathy extends beyond its impact on EET metabolism. sEH has been linked to the regulation of endothelial cell function, vascular permeability, and CNE / 10.07.2025 inflammation, all of which are critical factors in the development of diabetic retinopathy. Inhibition of sEH has shown promising results in preclinical studies, suggesting that targeting this enzyme could be a potential therapeutic strategy for diabetic retinopathy. Moreover, the interactions between sEH and other molecular pathways implicated in diabetic retinopathy, such as the vascular endothelial growth factor (VEGF) pathway, highlight the complexity of the disease and the potential for targeted interventions. Combining sEH inhibition with existing anti-VEGF therapies may offer a synergistic approach to address multiple aspects of diabetic retinopathy pathogenesis. Epoxidation of arachidonic acid by cytochrome P450 enzymes during inflammation and injury yields epoxyeicosatrienoic acids (EETs). The EETs have a variety of biological effects including modulation of inflammation, endothelial function and neuronal cell survival. EETs levels are regulated by soluble epoxide hydrolase (sEH), the major enzyme responsible for their degradation and conversion to inactive dihydroxyeicosatrienoic acids (DHETs). sEH, thereby, limits many of the biological actions of EETs. EETs produce important biological effects, particularly in the vascular and nervous systems. Inhibiting sEH increases the half-life of EETs, which in turn translates into beneficial therapeutic effects. sEH inhibitors may have utility in treatment of diabetic retinopathy [M.-H. Wang, A. S. Ibrahim, G. Hsiao, A. Tawfik, M. Al-Shabrawey, Prostaglandins Other Lipid Mediat. 2020, 148, 106449; J. Hu, S. Dziumbla, J. Lin,S.-I. Bibli, S. Zukunft, J. de Mos, K. Awwad, T. Frömel, A. Jungmann, K. Devraj, Z. Cheng, L. Wang, S. Fauser, C. G. Eberhart, A. Sodhi, B. D. Hammock, S. Liebner, O. J. Müller, C.Glaubitz, H.-P. Hammes, R. Popp, I. Fleming, Nature 2017, 552, 248–252], neuropathic andinflammatory pain [P. Sivaram, K. Ish, Inflamm. Allergy-drug Targets 2012, 11, 143–158; W.M. Karen, G. Aldrin, M. B. Cindy, H. D. Bruce, Neurotherapeutics 2020, 17, 900–916; C.Brenneis, M. Sisignano, O. Coste, K. Altenrath, M. J. Fischer, C. Angioni, I. Fleming, R. P.Brandes, P. W. Reeh, C. J. Woolf, G. Geisslinger, K. Scholich, Mol Pain 2011, 7, 78; P.Sivaram, K. Ish, Drug Discov. Today 2015, 20, 1382–1390; B. Inceoglu, S. L. Jinks, A. Ulu, C.M. Hegedus, K. Georgi, K. R. Schmelzer, K. Wagner, P. D. Jones, C. Morisseau, B. D.Hammock, Proc. National Acad. Sci. 2008, 105, 18901–18906; K. M. Wagner, C. B.McReynolds, W. K. Schmidt, B. D. Hammock, Pharmacol. Ther. 2017, 180, 62–76; K.Hiesinger, K. M. Wagner, B. D. Hammock, E. Proschak, S. H. Hwang, Prostaglandins OtherLipid Mediat. 2019, 140, 31–39; S. D. Kodani, C. Morisseau, Biochimie 2019, 159, 59–65; K.Wagner, B. Inceoglu, B. D. Hammock, Prostaglandins Other Lipid Mediat. 2011, 96, 76–83],neurodegenerative diseases [Z. Sydney, T. P. Julian, C. Sydney, S. Samantha, R. Mira, G. Anna,I. Diego, H. D. Bruce, B. V. Cesar, Prog. Neurobiol. 2019, 172, 23–39; R. Qian, M. Min, Y.Jun, N. Risa, Y. Akihiro, I. Kei-ichi, K. Kenta, M. Shigeo, H. Hee Sung, S. Shinji, A. Wado, H.Nobutaka, H. D. Bruce, H. Kenji, Proc. National Acad. Sci. 2018, 115, E5815; M. Pallàs, S.Vázquez, C. Sanfeliu, C. Galdeano, C. Griñán-Ferré, Biomolecules 2020, 10, 703; J. Atone, K.Wagner, K. Hashimoto, B. D. Hammock, Prostaglandins Other Lipid Mediat. 2020, 147,106385; C. Griñán-Ferré, S. Codony, E. Pujol, J. Yang, R. Leiva, C. Escolano, D. Puigoriol- Illamola, J. Companys-Alemany, R. Corpas, C. Sanfeliu, B. Pérez, M. I. Loza, J. Brea, C.Morisseau, B. D. Hammock, S. Vázquez, M. Pallàs, C. Galdeano, Neurotherapeutics 2020, 17,1825–1835; C. Griñán-Ferré, J. Jarné-Ferrer, A. Bellver-Sanchís, S. Codony, D. Puigoriol-Illamola, C. Sanfeliu, Y. Oh, S. Lee, S. Vázquez, M. Pallàs, CNS Neurosci. Ther. 2023, DOI10.1111 / cns.14511; Y. Wu, J.-H. Dong, Y.-F. Dai, M.-Z. Zhu, M.-Y. Wang, Y. Zhang, Y.-D.Pan, X.-R. Yuan, Z.-X. Guo, C.-X. Wang, Y.-Q. Li, X.-H. Zhu, Neuron 2023, 111, 2847-2862.e10], acute respiratory distress syndrome (ARDS) [W. Tao, G. Xu, Y. Luo, P.-S. Li,Inflammopharmacology 2022, 30, 2027–2033], cardiovascular diseases [L. Aurelien, G.Dominique, J. Robinson, B. Jeremy, Cardiovasc. Hematological Agents Medicinal Chem 2012,10, 212–222; I. D. John, H. D. Bruce, Nature Rev. Drug Discov. 2009, 8, 794–805]; rheumatoidarthritis (RA) [L. Qinglin, H. Shaoqi, H. Lichuang, Z. Jida, C. Gang, Front. Pharmacol. 2021,12, 648137], inflammatory bowel disease (IBD) and Crohn's disease [Y. Guang-Yu, Proc.National Acad. Sci. 2018, 115, 5827–5828; Z. Wanying, Y. L. Allison, L. Jie, L. Haonan, D.Hua, C. Tae Yeon, B. Han, M. A. Kristina, H. D. Bruce, Y. Guang-Yu, Digest. Dis. Sci. 2012,57, 2580–2591]. Accordingly, it is an object of the present disclosure to provide methods and novel compositions for the treatment of diabetic retinopathy, pain and neurodegenerative disease, specifically, selected spiropiperidine urea derived compounds for the treatment of diabetic retinopathy, neuropathic pain, Alzheimer’s Disease and Parkinson's Disease as well as methods of treatment of conditions and diseases mediated by soluble epoxide hydrolase. The identification of small molecule inhibitors of soluble epoxide hydrolase has been a field of extensive research both in academia and industry, summarized in several reviews, e.g. M.Nazari, E. Rezaee, S. A. Tabatabai, Mini-rev Med. Chem. 2023, 23, 99–117; M. R. Iyer, B.Kundu, C. M. Wood, Expert Opin. Ther. Pat. 2022, 32, 629–647; H. C. Shen, Expert Opin.Ther. Pat. 2010, 20, 941–956; K. Hiesinger, J. S. Kramer, S. Beyer, T. Eckes, S. Brunst, C.Flauaus, S. K. Wittmann, L. Weizel, A. Kaiser, S. B. M. Kretschmer, S. George, C. Angioni, J. Heering, G. Geisslinger, M. Schubert-Zsilavecz, A. Schmidtko, D. Pogoryelov, J. Pfeilschifter,B. Hofmann, D. Steinhilber, S. Schwalm, E. Proschak, J. Med. Chem. 2020, 63, 11498–11521.In conclusion, suppressing the action and / or the activation of sEH is a promising new therapeutic strategy for the treatment or prevention of various diseases and disorders, and there continues to be a high unmet medical need for new sEH inhibitors. of the Invention In a first aspect, the present invention provides a compound of formula (I) wherein R1, R2, A, X, RA1, RA2, and RA3 are as described herein.In further aspects, the present invention provides processes for manufacturing the compounds of formula (I), pharmaceutical compositions comprising the compounds of formula (I), as well as methods of using the compounds of formula (I) in the treatment or prophylaxis of diseases and disorders that are associated with sEH. Detailed of the Invention Definitions Features, integers, characteristics, compounds, chemical moieties or groups described in conjunction with a particular aspect, embodiment or example of the invention are to be understood to be applicable to any other aspect, embodiment or example described herein, unless incompatible therewith. All of the features disclosed in this specification (including any accompanying claims, abstract and drawings), and / or all of the steps of any method or process so disclosed, may be combined in any combination, except combinations where at least some of such features and / or steps are mutually exclusive. The invention is not restricted to the details of any foregoing embodiments. The invention extends to any novel one, or any novel combination, of the features disclosed in this specification (including any accompanying claims, abstract and drawings), or to any novel one, or any novel combination, of the steps of any method or process so disclosed. The term “alkyl” refers to a mono- or multivalent, e.g., a mono- or bivalent, linear or branched saturated hydrocarbon group of 1 to 6 carbon atoms (“C1-C6-alkyl”), e.g., 1, 2, 3, 4, 5, or 6 carbon atoms. In some preferred embodiments, the alkyl group contains 1 to 4 carbon atoms. In still other preferred embodiments, the alkyl group contains 1 to 3 carbon atoms. Some non- limiting examples of alkyl include methyl, ethyl, propyl, 2-propyl (isopropyl), n-butyl, iso-butyl, sec-butyl, tert-butyl, and 2,2-dimethylpropyl. Particularly preferred, yet non-limiting examples of alkyl include methyl, ethyl, isopropyl and iso-butyl. The term “alkoxy” refers to an alkyl group, as previously defined, attached to the parent molecular moiety via an oxygen atom. Unless otherwise specified, the alkoxy group contains 1 to 6 carbon atoms (“C1-6-alkoxy”). In some preferred embodiments, the alkoxy group contains contains 1 to 4 carbon atoms. In still other preferred embodiments, the alkoxy group contains 1 to 3 carbon atoms. Some non-limiting examples of alkoxy groups include methoxy, ethoxy, n- propoxy, isopropoxy, n-butoxy, isobutoxy and tert-butoxy. Particularly preferred, yet non- limiting examples of alkoxy are methoxy and ethoxy. The term “alkoxyalkyl” refers to an alkyl group as defined herein, wherein at least one of the hydrogen atoms of the alkyl group, preferably one hydrogen atom of the alkyl group have been replaced by an alkoxy group as defined herein. A particularly preferred, yet non-limiting example of alkoxyalkyl is 2-ethoxyethyl. The term “amino” alone or in combination with other groups, refers to -NH2. The term “alkylamino” refers to an amino group as defined herein, wherein at least one of the two hydrogen atoms of the amino group, preferably two hydrogen atoms of the amino group have been replaced by an alkyl group as defined herein (e.g. “C1-6-alkyl-amino” or “(C1-6- alkyl)2-amino”). Particularly preferred, yet non-limiting example of alkyl-amino group is dimethylamino ((CH3)2N-). The term "aryl" refers to a monocyclic, bicyclic, or tricyclic carbocyclic ring system having a total of 6 to 10 ring members (“C6-C10-aryl”), wherein at least one ring in the system is aromatic. Some non-limiting examples of aryl include phenyl and 9H-fluorenyl (e.g.9H-fluoren-9-yl). A particularly preferred, yet non-limiting example of aryl is phenyl. The term “cyano”, alone or in combination with other groups, refers to a –CN (nitrile) group. The term “cycloalkyl” refers to a saturated mono- or bicyclic hydrocarbon group having 3 to 8 ring carbon atoms (“C3-8-cycloalkyl”), preferably 3 to 6 ring carbon atoms (“C3-6-cycloalkyl”), more preferably 3 to 4 ring carbon atoms (“C3-4-cycloalkyl”). “Bicyclic cycloalkyl” refers to cycloalkyl moieties consisting of two saturated carbocycles having two carbon atoms in common, i.e., the bridge separating the two rings is either a single bond or a chain of one or two ring atoms, and to spirocyclic moieties, i.e., the two rings are connected via one common ring atom. Some non-limiting examples of cycloalkyl include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, bicyclo[1.1.1]pentanyl (1-bicyclo[1.1.1]pentanyl). Particulalryl preferred, yet non- limiting examples of cycloalkyl include cyclopropyl and cyclobutyl. The term “halo” or “halogen” refers to fluoro (F), chloro (Cl), bromo (Br) or iodo (I), particularly chloro (Cl) or fluoro (F). The term “haloalkyl” refers to an alkyl group, wherein at least one of the hydrogen atoms of the alkyl group has been replaced by a halogen atom, preferably fluoro. Preferably, “haloalkyl” refers to an alkyl group wherein 1, 2 or 3 hydrogen atoms of the alkyl group have been replaced by a halogen atom, most preferably fluoro. Some non-limiting examples of haloalkyl are trifluoromethyl, difluoromethyl, 1,1-difluoroethyl, 2,2-difluoroethyl, 2-fluoroethyl, and 2,2,2- trifluoroethyl. Particulalryl preferred, yet non-limiting examples of haloalkyl are trifluoromethyl and 2,2,2-trifluoroethyl. The term “haloalkoxy” refers to an alkoxy group, wherein at least one of the hydrogen atoms of the alkoxy group has been replaced by a halogen atom, preferably fluoro. Preferably, “haloalkoxy” refers to an alkoxy group wherein 1, 2 or 3 hydrogen atoms of the alkoxy group have been replaced by a halogen atom, most preferably fluoro. Some non-limiting examples of haloalkoxy are trifluoromethoxy, difluoromethoxy, 2,2,2-trifluoro-1,1-dimethyl-ethoxy, (1,1,1- trifluoropropan-2-yl)oxy, 2-fluoroethoxy, 2,2-difluoroethoxy, and 2,2,2-trifluoroethoxy. A particularly preferred, yet non-limiting example of haloalkoxy is 2,2,2-trifluoroethoxy. The term “hydroxyalkyl” refers to an alkyl group, wherein at least one of the hydrogen atoms of the alkyl group has been replaced by a hydroxy group. Preferably, “hydroxyalkyl” refers to an alkyl group wherein 1, 2 or 3 hydrogen atoms, most preferably 1 hydrogen atom of the alkyl group have been replaced by a hydroxy group. Some non-limiting examples of hydroxyalkyl are 2-hydroxy-1,1-dimethylethyl, 2-hydroxy-2-methyl-propyl, hydroxymethyl and hydroxyethyl (e.g.2-hydroxyethyl). A particularly preferred, yet non-limiting example of hydroxyalkyl is hydroxymethyl. The term "heteroaryl" refers to a mono- or multivalent, mono-, bi- or tricyclic ring system having a total of 5 to 14 ring members, and more preferably 5 to 11 ring members, wherein at least one ring in the ring system is aromatic, and at least one ring in the system contains one or more heteroatoms. Preferably, the heteroaryl comprises 1, 2, 3 or 4 heteroatoms independently selected from O, S and N. “Bicyclic heteroaryl” refers to ring moieties consisting of two cycles having two ring atoms in common, preferably, bicyclic heteroaryl is “fused bicyclic heteroaryl”, i.e., two cycles having two ring atoms and a single bond in common. “Tricyclic heteroaryl” refers to ring moieties consisting of three cycles, preferably, wherein the first ring is fused to the second ring, and the second ring is connected to the third ring via one common ring atom (spirocyclic moieties). In some preferred embodiments, the heteroaryl is a 5- to 6-membered monocyclic heteroaryl comprising 1 or 2 heteroatoms independently selected from S and N, or a 9- to 12-membered bicyclic or tricyclic heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O. In still other preferred embodiments, the heteroaryl is a 5- to 6- membered monocyclic heteroaryl comprising 1 to 3 nitrogen atoms. More preferably, the heteroaryl is 9-membered fused bicyclic heteroaryl comprising two nitrogen atoms. Some non- limiting examples of heteroaryl include thiazolyl (e.g. thiazol-2-yl), pyrazolyl (e.g.1H-pyrazol- 4-yl, 1H-pyrazol-3-yl), imidazolyl (e.g. imidazole-1-yl), pyridyl (e.g.2-pyridyl, 3-pyridyl) pyrimidinyl (e.g. pyrimidin-5-yl), pyrazinyl (pyrazine-2-yl), triazolyl (e.g.4H-1,2,4-triazol-3- yl), indazolyl (e.g.1H-indazol-4-yl, 1H-indazol-7-yl), benzotriazolyl (e.g 1H-benzotriazol-4-yl), quinazolinyl (e.g. quinazolin-8-yl), pyrazolo[1,5-a]pyridinyl (e.g. pyrazolo[1,5-a]pyridin-7-yl, pyrazolo[1,5-a]pyridin-4-yl), indolinyl (e.g. indolin-7-yl), spiro[cyclopropane-1,3'-indoline]yl (e.g. spiro[cyclopropane-1,3'-indoline]-7'-yl), ,benzoxazolyl (e.g.1,3-benzoxazol-7-yl), and imidazo[1,2-a]pyridinyl (e.g. imidazo[1,2-a]pyridin-5-yl). Particularly preferred, yet non- limiting examples of heteroaryl include 1H-indazol-4-yl, 1H-indazol-7-yl, imidazo[1,2- a]pyridin-5-yl. The term “heterocyclyl” refers to a saturated mono- or bicyclic, preferably monocyclic ring system having 3 to 10 ring atoms, preferably 5 to 6 ring atoms, more preferably 3 to 8 ring atoms, wherein 1, 2, or 3 of said ring atoms are heteroatoms independently selected from N, O and S, the remaining ring atoms being carbon. In some preferred embodiments, heterocyclyl is monocyclic ring system having 5 to 6 ring atoms, wherein 1 to 2 of said ring atoms are independently selected from N and O. In still other preferred embodiments, heterocyclyl is monocyclic ring system having 5 to 6 ring atoms, wherein one of said ring atoms is nitrogen. Some non-limiting examples of heterocyclyl groups include pyrrolidinyl (e.g. pyrrolidin-3-yl, pyrrolidin-2-yl), piperidyl (e.g.3-piperidyl, 4-piperidyl), morpholinyl (e.g. morpholin-2-yl, morpholin-3-yl), tetrahydrofuranyl (e.g. tetrahydrofuran-2-yl, tetrahydrofuran-3-yl), 2- azaspiro[3.3]heptan-2-yl, azetidinyl. A particularly preferred, yet non-limiting example of heterocyclyl is morpholin-3-yl. The term “hydroxy”, alone or in combination with other groups, refers to -OH. The term “methylsulfonyl” refers to a group CH3S(O)2-. The term “oxo”, alone or in combination with other groups, refers to =O. The term "pharmaceutically acceptable salt" refers to those salts which retain the biological effectiveness and properties of the free bases or free acids, which are not biologically or otherwise undesirable. The salts are formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid and the like, in particular hydrochloric acid, and organic acids such as acetic acid, propionic acid, glycolic acid, pyruvic acid, oxalic acid, maleic acid, malonic acid, succinic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, p- toluenesulfonic acid, salicylic acid, N-acetylcystein and the like. In addition, these salts may be prepared by addition of an inorganic base or an organic base to the free acid. Salts derived from an inorganic base include, but are not limited to, the sodium, potassium, lithium, ammonium, calcium, magnesium salts and the like. Salts derived from organic bases include, but are not limited to salts of primary, secondary, and tertiary amines, substituted amines including naturally occurring substituted amines, cyclic amines and basic ion exchange resins, such as isopropylamine, trimethylamine, diethylamine, triethylamine, tripropylamine, ethanolamine, lysine, arginine, N-ethylpiperidine, piperidine, polyimine resins and the like. Particular pharmaceutically acceptable salts of compounds of formula (I) are hydrochloride. The compounds of formula (I) can contain several asymmetric centers and can be present in the form of optically pure enantiomers, mixtures of enantiomers such as, for example, racemates, optically pure diastereioisomers, mixtures of diastereoisomers, diastereoisomeric racemates or mixtures of diastereoisomeric racemates. According to the Cahn-Ingold-Prelog Convention, the asymmetric carbon atom can be of the "R" or "S" configuration. The abbreviation “sEH” refers to soluble epoxide hydrolases. The abbreviation “hsEH” refers to human soluble epoxide hydrolases. The abbreviation “19,20-EpDPA” refers to (±)19,20-epoxy-4Z,7Z,10Z,13Z,16Z- docosapentaenoic acid. The abbreviation “19,20-DiHDPA” refers to (±)19,20-dihydroxy-4Z,7Z,10Z,13Z,16Z- docosapentaenoic acid. The term “treatment” as used herein includes: (1) inhibiting the state, disorder or condition (e.g. arresting, reducing or delaying the development of the disease, or a relapse thereof in case of maintenance treatment, of at least one clinical or subclinical symptom thereof); and / or (2) relieving the condition (i.e., causing regression of the state, disorder or condition or at least one of its clinical or subclinical symptoms). The benefit to a patient to be treated is either statistically significant or at least perceptible to the patient or to the physician. However, it will be appreciated that when a medicament is administered to a patient to treat a disease, the outcome may not always be effective treatment. The term “prophylaxis” as used herein includes: preventing or delaying the appearance of clinical symptoms of the state, disorder or condition developing in a human that may be afflicted with or predisposed to the state, disorder or condition but does not yet experience or display clinical or subclinical symptoms of the state, disorder or condition. The term “neurodegenerative diseases” relates to diseases that are related to the progressive loss of structure or function of neurons, including death of neurons. Examples of neurodegenerative diseases include, but are not limited to, multiple sclerosis, Alzheimer’s disease, Parkinson’s disease and amyotrophic lateral sclerosis. The term “pain” relates to an unpleasant sensory and emotional experience associated with actual or potential tissue damage. Examples of pain include, but are not limited to, nociceptive pain, chronic pain (including idiopathic pain), neuropathic pain including chemotherapy induced neuropathy, phantom pain and phsychogenic pain. A particular example of pain is neuropathic pain, which is caused by damage or disease affecting any part of the nervous system involved in bodily feelings (i.e., the somatosensory system). In one embodiment, “pain” is neuropathic pain, e.g. neuropathic pain resulting from amputation or thoracotomy. In one embodiment, “pain” is chemotherapy induced neuropathy. The term “diabetic retinopathy” as used herein refers to a medical condition characterized by damage to the blood vessels in the retina of the eye, primarily resulting from complications associated with diabetes mellitus. of the Invention In a first aspect, the present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0, 1 or 2; A is C3-8-cycloalkyl, or 3- to 10-membered heterocyclyl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; RA1is hydrogen, or a group ; RA2and RA3are each independently hydrogen, hydroxy, halogen, cyano, C1-6-alkyl, halo- C1-6-alkyl, or hydroxy-C1-6-alkyl; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl; B is C6-10-aryl or 5- to 14-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- to 10- membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; wherein said 5- to 10-membered heteroaryl is optionally substituted with 1 to 3 C1-6-alkyl substituents; and RB2is hydrogen, halogen, C1-6-alkyl, C1-6-alkoxy, or halo-C1-6-alkyl; 1 R is C1-6-alkyl or a group , wherein said C1-6-alkyl is optionally substituted with one or two substituents R1a; each R1ais independently hydroxy, halogen, cyano, halo-C1-6-alkyl, C1-6-alkoxy, amino, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-8-cycloalkyl,(ii) C6-10-aryl,(iii) 5- to 10-membered heteroaryl comprising 1 to 3 heteroatoms independentlyselected from N, O, and S, and the remaining atoms being carbon, or (iv) 3- to 10-membered heterocyclyl comprising 1 to 3 heteroatoms independentlyselected from N, O, and S, and the remaining atoms being carbon; RCis hydrogen, hydroxy-C1-6-alkyl, C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C6- 10-aryl, halo-C1-6-alkoxy, hydroxy, halogen, or cyano; and R2is selected from hydrogen, halogen, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, and halo-C1-6-alkoxy. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0, 1 or 2; A is C3-8-cycloalkyl, or 3- to 10-membered heterocyclyl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; RA1is a group ; RA2and RA3are each independently hydrogen, hydroxy, halogen, cyano, C1-6-alkyl, halo- C1-6-alkyl, or hydroxy-C1-6-alkyl; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl; B is C6-10-aryl or 5- to 14-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- to 10- membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; wherein said 5- to 10-membered heteroaryl is optionally substituted with 1 to 3 C1-6-alkyl substituents; and RB2is hydrogen, halogen, C1-6-alkyl, C1-6-alkoxy, or halo-C1-6-alkyl; R1is a group , C2-6-alkyl, or C1-6-alkyl substituted with one or two substituents R1a; each R1ais independently hydroxy, halogen, cyano, halo-C1-6-alkyl, C1-6-alkoxy, amino, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-8-cycloalkyl,(ii) C6-10-aryl,(iii) 5- to 10-membered heteroaryl comprising 1 to 3 heteroatoms independentlyselected from N, O, and S, and the remaining atoms being carbon, or (iv) 3- to 10-membered heterocyclyl comprising 1 to 3 heteroatoms independentlyselected from N, O, and S, and the remaining atoms being carbon; RCis hydrogen, hydroxy-C1-6-alkyl, C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C6- 10-aryl, halo-C1-6-alkoxy, hydroxy, halogen, or cyano; and R2is selected from hydrogen, halogen, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, and halo-C1-6-alkoxy wherein the term “cycloalkyl” refers to a saturated mono- or bicyclic hydrocarbon group; and the term “heterocyclyl” refers to a saturated mono- or bicyclic ring system. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein n is 0 or 1. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein n is 0. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is C3-6-cycloalkyl or 5- to 6- membered heterocyclyl comprising nitrogen and the remaining atoms being carbon. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is C3-6-cycloalkyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is 5- to 6-membered heterocyclyl comprising nitrogen and the remaining atoms being carbon. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is C3-4- cycloalkyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is: , In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is: , wherein RA1is as defined herein. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is: . In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein A is: ; wherein RA1is as defined herein. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: RA1is a group wherein RB1 and RB2 are as defined herein.In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: RA2is hydrogen, hydroxy, fluoro, methyl, trifluoromethyl, 2,2,2-trifluoroethyl, or hydroxymethyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form cyclopropyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein RA2and RA3are both hydrogen. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0 or 1; A is C3-6-cycloalkyl or 5- to 6-membered heterocyclyl comprising nitrogen and the remaining atoms being carbon; RA1is hydrogen, or a group ; RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl;wherein RB1 and RB2 are as defined herein.In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0 or 1; ; RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl;wherein RB1 and RB2 are as defined herein. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0 or 1; RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl;wherein RB1 and RB2 are as defined herein.In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0; A is C3-6-cycloalkyl; RA1is a group ; RA2and RA3are both hydrogen;wherein RB1 and RB2 are as defined herein. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0; ; RA2and RA3are both hydrogen;wherein RB1 and RB2 are as defined herein.In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0; ; RA2and RA3are both hydrogen;wherein RB1 and RB2 are as defined herein.In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is phenyl, 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, and the remaining atoms being carbon, or 9- to 12-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is phenyl, 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, and the remaining atoms being carbon, or 9- to 12-membered bi- or tricyclic heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is phenyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is 9- to 12-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is phenyl or 9- membered heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is phenyl or 9- membered fused bicyclic heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is 9-membered fused bicyclic heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: ,In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: .In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: , In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is:,. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: ,, , , , .In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: , , , .In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is:.In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- membered heteroaryl comprising 2 or 3 nitrogen atoms, the remaining atoms being carbon; wherein said 5-membered heteroaryl is optionally substituted with one or two C1-6-alkyl substituents; and RB2is hydrogen, halogen, or C1-6-alkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: RB1is hydrogen, halogen, or C1-6-alkyl; and RB2is hydrogen or C1-6-alkyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: RB1is hydrogen, fluoro, chloro, methyl, trifluoroalkyl, methoxy, cyano, oxo, 1- methylpyrazol-3-yl, 3,5-dimethyl-1H-pyrazol-4-yl or, 1H-1,2,4-triazol-5-yl; and RB2is hydrogen, chloro, methyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein B is: RB1is hydrogen, fluoro, or methyl; and RB2is hydrogen or methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: B is phenyl, 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, and the remaining atoms being carbon, or 9- to 12-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon; RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- membered heteroaryl comprising 2 or 3 nitrogen atoms, the remaining atoms being carbon; wherein said 5-membered heteroaryl is optionally substituted with one or two C1-6-alkyl substituents; and RB2is hydrogen, halogen, or C1-6-alkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: B is phenyl or 9-membered fused bicyclic heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon; RB1is hydrogen, halogen, or C1-6-alkyl; and RB2is hydrogen or C1-6-alkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: ;RB1is hydrogen, halogen, or C1-6-alkyl; and RB2is hydrogen or C1-6-alkyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: ;RB1is hydrogen, fluoro, or methyl; and RB2is hydrogen or methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is C1-6-alkyl or a group , wherein said C1-6-alkyl is optionally substituted with one or two substituents R1a; one R1ais hydroxy, halo-C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; and another R1a, if present, is hydroxy or C1-6-alkoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-4-cycloalkyl,(ii) phenyl,(iii) 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selectedfrom N and S, the remaining atoms being carbon, or (iv) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: 1 R is C1-6-alkyl or a group , wherein said C1-6-alkyl is substituted with one R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy; L is *–O(CH2)2– or -CH2-, wherein * denotes the point of attachment of L to ring C; C is (i) C3-4-cycloalkyl, or(ii) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis C1-6-alkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is C1-4-alkyl or a group , wherein said C1-6-alkyl is optionally substituted with one or two substituents R1a; wherein one R1ais hydroxy, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoroethoxy, difluoroethoxy, trifluoroethoxy, (CH3)2N-, CH3-C(O)NH-, (CH3)2N- C(O)-, methylsulfonyl; another R1a, if present, is hydroxy or ethoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; Cis cyclopropyl; cyclobuthyl; phenyl; ; RCis hydrogen, methyl, hydroxymethyl, ethoxy, ethoxymethyl, phenyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: 1 R is ethyl or a group , wherein said ethyl substituted with one R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy; L is *–O(CH2)2–, or -CH2-, wherein * denotes the point of attachment of L to ring C;C is cyclopropyl or ;RCis methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is a group , C2-6-alkyl, or C1-6-alkyl substituted with one or two substituents R1a; one R1ais hydroxy, halo-C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; and another R1a, if present, is hydroxy or C1-6-alkoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-4-cycloalkyl,(ii) phenyl,(iii) 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selectedfrom N and S, the remaining atoms being carbon, or (iv) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; and RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is a group or C1-6-alkyl substituted with one R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy; L is *–O(CH2)2– or -CH2-, wherein * denotes the point of attachment of L to ring C; C is(i) C3-4-cycloalkyl, or(ii) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; and RCis C1-6-alkyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is a group C2-4-alkyl or C2-4-alkyl substituted with one or two substituents R1a; wherein one R1ais hydroxy, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoroethoxy, difluoroethoxy, trifluoroethoxy, (CH3)2N-, CH3-C(O)NH-, (CH3)2N- C(O)-, methylsulfonyl; another R1a, if present, is hydroxy or ethoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; Cis cyclopropyl; cyclobuthyl; phenyl, ,, is hydrogen, methyl, hydroxymethyl, ethoxy, ethoxymethyl, phenyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is ethyl or a group , wherein said ethyl substituted with one R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy; L is *–O(CH2)2–, or -CH2-, wherein * denotes the point of attachment of L to ring C; Cis cyclopropyl or ;andRCis methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein R2is hydrogen, halogen or C1-6- alkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein R2is hydrogen or halogen. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein R2is hydrogen, chloro, fluoro or methyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein R2is hydrogen and fluoro. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is C1-6-alkyl or a group , wherein said C1-6-alkyl is optionally substituted with one or two substituents R1a; one R1ais hydroxy, halo-C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; and another R1a, if present, is hydroxy or C1-6-alkoxy; L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-4-cycloalkyl,(ii) phenyl,(iii) 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selectedfrom N and S, the remaining atoms being carbon, or (iv) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl; and R2is hydrogen, halogen or C1-6-alkyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: 1 R is C1-6-alkyl or a group , wherein said C1-6-alkyl is substituted with one R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy; L is *–O(CH2)2– or -CH2-, wherein * denotes the point of attachment of L to ring C; C is (i) C3-4-cycloalkyl, or(ii) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis C1-6-alkyl; and R2is hydrogen or halogen. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: 1 R is ethyl or a group , wherein said ethyl substituted with one R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy; L is *–O(CH2)2–, or -CH2-, wherein * denotes the point of attachment of L to ring C; Cis cyclopropyl or ; RCis methyl; and R2is hydrogen or fluoro. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is C1-6-alkyl optionally substituted with one or two substituents R1a;wherein R1a is as defined herein.In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1C1-6-alkyl substituted with one substituent R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: R1is ethyl substituted with one substituents R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: 1 R is a group ; wherein Rc, C and L are as defined herein. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: C is C3-4-cycloalkyl; RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: L is *–O(CH2)2–, wherein * denotes the point of attachment of L to ring C; C is C3-4-cycloalkyl; RCis C1-6-alkyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: C is cyclopropyl; RCis methyl. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is phenyl or 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, the remaining atoms being carbon; RCis hydrogen. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is phenyl, thiazol-2-yl, 1H-pyrazol-5-yl, or 2-pyridyl; RCis hydrogen. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independently selected from N and O, the remaining atoms being carbon; RCis hydrogen or C1-6-alkyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: L is -CH2-; C is 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independently selected from N and O, the remaining atoms being carbon; RCis hydrogen or C1-6-alkyl. In a particularly preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: ;RCis methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0 or 1 A is C3-6-cycloalkyl or 5- to 6-membered heterocyclyl comprising nitrogen and the remaining atoms being carbon; RA1is a group ; RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl; B is phenyl, 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, and the remaining atoms being carbon, or 9- to 12-membered bi- or tricyclic heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon; RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- membered heteroaryl comprising 2 or 3 nitrogen atoms, the remaining atoms being carbon; wherein said 5-membered heteroaryl is optionally substituted with one or two C1-6-alkyl substituents; and RB2is hydrogen, halogen, or C1-6-alkyl; 1 R is a group , C2-6-alkyl or C1-6-alkyl substituted with one or two substituents R1a; one R1ais hydroxy, halo-C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; and another R1a, if present, is hydroxy or C1-6-alkoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-4-cycloalkyl,(ii) phenyl,(iii) 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selectedfrom N and S, the remaining atoms being carbon, or (iv) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl; and R2is hydrogen, halogen, C1-6-alkyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: n is 0; A is C3-6-cycloalkyl; RA1is a group ; RA2and RA3are both hydrogen; B is phenyl or 9-membered fused bicyclic heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon; RB1is hydrogen, halogen, or C1-6-alkyl; and RB2is hydrogen or C1-6-alkyl; R1is a group , C2-6-alkyl, or C1-6-alkyl substituted with one R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy; L is *–O(CH2)2– or -CH2-, wherein * denotes the point of attachment of L to ring C; C is (i) C3-4-cycloalkyl, or(ii) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis C1-6-alkyl; and R2is hydrogen or halogen. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0 or 1 A is: ; RA2is hydrogen, hydroxy, fluoro, methyl, trifluoromethyl, 2,2,2-trifluoroethyl, or hydroxymethyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form cyclopropyl; B is: RB1is hydrogen, fluoro, chloro, methyl, trifluoroalkyl, methoxy, cyano, oxo, 1- methylpyrazol-3-yl, 3,5-dimethyl-1H-pyrazol-4-yl or, 1H-1,2,4-triazol-5-yl; and RB2is hydrogen, chloro, methyl; 1 R is a group , C2-4-alkyl, or C1-4-alkyl substituted with one or two substituents R1a; wherein one R1ais hydroxy, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoroethoxy, difluoroethoxy, trifluoroethoxy, (CH3)2N-, CH3-C(O)NH-, (CH3)2N- C(O)-, methylsulfonyl;another R1a, if present, is hydroxy or ethoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2;C is cyclopropyl, cyclobuthyl, phenyl, , , RCis hydrogen, methyl, hydroxymethyl, ethoxy, ethoxymethyl, phenyl; and R2is hydrogen, chloro, fluoro, or methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0 ; RA2and RA3are both hydrogen; B is: ;RB1is hydrogen, fluoro, or methyl; and RB2is hydrogen or methyl; 1 R is ethyl or a group , wherein said ethyl substituted with one R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy; L is *–O(CH2)2–, or -CH2-, wherein * denotes the point of attachment of L to ring C; Cis cyclopropyl or ; RCis methyl; and R2is hydrogen, chloro, fluoro, or methyl. In one embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein said compound of formula (I) is selected from the group consisting of: trans-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; cis-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[6-(trifluoromethyl)-2- pyridyl]cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[6-(trifluoromethyl)-2- pyridyl]cyclobutyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[2-(trifluoromethyl)-3- pyridyl]cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[2-(trifluoromethyl)-3- pyridyl]cyclobutyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-[2-(3,5-dimethyl-1H-pyrazol-4- yl)phenyl]cyclopropyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(2-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(2-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylbenzotriazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylbenzotriazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(4-methylquinazolin-8-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(4-methylquinazolin-8-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-(3-phenyl-1-bicyclo[1.1.1]pentanyl)pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[3-[3-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-N-[3-(1,3-benzoxazol-7-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; cis-N-[3-(1,3-benzoxazol-7-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-(3-fluoro-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-(3-fluoro-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide trans-1-(2-ethoxyethyl)-N-[3-(3-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(3-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1'-methyl-2'-oxo-spiro[cyclopropane-1,3'-indoline]-7'- yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1'-methyl-2'-oxo-spiro[cyclopropane-1,3'-indoline]-7'- yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; trans-N-[3-(2-chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(2-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; trans-N-[3-(3-chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide; trans-N-[3-(4-chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(o-tolyl)cyclobutyl]-6-oxo-pyridine-3-carboxami; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[4-(1H-1,2,4-triazol-5-yl)phenyl]cyclobutyl]pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-[3-(1-methylpyrazol-3-yl)phenyl]cyclobutyl]-6-oxo- pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[3-[4-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(5,6-dichloro-2-pyridyl)-pyrrolidin-3-yl]pyri-dine-3- carboxamide; N-[1-(2-cyano-3-pyridyl)pyrrolidin-3-yl]-1-(2-ethoxy-ethyl)-6-oxo-pyri-dine-3- carboxamide; N-[1-(2-cyano-3-pyridyl)pyrrolidin-3-yl]-1-(2-ethoxy-ethyl)-6-oxo-pyri-dine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(5-chloro-2-pyridyl)-pyrro-li-din-3-yl]pyri-dine-3- carboxamide; 1-(2-ethoxyethyl)-N-(3-methylcyclo-hexyl)-6-oxo-pyri-dine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[4-(3-pyridyl)cyclohexyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(hydroxymethyl)-3-phenyl-cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(hydroxymethyl)-3-phenyl-cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(4-methoxyphenyl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3-phenyl-1-bicyclo[1.1.1]pentanyl)methyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[(3-phenylcyclobutyl)methyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[(3-phenylcyclobutyl)methyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-thiazol-2-ylcyclobutyl)pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-thiazol-2-ylcyclobutyl)pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-(3-hydroxy-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylpyrazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylpyrazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-(2,2,2-trifluoroethyl)cyclobutyl]pyridine-3- carboxamide; cis 1-(2-ethoxyethyl)-6-oxo-N-[3-(2,2,2-trifluoroethyl)cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-(trifluoromethyl)cyclobutyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-(trifluoromethyl)cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-(3-pyridyl)cyclobutyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-(3-pyridyl)cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-7-ylcyclobutyl)pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-7-ylcyclobutyl)pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-4-ylcyclobutyl)pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-4-ylcyclobutyl)pyridine-3- carboxamide; trans-6-Oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-morpholin-2-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2R)-morpholin-2-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3S)-3-piperidyl]-methyl]-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3R)-3-piperidyl]-methyl]-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3R)-morpholin-3-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3S)-morpholin-3-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-4-methylmorpholin-2-yl]methyl]pyridine-3- carboxamide; trans-1-(2-acetamidoethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide trans-1-[1-(hydroxymethyl)cyclopropyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3- carboxamide; trans-5-chloro-6-oxo-N-(3-phenylcyclobutyl)-1-thiazol-2-yl-pyridine-3-carboxamide; trans-5-methyl-6-oxo-N-(3-phenyl-cyclo-butyl)-1-thiazol-2-yl-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-methyl-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-5-fluoro-1-[2-(1-methylcyclopro-po-xy)ethyl]-6-oxo-N-(3- phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[2-(1-methylcycloprop-oxy)ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3- carboxamide; 1-[2-(1-methylcyclopropoxy)ethyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 5-chloro-1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-5-methyl-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-benzyl-6-oxo-N-[(1R,2S)-2-phenylcyclo-propyl]-pyridine-3-carboxamide; 6-oxo-1-(1-phenyl-cyclopropyl)-N-[(1R,2S)-2-phenyl-cyclo-propyl]pyridi-ne-3- carboxamide; 6-oxo-1-phenyl-N-[ (1R,2S)-2-phenyl-cyclo-propyl]-pyridine-3-carboxamide; 6-oxo-1-(2-phenyl-ethyl)-N-[(1R,2S)-2-phenylcyclopropyl]-pyridine-3-carboxamide; 1-isobutyl-6-oxo-N-[(1R,2S)-2-phenyl-cyclopropyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(2-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-(2-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]-1-(tetrahydrofuran-2-ylmethyl)pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-(1-phenyl-4-piperidyl)pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(4-chlorophenyl)-cyclo-propyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(4-fluorophenyl)cyclo-propyl]pyridine-3- carboxamide; 6-oxo-1-(1H-pyrazol-5-yl)-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-phenylpyrrolidin-3-yl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3S)-1-phenylpyrrolidin-3-yl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(6R)-4-phenyl-4-azaspiro[2.4]heptan-6-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-pyri-midin-5-ylpyrrolidin-3-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(1-methylpyrazol-4-yl)pyrrolidin-3-yl]-pyri-dine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-pyrazin-2-ylpyrroli-din-3-yl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(4-chlorophenyl)pyrrolidin-3-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(3-chlorophenyl)pyrrolidin-3-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(2-chlorophenyl)pyrrolidin-3-yl]pyridine-3- carboxamide; trans-1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3- carboxamide; trans-1-(2-hydroxy-ethyl)-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[2-(dimethylamino)-ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[3-(dimethylamino)-3-oxo-propyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-(3,3,3-trifluoro-2-hydroxy-propyl)pyridine-3- carboxamide; trans-1-[2-(2-fluoroethoxy)ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[2-(2,2-difluoroethoxy)-ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[2-(2,2,2-trifluoroethoxy)-ethyl]pyridine-3- carboxamide; cis-1-(3-ethoxycyclo-butyl)-6-oxo-N-(trans-3-phenylcyclo-butyl)pyridine-3-carboxamide; trans-1-(methylsulfonylmethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; 6-Oxo-1-(2-phenoxyethyl)-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-(2-methoxyethyl)-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-[2-(difluorometho-xy)-ethyl]-6-oxo-N-[(1R,2S)-2-phenyl-cyclopropyl]pyridine-3- carboxamide; 1-[2-(trifluorometho-xy)-ethyl]-6-oxo-N-[(1R,2S)-2-phenyl-cyclopropyl]pyridine-3- carboxamide; 1-[(1-ethoxycyclo-pro-pyl)methyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-[1-(ethoxymethyl)-cyclopropyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]-1-thiazol-2-yl-pyridine-3-carboxamide; and 6-oxo-1-(2-pyridyl-methyl)-N-[(1R,2S)-2-phenylcyclopro-pyl]-pyridine-3-carboxamide. In a preferred embodiment, the present invention provides a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein said compound of formula (I) is selected from the group consisting of: trans-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-4-methylmorpholin-2-yl]methyl]pyridine-3- carboxamide; trans-5-fluoro-1-[2-(1-methylcyclopro-po-xy)ethyl]-6-oxo-N-(3- phenylcyclobutyl)-pyridine-3-carboxamide; and trans-6-oxo-N-(3-phenylcyclobutyl)-1-[2-(2,2,2-trifluoroethoxy)-ethyl]pyridine-3- carboxamide. In a particular embodiment, the present invention provides pharmaceutically acceptable salts of the compounds according to formula (I) as described herein, especially hydrochloride salts. In a further particular embodiment, the present invention provides compounds according to formula (I) as described herein. In some embodiments, the compounds of formula (I) are isotopically-labeled by having one or more atoms therein replaced by an atom having a different atomic mass or mass number. Such isotopically-labeled (i.e., radiolabeled) compounds of formula (I) are considered to be within the scope of this disclosure. Examples of isotopes that can be incorporated into the compounds of formula (I) include isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorous, sulfur,fluorine, chlorine, and iodine, such as, but not limited to, 2H, 3H, 11C, 13C, 14C, 13N, 15N, 15O,17O, 18O, 31P, 32P, 35S, 18F, 36Cl, 123I, and 125I, respectively. Certain isotopically-labeledcompounds of formula (I), for example, those incorporating a radioactive isotope, are useful indrug and / or substrate tissue distribution studies. The radioactive isotopes tritium, i.e. 3H, andcarbon-14, i.e., 14C, are particularly useful for this purpose in view of their ease of incorporationand ready means of detection. For example, a compound of formula (I) can be enriched with 1, 2, 5, 10, 25, 50, 75, 90, 95, or 99 percent of a given isotope.Substitution with heavier isotopes such as deuterium, i.e. 2H, may afford certain therapeuticadvantages resulting from greater metabolic stability, for example, increased in vivo half-life orreduced dosage requirements. Thus, the present invention encompasses compounds of formula (I) wherein one or more hydrogen atoms have been replaced by deuterium.Substitution with positron emitting isotopes, such as 11C, 18F, 15O and 13N, can be useful inPositron Emission Topography (PET) studies for examining substrate receptor occupancy. Isotopically-labeled compounds of formula (I) can generally be prepared by conventional techniques known to those skilled in the art or by processes analogous to those described in the Examples as set out below using an appropriate isotopically-labeled reagent in place of the non- labeled reagent previously employed. Processes of Manufacturing The preparation of compounds of formula (I) of the present invention may be carried out in sequential or convergent synthetic routes. Syntheses of the invention are shown in the following general schemes. The skills required for carrying out the reaction and purification of the resulting products are known to those persons skilled in the art. The substituents and indices used in the following description of the processes have the significance given herein, unless indicated to the contrary. If one of the starting materials, intermediates or compounds of formula (I) contain one or more functional groups which are not stable or are reactive under the reaction conditions of one or more reaction steps, appropriate protective groups (as described e.g., in “Protective Groups in Organic Chemistry” by T. W. Greene and P. G. M. Wutts, 5th Ed., 2014, John Wiley & Sons, N.Y.) can be introduced before the critical step applying methods well known in the art. Such protective groups can be removed at a later stage of the synthesis using standard methods described in the literature. If starting materials or intermediates contain stereogenic centers, compounds of formula (I) can be obtained as mixtures of diastereomers or enantiomers, which can be separated by methods well known in the art e.g., chiral HPLC, chiral SFC or chiral crystallization. Racemic compounds can e.g., be separated into their antipodes via diastereomeric salts by crystallization with optically pure acids or by separation of the antipodes by specific chromatographic methods using either a chiral adsorbent or a chiral eluent. It is equally possible to separate starting materials and intermediates containing stereogenic centers to afford diastereomerically / enantiomerically enriched starting materials and intermediates. Using such diastereomerically / enantiomerically enriched starting materials and intermediates in the synthesis of compounds of formula (I) will typically lead to the respective diastereomerically / enantiomerically enriched compounds of formula (I). A person skilled in the art will acknowledge that in the synthesis of compounds of formula (I) - insofar not desired otherwise - an “orthogonal protection group strategy” will be applied, allowing the cleavage of several protective groups one at a time each without affecting other protective groups in the molecule. The principle of orthogonal protection is well known in theart and has also been described in literature (e.g. Barany and R. B. Merrifield, J. Am. Chem. Soc.1977, 99, 7363; H. Waldmann et al., Angew. Chem. Int. Ed. Engl. 1996, 35, 2056). A person skilled in the art will acknowledge that the sequence of reactions may be varied depending on reactivity and nature of the intermediates. In more detail, the compounds of formula (I) can be manufactured by the methods given below, by the methods given in the examples or by analogous methods. Appropriate reaction conditions for the individual reaction steps are known to a person skilled in the art. Also, for reaction conditions described in literature affecting the described reactions see for example: Comprehensive Organic Transformations: A Guide to Functional Group Preparations, 2nd Edition, Richard C. Larock. John Wiley & Sons, New York, NY.1999). It was found convenient to carry out the reactions in the presence or absence of a solvent. There is no particular restriction on the nature of the solvent to be employed, provided that it has no adverse effect on the reaction or the reagents involved and that it can dissolve the reagents, at least to some extent. The described reactions can take place over a wide range of temperatures, and the precise reaction temperature is not critical to the invention. It is convenient to carry out the described reactions in a temperature range between -78 °C to reflux. The time required for the reaction may also vary widely, depending on many factors, notably the reaction temperature and the nature of the reagents. However, a period of from 0.5 hours to several days will usually suffice to yield the described intermediates and compounds. The reaction sequence is not limited to the one displayed in the schemes, however, depending on the starting materials and their respective reactivity, the sequence of reaction steps can be freely altered. If starting materials or intermediates are not commercially available or their synthesis not described in literature, they can be prepared in analogy to existing procedures for close analogues or as outlined in the experimental section. In general, the compounds of formula (I) according to the invention, wherein A, X, RA1, RA2, RA3, R1and R2are as defined herein, can be synthesized as shown in Scheme 1. Thus, a compound of formula (II), wherein A, X, RA1, RA2, and RA3are as defined herein, can be reacted with a compound of formula (III), wherein R1and R2are as defined herein, under conditions used generally for the formation of amides, known in the art, or mentioned, forexample, in P. Acosta-Guzmán, A. Ojeda-Porras, D. Gamba-Sánchez, Adv. Synth. Catal. 2023,365, 4359–4391. Scheme 1 As an example, a compound of formula (II), wherein A, X, RA1, RA2, and RA3are as defined herein, can be reacted with a stoichiometric amount of a compound of formula (III), wherein R1and R2are as defined herein, in the presence of a stoichiometric amount of an appropriate coupling agent, e.g. hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1]), further in the presence of an over-stoichiometric amount of an appropriate non- nucleophlic base, e.g. triethylamine or diisopropyl ethylamine, in an aprotic solvent, such as dimethylformamide, or dichloromethane. The obtained reaction mixtures may be purified by methods known in art, e.g. by column chromatography, reversed phase HPLC, normal phase HPLC, or supercritical fluid chromatography (SFC), using achiral or chiral solid phases. Alternatively, a compound of formula (I), wherein A, X, RA1, RA2, RA3, R1and R2are as defined herein, can be prepared as depicted in Scheme 2. Scheme 2 Thus, a compound of formula (II), wherein A, X, RA1, RA2, and RA3are as defined herein, can be reacted with an ester of formula (IV), wherein R1and R2are as defined herein, and R is methyl or ethyl, in the presence of catalytic or stoichiometric amounts of a suitable strong base, such as 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD, CAS [5807-14-7]), in a suitable aprotic solvent, e.g. tetrahydrofuran, at elevated temperatures, such as 40 – 80 °C. The obtained reaction mixtures may be purified by methods known in art, e.g. by column chromatography, reversed phase HPLC, normal phase HPLC, or supercritical fluid chromatography (SFC), using achiral or chiral solid phases. Yet alternatively, a compound of formula (I), wherein A, X, RA1, RA2, RA3, R1and R2are as defined herein, can be prepared as depicted in Scheme 3. A compound of formula (IV), wherein R1and R2are as defined herein, and R is methyl or ethyl, can be hydrolysed in the presence of stoichiometric amounts of a suitable base, such as sodium hydroxide, or lithium hydroxide, in an appropriate solvent, like water, lower alcohol, such as methanol or ethanol, or tetrahydrofuran, or mixtures thereof, to form respective compounds of formula (V), wherein R1and R2are as defined herein, and M is an alkali metal, such as lithium, sodium, or, potassium, preferably sodium or lithium. The resulting alkali carboxylates of formula (V) can be reacted with compounds of formula (III), wherein A, X, RA1, RA2, and RA3are as defined herein, under conditions described above for the reaction of carboxylic acids of formula (III) with amine of formula (II). As an example, a compound of formula (II), wherein A, X, RA1, RA2, and RA3are as defined herein, can be reacted with a stoichiometric amount of a compound of formula (V), in the presence of a stoichiometric amount of an appropriate coupling agent, e.g. hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1]), further in the presence of an over-stoichiometric amount of an appropriate non-nucleophlic base, e.g. triethylamine or diisopropyl ethylamine, in an aprotic solvent, such as dimethylformamide, or dichloromethane. The obtained reaction mixtures may be purified by methods known in art, e.g. by column chromatography, reversed phase HPLC, normal phase HPLC, or supercritical fluid chromatography (SFC), using achiral or chiral solid phases. Scheme 3 Compounds of formula (II) are either commercially available or can be synthesized using methods known in the art. Further, compounds of formula (II) can be accessed by a sequence depicted in Scheme 4. Scheme 4 Thus, compounds of formula (VI), wherein B, and RB1, RB2, RB3, RB4, are as defined herein, and Y is an appropriate reactive group, selected from halide, boronic ester, boronic acid, trisalkyltin, preferably bromide, or chloride, can be reacted with a compound of formula (VII), wherein A, RA2, RA3are as defined herein, PG is an appropriate base stabile protecting group, such as a carbamate, e.g. tert-butoxycarbonyl-, or benzyloxycarbonyl- carbamate, and Z is halide, preferably iodide, or bromide, in the presence of a stoichiometric amount of an appropriate inert base, e.g. alkali carbonate, such as sodium carbonate as well as in the presence of a catalytic or stoichiometric amount of one or more transition metal complexes, such as Palladium- and / or Iridium- and / or Nickel complexes, preferably [4,4′-bis(1,1-dimethylethyl)-2,2′-bipyridine- N1,N1′]bis[3,5-difluoro-2-[5-(trifluoromethyl)-2-pyridinyl-N]phenyl-C]Iridium(III) hexafluorophosphate (Ir[dF(CF3)ppy]2(dtbpy)(PF6), CAS [870987-63-6]), and [4,4′-bis(1,1- dimethylethyl)-2,2′-bipyridine] nickel (II) dichloride (NiCl2.dtbbpy, CAS [1034901-50-2]), further optionally in the presence of a stoichiometric amount of an appropriate reducing agent, e.g. tris(trimethylsilyl)silane (TTMSS, CAS [1873-77-4]), optionally under irradiation of visible or ultraviolet light, preferably LED light with a wavelength of 455 nm, in a polar aprotic solvent, such as dioxane or dimethoxyethane, under an inert atmosphere. The resulting compounds of formula (VIII) can then be deprotected to obtain compounds of formula (II), depending on the protecting group PG, by methods known in the art, e.g. as described in the book “Greene's Protective Groups in Organic Synthesis”, written by Peter G. M. Wuts, Theodora W. Greene (2006). In the case of PG being tert-butoxycarbonyl (Boc), cleavage of the protection group PG can be achieved e.g. by stirring with an excess of an appropriate organic or inorganic acid, such as trifluoroacetic acid or hydrochloric acid, either neat or in an appropriate organic solvent, such as dichloromethane, or 1,4-dioxane. In some cases, depending on the method of isolation, the compound of formula (II) is isolated as a salt of the potential acid used for the deprotection, or the purification. Likewise, the compound of formula (II) can be isolated e.g. as trifluoroacetate, hydrochloride, hydrobromide, or formate salt. Compounds of formulae (III) or (IV) are either commercially available or can be synthesized using methods known in the art. Further, compounds of formulae (III) or (IV) can be accessed by a sequence depicted in Scheme 5. Scheme 5 A compound of formula (IX), wherein R2is as defined herein, and R is methyl or ethyl, and which is either commercially available or can be synthesized using methods known in the art, can be reacted with a compound of formula (X), wherein R1is as defined herein, and W is a suitable leaving group, such as halogen, or sulfonate OSO2R’, wherein R’ is C1-6-alkyl, optionally substituted by 1-7 fluorine, or phenyl, optionally substituted by 1-2 halogen, nitro or C1-6-alkyl, e.g. bromine, chlorine, methylsulfonate, ethylsulfonate, trifluoromethylsulfonate or tolylsulfonate, in the presence of a suitable base, such as trialkylamine, or alkali carbonate, e.g. triethylamine or potassium carbonate, in an appropriate aprotic solvent, such as dichloromethane, or dimethylformamide. The resulting compounds of formula (IV) can be hydrolysed by standard methods known in the art, e.g. under aqueous basic conditions using sodium hydroxide and subsequent acidification and isolation of the corresponding acid of formula (III). Alternatively, compounds of formulae (III) or (IV) can be accessed by a sequence depicted in Scheme 6. Scheme 6 A compound of formula (XI), wherein R2is as defined herein, and R is methyl or ethyl, and which is either commercially available or can be synthesized using methods known in the art, can be reacted with a compound of formula (XII), wherein R1is as defined herein, optionally in the presence of a suitable base, such as alkali alkoxide, e.g. sodium methoxide, in an appropriate solvent, such as a lower alcohol, e.g. methanol or ethanol, or dimethylformamide, at elevated temperatures, such as 30 – 80 °C. The resulting compounds of formula (IV) can be hydrolysed by standard methods known in the art, e.g. under aqueous basic conditions using sodium hydroxide and subsequent acidification and isolation of the corresponding acid of formula (III). In some cases, the synthesis of compounds of formula (I), wherein A, X, RA1, RA2, RA3, R1and R2are as defined herein, requires the use of a suitable protection group, because the present functional groups are not compatible with the reaction conditions applied or would give rise to complex reaction mixtures. In this case, the synthesis of the final compound of formula (I) involves a final deprotection step. The deprotection can be performed, depending on the protection group, under conditions known in the art, e.g. described in the book “Greene's Protective Groups in Organic Synthesis”, written by Peter G. M. Wuts, Theodora W. Greene (2006). In the case of PG being tert-butoxycarbonyl (Boc), cleavage of the protection group PG can be achieved e.g. by stirring with an excess of an appropriate organic or inorganic acid, such as trifluoroacetic acid or hydrochloric acid, either neat or in an appropriate organic solvent, such as dichloromethane, or 1,4-dioxane. The obtained reaction mixtures may be purified by methods known in art, e.g. by column chromatography, reversed phase HPLC, normal phase HPLC, or supercritical fluid chromatography (SFC), using achiral or chiral solid phases.In some cases, depending on the method of isolation, the compound of formula (I) is isolated as a salt of the potential acid used for the deprotection, or the purification. Likewise, the compound of formula (I) can be isolated e.g. as trifluoroacetate, hydrochloride, hydrobromide, or formate salt. In one aspect, the present invention provides a process of manufacturing a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, wherein said process is as described in any one of schemes 1 to 6, or a combination thereof. In a further aspect, the present invention provides a compound of formula (I) as described herein, when manufactured according to any one of the processes described herein. sEH Inhibitory Activity Compounds of the present invention are sEH inhibitors. Thus, in one aspect, the present invention provides the use of compounds of formula (I) as described herein for inhibiting sEH in a human. In a further aspect, the present invention provides compounds of formula (I) as described herein for use in a method of inhibiting sEH in a human. In a further aspect, the present invention provides the use of compounds of formula (I) as described herein for the preparation of a medicament for inhibiting sEH in a human. In a further aspect, the present invention provides a method for inhibiting sEH in a human, which method comprises administering an effective amount of a compound of formula (I) as described herein to the human. Determination of enzymatic inhibitory IC50values reported herein were perfomed using a RapidFire Mass Sepctrometry (RFMS) based assay, with purified recombinant human soluble epoxide hydrolases proteins (hsEH). Enzyme concentrations were set to 0.5 nM. The enzyme was incubated at room temperature for 15min with compounds (top concentration: 10µM; semi- log dilution, 11 doses) in 50mM TRIS pH 8.0 buffer, containing also 1mM EDTA, 0.01% Tween20, 0.05% BSA and 2% DMSO. The substrate (19,20-EpDPA) was then added ([Substrate]= 4µM), and enzymatic reactions (final volume 20µL) were stopped after 1 hour of incubation at room temperature by addition of 40µL of 50:50 H2O:CH3CN stop solution. Those final mixtures were injected on RFMS platform (Agilent RapidFire 300 coupled with Thermo Scientific TSQ Quantiva mass spectrometer) to accurately quantify substrate (19,20-EpDPA, S) and product (19,20-DiHDPA, P) of the reaction. All measurements were done in triplicate, and P / (P+S) ratio was calculated for each sample. Compound activity was then determined by using Genedata analysis software. Results in the hsEH activity enzymatic assay are provided for compounds of formula (I) in Table 1. Table 1. Results in hsEH inhibitory activity Example No. IC50 (hsEH, nM) Example No. IC50 (hsEH, nM)1 0.5 73 2570.92 3541.2 74 42.5Example No. IC50 (hsEH, nM) Example No. IC50 (hsEH, nM)3 26.9 75 4.24 1.8 76 15.45 5.8 77 343.36 11.4 78 4.87 152.4 79 439.28 0.6 80 12.69 16.9 81 20.110 0.5 82 2.911 76.5 83 10.312 1.8 84 76.413 31.0 85 1024.615 0.4 86 36.616 148.6 87 29.217 1.0 88 0.918 0.6 89 341.119 0.3 90 1059.120 104.6 91 18.721 2.4 92 62.522 59.7 93 29.223 30.6 94 0.524 664.1 95 1.125 5.9 96 12.826 321.4 97 25.727 36.9 98 3.828 6.1 99 25.029 151.5 100 83.130 1.1 101 101.231 0.6 102 23.832 293.1 103 141.233 2.4 104 93.634 3.8 105 217.635 9.4 106 217.8Example No. IC50 (hsEH, nM) Example No. IC50 (hsEH, nM)36 10.8 107 23.037 2.1 108 46.538 36.1 109 19.139 3.0 110 245.540 54.7 111 176.341 0.8 112 175.642 6.3 113 19.843 1.0 114 63.644 1.5 115 209.245 12.8 116 18.346 92.6 117 292.247 43.9 118 154.548 2.3 119 36.449 40.8 120 175.750 14.3 121 62.151 55.3 122 13.552 148.6 123 3.153 56.5 124 5.454 133.8 125 25.155 87.5 126 298.656 4761.8 127 91.157 28.9 128 32.258 76.0 129 35.559 17.5 130 11.560 33.3 131 8.361 108.7 132 1.662 2156.0 133 64.563 188.4 134 25.464 134.0 135 29.665 345.2 136 195.966 124.8 137 336.467 1420.0 138 128.0Example No. IC50 (hsEH, nM) Example No. IC50 (hsEH, nM)68 143.7 139 295.769 8724.1 140 37.370 86.1 141 18.471 10000.0 142 169.572 9.8In one aspect, the present invention provides compounds of formula (I) and their pharmaceutically acceptable salts or esters as described herein, wherein said compounds of formula (I) and their pharmaceutically acceptable salts or esters have IC50’s for hsEH inhibition below 25 µM, preferably below 10 µM, more preferably below 5 µM as measured in the hsEH inhibitory assay described herein. In one embodiment, compounds of formula (I) and their pharmaceutically acceptable salts or esters as described herein have IC50(hsEH inhibition) values between 0.000001 µM and 25 µM, particular compounds have IC50 values between 0.000005 µM and 10 µM, further particular compounds have IC50 values between 0.00005 µM and 5 µM, as measured in the hsEH assay described herein. Using the Compounds of the Invention In one aspect, the present invention provides a compound of formula (I) as described herein for use as therapeutically active substance. In a further aspect, the present invention provides a compound of formula (I) as described herein for use in the treatment or prophylaxis of diseases and disorders that are associated with sEH. In a further aspect, the present invention provides a method for the treatment or prophylaxis of diseases and disorders that are associated with sEH in a human, which method comprises administering an effective amount of a compound of formula (I) as described herein to the human. In a further aspect, the present invention provides the use of a compound of formula (I) as described herein for the treatment or prophylaxis of diseases and disorders that are associated with sEH. In a further aspect, the present invention provides the use of a compound of formula (I) as described herein in the preparation of a medicament for the treatment or prophylaxis of diseases and disorders that are associated with sEH. In one embodiment, said diseases and disorders that are associated with sEH are selected from diabetic retinopathy, pain and neurodegenerative diseases. In one embodiment, said diseases and disorders that are associated with sEH are selected from diabetic retinopathy, neuropathic pain and neurodegenerative diseases. In a preferred embodiment, said diseases and disorders that are associated with sEH are diabetic retinopathy. In one embodiment, said diseases and disorders that are associated with sEH are neuropathic pain. In one embodiment, said diseases and disorders that are associated with sEH are neurodegenerative diseases. Pharmaceutical Compositions and Administration In one aspect, the present invention provides a pharmaceutical composition comprising a compound of formula (I) as described herein and a therapeutically inert carrier. The compounds of formula (I) and their pharmaceutically acceptable salts and esters can be used as medicaments (e.g. in the form of pharmaceutical preparations). The pharmaceutical preparations can be administered internally, such as orally (e.g. in the form of tablets, coated tablets, dragées, hard and soft gelatin capsules, solutions, emulsions or suspensions), nasally (e.g. in the form of nasal sprays) or rectally (e.g. in the form of suppositories). However, the administration can also be effected parentally, such as intramuscularly or intravenously (e.g. in the form of injection solutions). The compounds of formula (I) and their pharmaceutically acceptable salts and esters can be processed with pharmaceutically inert, inorganic or organic adjuvants for the production of tablets, coated tablets, dragées and hard gelatin capsules. Lactose, corn starch or derivatives thereof, talc, stearic acid or its salts etc. can be used, for example, as such adjuvants for tablets, dragées and hard gelatin capsules. Suitable adjuvants for soft gelatin capsules are, for example, vegetable oils, waxes, fats, semi- solid substances and liquid polyols, etc. Suitable adjuvants for the production of solutions and syrups are, for example, water, polyols, saccharose, invert sugar, glucose, etc. Suitable adjuvants for injection solutions are, for example, water, alcohols, polyols, glycerol, vegetable oils, etc. Suitable adjuvants for suppositories are, for example, natural or hardened oils, waxes, fats, semi- solid or liquid polyols, etc. Moreover, the pharmaceutical preparations can contain preservatives, solubilizers, viscosity- increasing substances, stabilizers, wetting agents, emulsifiers, sweeteners, colorants, flavorants, salts for varying the osmotic pressure, buffers, masking agents or antioxidants. They can also contain still other therapeutically valuable substances. The dosage can vary in wide limits and will, of course, be fitted to the individual requirements in each particular case. In general, in the case of oral administration a daily dosage of about 0.1 mg to 20 mg per kg body weight, preferably about 0.5 mg to 4 mg per kg body weight (e.g. about 300 mg per person), divided into preferably 1-3 individual doses, which can consist, for example, of the same amounts, should be appropriate. It will, however, be clear that the upper limit given herein can be exceeded when this is shown to be indicated. Tablet Formulation (Wet Granulation)Item Ingredients mg / tablet1. Compound of formula (I) 5 25 100 5002. Lactose Anhydrous DTG 125 105 30 1503. Sta-Rx 1500 6 6 6 304. Microcrystalline Cellulose 30 30 30 1505. Magnesium Stearate 1 1 1 1Total 167 167 167 831Manufacturing Procedure 1. Mix items 1, 2, 3 and 4 and granulate with purified water. 2. Dry the granules at 50°C. 3. Pass the granules through suitable milling equipment. 4. Add item 5 and mix for three minutes; compress on a suitable press. Capsule FormulationItem Ingredients mg / capsule1. Compound of formula (I) 5 25 100 5002. Hydrous Lactose 159 123 148 ---3. Corn Starch 25 35 40 704. Talc 10 15 10 255. Magnesium Stearate 1 2 2 5Total 200 200 300 600Manufacturing Procedure 1. Mix items 1, 2 and 3 in a suitable mixer for 30 minutes. 2. Add items 4 and 5 and mix for 3 minutes. 3. Fill into a suitable capsule. Examples The invention will be more fully understood by reference to the following examples. The claims should not, however, be construed as limited to the scope of the examples. In case the preparative examples are obtained as a mixture of enantiomers, the pure enantiomers can be separated by methods described herein or by methods known to the man skilled in the art, such as e.g., chiral chromatography (e.g., chiral SFC) or crystallization. All reaction examples and intermediates were prepared under an argon atmosphere if not specified otherwise. The compounds disclosed and described herein have been named using the IUPAC naming function of Biovia Draw 22.1. If there is a discrepancy between a depicted structure and a name given to that structure, then the depicted structure controls. The following abbreviations are used in the experimental part: THF = tetrahydrofuran; MTBE = methyl-tert-butylether; DMF = dimethylformamide; rt = room temperature, 20-25°C: Boc = t-butyloxycarbonyl: HPLC = High Performance Liquid Chromatography; HBTU = Hexafluorophosphate Benzotriazole Tetramethyl Uronium; HATU = Hexafluorophosphate Azabenzotriazole Tetramethyl Uronium; SFC = Supercritical Liquid Chromatography; Starting materials Basic chemicals and solvents were purchased and used as is without further purification. Intermediates Int-1, Int-2, Int-5, Int-8, Int-11, Int-12, Int-31, Int-34, Int-37, Int-38, Int-48, Int-51, Int-55, Int-56, Int-60, Int-63, Int-67, Int-68, Int-75 – Int-79, Int-83 – Int-85, Int-88, Int-96, Int- 97, Int-105 – Int-111, Int-125 – Int-135, Int-139, Int-140, Int-142, Int-147, Int-150, Int-153, Int- 156, Int-158, Int-162 – Int-165, Int-167, Int-170, Int-171, Int-177 – Int-198, Int-204 – Int-206, Int-208 – Int-210, Int-215, Int-218 are commercially available, or they can be synthesized using methods known in the art. INTERMEDIATES Intermediate 4: 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4) Step 1: Methyl 1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-3) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 1.00 g, 6.53 mmol) was dissolved in dimethylformamide (10 mL) and potassium carbonate (1.35 g, 9.79 mmol) was added. The suspension was stirred for 10 min at 25 °C. Then, 1-chloro-2-ethoxy-ethane (Int-2, 922 mg, 8.49 mmol) was added and the mixture was stirred at 80 °C for 110 min. After cooling, the mixture was filtered, and the filtrate was purified directly by reversed phase chromatography (40 g, Flash Column Welch Ultimate XB_C1820-40 μm, flow rate 20 ml / min, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 50:50 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to obtain the title compound as a yellow oil (983 mg, 4.36 mmol, 67% yield). MS m / z (ESI): 225.9 [M+H]+. Step 2: 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4) Methyl 1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-3, 1.80 g, 7.99 mmol) was dissolved in methanol (10 mL), and an aqueous solution of sodium hydroxide (4 M, 5.8 mL, 23.2 mmol) was added. The mixture was stirred at 25 °C for 1 h. Then, the mixture was concentrated in vacuo, the pH was adjusted to 5-6 by addition of 1M hydrochloric acid. The aqueous solution was extracted with ethyl acetate (3 x 50 mL), the combined extracts were dried over sodium sulfate, filtered and the filtrate was concentrated in vacuo to yield the title compound as a white solid (1.60 g, 7.58 mmol, 95% yield). MS m / z (ESI): 212.1 [M+H]+. Intermediate 7: 1-(2-ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-7) Step 1: Methyl 1-(2-ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylate (Int-6) Methyl 5-fluoro-6-oxo-1H-pyridine-3-carboxylate (Int-5, 700 mg, 4.09 mmol) was dissolved in dimethylformamide (5 mL) and potassium carbonate (848 mg, 6.14 mmol) was added. The suspension was stirred for 10 min at 25 °C. Then, 1-chloro-2-ethoxy-ethane (Int-2, 577 mg, 5.32 mmol) was added and the mixture was stirred at 80 °C for 16 h. After cooling, the mixture was filtered, and the filtrate was purified directly by reversed phase chromatography (40 g, Flash Column Welch Ultimate XB_C1820-40 μm, flow rate 20 ml / min, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 50:50 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to obtain the title compound as a white solid (610 mg, 2.51 mmol, 61% yield). MS m / z (ESI): 244.0 [M+H]+. Step 2: 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-7) Methyl 1-(2-ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylate (Int-6, 600 mg, 2.47 mmol) was dissolved in methanol (3 mL), and an aqueous solution of sodium hydroxide (2 M, 5.6 mL, 11.2 mmol) was added. The mixture was stirred at 25 °C for 1 h. Then, the mixture was concentrated in vacuo, the pH was adjusted to 3-4 by addition of 1 M hydrochloric acid. The aqueous solution was extracted with ethyl acetate (3 x 30 mL), the combined extracts were dried over sodium sulfate, filtered and the filtrate was concentrated in vacuo to yield the title compound as a white solid (570 g, 2.47 mmol, 100% yield). MS m / z (ESI): 229.9 [M+H]+. Intermediate 10: Methyl 5-chloro-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-10) Step 1: Methyl 5-chloro-6-oxo-1H-pyridine-3-carboxylate (Int-9) 5-Chloro-6-oxo-1H-pyridine-3-carboxylic acid (Int-8, 2.00 g, 11.5 mmol) was dissolved in methanol (28 mL) and hydrochloric acid (1.25 M, 28 mL, 35 mmol) was added. The mixture was stirred at 25 °C for 16 h. After that, it was concentrated in vacuo to obtain the title compound as a light yellow oil (2.20 g, quant.), that was used in the next step without further purification. MS m / z (ESI): 187.9 [M+H]+. Step 2: Methyl 5-chloro-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-10) Methyl 5-chloro-6-oxo-1H-pyridine-3-carboxylate (Int-9, 1.00 g, 5.33 mmol) was dissolved in dimethylformamide (10 mL) and potassium carbonate (2.21 g, 16.0 mmol) was added. The suspension was stirred for 10 min at 25 °C. Then, 1-chloro-2-ethoxy-ethane (579 mg, 5.33 mmol) was added and the mixture was stirred at 80 °C for 110 min. After cooling, the mixture was filtered, and the filtrate was purified directly by reversed phase chromatography (40 g, Flash Column Welch Ultimate XB_C1820-40 μm, flow rate 20 ml / min, acetonitrile / (water + 0.1% formic acid), gradient, 30:70 to 50:50 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to obtain the title compound as a yellow oil (200 mg, 0.77 mmol, 14% yield). MS m / z (ESI): 260.1 [M+H]+. Intermediate 14: 3-(1-Methylindazol-4-yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int- 14) Step 1: tert-Butyl N-[3-(1-methylindazol-4-yl)cyclobutyl]carbamate (Int-13)4-Bromo-1-methyl-indazole (Int-11, 150 mg, 0.71 mmol) was dissolved in degassed dimethoxyethane (4 mL), tert-butyl N-(3-iodocyclobutyl)carbamate (Int-12, 275 mg, 0.92 mmol), [4,4′-bis(1,1-dimethylethyl)-2,2′-bipyridine-N1,N1′]bis[3,5-difluoro-2-[5- (trifluoromethyl)-2-pyridinyl-N]phenyl-C]Iridium(III) hexafluorophosphate (Ir[dF(CF3)ppy]2(dtbpy)(PF6), CAS [870987-63-6], 8.0 mg, 0.01 mmol), [4,4′-bis(1,1- dimethylethyl)-2,2′-bipyridine] nickel (II) dichloride (NiCl2.dtbbpy, CAS [1034901-50-2], 1.4 mg, 0.01 mmol), tris(trimethylsilyl)silane (TTMSS, CAS [1873-77-4], 177 mg, 0.71 mmol) and sodium carbonate (151 mg, 1.42 mmol) were added. The mixture was again degassed and stirred at 25°C for 16 h under irradiation with a 455 nm blue LED. After that, the mixture was diluted with ethyl acetate (10 mL), and water (20 mL). Phases were separated, the aqueous phase was extracted with ethyl acetate (2 x 30 mL). The combined extracts were washed with brine (60 mL) and a saturated aqueous solution of calcium chloride (10 mL), dried over magnesium sulfate, filtered, and concentrated in vacuo. The residue was purified by preparative tlc (petroleum ether / ethyl acetate 5:1 (v / v), 254 nm, Rf = 0.25), followed by preparative HPLC (Phenomenex luna C18150 x 25 mm x 10 um, flow 25 mL / min, water (+0.1% formic acid) / acetonitrile, gradient 55:45 to 25:75). The product containing fractions were lyophilized to yield the title compound as a white solid (160 mg, 0.53 mmol, 75% yield). MS m / z (ESI): 302.2 [M+H]+. Step 2: 3-(1-Methylindazol-4-yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-14)tert-Butyl N-[3-(1-methylindazol-4-yl)cyclobutyl]carbamate (Int-13, 36 mg, 0.12 mmol) wasdissolved in dichloromethane (0.5 mL) and a solution of 2,2,2-trifluoroacetic acid in dichloromethane (1:5 (v / v), 2 mL) was added. The mixture was stirred at 25°C for 2 h. After that, it was concentrated in vacuo to yield the title compound as a light brown oil (36 mg, 0.11 mmol, 92% yield). MS m / z (ESI): 202.1 [M+H]+. In analogy to the procedure described for the preparation of intermediate Int-14, the following intermediates were prepared using the appropriate (het)aryl bromide instead of intermediate Int- 11: Code Structure Name Yieldm / z step (ESI) 1 / 2 (%) Int-15 3-(1,3-dimethylindazol-4-71 / 96 216.1yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-16 3-[6-(trifluoromethyl)-2-67 / 81 217.2pyridyl]cyclobutanamine 2,2,2- [M+H]+trifluoroacetate salt *TFA Int-17 3-[2-(trifluoromethyl)-3-70 / 94 217.1pyridyl]cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-18 3-(1-methylindazol-7-75 / 96 202.1yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-19 3-(5-fluoro-1-methyl-indazol-4-82 / 96 220.2yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-20 3-(6-fluoro-1-methyl-indazol-4-48 / 96 220.1yl)cyclobutanamine 2,2,2- [M+H]+trifluoroacetate salt *TFA Int-21 3-(2-methylindazol-4-70 / 97 202.1yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-22 3-(1-methylbenzotriazol-4-42 / 96 203.2yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-23 3-(4-methylquinazolin-8-83 / 96 214.1yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-24 3-(1,3-benzoxazol-7-34 / 98 189.2yl)cyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-25 3-(3-fluorophenyl)cyclobutanamine20 / 76 166.12,2,2-trifluoroacetate salt [M+H]+*TFA Int-26 7'-(3-aminocyclobutyl)-1'-methyl-65 / 96 243.2spiro[cyclopropane-1,3'-indoline]-2'- [M+H]+*TFA one 2,2,2-trifluoroacetate salt Int-27 3-[2-70 / 75 215.2(trifluoromethyl)phenyl]cyclobutan- [M+H]+amine 2,2,2-trifluoroacetate salt *TFA Int-28 3-pyrazolo[1,5-a]pyridin-7-57 / 95 188.2ylcyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-29 3-imidazo[1,2-a]pyridin-5-41 / 79 188.2ylcyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Int-30 3-pyrazolo[1,5-a]pyridin-4-48 / 95 188.2ylcyclobutanamine 2,2,2- [M+H]+*TFA trifluoroacetate salt Intermediate 33: (3-Phenyl-1-bicyclo[1.1.1]pentanyl)methanamine (Int-33) Step 1: 3-Phenylbicyclo[1.1.1]pentane-1-carboxamide (Int-32) 3-Phenylbicyclo[1.1.1]pentane-1-carboxylic acid (Int-31, 300 mg, 1.59 mmol) was dissolved in dimethylformamide (6 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 727 mg, 1.91 mmol) as well as diisopropyl ethylamine (1.39 mL, 7.97 mmol) were added. After stirring for 5 min at 0 – 4 °C (ice bath), ammonium chloride (174 mg, 3.19 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo, and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a yellow oil (238 mg, 1.27 mmol, 80% yield). MS m / z (ESI): 188.0 [M+H]+. Step 2: (3-Phenyl-1-bicyclo[1.1.1]pentanyl)methanamine (Int-33) 3-Phenylbicyclo[1.1.1]pentane-1-carboxamide (Int-32, 100 mg, 0.53 mmol) was dissolved in tetrahydrofuran (2 mL), the solution was cooled to 0 – 4 °C (ice bath), and a solution of lithium aluminum hydride (2.5 M in tetrahydrofuran, 0.85 mL, 2.14 mmol) was added. The mixture was stirred at 25 °C for 1 h. After that, the suspension was again cooled to 0 – 4 °C (ice bath), sodium sulfate decahydrate was added, the suspension stirred for 15 min, filtered, and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 96:4 to 66:34 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a yellow oil (70 mg, 0.40 mmol, 76% yield). MS m / z (ESI): 174.2 [M+H]+. Intermediate 36: (3-Phenylcyclobutyl)methanamine (Int-36) Step 1: 3-Phenylcyclobutanecarboxamide (Int-35) 3-Phenylcyclobutanecarboxylic acid (Int-34, 895 mg, 5.08 mmol) was dissolved in dimethylformamide (5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 2316 mg, 6.10 mmol) as well as diisopropyl ethylamine (4.42 mL, 25.40 mmol) were added. After stirring for 15 min at 0 – 4 °C (ice bath), ammonium chloride (554 mg, 10.16 mmol) was added at 15 °C and the resulting mixture was stirred at 15 °C for 1 h. Then, it was concentrated in vacuo, and the residue was purified by reversed phase chromatography (Phenomenex luna C18, 150 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v)). The product containing fraction was lyophilized to yield the title compound as a yellow solid (650 mg, 3.71 mmol, 73% yield). MS m / z (ESI): 176.1 [M+H]+. Step 2: (3-Phenylcyclobutyl)methanamine (Int-36) 3-Phenylcyclobutanecarboxamide (Int-35, 200 mg, 1.21 mmol) was dissolved in tetrahydrofuran (2 mL), the solution was cooled to 0 – 4 °C (ice bath), and a solution of lithium aluminum hydride (2.5 M in tetrahydrofuran, 1.83 mL, 4.57 mmol) was added. The mixture was stirred at 25 °C for 1 h. After that, the suspension was again cooled to 0 – 4 °C (ice bath), sodium sulfate decahydrate was added, the suspension stirred for 15 min, filtered, and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 96:4 to 66:34 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a yellow oil (92 mg, 0.57 mmol, 47% yield). MS m / z (ESI): 162.0 [M+H]+.Intermediates 43 and 44: cis-[3-(Benzylamino)-1-phenyl-cyclobutyl]methanol (Int-43) andtrans-[3-(benzylamino)-1-phenyl-cyclobutyl]methanol (Int-44) Step 1: 3,3-Dimethoxy-1-phenyl-cyclobutanecarbonitrile (Int-39) Sodium hydride (60% m / m dispersion in mineral oil, 764 mg, 19.1 mmol) was supended in dimethylsulfoxide (15 mL) and the suspension was cooled to 0 – 4 °C (ice bath). Benzyl cyanide (Int-37, 1.79 g, 15.3 mmol) was added slowly. The mixture was stirred at 0°C for 10 min and 1,3-dibromo-2,2-dimethoxypropane (Int-38, 2.00 g, 7.64 mmol) was added. The reaction mixture was stirred at 60 °C for 18 h. After cooling, it was poured into water (40 mL), and extracted with ethyl acetate (2 x 20mL). The combined organic layers were concentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, petroleum ether / ethyl acetate, gradient 100:1 to 20:1 (v / v)). The product containing fraction was concentrated invacuo to yield the title compound as an off-white solid (1.20 g, 5.52 mmol, 72% yield). 1H NMR(400 MHz, CDCl3): δ ppm 7.43 – 7.23 (m, 5H), 3.21 (s, 3H), 3.11 (s, 3H), 3.05 – 3.01 (m, 2H), 2.69 – 2.63 (m, 2H). Step 2: 3-Oxo-1-phenyl-cyclobutanecarbonitrile (Int-40) 3,3-Dimethoxy-1-phenyl-cyclobutanecarbonitrile (Int-39, 1.20 g, 5.52 mmol) was dissolved in acetone (10 mL) aqueous sulphuric acid (50% m / m, 0.1 mL) was added. The mixture was stirred at 75 °C for 6 h. After cooling, it was conentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, petroleum ether / ethyl acetate, gradient 100:1 to 10:1 (v / v)). The product containing fraction was concentrated in vacuo to afford the title compound as acolorless oil (900 mg, 5.26 mmol, 95% yield). 1H NMR (400 MHz, CDCl3): δ ppm 7.55 – 7.38(m, 5H), 4.11 – 4.02 (m, 2H), 3.78 – 3.69 (m, 2H). Step 3: 3-(Benzylamino)-1-phenyl-cyclobutanecarbonitrile (Int-41) 3-Oxo-1-phenyl-cyclobutanecarbonitrile (Int-40, 920 mg, 5.37 mmol) was dissolved in 1,2- dichloroethane (10 mL), acetic acid (161 mg, 2.69 mmol) and benzylamine (0.88 mL, 8.06 mmol) were added and the mixture was stirred for 30 min at 25 °C. Then, sodium triacetoxyborohydride (2.28 g, 10.75 mmol) was added and the mixture was stirred at 25 °C for 4.5 h. After that, the reaction was stopped by addition of saturated aqueous sodium hydrogencarbonate solution (10 mL), extracted with dichloromethane (2 x 20 mL), the combined organic layers were concentrated in vacuo. The residue was purified by column chromatography (silica gel, 20 g, petroleum ether / ethyl acetate, 3:1 (v / v)). The product containing fraction was concentrated in vacuo to yield the title compound as a colorless oil (1.10 g, 4.19 mmol, 78% yield). MS m / z (ESI): 263.4 [M+H]+. Step 4: Methyl 3-(benzylamino)-1-phenyl-cyclobutanecarboxylate (Int-42) 3-(Benzylamino)-1-phenyl-cyclobutanecarbonitrile (Int-41, 900 mg, 3.43 mmol) was dissolved in methanol (12 mL), and concentrated sulphuric acid (2.5 mL) was added. The mixture was stirred at 80 °C for 12 h. After cooling, it was concentrated in vacuo, aqueous sodium carbonate solution was added until the pH was greater than 8, the product was extracted with ethyl acetate (2 x 20 mL), and the combined organic layers were concentrated in vacuo. The residue was purified by column chromatography (silica gel, 20 g, petroleum ether / ethyl acetate, 3:1 (v / v)). The product containing fraction was concentrated in vacuo to yield the title compound as a colorless oil (600 mg, 2.03 mmol, 59% yield). MS m / z (ESI): 296.3 [M+H]+.Step 5: cis-[3-(Benzylamino)-1-phenyl-cyclobutyl]methanol (Int-43) and trans-[3-(benzylamino)-1-phenyl-cyclobutyl]methanol (Int-44) Methyl 3-(benzylamino)-1-phenyl-cyclobutanecarboxylate (Int-42, 600 mg, 2.03 mmol) was dissolved in tetrahydrofuran (10 mL), the solution was cooled to -20 °C and a solution of lithium aluminiumhydride in tetrahydrofuran (2.5 M, 0.81 mL, 2.03 mmol) was added dropwise. The mixture was stirred at -20 °C for 0.5 h. Then, the reaction was stopped by addition of sodium sulfate decahydrate (ca.1 g), stirred for 15 min and filtered. The filtrate was concentrated in vacuo. The residue was purified by reversed phase chromatography (20 g, Flash Column Welch Ultimate XB_C1820-40 μm, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 60:40 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, thenlyophilized to yield the cis-isomer Int-43 as second eluting isomer as an off-white solid (200 mg,0.68 mmol, 20% yield). MS m / z (ESI): 268.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.51 (s, 1H), 7.45 – 7.29 (m, 7H), 7.25 – 7.19 (m, 1H), 7.10 – 7.05 (m, 2H), 5.79 (br s, 1H), 3.99 (s, 3H), 3.45 – 3.37 (m, 1H), 3.38 (s, 3H), 2.74 – 2.64 (m, 4H). Analogously, intermediate Int-44 (trans isomer) was obtained as first eluting stereoisomer as an off-white solid (200 mg, 0.68 mmol, 20% yield). MS m / z (ESI): 268.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.00 (s, 1H), 7.31 – 7.20 (m, 7H), 7.16 – 7.10 (m, 1H), 6.99 – 6.94 (m, 2H), 5.09 (br s, 1H), 3.71 (s, 3H), 3.63 – 3.53 (m, 1H), 3.50 (s, 3H), 2.57 – 2.49 (m, 2H), 2.35 – 2.26 (m, 2H).Intermediate 46: cis-(3-Amino-1-phenyl-cyclobutyl)methanol (Int-46) Int-43Int-46 cis-[3-(Benzylamino)-1-phenyl-cyclobutyl]methanol (Int-43, 175 mg, 0.65 mmol) was dissolved in 1,1,1,3,3,3-hexafluoroisopropanol (HFIP, 6.0 mL) and wet palladium on charcoal (Pd / C, 10% m / m, 200 mg) was added under nitrogen. The mixture was saturated with hydrogen and set under a hydrogen atmosphere by three times evacuating and refill with hydrogen. The mixture was stirred at 25 °C for 12 h under a hydrogen atmosphere (balloon). After that, it was filtered, the filter cake was washed with 1,1,1,3,3,3-hexafluoroisopropanol (15 mL) and the combined filtrate was concentrated in vacuo to obtain the title compound as a colorless oil (115 mg, 0.65 mmol, 89% yield), that was used in the next step without further purification. MS m / z (ESI): 178.1 [M+H]+In analogy to the procedure described for the preparation of intermediate Int-46, the following intermediate was prepared using the respective benzyl amine instead of Int-43: Int.-Structure Name Benzyl amine Yieldm / z No. (%) (ESI) Int- trans-(3-amino-1-97 178.147 phenyl- [M+H]+cyclobutyl)methanol Int-44 Intermediate 50: 3-Fluoro-3-phenyl-cyclobutanamine hydrochloride (Int-50) Step 1: tert-Butyl N-(3-fluoro-3-phenyl-cyclobutyl)carbamate (Int-49)3-Fluoro-3-phenyl-cyclobutanecarboxylic acid (Int-48, 300 mg, 1.54 mmol) was dissolved in toluene (10 mL), and triethylamine (0.26 mL, 1.85 mmol) as well as diphenylphosphoryl azide (DPPA, CAS [26386-88-9], 468 mg, 1.70 mmol) were added. The reaction mixture was slowly heated to 100 °C and stirred for 15 min. Then, tert-butanol (2 mL) was added and the resulting mixture was stirred at 100 °C for 12 h. After cooling, it was diluted with ethyl acetate (50 mL), washed with a saturated aqueous solution of sodium hydrogencarbonate (50 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 12 g, petroleum ether / ethyl acetate, 8:1 (v / v)). The product containing fraction was concentrated in vacuo to obtain the title compound as a white solid (150 mg, 0.57 mmol, 37% yield). MS m / z (ESI): 210.5 [M+H-CH2=C(CH3)2]+. Step 2: 3-Fluoro-3-phenyl-cyclobutanamine hydrochloride (Int-50)tert-Butyl N-(3-fluoro-3-phenyl-cyclobutyl)carbamate (Int-49, 50 mg, 0.19 mmol) was dissolvedin 1,4-dioxane (2 mL) and a solution of hydrogen chloride in 1,4-dioxane (4.0 M, 1.0 mL, 4.0 mmol) was added. The mixture was stirred at 25°C for 30 min. After that, it was concentrated in vacuo to afford the title compound as a white solid (40 mg, 0.19 mmol, quant. yield), that was used in the next step without further purification. MS m / z (ESI): 166.1 [M+H]+. Intermediate 54: 3-Thiazol-2-ylcyclobutanamine (Int-54) Int-53 Int-54Step 1: tert-Butyl N-(3-carbamoylcyclobutyl)carbamate (Int-52)3-(tert-Butoxycarbonylamino)cyclobutanecarboxylic acid (Int-51, 3.000 g, 13.94 mmol) was dissolved in dimethylformamide (30 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 4.26 g, 18.1 mmol) as well as diisopropyl ethylamine (5.40 g, 41.8 mmol) were added. After stirring for 5 min at 20 °C, ammonium chloride (1.49 g, 27.9 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, it was poured into water (60 mL) and extracted with ethyl acetate (3 x 50 mL). The combined organic layers were washed with brine (2 x 30 mL), dried over sodium sulfate, filtered and concentrated in vacuo to give the title compound as a white solid (2.30 g, 10.73 mmol, 77% yield), that was used to the next step without further purification. MS m / z (ESI): 215.1 [M+H]+.Step 2: tert-Butyl N-(3-carbamothioylcyclobutyl)carbamate (Int-53)tert-Butyl N-(3-carbamoylcyclobutyl)carbamate (Int-52, 2.30 g, 10.73 mmol) was dissolved intetrahydrofuran (50 mL), and Lawesson's reagent (CAS [19172-47-5]), 4.34 g, 10.73 mmol) was added. The mixture was stirred under reflux (heating bath 100 °C) for 1 h. The reaction mixture was poured into a saturated aqueous solution of sodium hydrogencarbonate (100 mL), and extracted with ethyl acetate (2 x 80 mL). The combined organic layers were washed with brine (2 x 50 mL), dried over sodium sulfate, filtered and concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 40 mm x 15 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a brown solid (700 mg, 3.03 mmol, 28% yield). MS m / z (ESI): 231.1 [M+H]+. Step 3: 3-Thiazol-2-ylcyclobutanamine (Int-54)tert-Butyl N-(3-carbamothioylcyclobutyl)carbamate (Int-53, 500 mg, 2.17 mmol) was dissolvedin ethanol (5 mL) and 2-bromoacetaldehyde diethyl acetal (856 mg, 4.34 mmol) was added. The reaction was stirred at 80 °C for 1 h. After cooling, the pH of the mixture was adjusted to 12 by addition of aqueous sodium hydroxide solution (2 M), ethyl acetate (50 mL) and water (50 mL) were added, and the phases separated. The aqueous layer was extracted with ethyl acetate (2 x 60 mL), the combined organic extracts were washed with brine (2 x 50 mL), dried over sodium sulfate, and concentrated in vacuo to yield the title compound as a brown oil (130 mg, 0.84 mmol, 39% yield). MS m / z (ESI): 155.2 [M+H]+. Intermediate 59: 3-(1-Methylpyrazol-4-yl)cyclobutanamine hydrobromide (Int-59) Step 1: Benzyl N-[3-hydroxy-3-(1-methylpyrazol-4-yl)cyclobutyl]carbamate (Int-57)1-Methyl-4-iodo-1H-pyrazole (Int-56, 949 mg, 4.56 mmol) was dissolved in tetrahydrofuran (20 mL) and the solution was cooled to -78 °C. A solution of n-butyllithium in hexane (2.5 M, 1.82 mL, 4.56 mmol) was added dropwise and the resulting mixture was stirred at -78 °C for 20 min.Then, a solution of benzyl N-(3-oxocyclobutyl)carbamate (Int-55, 500 mg, 2.28 mmol) intetrahydrofuran (2.7 mL) was added and the reaction mixture was stirred at -78 °C for 1 h. After that, it was poured into a saturated aqueous solution of ammonium chloride (40 mL) and extracted with ethyl acetate (3 x 50 mL). The combined extracts were concentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, dichloromethane / methanol, gradient 10:0 to 9:1 (v / v)). The product containing fraction was concentrated in vacuo to yield the title compound as a white solid (156 mg, 0.52 mmol, 23% yield). MS m / z (ESI): 302.1 [M+H]+.Step 2: Benzyl N-[3-(1-methylpyrazol-4-yl)cyclobutyl]carbamate (Int-58)Benzyl N-[3-hydroxy-3-(1-methylpyrazol-4-yl)cyclobutyl]carbamate (Int-57, 450 mg, 1.49mmol) was dissolved in dichloromethane (5 mL), the solution was cooled to 0 – 4 °C (ice bath), and triethylsilane (0.50 mL, 3.14 mmol) was added dropwise. The resulting mixture was stirred at 0 – 4 °C for 20 min. Then, 2,2,2-trifluoroacetic acid (0.46 mL, 5.97 mmol) was added, the mixture reaction was allowed to warm to 20 °C and stirred at 20 °C for 4 h 40 min. The mixture was poured into an aqueous solution of sodium carbonate (2 M, 100 mL), extracted with ethyl acetate (3 x 100 mL), the combined organic extracts were washed with brine (50 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, dichloromethane / methanol, gradient 10:0 to 9:1 (v / v)). The product containing fraction was concentrated in vacuo to yield the title compound as a white solid (200 mg, 0.70 mmol, 47% yield). MS m / z (ESI): 286.4 [M+H]+. Step 3: 3-(1-Methylpyrazol-4-yl)cyclobutanamine hydrobromide (Int-59)Benzyl N-[3-(1-methylpyrazol-4-yl)cyclobutyl]carbamate (Int-58, 170 mg, 0.60 mmol) wasdissolved in ethyl acetate (2 mL) and acetic acid (2 mL) and a solution of hydrogen bromide in acetic acid (33% (m / m), 0.48 mL, 3.57 mmol) was added. The resulting mxiture was stirred at 20 °C for 1 h. After that, the reaction mixture was concentrated in vacuo to afford the title compound as a light brown solid (138 mg, 0.59 mmol, 99% yield). MS m / z (ESI): 152.1 [M+H]+. Intermediate 62: 3-(3-Pyridyl)cyclobutanamine (Int-62) Step 1: N,N-Dibenzyl-3-(3-pyridyl)cyclobutanamine (Int-61) 3-(3-Pyridyl)cyclobutanone (Int-60, 250 mg, 1.70 mmol) was dissolved in dichloromethane (3 mL), dibenzylamine (369 mg, 1.87 mmol) and sodium triacetoxyborohydride (STAB, CAS [56553-60-7], 1080 mg, 5.10 mmol) were added and the reaction mixture was stirred at 20 °C for 2 h. After that, it was poured into water (30 mL) and extracted with ethyl acetate (2 x 30 mL). The combined organic layers were washed with brine (2 x 20 mL), dried over sodium sulfate, and concentrated in vacuo to obtain the title compound as a colorless oil (530 mg, 1.61 mmol, 95% yield), that was used in the next step without further purification. MS m / z (ESI): 329.2 [M+H]+. Step 2: 3-(3-Pyridyl)cyclobutanamine (Int-62) N,N-Dibenzyl-3-(3-pyridyl)cyclobutanamine (Int-61, 530 mg, 1.61 mmol) was dissolved in methanol (3 mL), palladium hydroxide on charcoal (30 mg, 0.16 mmol) was added, the mixture was saturated with hydrogen and stirred at 50 °C for 6 h under a hydrogen atmosphere (balloon). After cooling, the mixture was filtered over a short pad of Celite, washed (methanol), and the combined filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 40 mm x 15 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a colorless oil (100 mg, 0.67 mmol, 42% yield). MS m / z (ESI): 149.2 [M+H]+.Intermediate 66: cis-3-Ethoxycyclobutanamine hydrobromide (Int-66) Step 1: cis-Benzyl N-(3-hydroxycyclobutyl)carbamate (Int-64)cis-3-Aminocyclobutanol hydrochloride (Int-63, 293 mg, 2.37 mmol) was dissolved in saturated aqueous sodium hydrogencarbonate solution (1.5 mL) and tetrahydrofuran (1.5 mL), the solution was cooled to 0 – 4 °C (ice bath), and benzyl chloroformate (504 mg, 2.95 mmol) was added dropwise at 0 °C. The mixture was stirred at 25 °C for 30 min. After that, it was diluted with ethyl acetate (20 mL) and water (10 mL), The aqueous phase was extracted with ethyl acetate (2 x 30 mL), the combined organic layers were washed with brine (60 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 5 g, petroleum ether / ethyl acetate, gradient 4:1 to 2:1 (v / v)) to obtain the title compound as a light green oil (150 mg, 0.68 mmol, 29% yield). MS m / z (ESI): 222.2 [M+H]+.Step 2: cis-Benzyl N-(3-ethoxycyclobutyl)carbamate (Int-65)cis-Benzyl N-(3-hydroxycyclobutyl)carbamate (Int-64, 405 mg, 1.83 mmol) was dissolved intetrahydrofuran (6 mL) and the solution was cooled to 0 – 4 °C (ice bath). Sodium hydride (60% m / m dispersion in mineral oil, 90 mg, 2.25 mmol) was added and the mixture was stirred at 0 °C for 30 min. Iodoethane (343 mg, 2.20 mmol) was then added and the reaction mixture was stirred at 35 °C for 6 h. After that, it was cooled again to 0 – 4 °C, saturated aqueous ammonium chloride solution (20 mL) was added, followed by ethyl acetate (10 mL). The aqueous layer was extracted with ethyl acetate (3 x 30 mL), the combined organic layers were dried over sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by column chromatography (silica gel, 5 g, petroleum ether / ethyl acetate, gradient 4:1 to 2:1 (v / v)) to afford the title compound as a light yellow solid (180 mg, 0.72 mmol, 39% yield). MS m / z (ESI): 272.2 [M+Na]+.Step 3: cis-3-Ethoxycyclobutanamine hydrobromide (Int-66)cis-Benzyl N-(3-ethoxycyclobutyl)carbamate (Int-65, 100 mg, 0.40 mmol) was dissolved indichloromethane (2 mL), the solution was cooled to 0 – 4 °C (ice bath), and a solution of hydrogen bromide in acetic acid (33% m / m, 0.2 mL) was added. The mixture was stirred at 0 °C for 1 h and at 25 °C for 2 h. After that, it was was concentrated in vacuo. The residue was dissolved in methanol (2 mL) and amberlyst® A21 resin (100 mg) was added. The mixture was stirred at 25 °C for 0.5 h. Then, it was filtered and the filtrate was concentrated in vacuo to givethe title compound as a light green oil (40 mg, 0.20 mmol, 50% yield). 1H NMR (400 MHz,CDCl3): δ ppm 8.45 (br s, 3H), 3.84 – 3.72 (m, 1H), 3.53 – 3.36 (m, 3H), 2.84 – 2.70 (m, 2H), 2.40 – 2.25 (m, 2H), 1.19 (t, J = 7.0 Hz, 3H). Intermediate 70: (3R)-1-(4-Chlorophenyl)pyrrolidin-3-amine 2,2,2-trifluoroacetate salt (Int-70) Int-67 Int-68 Int-69 Int-70Step 1: tert-Butyl N-[(3R)-1-(4-chlorophenyl)pyrrolidin-3-yl]carbamate (Int-69) 1-Chloro-4-iodobenzene (Int-67, 192 mg, 0.81 mmol) was dissolved in degassed 1,4-dioxane (4mL), tert-butyl N-[(3R)-pyrrolidin-3-yl]carbamate (Int-68, 150 mg, 0.81 mmol),[dicyclohexyl(2′,6′-diisopropoxy-2-biphenylyl)phosphine-κP](methanesulfonatato-κO)[2′- (methylamino-κN)-2-biphenylyl-κC2]palladium (RuPhos Pd G4, CAS [1599466-85-9], 68 mg, 0.08 mmol), and cesium carbonate (787 mg, 2.42 mmol) were added under nitrogen atmosphere. The mixture was again degassed and stirred at 90°C for 1 h. After cooling, the mixture was filtered and concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18150 x 25 mm x 10 um, flow 25 mL / min, water (+0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70). The product containing fractions were lyophilized to yield the title compound as a white solid (200 mg, 0.67 mmol, 83% yield). MS m / z (ESI): 297.1 [M+H]+. Step 2: (3R)-1-(4-Chlorophenyl)pyrrolidin-3-amine 2,2,2-trifluoroacetate salt (Int-70)tert-Butyl N-[(3R)-1-(4-chlorophenyl)pyrrolidin-3-yl]carbamate (Int-69, 100 mg, 0.34 mmol)was dissolved in dichloromethane (2 mL) and a solution of 2,2,2-trifluoroacetic acid in dichloromethane (1:5 (v / v), 4 mL) was added. The mixture was stirred at 25°C for 1 h. After that, it was concentrated in vacuo to yield the title compound as a yellow oil (65 mg, 0.21 mmol, 98% yield). MS m / z (ESI): 197.1 [M+H]+. In analogy to the procedure described for the preparation of intermediate Int-70, the following intermediates were prepared using the respective (het)aryl halides instead of Int-67: Int.-Structure Name (Het)arylm / z No. halide (ESI) Int- (3R)-1-(3-chlorophenyl)- 197.0 71 * TFApyrrolidin-3-amine 2,2,2- [M+H]+trifluoroacetate salt Int-75Int- (3R)-1-(2-chlorophenyl)- 197.0 72 pyrrolidin-3-amine 2,2,2- [M+H]+* TFA trifluoroacetate salt Int-76Int- (3R)-1-pyrimidin-5- 165.1 73 * TFAylpyrrolidin-3-amine [M+H]+2,2,2-trifluoroacetate salt Int-77 Int- (3R)-1-(1-methylpyrazol- 167.1 74 * TFA4-yl)pyrrolidin-3-amine [M+H]+2,2,2-trifluoroacetate salt Int-78Intermediate 81: (3R)-1-Pyrazin-2-ylpyrrolidin-3-amine hydrochloride (Int-81) Step 1: tert-Butyl N-[(3R)-1-pyrazin-2-ylpyrrolidin-3-yl]carbamate (Int-80)2-Chloropyrazine (Int-79, 101 mg, 0.89 mmol) was dissolved in dimethylsulfoxide (4 mL), andcesium carbonate (787 mg, 2.42 mmol) followed by a solution of tert-butyl N-[(3R)-pyrrolidin-3-yl]carbamate (Int-68, 150 mg, 0.81 mmol) in dimethylsulfoxide (4 mL) were added. The mixture was stirred at 140°C for 16 h under nitrogen atmosphere. After cooling, the mixture was filtered and concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18150 x 25 mm x 10 um, flow 25 mL / min, water (+0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70). The product containing fractions were lyophilized to afford the title compound as a yellow oil (185 mg, 0.70 mmol, 87% yield). MS m / z (ESI): 265.1 [M+H]+. Step 2: (3R)-1-Pyrazin-2-ylpyrrolidin-3-amine hydrochloride (Int-81)tert-Butyl N-[(3R)-1-pyrazin-2-ylpyrrolidin-3-yl]carbamate (Int-80, 185 mg, 0.70 mmol) wasdissolved in 1,4-dioxane (2 mL) and a solution of hydrogen chloride in 1,4-dioxane (4 M, 1 mL, 4 mmol) was added. The mixture was stirred at 25°C for 1 h. After that, it was concentrated in vacuo to obtain the title compound as a yellow oil (114 mg, 0.57 mmol, 81% yield). MS m / z (ESI): 165.1 [M+H]+. In analogy to the procedure described for the preparation of intermediate Int-81, the following intermediate was prepared using the respective (het)aryl halide instead of Int-79: Int.-Structure Name (Het)arylm / z (ESI) No. halide Int- (3R)-1-(5-chloro-2- 198.2 82 pyridyl)pyrro+* HCl lidin-3-amine [M+H] hydrochloride Int-83Intermediate 87: 2-Phenoxyethanamine hydrochloride (Int-87) Int-84 Int-85 Int-86 Int-87Step 1: tert-Butyl N-(2-phenoxyethyl)carbamate (Int-86)tert-Butyl N-(2-bromoethyl)carbamate (Int-85, 1.00 g, 4.46 mmol) was dissolved in dimethylformamide (10 mL), and potassium carbonate (1.11 g, 8.03 mmol) followed by phenol (Int-84, 630 mg, 6.69 mmol) were added. The mixture was stirred at 30°C for 16 h. Then, a saturated aqueous solution of sodium carbonate (30 mL) was added, it was extracted with ethyl acetate (3 x 30 mL), the combined organic phases were washed with brine (50 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, petroleum ether / ethyl acetate, 10:1 (v / v)) to afford the title compound as a colorless oil (940 mg, 3.97 mmol, 89% yield). MS m / z (ESI): 138.2 [M+H-tBuOCO]+. Step 2: 2-Phenoxyethanamine hydrochloride (Int-87)tert-Butyl N-(2-phenoxyethyl)carbamate (Int-86, 940 mg, 3.96 mmol) was dissolved in 1,4-dioxane (5 mL) and a solution of hydrogen chloride in 1,4-dioxane (4.0 M, 5.0 mL, 20.0 mmol) was added. The mixture was stirred at 20°C for 3 h. After that, it was concentrated in vacuo, ethyl acetate (30 mL) was added and the resulting slurry was stirred at 20 °C for 30 min. It was filtered, the solid was washed with ethyl acetate (3 x 10 mL) and dried in vacuo to afford the title compound as a white solid (535 mg, 3.08 mmol, 78% yield). MS m / z (ESI): 138.1 [M+H]+. Intermediate 95: (6R)-4-Phenyl-4-azaspiro[2.4]heptan-6-amine 2,2,2-trifluoroacetate salt (Int-95) Int-92 Int-93 Int-94 Int-95Step 1: (4S)-4-[tert-Butyl(diphenyl)silyl]oxypyrrolidin-2-one (Int-89)(4S)-4-Hydroxypyrrolidin-2-one (Int-88, 3.00 g, 29.7 mmol) was dissolved in dichloromethane (90 mL) and imidazole (4.04 g, 59.3 mmol) was added. After stirring for 5 min at 25 °C, tert- butylchlorodiphenylsilane (8.97 g, 32.6 mmol) was added and the resulting mixture was stirred for 2 h at 25 °C. Then, it was filtered and the filtrate was concentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, petroleum ether / ethyl acetate, gradient 2:1 to 1:1 (v / v)) to obtain the title compound as a light yellow oil (10.1 g, 29.7 mmol, quant. yield). MS m / z (ESI): 340.2 [M+H]+. Step 2: (4S)-4-[tert-Butyl(diphenyl)silyl]oxy-1-phenyl-pyrrolidin-2-one (Int-90) (4S)-4-[tert-Butyl(diphenyl)silyl]oxypyrrolidin-2-one (Int-89, 10.0 g, 29.4 mmol) was dissolved in degassed toluene (120 mL), and tris(dibenzylideneacetone)dipalladium(0) (Pd2(dba)3, CAS [51364-51-3], 1.35 g, 1.47 mmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (Xantphos, CAS [161265-03-8], 2.56 g, 4.42 mmol), cesium carbonate (14.40 g, 44.2 mmol), and iodobenzene (6.91 g, 33.9 mmol) were added subsequently under nitrogen. The mixture was again degassed and stirred under nitrogen atmosphere at 80 °C for 4 h. After cooling, ethyl acetate (120 mL) and water (120 mL) were added, layers were separated. The aqueous layer was extracted with ethyl acetate (4 x 80 mL), the combined organic phases were washed with brine (2 x 90 mL), dried over sodium sulfate, and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 80 g, petroleum ether / ethyl acetate, 10:1 (v / v)) to yield the title compound as a dark red oil (10.82 g, 26.03 mmol, 88% yield). MS m / z (ESI): 416.2 [M+H]+.Step 3: tert-Butyl-diphenyl-[[(6S)-4-phenyl-4-azaspiro[2.4]heptan-6-yl]oxy]silane (Int-91)A solution of ethylmagnesium bromide in tetrahydrofuran (3.0 M, 8.02 mL, 24.06 mmol) was diluted with tetrahydrofuran (50 mL) and the solution was cooled to -78 °C (dry ice / acetone). A solution of methyltitanium triisopropoxide in tetrahydrofuran (1.0 M, 18.05 mL, 18.05 mmol) was added and the resulting mixture was stirred for 15 min at -78 °C. Then, a solution (4S)-4- [tert-butyl(diphenyl)silyl]oxy-1-phenyl-pyrrolidin-2-one (Int-90, 5.00 g, 12.03 mmol) in tetrahydrofuran (20 mL) was added. The mixture was allowed to warm to 25 °C and stirred for 4 h. Then, it was diluted with water (80 mL) and ethyl acetate (80 mL). Phases were separated, the aqueous layer was extracted with ethyl acetate (2 x 200 mL), the combined organic phases were washed with brine (200 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 40 g, petroleum ether / ethyl acetate, gradient 100:1 to 10:1 (v / v)) to afford the title compound as a colorless oil (4.50 g, 10.52 mmol, 87% yield). MS m / z (ESI): 428.3 [M+H]+. Step 4: (6S)-4-Phenyl-4-azaspiro[2.4]heptan-6-ol (Int-92) tert-Butyl-diphenyl-[[(6S)-4-phenyl-4-azaspiro[2.4]heptan-6-yl]oxy]silane (Int-91, 3.90 g, 9.12 mmol) was dissolved in dichloromethane (30 mL), and the solution was cooled to 0 – 4 °C (ice bath). Then, a solution of tetrabutylammonium fluoride in tetrahydrofuran (1.0 M, 10.95 mL, 10.95 mmol) was added and the mixture was stirred for 4 h at 25 °C. After that, it was concentrated in vacuo, the residue was purified by column chromatography (silica gel, 80 g, petroleum ether / ethyl acetate, gradient 100:1 to 20:1 (v / v)) to yield the title compound as a yellow oil (1.60 g, 8.45 mmol, 93% yield). MS m / z (ESI): 190.2 [M+H]+. Step 5: [(6S)-4-Phenyl-4-azaspiro[2.4]heptan-6-yl] ethanesulfonate (Int-93) (6S)-4-Phenyl-4-azaspiro[2.4]heptan-6-ol (Int-92, 140 mg, 0.74 mmol) was dissolved in dichloromethane (3 mL), and triethylamine (150 mg, 1.48 mmol) as well as ethanesulfonyl chloride (0.08 mL, 0.89 mmol) were added. The reaction mixture was stirred at 20 °C for 4 h. After that, it was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18150 x 25 mm x 10 um, flow 25 mL / min, water (+0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70). The product containing fractions were lyophilized to afford the title compound as a yellow oil (45 mg, 0.16 mmol, 22% yield). MS m / z (ESI): 282.1 [M+H]+. Step 6: (6R)-6-Azido-4-phenyl-4-azaspiro[2.4]heptane (Int-94) [(6S)-4-Phenyl-4-azaspiro[2.4]heptan-6-yl] ethanesulfonate (Int-93, 2.14 g, 7.62 mmol) was dissolved in dimethylformamide (10 mL) and sodium azide (680 mg, 10.46 mmol) was added. The mixture was stirred at 80 °C for 4 h. After cooling, a saturated aqueous solution of sodium carbonate was added until the pH was greater than 9. The mixture was extracted with ethyl acetate (3 x 100 mL), the combined organic phases were washed with brine (3 x 70 mL), dried over sodium sulfate and concentrated in vacuo to obtain the title compound as a yellow oil, that was used in the next step with further purification (1.50 g, 7.00 mmol, 92% yield). MS m / z (ESI): 215.2 [M+H]+. Step 7: (6R)-4-Phenyl-4-azaspiro[2.4]heptan-6-amine 2,2,2-trifluoroacetate salt (Int-95) (6R)-6-Azido-4-phenyl-4-azaspiro[2.4]heptane (Int-94, crude from preceeding step, 1.50 g, 7.00 mmol) was dissolved in tetrahydrofuran (35 mL) and water (5 mL). Triphenylphosphine (2.20 g, 8.40 mmol) was added and the reaction mixture was stirred at 20 °C for 2 h. After that, it was concentrated in vacuo and the residue was purified by reversed phase chromatography (40 g, Flash Column Welch Ultimate XB_C1820-40 μm, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 60:40 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to yield the title compound as a white solid (1.20 g, 3.97 mmol, 57% yield). MS m / z (ESI): 189.2 [M+H]+.Intermediate 98: Butyl (2R)-2-[(5-methoxycarbonyl-2-oxo-1-pyridyl)methyl]morpholine-4-carboxylate (Int-98) Methyl 6-oxopyran-3-carboxylate (Int-96, 300 mg, 1.95 mmol) was dissolved in methanol (7 mL) and tert-butyl (2R)-2-(aminomethyl)morpholine-4-carboxylate (Int-97, 484 mg, 2.24 mmol) was added. The mixture was stirred at 35 °C for 1 h. After cooling, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 40 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 65:35 to 35:65 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a yellow solid (150 mg, 0.43 mmol, 22% yield). MS m / z (ESI): 253.1 [M–Boc+H]+. In analogy to the procedure described for the preparation of intermediate Int-98, the following intermediates were prepared using the respective amines instead of Int-97: Int.-Structure Name Amine Yieldm / z No. (%) (ESI) Int- tert-butyl (2S)-2-[(5-48 353.299 methoxycarbonyl-2-oxo-1- [M+H]+pyridyl)methyl]- Int-105 morpholine-4-carboxylate Int- methyl 6-oxo-1-[[(3R)-1-31 251.1100 tert-butoxycarbonyl-3- [M– piperidyl]methyl]pyridine- Boc+H]+3-carboxylate Int-106Int- methyl 6-oxo-1-[[(3S)-1-62 251.2101 tert-butoxycarbonyl-3- [M– piperidyl]methyl]pyridine- Boc+H]+3-carboxylate Int-107Int- tert-butyl (3R)-3-[(5-8 253.2102 methoxycarbonyl-2-oxo-1- [M– pyridyl)methyl]- Boc+H]+morpholine-4-carboxylate Int-108Int- tert-butyl (3S)-3-[(5-26 253.1103 methoxycarbonyl-2-oxo-1- [M– pyridyl)methyl]- Boc+H]+morpholine-4-carboxylate Int-109Int- methyl 1-[2-(tert-49 197.1104 butoxycarbonylamino)ethy [M– l]-6-oxo-pyridine-3- Int-110 Boc+H]+carboxylate Intermediate 112: Methyl 1-(2-hydroxyethyl)-6-oxo-pyridine-3-carboxylate (Int-112) Methyl 6-oxopyran-3-carboxylate (Int-96, 300 mg, 1.95 mmol) was dissolved in methanol (4 mL) and 2-hydroxyethylamine (Int-111, 0.23 mL, 3.89 mmol) was added. The mixture was stirred at 60 °C for 2 h. After cooling, it was filtered and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 40 mm x 15 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 65:35 to 35:65 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a yellow solid (320 mg, 1.62 mmol, 80% yield). MS m / z (ESI): 198.1 [M+H]+. In analogy to the procedure described for the preparation of intermediate Int-112, the following intermediates were prepared using the respective amines instead of Int-111: Int.-Structure Name Amine Yieldm / z No. (%) (ESI) Int- methyl 6-oxo-1-(3,3,3-88 266.1113 trifluoro-2-hydroxy- [M+H]+propyl)pyridine-3- Int-125 carboxylate Int- methyl 1-[2-69 225.2114 (dimethylamino)ethyl]-6- [M+H]+oxo-pyridine-3- Int-126 carboxylate Int- methyl 1-[3-46 253.2115 (dimethylamino)-3-oxo- [M+H]+propyl]-6-oxo-pyridine-3- Int-127 carboxylate Int- methyl 1-[2-(2,2-40 262.2116 difluoroethoxy)ethyl]-6- [M+H]+oxo-pyridine-3- Int-128 carboxylate Int- cis-methyl 1-(3-28 252.2* HBr 117 ethoxycyclobutyl)-6-oxo- [M+H]+pyridine-3-carboxylate Int-66 Int- methyl 6-oxo-1-(2-55 261.4*HCl 118 phenoxyethyl)pyridine-3- [M+H]+carboxylate Int-87 Int- methyl 1-[2-95 248.0119 (difluoromethoxy)ethyl]-6- [M+H]+oxo-pyridine-3- carboxylate Int-129Int- methyl 1-[2-31 266.1120 (trifluoromethoxy)ethyl]- [M+H]+6-oxo-pyridine-3- carboxylate Int-130Int- methyl 1-[(1-66 224.1121 hydroxycyclopropyl)meth [M+H]+yl]-6-oxo-pyridine-3- Int-131 carboxylate Int- methyl 1-(2-23 212.2122 methoxyethyl)-6-oxo- [M+H]+pyridine-3-carboxylate Int-132 Int- methyl 6-oxo-1-(1H-32 220.1123 pyrazol-5-yl)pyridine-3- [M+H]+carboxylate Int-133 Int- rac-methyl 6-oxo-1-48 238.1124 (tetrahydrofuran-2- [M+H]+ylmethyl)pyridine-3- Int-134 carboxylate Intermediate 136: Methyl 1-[1-(hydroxymethyl)cyclopropyl]-6-oxo-pyridine-3-carboxylate (Int-136) Methyl 6-oxopyran-3-carboxylate (Int-96, 180 mg, 1.20 mmol) was dissolved in methanol (4 mL) and (1-aminocyclopropyl)methanol (Int-135, 203.5 mg, 2.34 mmol) was added. The mixture was stirred at 60 °C for 16 h. After cooling, sodium methoxide (31.5 mg, 0.58 mmol) was added and the mixture was stirred at 60 °C for 10 min. Then, after cooling again, it was filtered, and the filtrate directly purified by preparative HPLC (Phenomenex luna C18, 150 x 40 mm x 15 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a brown oil (160 mg, 0.72 mmol, 60% yield). MS m / z (ESI): 224.1 [M+H]+. Intermediate 137: Methyl 1-[1-(ethoxymethyl)cyclopropyl]-6-oxo-pyridine-3-carboxylate (Int-137) Int-136 Int-137 Methyl 1-[1-(hydroxymethyl)cyclopropyl]-6-oxo-pyridine-3-carboxylate (Int-136, 100 mg, 0.45 mmol) was dissolved in dimethylformamide (4 mL) and the solution was cooled to 0 – 4 °C (ice bath). Sodium hydride (60% m / m dispersion in mineral oil, 27 mg, 0.67 mmol) was added and the mixture was stirred at 0 °C for 5 min. Iodoethane (0.05 mL, 0.67 mmol) was then added and the reaction mixture was stirred at 50 °C for 16 h under nitrogen atmosphere. After cooling, it was filtered and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a yellow solid (64 mg, 0.25 mmol, 57% yield). MS m / z (ESI): 238.1 [M+H]+. In analogy to the procedure described for the preparation of intermediate Int-137, the following intermediate was prepared using the respective alcohol instead of Int-136: Int.-Structure Name Alcohol Yieldm / z No. (%) (ESI) Int- methyl 1-[(1-28 238.1138 ethoxycyclopropyl)methyl [M+H]+]-6-oxo-pyridine-3- carboxylate Int-121Intermediate 139: Methyl 5-chloro-6-oxo-pyran-3-carboxylate (Int-139) Methyl 2-oxo-2H-pyran-5-carboxylate (Int-96, 500 mg, 3.24 mmol) was dissolved in acetic acid (15 mL) and N-chlorosuccinimide (1.30 g, 9.73 mmol) was added. The mixture was stirred at 90 °C for 24 h. After cooling, the pH of the mixture was adjusted to >9 by addition of solid sodium hydrogencarbonate. The mixture was extracted with ethyl acetate (3 x 20 mL), the combined organic extracts were dried (sodium sulfate) and concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% 2,2,2- trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a brown solid (268 mg, 1.42 mmol, 44% yield). MS m / z (ESI): 189.0 [M+H]+. Intermediate 141: Methyl 5-chloro-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-141) Methyl 5-chloro-6-oxo-pyran-3-carboxylate (Int-139, 140 mg, 0.74 mmol) was dissolved in methanol (3 mL) and thiazol-2-amine (Int-140, 82 mg, 0.82 mmol) was added. The mixture was stirred at 60 °C for 4 h. After cooling, the mixture was filtered, the precipitate washed with petroleum ether (20 mL) and dried in vacuo to yield the title compound as a brown solid (98 mg, 0.36 mmol, 49% yield). MS m / z (ESI): 271.0 [M+H]+. Intermediate 144: Methyl 5-methyl-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-144) Step 1: Methyl 5-bromo-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-143) Methyl 5-bromo-6-oxo-pyran-3-carboxylate (Int-142, 500 mg, 2.15 mmol) was dissolved in methanol (6 mL) and thiazol-2-amine (Int-140, 430 mg, 4.29 mmol) was added. The mixture was stirred at 60 °C for 2 h. After cooling, the mixture was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as mixture as a brown solid (210 mg, 0.67 mmol, 31% yield). MS m / z (ESI): 316.9 [M+H]+. Step 2: Methyl 5-methyl-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-144) Methyl 5-bromo-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-143, 180 mg, 0.57 mmol) and methyl-boron-dihydroxide (60 mg, 1.0 mmol) were dissolved in 1,4-dioxane (2 mL), water (0.3 mL) and potassium carbonate (236 mg, 1.71 mmol) were added, the resulting suspension was degassed and stirred at 25 °C for 3 min under a nitrogen atmosphere. Then, [1,1- bis(diphenylphosphino)ferrocene] dichloropalladium (II) (Pd(dppf)Cl2, CAS [72287-26-4], 42 mg, 0.06 mmol) was added, the mixture was degassed, and the reaction was stirred at 80 °C for 1 h under nitrogen atmosphere. After cooling, the mixture was diluted with ethyl acetate (30 mL), filtered through a short pad of celite, and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a brown solid (175 mg, 0.70 mmol, 86% yield). MS m / z (ESI): 251.0 [M+H]+. Intermediate 146: Methyl 1-(2-ethoxyethyl)-5-methyl-6-oxo-pyridine-3-carboxylate (Int- 146) Step 1: Methyl 5-bromo-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-145) Methyl 5-bromo-6-oxo-pyran-3-carboxylate (Int-142, 500 mg, 2.15 mmol) was dissolved in methanol (5 mL) and 2-ethoxyethylamine (210 mg, 2.36 mmol) was added. The mixture was stirred at 60 °C for 1 h. After cooling, the mixture was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a colorless oil (350 mg, 1.15 mmol, 54% yield). MS m / z (ESI): 304.0 [M+H]+. Step 2: Methyl 1-(2-ethoxyethyl)-5-methyl-6-oxo-pyridine-3-carboxylate (Int-146) Methyl 5-bromo-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-145, 200 mg, 0.66 mmol) was dissolved in 1,4-dioxane (2.5 mL), water (0.3 mL), a solution of trimethylboroxine in tetrahydrofuran (3.5 M, 0.33 mL, 1.2 mmol), and potassium carbonate (272 mg, 1.97 mmol) were added, the resulting suspension was degassed and stirred at 25 °C for 3 min under a nitrogen atmosphere. Then, [1,1-bis(diphenylphosphino)ferrocene] dichloropalladium (II) (Pd(dppf)Cl2, CAS [72287-26-4], 48 mg, 0.07 mmol) was added, the mixture was degassed, and the reaction was stirred at 80 °C for 1 h under nitrogen atmosphere. After cooling, the mixture was diluted with ethyl acetate (30 mL), filtered through a short pad of Celite, and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a brown solid (100 mg, 0.42 mmol, 63% yield). MS m / z (ESI): 240.1 [M+H]+. Intermediate 149: Methyl 1-[2-(2-fluoroethoxy)ethyl]-6-oxo-pyridine-3-carboxylate (Int- 149) Step 1: 2-(2-Fluoroethoxy)ethyl ethanesulfonate (Int-148) 2-(2-Fluoroethoxy)ethanol (Int-147, 160 mg, 1.48 mmol) was dissolved in dichloromethane (8 mL), triethylamine (0.24 mL, 1.78 mmol) was added and the solution was cooled to 0 – 4 °C (ice bath). Ethanesulfonyl chloride (0.17 mL, 1.78 mmol) was added dropwise, and the reaction mixture was stirred at 0 – 4 °C for 3 h. After that, it was diluted with a saturated aqueous solution of ammonium chloride (5 mL), and extracted with ethyl acetate (3 x 20 mL). The combined organic fractions were dried over sodium sulfate and concentrated in vacuo to afford the title compound as a light yellow oil (250 mg, 1.25 mmol, 84% yield), that was used in the next step without further purification. Step 2: Methyl 1-[2-(2-fluoroethoxy)ethyl]-6-oxo-pyridine-3-carboxylate (Int-149) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 229 mg, 1.5 mmol) was dissolved in dimethylformamide (5 mL) and cesium carbonate (895 mg, 2.75 mmol) was added. After stirring at 25 °C for 30 min, a solution of 2-(2-fluoroethoxy)ethyl ethanesulfonate (Int-148, 250 mg, 1.25 mmol) in dimethylformamide (3 mL). The reaction was stirred under a nitrogen atmosphere at 100 °C for 3.5 h. After cooling, it was diluted with water (10 mL), and extracted with ethyl acetate (3 x 20 mL). The combined organic fractions were dried over sodium sulfate and concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 85:15 to 55:45 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a white solid (150 mg, 0.62 mmol, 49% yield). MS m / z (ESI): 244.2 [M+H]+. Intermediate 152: Methyl 6-oxo-1-[2-(2,2,2-trifluoroethoxy)ethyl]pyridine-3-carboxylate (Int-152) Step 1: 2-(2,2,2-Trifluoroethoxy)ethyl 4-methylbenzenesulfonate (Int-151) 2-(2,2,2-Trifluoroethoxy)ethanol (Int-150, 2.00 g, 13.9 mmol) was dissolved in anhydrous pyridine (40 mL), p-toluenesulfonyl chloride (3.97 g, 20.8 mmol) and 4-N,N- dimethylaminopyridine (DMAP, 424 mg, 3.47 mmol) were added and the solution was stirred at 20 °C under nitrogen atmosphere for 16 h. After that, it was concentrated in vacuo, the residue was diluted with ethyl acetate (100 mL) and aqueous hydrochloric acid (1M, 50 mL), After phase separation, the organic layer was washed with aqueous hydrochloric acid (1M, 50 mL) and aqueous sodium hydrogencarbonate solution (3 x 50 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 20 g, petroleum ether / ethyl acetate, gradient 5:1 to 1:1 (v / v)) to obtain the title compound as a colorless oil (300 mg, 1.01 mmol, 7% yield). Step 2: Methyl 6-oxo-1-[2-(2,2,2-trifluoroethoxy)ethyl]pyridine-3-carboxylate (Int-152) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 101 mg, 0.66 mmol) was dissolved in dimethylformamide (1 mL) and cesium carbonate (215 mg, 0.66 mmol) was added. After stirring at 20 °C for 30 min, a solution of 2-(2,2,2-trifluoroethoxy)ethyl 4- methylbenzenesulfonate (Int-151, 113 mg, 0.38 mmol) in dimethylformamide (1 mL). The reaction was stirred under a nitrogen atmosphere at 100 °C for 1 h. After cooling, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 75:25 to 45:55 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a white solid (50 mg, 0.18 mmol, 47% yield). MS m / z (ESI): 280.0 [M+H]+. Intermediate 155: Methyl 1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-pyridine-3-carboxylate (Int-155) Step 1: [2-Ethoxy-1-(ethoxymethyl)ethyl] 4-methylbenzenesulfonate (Int-154) 1,3-Diethoxypropan-2-ol (Int-153, 1.53 g, 10.3 mmol) was dissolved in anhydrous pyridine (30 mL), p-toluenesulfonyl chloride (2.94 g, 15.5 mmol) and 4-N,N-dimethylaminopyridine (DMAP, 314 mg, 2.57 mmol) were added and the solution was stirred at 20 °C under nitrogen atmosphere for 16 h. After that, it was concentrated in vacuo, the residue was diluted with ethyl acetate (100 mL) and aqueous hydrochloric acid (1M, 50 mL). After phase separation, the organic layer was washed with aqueous hydrochloric acid (1M, 50 mL) and aqueous sodium hydrogencarbonate solution (3 x 50 mL), dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 20 g, petroleum ether / ethyl acetate, gradient 5:1 to 1:1 (v / v)) to yield the title compound as a colorless oil (440 mg, 1.46 mmol, 14% yield). MS m / z (ESI): 325.1 [M+Na]+. Step 2: Methyl 1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-pyridine-3-carboxylate (Int-155) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 165 mg, 1.08 mmol) was dissolved in dimethylformamide (2 mL) and cesium carbonate (421 mg, 1.29 mmol) was added. After stirring at 15 °C for 30 min, a solution of [2-ethoxy-1-(ethoxymethyl)ethyl] 4- methylbenzenesulfonate (Int-154, 217 mg, 0.72 mmol) in dimethylformamide (2 mL) was added. The reaction was stirred under a nitrogen atmosphere at 100 °C for 3.5 h. After cooling, it was purified directly by preparative HPLC (Waters Xbridge, 150 x 25 mm x 5 um, (water + 0.1% ammonia) / acetonitrile, gradient 63:37 to 33:67 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a light green oil (78 mg, 0.28 mmol, 26% yield). MS m / z (ESI): 284.1 [M+H]+. Intermediate 157: Methyl 6-oxo-1-(2-pyridylmethyl)pyridine-3-carboxylate (Int-157) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 200 mg, 1.31 mmol) was dissolved in dimethylformamide (4 mL) and sodium hydride (60% m / m dispersion in mineral oil, 157 mg, 3.92 mmol) was added. After stirring at 25 °C for 30 min, 2-(bromomethyl)pyridine hydrobromide (Int-156, 225 mg, 1.31 mmol) was added. The mixture was stirred at 25 °C for 1 h. Then, it was diluted with water (30 mL), and extracted with ethyl acetate (3 x 80 mL). The combined organic extracts were concentrated in vacuo, the residue was recrystallized from water and dried by lyophilisation to yield the title compound as a white solid (100 mg, 0.41 mmol, 31% yield). MS m / z (ESI): 245.1 [M+H]+. Intermediate 159: Methyl 1-benzyl-6-oxo-pyridine-3-carboxylate (Int-159) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 300 mg, 1.96 mmol) was dissolved in dimethylformamide (5 mL) and sodium hydride (60% m / m dispersion in mineral oil, 118 mg, 2.95 mmol) was added. After stirring at 25 °C for 30 min, benzyl bromide (Int-158, 335 mg, 2.94 mmol) was added. The mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 75:25 to 35:ä65 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (250 mg, 1.03 mmol, 52% yield). MS m / z (ESI): 244.1 [M+H]+. In analogy to the procedure described for the preparation of intermediate Int-159, the following intermediates were prepared using the respective bromides instead of Int-158: Int.-Structure Name Bromide Yieldm / z No. (%) (ESI) Int- methyl 6-oxo-1-(2-59 258.0160 phenylethyl)pyridine-3- [M+H]+carboxylate Int-162Int- methyl 1-isobutyl-6-oxo-45 210.1161 pyridine-3-carboxylate [M+H]+Int-163 Intermediate 166: Methyl 6-oxo-1-(1-phenylcyclopropyl)pyridine-3-carboxylate (Int-166) Int-164 Int-165 Int-166Dimethyl (E,4E)-4-(methoxymethylene)pent-2-enedioate (Int-164, 550 mg, 2.75 mmol) was dissolved in dimethylformamide (2 mL) and the solution was cooled to -20 °C.1-Phenyl- cyclopropylamine (Int-165, 403 mg, 3.02 mmol) was added and the mixture was stirred for 1 h at -20 °C, followed by 3 h at 100 °C. After cooling, it was filtered, the filtrate was concentrated in vacuo. The residue was purified by reversed phase chromatography (12 g, Flash Column Welch Ultimate XB_C1820-40 μm, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 70:30 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to yield the title compound as a yellow solid (110 mg, 0.41 mmol, 15% yield). MS m / z (ESI): 270.1 [M+H]+. Intermediate 169: Methyl 1-benzyl-6-oxo-pyridine-3-carboxylate (Int-169) Step 1: Methyl 1-(methylsulfanylmethyl)-6-oxo-pyridine-3-carboxylate (Int-168) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 1.00 g, 6.53 mmol) was dissolved in dimethylformamide (6 mL) and potassium carbonate (1.35 g, 9.79 mmol) was added. After stirring at 25 °C for 20 min, chloromethyl methyl sulfide (Int-167, 820 mg, 8.49 mmol) was added and the mixture was stirred at 80 °C for 12 h. After cooling, it was filtered and the filtrate was concentrated in vacuo. The residue was purified by reversed phase chromatography (20 g, Flash Column Welch Ultimate XB_C1820-40 μm, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 70:30 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to yield the title compound as a black oil (393 mg, 1.84 mmol, 28% yield). MS m / z (ESI): 214.0 [M+H]+. Step 2: Methyl 1-(methylsulfonylmethyl)-6-oxo-pyridine-3-carboxylate (Int-169) Methyl 1-(methylsulfanylmethyl)-6-oxo-pyridine-3-carboxylate (Int-168, 190 mg, 0.89 mmol) was dissolve in dichloromethane (1.5 mL) and the solution was cooled to 0 – 4 °C (ice bath). Then, 3-chlorobenzenecarboperoxoic acid (mCPBA, 80% m / m, 577 mg, 2.67 mmol) was added and the mixture was stirred at 25 °C for 15 min. After that, it was filtered, ethyl acetate (3 mL) and water (2 mL) were added. Phases were separated, the aqueous phase was extracted with ethyl acetate (4 x 6 mL), the combined organic layers were washed with brine (5 mL), dried over sodium sulfate and concentrated in vacuo to give the crude title compound as a yellow solid (120 mg, 0.49 mmol, 55% yield), that was used in the next step without further purification. MS m / z (ESI): 246.0 [M+H]+. Intermediate 175: Methyl 1-[2-(1-methylcyclopropoxy)ethyl]-6-oxo-pyridine-3-carboxylate (Int-175) Step 1: Ethyl 2-(1-methylcyclopropoxy)acetate (Int-172) 1-Methylcyclopropanol (Int-171, 2.00 g, 27.7 mmol) was dissolved in dichloromethane (5 mL) and the solution was cooled to 0 – 4 °C (ice bath). Dirhodium tetraacetate (CAS [15956-28- 2], 123 mg, 0.28 mmol) and ethyl 2-diazoacetate (Int-170, 3.16 g, 27.7 mmol) were added and the reaction mixture was stirred at 20 °C for 10 h under a nitrogen atmosphere. After that, it was diluted with dichloromethane (30 mL), filtered through a short pad of Celite and the filtrate was concentrated in vacuo. The crude product was purified by column chromatography (silica gel, 20 g, petroleum ether / ethyl acetate, gradient 19:1 to 9:1 (v / v)) to obtain the title compound as a colorless oil (680 mg, 4.30 mmol, 15% yield). Step 2: 2-(1-Methylcyclopropoxy)ethanol (Int-173) Ethyl 2-(1-methylcyclopropoxy)acetate (Int-172, 3.11 g, 19.6 mmol) was dissolved in tetrahydrofuran (60 mL) and the solution was cooled to 0 – 4 °C (ice bath). A solution of lithium aluminum hydride in tetrahydrofuran (2.5 M, 11.8 mL, 29.5 mmol) was added and the reaction mixture was stirred at 20 °C for 30 min under a nitrogen atmosphere. After that, it was diluted with tetrahydrofuran (60 mL), and sodium sulfate decahydrate (5.0 g) was added. After stirring for 10 min, it was filtered, the filter cake was washed with ethyl acetate (30 mL), and the combined filtrate was concentrated in vacuo to afford the title compound as a light brown oil (2.17 g, 18.7 mmol, 95% yield). Step 3: 2-(1-Methylcyclopropoxy)ethyl 4-methylbenzenesulfonate (Int-174) 2-(1-Methylcyclopropoxy)ethanol (Int-173, 2.60 g, 22.4 mmol) was dissolved in dichloromethane (75 mL), p-toluenesulfonyl chloride (8.53 g, 44.8 mmol), triethylamine (9.36 mL, 67.1 mmol) and 4-N,N-dimethylaminopyridine (DMAP, 1.37 g, 11.2 mmol) were added and the solution was stirred at 20 °C under nitrogen atmosphere for 16 h. After that, it was concentrated in vacuo, the residue was purified by column chromatography (silica gel, 200 g, petroleum ether / ethyl acetate, gradient 9:1 to 6:1 (v / v)) to obtain the title compound as a light yellow oil (4.10 g, 15.2 mmol, 68% yield). Step 4: Methyl 1-[2-(1-methylcyclopropoxy)ethyl]-6-oxo-pyridine-3-carboxylate (Int-175) Methyl 6-hydroxy-3-pyridinecarboxylate (Int-1, 170 mg, 1.11 mmol) was dissolved in dimethylformamide (3.5 mL) and potassium carbonate (205 mg, 1.48 mmol) was added. After stirring at 15 °C for 5 min, 2-(1-methylcyclopropoxy)ethyl 4-methylbenzenesulfonate (Int-174, 200 mg, 0.74 mmol) was added. The reaction was stirred under a nitrogen atmosphere at 90 °C for 16 h. After cooling, it was filtered and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 50:50 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a white solid (72 mg, 0.29 mmol, 39% yield). MS m / z (ESI): 252.1 [M+H]+. Intermediate 176: Methyl 5-fluoro-1-[2-(1-methylcyclopropoxy)ethyl]-6-oxo-pyridine-3- carboxylate (Int-176) Methyl 5-fluoro-6-oxo-1H-pyridine-3-carboxylate (Int-5, 190 mg, 1.11 mmol) was dissolved in dimethylformamide (2 mL) and potassium carbonate (205 mg, 1.48 mmol) was added. After stirring at 15 °C for 5 min, a solution of 2-(1-methylcyclopropoxy)ethyl 4- methylbenzenesulfonate (Int-174, 200 mg, 0.74 mmol) in dimethylformamide (2 mL) was added. The reaction was stirred under a nitrogen atmosphere at 90 °C for 16 h. After cooling, it was filtered and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 65:35 to 40:55 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a white solid (85 mg, 0.32 mmol, 43% yield). MS m / z (ESI): 270.1 [M+H]+. Intermediate 219: Methyl 6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-219) Methyl 6-oxo-1H-pyridine-3-carboxylate (Int-1, 228 mg, 1.49 mmol) was dissolved in dimethylformamide (4 mL) and 2-bromothiazole (Int-218, 0.11 mL, 1.22 mmol), (1S,2S)-N,N’- dimethylcyclohexane-1,2-diamine (26 mg, 0.18 mmol) and potassium carbonate (337 mg, 2.44 mmol) were added. The mixture was degassed and stirred at 90 °C for 5 min. Then, copper(I) iodide (348.34 mg, 1.83 mmol) was added and the reaction was stirred under nitrogen atmosphere at 90 ºC for 16 h. After cooling, the mixture was filtered through a short pad of celite and the filtrate was concentrated in vacuo. The residue was purified by reversed phase chromatography (10 g, Flash Column Welch Ultimate XB_C1820-40 μm, acetonitrile / (water + 0.1% trifluoroacetic acid), gradient, 30:70 to 70:30 (v / v)). The product containing fractions were concentrated to remove the acetonitrile, then lyophilized to yield the title compound as a white solid (40 mg, 0.17 mmol, 14% yield). MS m / z (ESI): 237.0 [M+H]+. EXAMPLES Example 1 and example 2 trans-N-[3-(1,3-Dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (1) and cis-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (2) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 35 mg, 0.17 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 63.5 mg, 0.17 mmol) as well as diisopropyl ethylamine (0.11 mL, 0.61 mmol) were added. After stirring for 10 min at 25 °C, 3-(1,3-dimethylindazol-4- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-15, 50 mg, 0.15 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 50:50 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless oil (54 mg, 0.13 mmol, 87% yield). The mixture (54 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 65:35 (v / v)). The product containing fractions were concentrated in vacuo to yield example 1 as first eluting stereoisomer as a colorless oil (34 mg, 62% yield). MS m / z(ESI): 409.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.24 (d, J = 2.4 Hz, 1H), 7.82 (dd, J = 2.6, 9.4 Hz, 1H), 7.44 - 7.37 (m, 1H), 7.26 (d, J = 8.3 Hz, 1H), 7.20 (d, J = 7.1 Hz, 1H), 6.87 (br d, J = 6.7 Hz, 1H), 6.59 (d, J = 9.4 Hz, 1H), 4.87 - 4.74 (m, 1H), 4.28 - 4.16 (m, 3H), 4.04 (s, 3H), 3.77 (br t, J = 4.8 Hz, 2H), 3.53 (q, J = 6.9 Hz, 2H), 2.86 - 2.75 (m, 2H), 2.67 (s, 3H), 2.65 - 2.56 (m, 2H), 1.21 (t, J = 7.0 Hz, 3H). Analogously, example 2 was obtained as second elutingstereoisomer as a colorless oil (19 mg, 35% yield). MS m / z (ESI): 409.3 [M+H]+. 1H NMR (400MHz, CDCl3): 8.14 (d, J = 2.6 Hz, 1H), 7.67 (dd, J = 2.6, 9.5 Hz, 1H), 7.30 (dd, J = 7.1, 8.2 Hz, 1H), 7.18 (d, J = 8.3 Hz, 1H), 7.18 (d, J = 7.1 Hz, 1H), 6.52 (d, J = 9.4 Hz, 1H), 6.38 (d, J = 7.6 Hz, 1H), 4.71 - 4.59 (m, 1H), 4.13 (t, J = 5.0 Hz, 2H), 3.97 (s, 3H), 3.90 – 3.78 (m, 1H), 3.69 (t, J = 5.0 Hz, 2H), 3.45 (q, J = 7.0 Hz, 2H), 2.96 - 2.86 (m, 2H), 2.70 (s, 3H), 2.25 - 2.14 (m, 2H), 1.14 (t, J = 7.0 Hz, 3H). Example 3 and example 4 cis-1-(2-Ethoxyethyl)-5-fluoro-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3-carboxamide (3) and trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3-carboxamide (4) 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-7, 40 mg, 0.17 mmol) wasdissolved in dimethylformamide (2 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 68 mg, 0.18 mmol) as well as diisopropyl ethylamine (0.11 mL, 0.61 mmol) were added. After stirring for 10 min at 25 °C, 3-[6-(trifluoromethyl)-2- pyridyl]cyclobutanamine 2,2,2-trifluoroacetate salt (Int-16, 60 mg, 0.18 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 64:36 to 34:66 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a green oil (34 mg, 0.08 mmol, 49% yield). The mixture (34 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (2-propanol + 0.1% ammonia), isocratic 70:30 (v / v)). The product containing fractions were concentrated in vacuo to yield example 3 as first eluting stereoisomer as a light green oil (9 mg, 14% yield). MS m / z(ESI): 428.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.01 - 7.95 (m, 1H), 7.78 (t, J = 7.8Hz, 1H), 7.61 - 7.52 (m, 2H), 7.33 (d, J = 7.7 Hz, 1H), 7.14 (br d, J = 8.4 Hz, 1H), 4.77 - 4.64 (m, 1H), 4.23 (t, J = 4.9 Hz, 2H), 3.74 (t, J = 5.0 Hz, 2H), 3.52 - 3.38 (m, 3H), 2.97 - 2.86 (m, 2H), 2.42 - 2.30 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Analogously, example 4 was obtained as second eluting stereoisomer as a light green oil (22 mg, 30% yield). MS m / z (ESI): 428.1[M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.01 (s, 1H), 7.80 (t, J = 7.8 Hz, 1H), 7.61 (dd, J =2.1, 9.9 Hz, 1H), 7.52 (d, J = 7.6 Hz, 1H), 7.41 (d, J = 7.9 Hz, 1H), 6.85 (br d, J = 6.6 Hz, 1H), 4.81 - 4.70 (m, 1H), 4.22 (t, J = 4.9 Hz, 2H), 3.80 - 3.69 (m, 3H), 3.47 (q, J = 7.0 Hz, 2H), 2.86 - 2.74 (m, 2H), 2.60 - 2.49 (m, 2H), 1.14 (t, J = 7.0 Hz, 3H). Example 5 and example 6 cis-1-(2-Ethoxyethyl)-5-fluoro-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3-carboxamide (5) and trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3-carboxamide (6) 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-7, 44 mg, 0.19 mmol) wasdissolved in dimethylformamide (2 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 76 mg, 0.20 mmol) as well as diisopropyl ethylamine (0.13 mL, 0.73 mmol) were added. After stirring for 10 min at 25 °C, 3-[2-(trifluoromethyl)-3- pyridyl]cyclobutanamine 2,2,2-trifluoroacetate salt (Int-17, 60 mg, 0.18 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 71:29 to 41:59 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a light green oil (54 mg, 0.13 mmol, 67% yield). The mixture (54 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak IK, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 5 as first eluting stereoisomer as a light green oil (18 mg, 22% yield). MS m / z(ESI): 428.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.47 (d, J = 4.3 Hz, 1H), 7.92 (s, 1H), 7.82 (d, J = 7.9 Hz, 1H), 7.51 - 7.38 (m, 2H), 6.62 (br d, J = 6.8 Hz, 1H), 4.52 - 4.39 (m, 1H), 4.11 (t, J = 4.8 Hz, 2H), 3.62 (t, J = 4.9 Hz, 2H), 3.60 - 3.48 (m, 1H), 3.38 (q, J = 7.0 Hz, 2H), 2.89 - 2.76 (m, 2H), 2.21 - 2.07 (m, 2H), 1.06 (t, J = 7.0 Hz, 3H). Analogously, example 6 was obtained as second eluting stereoisomer as a light green oil (29 mg, 36% yield). MS m / z (ESI):428.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.57 (d, J = 3.9 Hz, 1H), 8.10 - 8.00 (m,2H), 7.68 (dd, J = 1.8, 9.8 Hz, 1H), 7.56 (dd, J = 4.7, 8.0 Hz, 1H), 7.17 (br s, 1H), 4.78 - 4.66 (m, 1H), 4.25 (t, J = 4.8 Hz, 2H), 4.12 - 3.99 (m, 1H), 3.74 (t, J = 4.9 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 2.71 - 2.54 (m, 4H), 1.15 (t, J = 7.0 Hz, 3H). Example 7 1-(2-Ethoxyethyl)-6-oxo-N-[(1R,2S)-2-[2-(3,5-dimethyl-1H-pyrazol-4- yl)phenyl]cyclopropyl]pyridine-3-carboxamide (7) Step 1: 1-(2-Ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(2-bromophenyl)cyclopropyl]pyridine-3- carboxamide (Int-177) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 80 mg, 0.38 mmol) was dissolved in dimethylformamide (2 mL), (1R,2S)-2-(2-bromophenyl)cyclopropanamine (80 mg, 0.38 mmol), N-methylimidazole (NMI, 155 mg, 1.89 mmol), as well as chloro-N,N,N′,N′- tetramethylformamidinium hexafluorophosphate (TCFH, CAS [207915-99-9], 212 mg, 0.75 mmol) were added. The mixture was stirred under a nitrogen atmosphere at 20 °C for 1 h. After that, the mixture was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% 2,2,2-trifluoroacetic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (144 mg, 0.36 mmol, 94% yield). MS m / z (ESI): 405.2 [M+H]+. Step 2: 1-(2-Ethoxyethyl)-6-oxo-N-[(1R,2S)-2-[2-(3,5-dimethyl-1H-pyrazol-4-yl)phenyl]cyclo- propyl]pyridine-3-carboxamide (7) 1-(2-Ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(2-bromophenyl)cyclopropyl]pyridine-3-carboxamide (Int-177, 80 mg, 0.20 mmol) was dissolved in 1,4-dioxane (4 mL), and water (0.4 mL), 3,5- dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (66 mg, 0.30 mmol), and potassium carbonate (126 mg, 0.59 mmol) were added. The mixture was degassed and [(di(1- adamantyl)-n-butylphosphine)-2-(2′-amino-1,1′-biphenyl)]palladium(II) methanesulfonate (Ad2nBuP-Pd-G3, cataCXium-A-Pd-G3, CAS [1651823-59-4], 7.2 mg, 0.01 mmol) was added under nitrogen. The mixture was again degassed and stirred at 100 °C for 1.5 h under a nitrogen atmosphere. After cooling to 25 °C, it was diluted with ethyl acetate (10 mL) and water (10 mL), the aqueous layer was extracted with ethyl acetate (2 x 10 mL). The combined organic phases were washed with brine (2 x 15 mL), dried over sodium sulfate, and concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a white solid (64 mg,0.15 mmol, 76% yield). MS m / z (ESI): 421.3 [M+H]+. 1H NMR (400 MHz, DMSO-d6) δ ppm12.24 (s, 1H), 8.24 (d, J = 6.2 Hz, 1H), 8.19 (d, J = 2.1 Hz, 1H), 7.80 (dd, J = 2.3, 9.5 Hz, 1H), 7.25 – 7.22 (m, 1H), 7.20 – 7.14 (m, 1H), 7.05 (d, J = 7.5 Hz, 1H), 6.91 (d, J = 8.3 Hz, 1H), 6.39 (d, J = 9.4 Hz, 1H), 4.07 (t, J = 5.1 Hz, 2H), 3.59 (t, J = 5.1 Hz, 2H), 3.41 (q, J = 7.0 Hz, 2H), 3.34 – 3.25 (m, 1H), 2.01 (s, 3H), 1.96 (s, 3H), 1.90 – 1.82 (m, 1H), 1.29 – 1.22 (m, 1H), 1.15 – 1.05 (m, 1H), 1.03 (t, J = 7.0 Hz, 3H). Example 8 and example 9 trans-1-(2-Ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (8) and cis-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (9) 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-9, 28 mg, 0.12 mmol) wasdissolved in dimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 56 mg, 0.15 mmol) as well as diisopropyl ethylamine (0.11 mL, 0.61 mmol) were added. After stirring for 10 min at 25 °C, 3-(1-methylindazol-7- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-18, 40 mg, 0.13 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a light green oil (54 mg, 0.13 mmol, 67% yield). The mixture (54 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 50:50 (v / v)). The product containing fractions were concentrated in vacuo to yield example 8 as second eluting stereoisomer as a light brown solid (12 mg, 24% yield). MSm / z (ESI): 413.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 7.96 (s, 1H), 7.98 – 7.95 (m,1H), 7.61 (d, J = 7.9 Hz, 1H), 7.49 (dd, J = 9.7, 2.3 Hz, 1H), 7.42 (d, J = 7.2 Hz, 1H), 7.14 (t, J = 7.6 Hz, 1H), 6.22 (br d, J = 7.0 Hz, 1H), 4.72 (sxt, J = 7.6 Hz, 1H), 4.24 (s, 3H), 4.29 – 4.24 (m, 1H), 4.25 – 4.22 (m, 2H), 3.74 (t, J = 5.0 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 2.88 – 2.80 (m, 2H), 2.65 – 2.54 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 9 was obtained as first eluting stereoisomer as a light brown solid (11 mg, 22% yield). MS m / z (ESI): 413.3 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 7.96 (s, 1H), 7.95 (dd, J = 2.1, 1.1 Hz, 1H), 7.61 (d, J = 7.9 Hz, 1H), 7.46 (dd, J = 9.7, 2.3 Hz, 1H), 7.24 (d, J = 7.1 Hz, 1H), 7.12 (t, J = 7.7 Hz, 1H), 6.07 (br d, J = 7.5 Hz, 1H), 4.73 – 4.61 (m, 1H), 4.32 (s, 3H), 4.22 (t, J = 4.8 Hz, 2H), 3.96 – 3.85 (m, 1H), 3.73 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.01 – 2.90 (m, 2H), 2.32 – 2.20 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 10 and example 11 trans-1-(2-Ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (10) and cis-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (11) 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-7, 40 mg, 0.17 mmol) wasdissolved in dimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 66 mg, 0.17 mmol) as well as diisopropyl ethylamine (0.11 mL, 0.63 mmol) were added. After stirring for 10 min at 25 °C, 3-(1-methylindazol-4- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-14, 40 mg, 0.13 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 48:52 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless oil (54 mg, 0.13 mmol, 77% yield). The mixture (54 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel AD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 10 as second eluting stereoisomer as a colorless oil (34.5 mg, 49% yield). MS m / z(ESI): 413.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.04 (s, 1H), 7.89 (s, 1H), 7.65 (dd, J= 1.9, 9.9 Hz, 1H), 7.41 - 7.33 (m, 1H), 7.29 - 7.23 (m, 1H), 7.08 (d, J = 7.0 Hz, 1H), 7.02 (d, J = 6.5 Hz, 1H), 4.74 - 4.62 (m, 1H), 4.21 (br t, J = 4.7 Hz, 2H), 4.07 (s, 3H), 4.05 - 3.97 (m, 1H), 3.72 (br t, J = 4.8 Hz, 2H), 3.46 (q, J = 7.0 Hz, 2H), 2.86 - 2.73 (m, 2H), 2.67 - 2.56 (m, 2H), 1.14 (t, J = 6.9 Hz, 3H). Analogously, example 11 was obtained as first eluting stereoisomer as acolorless oil (13.5. mg, 19% yield). MS m / z (ESI): 413.2 [M+H]+. 1H NMR (400 MHz, CDCl3):δ ppm 7.98 - 7.92 (m, 2H), 7.56 - 7.49 (m, 1H), 7.36 - 7.29 (m, 1H), 7.29 - 7.21 (m, 1H), 6.90 (d, J = 6.9 Hz, 1H), 6.65 (br d, J = 7.4 Hz, 1H), 4.72 - 4.59 (m, 1H), 4.15 (t, J = 4.9 Hz, 2H), 4.06 (s, 3H), 3.71 - 3.57 (m, 3H), 3.44 (q, J = 7.0 Hz, 2H), 3.09 - 2.96 (m, 2H), 2.31 - 2.18 (m, 2H), 1.12 (t, J = 7.0 Hz, 3H). Example 12 trans-1-(2-Ethoxyethyl)-5-fluoro-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (12) 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylic acid (Int-7, 390 mg, 1.70 mmol) wasdissolved in dimethylformamide (4 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 970 mg, 2.55 mmol) as well as diisopropyl ethylamine(1.19 mL, 6.81 mmol) were added. After stirring for 30 min at 0-4 °C (ice bath), trans-3-phenylcyclobutanamine (Int-178, 251 mg, 1.71 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 64:36 to 34:66 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as a yellow oil (325 mg, 0.91mmol, 53% yield). MS m / z (ESI): 359.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.01 –7.96 (m, 1H), 7.52 (dd, J = 2.3, 9.7 Hz, 1H), 7.38 – 7.20 (m, 5H), 6.29 (d, J = 6.0 Hz, 1H), 4.72 – 4.61 (m, 1H), 4.24 (t, J = 4.9 Hz, 2H), 3.74 (t, J = 4.9 Hz, 2H), 3.70 – 3.61 (m, 1H), 3.49 (q, J = 7.0 Hz, 2H), 2.72 – 2.62 (m, 2H), 2.54 – 2.44 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Example 13 and example 14 trans-1-(2-Ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (13) and cis-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (14) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 56 mg, 0.26 mmol) was dissolved in dimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 100 mg, 0.26 mmol) as well as diisopropyl ethylamine (0.17 mL, 0.96 mmol) were added. After stirring for 10 min at 25 °C, a solution of 3-(5-fluoro-1-methyl- indazol-4-yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-19, 80 mg, 0.24 mmol) in dimethylformamide (1 mL) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 76:24 to 46:54 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a light green oil (35 mg, 0.08 mmol, 33% yield). The mixture (35 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel IK, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (2-propanol + 0.1% ammonia), isocratic 50:50 (v / v)). The product containing fractions were concentrated in vacuo to yield example 13 as second elutingstereoisomer as a light green oil (21.4 mg, 20% yield). MS m / z (ESI): 413.2 [M+H]+. 1H NMR(400 MHz, CDCl3): δ ppm 8.18 (d, J = 2.4 Hz, 1H), 8.03 (s, 1H), 7.73 (dd, J = 2.5, 9.5 Hz, 1H), 7.23 – 7.09 (m, 2H), 6.58 (d, J = 9.4 Hz, 1H), 6.40 (d, J = 5.7 Hz, 1H), 4.79 – 4.68 (m, 1H), 4.30 – 4.15 (m, 3H), 4.07 (s, 3H), 3.74 (t, J = 5.0 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 3.11 – 3.00 (m, 2H), 2.68 – 2.57 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 14 was obtained as first eluting stereoisomer as a light green oil (9.7 mg, 9% yield). MS m / z (ESI): 413.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J = 2.4 Hz, 1H), 7.99 (s, 1H), 7.65 (dd, J = 9.5, 2.6 Hz, 1H), 7.19 (dd, J = 8.9, 3.8 Hz, 1H), 7.18 – 7.09 (m, 1H), 6.54 (d, J = 9.5 Hz, 1H), 6.24 (br d, J = 7.4 Hz, 1H), 4.71 – 4.60 (m, 1H), 4.15 (t, J = 4.9 Hz, 2H), 4.06 (s, 3H), 3.71 (t, J = 4.9 Hz, 2H), 3.69 – 3.60 (m, 1H), 3.47 (q, J = 7.0 Hz, 2H), 3.14 – 3.04 (m, 2H), 2.51 – 2.41 (m, 2H), 1.15 (t, J = 6.9 Hz, 3H). Example 15 and example 16 trans-1-(2-Ethoxyethyl)-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (15) and cis-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (16) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 44 mg, 0.21 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 80 mg, 0.21 mmol) as well as diisopropyl ethylamine (0.13 mL, 0.76 mmol) were added. After stirring for 10 min at 25 °C, 3-(1-methylindazol-7- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-18, 60 mg, 0.19 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless oil (40 mg, 0.10 mmol, 53% yield). The mixture (40 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel IK, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 45:55 (v / v)). The product containing fractions were concentrated in vacuo to yield example 15 as second eluting stereoisomer as a light yellow solid (21.5 mg, 29% yield).MS m / z (ESI): 395.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.15 (d, J = 2.3 Hz, 1H),7.95 (s, 1H), 7.69 (dd, J = 2.5, 9.5 Hz, 1H), 7.60 (d, J = 7.9 Hz, 1H), 7.42 (d, J = 7.2 Hz, 1H), 7.13 (t, J = 7.6 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.40 (br d, J = 6.5 Hz, 1H), 4.78 - 4.66 (m, 1H), 4.30 - 4.20 (m, 4H), 4.16 (t, J = 4.9 Hz, 2H), 3.72 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 2.89 - 2.77 (m, 2H), 2.65 - 2.53 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 16 was obtained as first eluting stereoisomer as a light yellow solid (15 mg, 20% yield). MS m / z(ESI): 395.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.14 (d, J = 2.3 Hz, 1H), 7.95 (s,1H), 7.67 (dd, J = 2.6, 9.5 Hz, 1H), 7.59 (d, J = 7.9 Hz, 1H), 7.22 (d, J = 7.2 Hz, 1H), 7.14 - 7.06 (m, 1H), 6.52 (d, J = 9.5 Hz, 1H), 6.36 (br d, J = 7.5 Hz, 1H), 4.74 - 4.61 (m, 1H), 4.30 (s, 3H), 4.14 (t, J = 4.9 Hz, 2H), 3.94 - 3.81 (m, 1H), 3.70 (t, J = 5.0 Hz, 2H), 3.46 (q, J = 7.0 Hz, 2H), 2.99 - 2.87 (m, 2H), 2.32 - 2.18 (m, 2H), 1.14 (t, J = 7.0 Hz, 3H). Example 17 and example 18 trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3-carboxamide (17) and cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3-carboxamide (18) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 111 mg, 0.52 mmol) was dissolvedin dimethylformamide (3 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 199 mg, 0.52 mmol) as well as diisopropyl ethylamine (0.42 mL, 2.38 mmol) were added. After stirring for 10 min at 25 °C, 3-[2- (trifluoromethyl)phenyl]cyclobutanamine hydrochloride salt (Int-27, 120 mg, 0.48 mmol) was added at 20 °C and the resulting mixture was stirred at 20 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a light green oil (150 mg, 0.37 mmol, 76% yield). The mixture (40 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel IK, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (methanol + 0.1% ammonia), isocratic 65:35 (v / v)). The product containing fractions were concentrated in vacuo to yield example 17 as second eluting stereoisomer as a light greenoil (80.6 mg, 41% yield). MS m / z (ESI): 409.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm8.20 (d, J = 2.3 Hz, 1H), 7.81 (dd, J = 2.1, 9.5 Hz, 1H), 7.70 - 7.52 (m, 3H), 7.36 - 7.28 (m, 1H), 7.05 - 6.93 (m, 1H), 6.52 (d, J = 9.5 Hz, 1H), 4.79 - 4.66 (m, 1H), 4.16 (t, J = 5.0 Hz, 2H), 4.08 - 3.95 (m, 1H), 3.71 (t, J = 5.0 Hz, 2H), 3.45 (q, J = 7.0 Hz, 2H), 2.68 - 2.58 (m, 2H), 2.58 - 2.47 (m, 2H), 1.13 (t, J = 7.0 Hz, 3H). Analogously, example 18 was obtained as first elutingstereoisomer as a light green oil (53.1 mg, 27% yield). MS m / z (ESI): 409.1 [M+H]+. 1H NMR(400 MHz, CDCl3): δ ppm 8.16 (d, J = 2.4 Hz, 1H), 7.73 (dd, J = 2.3, 9.5 Hz, 1H), 7.60 (d, J = 7.8 Hz, 1H), 7.55 - 7.44 (m, 2H), 7.34 - 7.25 (m, 1H), 6.82 - 6.70 (m, 1H), 6.48 (d, J = 9.4 Hz, 1H), 4.59 - 4.45 (m, 1H), 4.10 (t, J = 5.0 Hz, 2H), 3.66 (t, J = 5.0 Hz, 2H), 3.63 - 3.51 (m, 1H), 3.42 (q, J = 7.0 Hz, 2H), 2.92 - 2.79 (m, 2H), 2.23 - 2.10 (m, 2H), 1.11 (t, J = 7.0 Hz, 3H). Example 19 and example 20 trans-1-(2-Ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (19) and cis-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (20) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 29 mg, 0.14 mmol) was dissolved in dimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 53 mg, 0.14 mmol) as well as diisopropyl ethylamine (0.09 mL, 0.50 mmol) were added. After stirring for 10 min at 25 °C, 3-(6-fluoro-1-methyl-indazol-4- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-20, 42 mg, 0.13 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 76:24 to 46:54 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a light green oil (35 mg, 0.08 mmol, 67% yield). The mixture (35 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (2-propanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 19 as second eluting stereoisomer as a light green oil (21.3 mg, 40%yield). MS m / z (ESI): 413.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.16 (d, J = 2.4 Hz, 1H), 7.87 (d, J = 0.6 Hz, 1H), 7.69 (dd, J = 9.5, 2.6 Hz, 1H), 6.93 – 6.87 (m, 2H), 6.57 (d, J = 9.4 Hz, 1H), 6.31 (br d, J = 6.6 Hz, 1H), 4.67 (sxt, J = 6.9 Hz, 1H), 4.17 (t, J = 5.0 Hz, 2H), 4.03 (s, 3H), 4.06 – 3.98 (m, 1H), 3.73 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.1 Hz, 2H), 2.82 – 2.74 (m, 2H), 2.65 – 2.55 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H).Analogously, example 20 was obtained as firsteluting stereoisomer as a light green oil (9.5 mg, 18% yield). MS m / z (ESI): 413.3 [M+H]+. 1HNMR (400 MHz, CDCl3): δ ppm 8.13 (d, J = 2.6 Hz, 1H), 7.91 (d, J = 0.7 Hz, 1H), 7.63 (dd, J = 9.5, 2.6 Hz, 1H), 6.89 (d, J = 8.8 Hz, 1H), 6.72 (d, J = 10.3 Hz, 1H), 6.53 (d, J = 9.5 Hz, 1H), 6.16 (br d, J = 7.5 Hz, 1H), 4.74 – 4.61 (m, 1H), 4.14 (t, J = 5.0 Hz, 2H), 4.02 (s, 3H), 3.71 (t, J = 5.0 Hz, 2H), 3.69 – 3.58 (m, 1H), 3.46 (q, J = 7.0 Hz, 2H), 3.09 – 3.01 (m, 2H), 2.25 – 2.15 (m, 2H), 1.14 (t, J = 7.0 Hz, 3H). Example 21 and example 22 trans-1-(2-Ethoxyethyl)-N-[3-(2-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (21) and cis-1-(2-ethoxyethyl)-N-[3-(2-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (22) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 57 mg, 0.27 mmol) was dissolved in dimethylformamide (2 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 103 mg, 0.27 mmol) as well as diisopropyl ethylamine (0.17 mL, 0.99 mmol) were added. After stirring for 10 min at 25 °C, 3-(2-methylindazol-4- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-21, 78 mg, 0.25 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 77:23 to 50:50 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a white solid (80 mg, 0.20 mmol, 81% yield). The mixture (80 mg) was separated into its diastereoisomers by preparative chiral HPLC (Welch Ultimate XB-NH2, 250 mm x 50 mm x 10 um, n-hexane / ethanol, gradient 75:25 to 35:65 (v / v)). The product containing fractions were concentrated in vacuo to obtain example 21 as second eluting stereoisomer using the following analytical method: SFC (Daicel Chiralpak IG-3, 50 mm x 4.6 mm x 3 um, supercritical carbon dioxide / (ethanol + 0.05% diethylamine), gradient 80:20 to 40:60 (v / v)) as a light yellow oil (43.6 mg, 44% yield). MS m / z (ESI): 395.2[M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.17 (d, J = 2.3 Hz, 1H), 7.80 - 7.71 (m, 2H), 7.54(d, J = 8.7 Hz, 1H), 7.29 - 7.21 (m, 1H), 6.97 (d, J = 6.8 Hz, 1H), 6.84 (br s, 1H), 6.51 (d, J = 9.4 Hz, 1H), 4.70 - 4.58 (m, 1H), 4.18 (s, 3H), 4.13 (br t, J = 4.8 Hz, 2H), 3.89 - 3.80 (m, 1H), 3.69 (br t, J = 4.8 Hz, 2H), 3.45 (q, J = 7.1 Hz, 2H), 2.81 - 2.70 (m, 2H), 2.58 - 2.47 (m, 2H), 1.13 (t, J = 7.0 Hz, 3H). Analogously, example 22 was obtained as first eluting stereoisomer using the analytical SFC method detailed above as a light yellow oil (16.2 mg, 16% yield). MS m / z (ESI):395.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.17 - 8.11 (m, 1H), 7.84 (s, 1H), 7.68 (dd,J = 2.2, 9.5 Hz, 1H), 7.53 (d, J = 8.7 Hz, 1H), 7.21 (t, J = 7.7 Hz, 1H), 6.79 (d, J = 6.7 Hz, 1H), 6.65 (br d, J = 7.3 Hz, 1H), 6.47 (d, J = 9.4 Hz, 1H), 4.72 - 4.58 (m, 1H), 4.19 (s, 3H), 4.09 (br t, J = 4.8 Hz, 2H), 3.66 (br t, J = 4.8 Hz, 2H), 3.55 - 3.39 (m, 3H), 3.01 - 2.90 (m, 2H), 2.24 - 2.11 (m, 2H), 1.12 (t, J = 7.0 Hz, 3H). Example 23 and example 24 trans-1-(2-Ethoxyethyl)-N-[3-(1-methylbenzotriazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (23) and cis-1-(2-ethoxyethyl)-N-[3-(1-methylbenzotriazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (24) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 20 mg, 0.10 mmol) was dissolved in dimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 37 mg, 0.10 mmol) as well as diisopropyl ethylamine (0.06 mL, 0.35 mmol) were added. After stirring for 10 min at 25 °C, 3-(1-methylbenzotriazol-4- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-22, 28 mg, 0.09 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless gum (35 mg, 0.09 mmol, 99% yield). The mixture (35 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 55:45 (v / v)). The product containing fractions were concentrated in vacuo to afford example 23 as second eluting stereoisomer as a light green oil (20 mg, 56% yield). MSm / z (ESI): 396.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.17 (d, J = 2.4 Hz, 1H), 7.73(dd, J = 9.5, 2.6 Hz, 1H), 7.50 (dd, J = 8.3, 7.1 Hz, 1H), 7.39 (d, J = 8.1 Hz, 1H), 7.34 (d, J = 7.1 Hz, 1H), 6.57 (d, J = 9.5 Hz, 1H), 6.49 (br d, J = 6.4 Hz, 1H), 4.78 (sxt, J = 6.8 Hz, 1H), 4.50 – 4.40 (m, 1H), 4.31 (s, 3H), 4.18 (t, J = 5.0 Hz, 2H), 3.73 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 2.92 – 2.83 (m, 2H), 2.71 – 2.61 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 24 was obtained as first eluting stereoisomer as a light green oil (14 mg, 39% yield). MS m / z(ESI): 396.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.52 (d, J = 9.0 Hz, 1H), 8.31 (d, J =2.5 Hz, 1H), 7.97 (dd, J = 2.6, 9.5 Hz, 1H), 7.44 – 7.37 (m, 2H), 7.14 (dd, J = 2.2, 5.6 Hz, 1H), 6.62 (d, J = 9.5 Hz, 1H), 4.94 – 4.82 (m, 1H), 4.34 (s, 3H), 4.22 (t, J = 5.3 Hz, 2H), 3.75 (t, J = 5.1 Hz, 2H), 3.69 – 3.59 (m, 1H), 3.49 (q, J = 7.0 Hz, 2H), 3.16 – 3.06 (m, 2H), 2.81 – 2.71 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 25 and example 26 trans-1-(2-Ethoxyethyl)-N-[3-(4-methylquinazolin-8-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (25) and cis-1-(2-ethoxyethyl)-N-[3-(4-methylquinazolin-8-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (26) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 57 mg, 0.27 mmol) was dissolved in dimethylformamide (3 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 102 mg, 0.27 mmol) as well as diisopropyl ethylamine (0.17 mL, 0.98 mmol) were added. After stirring for 10 min at 25 °C, 3-(4-methylquinazolin-8- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-23, 80 mg, 0.24 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 77:23 to 50:50 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless gum. The mixture was separated into its diastereoisomers by preparative chiral HPLC (Welch Ultimate XB-NH2, 250 mm x 50 mm x 10 um, n-hexane / ethanol, gradient 85:15 to 45:55 (v / v)). The product containing fractions were concentrated in vacuo to obtain example 25 as second eluting stereoisomer using the following analytical method: SFC (Cellulose-2-3, 50 mm x 4.6 mm x 3 um, supercritical carbon dioxide / (ethanol + 0.05% diethylamine), isocratic, 50:50 (v / v)) as alight red gum (7.8 mg, 8% yield). MS m / z (ESI): 407.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δppm 9.18 (s, 1H), 8.17 (d, J = 2.6 Hz, 1H), 8.01 (d, J = 8.3 Hz, 1H), 7.93 (d, J = 7.2 Hz, 1H), 7.72 (dd, J = 9.5, 2.6 Hz, 1H), 7.66 (t, J = 7.8 Hz, 1H), 6.59 (d, J = 9.5 Hz, 1H), 6.36 (br d, J = 6.7 Hz, 1H), 4.75 – 4.63 (m, 1H), 4.19 (t, J = 5.0 Hz, 2H), 3.74 (t, J = 5.0 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 2.98 (s, 3H), 2.77 – 2.69 (m, 2H), 2.67 – 2.58 (m, 2H), 1.18 (t, J = 7.0 Hz, 3H). Analogously, example 26 was isolated as first eluting stereoisomer using the analytical SFCmethod detailed above as a light red gum (6.8 mg, 7% yield). MS m / z (ESI): 407.3 [M+H]+. 1HNMR (400 MHz, CDCl3): δ ppm 9.19 (s, 1H), 8.14 (d, J = 2.4 Hz, 1H), 7.99 (dd, J = 1.1, 8.3 Hz, 1H), 7.75 (d, J = 7.2 Hz, 1H), 7.67 – 7.58 (m, 2H), 7.55 (t, J = 9.5 Hz, 1H), 6.19 (d, J = 7.6 Hz, 1H), 4.76 – 4.64 (m, 1H), 4.22 – 4.11 (m, 3H), 3.72 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.15 – 3.05 (m, 2H), 2.97 (s, 3H), 2.30 – 2.20 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 27 cis-1-(2-Ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (27) Methyl 1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylate (Int-4, 30 mg, 0.13 mmol) wasdissolved in tetrahydrofuran (1 mL) and cis-3-phenylcyclobutanamine (Int-179, 39 mg, 0.27mmol) followed by 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD, CAS [5807-14-7], 18.5 mg, 0.13 mmol) were added. The mixture was stirred at 60 °C for 32 h. After that, the reaction mixture was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the titlecompound as a colorless gum (11 mg, 0.03 mmol, 26% yield). MS m / z (ESI): 341.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.12 (s, 1H), 7.62 (d, J = 7.8 Hz, 1H), 7.37 – 7.29 (m, 2H), 7.26 – 7.19 (m, 3H), 6.56 (d, J = 9.4 Hz, 1H), 6.00 – 5.92 (m, 1H), 4.63 – 4.52 (m, 1H), 4.19 – 4.13 (m, 2H), 3.76 – 3.69 (m, 2H), 3.47 (q, J = 7.0 Hz, 2H), 3.35 – 3.24 (m, 1H), 2.96 – 2.86 (m, 2H), 2.12 – 2.01 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 28 trans-1-(2-Ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (28) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 400 mg, 1.89 mmol) was dissolvedin dimethylformamide (4 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 1079 mg, 2.84 mmol) as well as diisopropyl ethylamine (985 mg,7.58 mmol) were added. After stirring for 20 min at 0-4 °C (ice bath), trans-3-phenylcyclobutanamine (Int-178, 279 mg, 1.89 mmol) was added at 20 °C and the resulting mixture was stirred at 20 °C for 1 h. Then, it was filtered and the filtrate was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a pink solid (377 mg, 1.11 mmol, 58% yield). MSm / z (ESI): 341.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.14 (s, 1H), 7.68 (d, J = 8.4 Hz,1H), 7.40 – 7.19 (m, 5H), 6.57 (d, J = 9.4 Hz, 1H), 6.26 – 6.16 (m, 1H), 4.73 – 4.62 (m, 1H), 4.22 – 4.14 (m, 2H), 3.77 – 3.70 (m, 2H), 3.69 – 3.61 (m, 1H), 3.48 (q, J = 7.0 Hz, 2H), 2.73 – 2.62 (m, 2H), 2.53 – 2.42 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Example 29 1-(2-Ethoxyethyl)-6-oxo-N-(3-phenyl-1-bicyclo[1.1.1]pentanyl)pyridine-3-carboxamide (29) 3-Phenylbicyclo[1.1.1]pentan-1-amine hydrochloride (Int-180, 30 mg, 0.15 mmol) was dissolved in dimethylformamide (1.5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 87 mg, 0.23 mmol) as well as diisopropyl ethylamine (0.13 mL, 0.77 mmol) were added at 0-4 °C (ice bath). After stirring for 30 min at 25°C, 1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 32 mg, 0.15 mmol) was addedand the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 64:36 to 34:66 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a white solid (12 mg,0.03 mmol, 22% yield). MS m / z (ESI): 353.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.27– 8.14 (m, 1H), 7.77 – 7.65 (m, 1H), 7.37 – 7.21 (m, 5H), 6.67 – 6.45 (m, 2H), 4.28 – 4.12 (m, 2H), 3.83 – 3.67 (m, 2H), 3.56 – 3.44 (m, 2H), 2.45 (s, 6H), 1.22 – 1.12 (m, 3H). Example 30 1-(2-Ethoxyethyl)-6-oxo-N-[3-[3-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide (30) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 19 mg, 0.09 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 41 mg, 0.11 mmol) as well as diisopropyl ethylamine (93 mg, 126 uL, 0.72 mmol) were added. After stirring for 15 min at 25 °C, 3-[3- (trifluoromethyl)phenyl]cyclobutanamine (Int-181, 31 mg, 0.14 mmol) was added and the resulting mixture was stirred at 25 °C for 18 h. Then, it was purified directly by preparative HPLC (Gemini NX, 100 x 30 mm x 5 um, (water + 0.1% formic acid) / acetonitrile, gradient 80:20 to 2:98 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (28.5 mg, 0.07 mmol, 77% yield). MS m / z (ESI): 409.2 [M+H]+. Example 31 and example 32 trans-1-(2-Ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (31) and cis-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (32) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 22 mg, 0.11 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 57 mg, 0.15 mmol) as well as diisopropyl ethylamine (0.07 mL, 0.42 mmol) were added. After stirring for 5 min at 25 °C, 3-(1-methylindazol-4- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-14, 35 mg, 0.11 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 73:27 to 43:57 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless oil. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD-H, 250 mm x 30 mm x 5 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 31 as second elutingstereoisomer as a colorless oil (12.6 mg, 29% yield). MS m / z (ESI): 395.2 [M+H]+. 1H NMR(400 MHz, CDCl3): δ ppm 8.15 (d, J = 2.4 Hz, 1H), 7.92 (s, 1H), 7.69 (dd, J = 9.4, 2.6 Hz, 1H), 7.39 (dd, J = 8.6, 7.2 Hz, 1H), 7.30 – 7.27 (m, 1H), 7.12 (d, J = 7.0 Hz, 1H), 6.58 (d, J = 9.4 Hz, 1H), 6.23 (br d, J = 6.1 Hz, 1H), 4.74 – 4.65 (m, 1H), 4.18 (t, J = 5.0 Hz, 2H), 4.09 (s, 3H), 4.08 – 4.01 (m, 1H), 3.74 (t, J = 5.0 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 2.88 – 2.79 (m, 2H), 2.63 – 2.54 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 32 was obtained as first elutingstereoisomer as a colorless oil (6.5 mg, 15% yield). MS m / z (ESI): 395.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.12 (d, J = 2.6 Hz, 1H), 7.97 (s, 1H), 7.62 (dd, J = 9.6, 2.6 Hz, 1H), 7.36 (dd, J = 8.4, 7.3 Hz, 1H), 7.27 (d, J = 8.1 Hz, 1H), 6.94 (d, J = 7.1 Hz, 1H), 6.54 (d, J = 9.4 Hz, 1H), 6.07 (br d, J = 7.6 Hz, 1H), 4.74 – 4.63 (m, 1H), 4.15 (t, J = 5.0 Hz, 2H), 4.08 (s, 3H), 3.72 (t, J = 5.0 Hz, 2H), 3.70 – 3.62 (m, 1H), 3.47 (q, J = 7.0 Hz, 2H), 3.12 – 3.02 (m, 2H), 2.29 – 2.17 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 33 and example 34 trans-N-[3-(1,3-Benzoxazol-7-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (33) and cis-N-[3-(1,3-benzoxazol-7-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (34) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 34 mg, 0.16 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 62 mg, 0.16 mmol) as well as diisopropyl ethylamine (0.11 mL, 0.64 mmol) were added. After stirring for 10 min at 25 °C, 3-(1,3-benzoxazol-7- yl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-24, 41 mg, 0.14 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Waters xbridge, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 79:21 to 49:51 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless oil. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak IG, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 50:50 (v / v)). The product containing fractions were concentrated in vacuo to yield example 33 as second elutingstereoisomer as a light green solid (16 mg, 30% yield). MS m / z (ESI): 382.2 [M+H]+. 1H NMR(400 MHz, CDCl3): δ ppm 8.18 (d, J = 2.2 Hz, 1H), 8.11 (s, 1H), 7.74 (dd, J = 9.4, 2.4 Hz, 1H), 7.67 (dd, J = 7.3, 1.0 Hz, 1H), 7.38 – 7.30 (m, 2H), 6.63 (br d, J = 6.5 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 4.78 (sxt, J = 7.0 Hz, 1H), 4.17 (t, J = 4.9 Hz, 2H), 4.04 – 3.94 (m, 1H), 3.72 (t, J = 4.9 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 2.88 – 2.78 (m, 2H), 2.64 – 2.54 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Analogously, example 34 was obtained as first eluting stereoisomer as a light green gum(8.2 mg, 14% yield). MS m / z (ESI): 382.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.14(d, J = 2.6 Hz, 1H), 8.12 (s, 1H), 7.69 – 7.62 (m, 2H), 7.33 (t, J = 7.8 Hz, 1H), 7.21 (d, J = 7.5 Hz, 1H), 6.55 (d, J = 9.5 Hz, 1H), 6.15 (br d, J = 7.5 Hz, 1H), 4.75 – 4.59 (m, 1H), 4.16 (t, J = 4.9 Hz, 2H), 3.72 (t, J = 5.0 Hz, 2H), 3.66 – 3.54 (m, 1H), 3.51 – 3.44 (m, 2H), 3.05 – 2.96 (m, 2H), 2.36 – 2.26 (m, 2H), 1.15 (t, J = 6.9 Hz, 3H). Example 35 and example 36 trans-1-(2-Ethoxyethyl)-N-(3-fluoro-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide(35) and cis-1-(2-ethoxyethyl)-N-(3-fluoro-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide (36) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 42 mg, 0.20 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 98 mg, 0.26 mmol) as well as diisopropyl ethylamine (0.10 mL, 77 mg, 0.60 mmol) were added. After stirring for 5 min at 25 °C, 3-fluoro-3-phenyl- cyclobutanamine hydrochloride (Int-50, 40 mg, 0.20 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 30 min. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a colorless oil. The mixture (ca.40 mg) was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak AD-H, 250 mm x 30 mm x 5 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 75:25 (v / v)). The product containing fractions were concentrated in vacuo to afford example 35 as second elutingstereoisomer as a white solid (13 mg, 18% yield). MS m / z (ESI): 359.3 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.15 (s, 1H), 7.68 (d, J = 9.5 Hz, 1H), 7.50 – 7.33 (m, 5H), 6.57 (d, J = 9.5 Hz, 1H), 6.30 (d, J = 6.6 Hz, 1H), 4.50 – 4.40 (m, 1H), 4.18 (t, J = 4.7 Hz, 2H), 3.73 (t, J = 4.7 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 3.22 – 3.10 (m, 2H), 2.72 – 2.58 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 36 was obtained as first eluting stereoisomer as a light brown gum(23 mg, 31% yield). MS m / z (ESI): 359.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.11 (s, 1H), 7.61 (d, J = 9.4 Hz, 1H), 7.47 – 7.32 (m, 5H), 6.52 (d, J = 9.3 Hz, 1H), 6.24 – 6.17 (m, 1H), 4.94 – 4.82 (m, 1H), 4.17 (t, J = 4.6 Hz, 2H), 3.71 (t, J = 4.6 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 3.18 – 3.04 (m, 2H), 2.73 – 2.57 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 37 and example 38 trans-1-(2-Ethoxyethyl)-N-[3-(3-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide(37) and cis-1-(2-ethoxyethyl)-N-[3-(3-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (38) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 21 mg, 0.10 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 37 mg, 0.10 mmol) as well as diisopropyl ethylamine (0.06 mL, 0.36 mmol) were added. After stirring for 10 min at 25 °C, 3-(3-fluorophenyl)cyclobutanamine 2,2,2-trifluoroacetate salt (Int-25, 25 mg, 0.09 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 66:34 to 36:64 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 75:25 (v / v)). The product containing fractions were concentrated in vacuo to yield example 37 as second eluting stereoisomer as a light yellow oil(9.6 mg, 30% yield). MS m / z (ESI): 395.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.15(d, J = 2.6 Hz, 1H), 7.69 (dd, J = 9.5, 2.6 Hz, 1H), 7.33 – 7.26 (m, 1H), 7.06 (d, J = 7.7 Hz, 1H), 6.98 (dt, J = 10.2, 1.9 Hz, 1H), 6.91 (td, J = 8.4, 2.4 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.33 (br d, J = 6.5 Hz, 1H), 4.65 (sxt, J = 6.9 Hz, 1H), 4.17 (t, J = 5.0 Hz, 2H), 3.73 (t, J = 5.0 Hz, 2H), 3.68 – 3.59 (m, 1H), 3.48 (q, J = 7.0 Hz, 2H), 2.68 – 2.60 (m, 2H), 2.52 – 2.44 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 38 was obtained as first eluting stereoisomer as a lightyellow oil (5.4 mg, 17% yield). MS m / z (ESI): 395.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δppm 8.12 (d, J = 2.7 Hz, 1H), 7.64 (dd, J = 9.5, 2.6 Hz, 1H), 7.32 – 7.23 (m, 1H), 6.98 (d, J = 7.6 Hz, 1H), 6.92 (d, J = 8.9 Hz, 1H), 6.94 – 6.87 (m, 1H), 6.54 (d, J = 9.5 Hz, 1H), 6.12 (br d, J = 7.2 Hz, 1H), 4.62 – 4.50 (m, 1H), 4.15 (t, J = 5.0 Hz, 2H), 3.71 (t, J = 5.0 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 3.34 – 3.22 (m, 1H), 2.95 – 2.85 (m, 2H), 2.10 – 1.99 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 39 and example 40 trans-1-(2-Ethoxyethyl)-N-[3-(1'-methyl-2'-oxo-spiro[cyclopropane-1,3'-indoline]-7'-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (39) and cis-1-(2-ethoxyethyl)-N-[3-(1'-methyl-2'-oxo-spiro[cyclopropane-1,3'-indoline]-7'-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide (40) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 71 mg, 0.34 mmol) was dissolved indimethylformamide (3 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 128 mg, 0.34 mmol) as well as diisopropyl ethylamine (0.24 mL, 1.40 mmol) were added. After stirring for 10 min at 25 °C, 7'-(3-aminocyclobutyl)-1'-methyl- spiro[cyclopropane-1,3'-indoline]-2'-one 2,2,2-trifluoroacetate salt (Int-26, 100 mg, 0.28 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 43:57 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 39 as second elutingstereoisomer as a white solid (57 mg, 46% yield). MS m / z (ESI): 436.3 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.14 (d, J = 2.4 Hz, 1H), 7.66 (dd, J = 9.4, 2.6 Hz, 1H), 7.39 (d, J = 7.9 Hz, 1H), 7.07 (t, J = 7.7 Hz, 1H), 6.72 (dd, J = 7.3, 1.0 Hz, 1H), 6.57 (d, J = 9.5 Hz, 1H), 6.15 (br d, J = 6.7 Hz, 1H), 4.73 (sxt, J = 7.6 Hz, 1H), 4.23 – 4.19 (m, 1H), 4.17 (t, J = 4.9 Hz, 2H), 3.73 (t, J = 5.0 Hz, 2H), 3.52 (s, 3H), 3.48 (q, J = 7.0 Hz, 2H), 2.82 – 2.74 (m, 2H), 2.57 – 2.46 (m, 2H), 1.76 (q, J = 3.9 Hz, 2H), 1.51 (q, J = 4.0 Hz, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 40 was obtained as first eluting stereoisomer as a white solid (40 mg, 32% yield). MSm / z (ESI): 436.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.14 (d, J = 2.4 Hz, 1H), 7.65(dd, J = 9.4, 2.4 Hz, 1H), 7.24 (d, J = 7.9 Hz, 1H), 7.04 (t, J = 7.6 Hz, 1H), 6.70 (dd, J = 7.3, 1.0 Hz, 1H), 6.56 (d, J = 9.4 Hz, 1H), 6.11 (br d, J = 7.3 Hz, 1H), 4.65 – 4.52 (m, 1H), 4.17 (t, J = 5.0 Hz, 2H), 3.88 – 3.78 (m, 1H), 3.73 (t, J = 5.0 Hz, 2H), 3.60 (s, 3H), 3.48 (q, J = 7.0 Hz, 2H), 2.91 – 2.82 (m, 2H), 2.28 – 2.17 (m, 2H), 1.76 (q, J = 3.8 Hz, 2H), 1.50 (q, J = 4.1 Hz, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 41 trans-N-[3-(2-Chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (41) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 58 mg, 0.28 mmol) was dissolved indimethylformamide (1.5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 104 mg, 0.28 mmol) as well as diisopropyl ethylamine (0.16 mL,0.92 mmol) were added. After stirring for 10 min at 25 °C, trans-3-(2-chlorophenyl)cyclobutanamine hydrochloride (Int-182, 50 mg, 0.23 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 62:38 to 32:68 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a white solid (17 mg, 0.05mmol, 20% yield). MS m / z (ESI): 375.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.19 -8.14 (m, 1H), 7.77 - 7.66 (m, 1H), 7.47 - 7.42 (m, 1H), 7.40 - 7.34 (m, 1H), 7.33 - 7.27 (m, 1H), 7.22 - 7.15 (m, 1H), 6.62 - 6.55 (m, 1H), 6.49 - 6.14 (m, 1H), 4.66 - 4.54 (m, 1H), 4.23 - 4.14 (m, 2H), 3.99 - 3.87 (m, 1H), 3.79 - 3.68 (m, 2H), 3.55 - 3.43 (m, 2H), 2.71 - 2.59 (m, 1H), 2.56 - 2.44 (m, 2H), 1.22 - 1.09 (m, 3H). Example 42 trans-1-(2-Ethoxyethyl)-N-[3-(2-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (42) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 35 mg, 0.16 mmol) was dissolved indimethylformamide (0.5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 65 mg, 0.17 mmol) as well as diisopropyl ethylamine (0.10 mL,0.60 mmol) were added. After stirring for 10 min at 15 °C, trans-3-(2-fluorophenyl)cyclobutanamine hydrochloride (Int-183, 30 mg, 0.15 mmol) was added and the resulting mixture was stirred at 15 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 250 x 50 mm x 15 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 48:52 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a light brown oil (29 mg,0.08 mmol, 54% yield). MS m / z (ESI): 359.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.17(s, 1H), 7.74 (d, J = 9.4 Hz, 1H), 7.43 – 6.97 (m, 4H), 6.62 – 6.51 (m, 2H), 4.72 – 4.60 (m, 1H), 4.24 – 4.13 (m, 2H), 3.92 – 3.80 (m, 1H), 3.77 – 3.69 (m, 2H), 3.47 (q, J = 7.0 Hz, 2H), 2.74 – 2.62 (m, 2H), 2.56 – 2.44 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 43 trans-N-[3-(3-Chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (43) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 58 mg, 0.28 mmol) was dissolved indimethylformamide (1.5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 104 mg, 0.28 mmol) as well as diisopropyl ethylamine (0.16 mL,0.92 mmol) were added. After stirring for 10 min at 25 °C, trans-3-(3-chlorophenyl)cyclobutanamine hydrochloride (Int-184, 50 mg, 0.23 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a white solid (53 mg, 0.14mmol, 61% yield). MS m / z (ESI): 375.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.15 (d, J= 2.6 Hz, 1H), 7.67 (dd, J = 2.6, 9.5 Hz, 1H), 7.32 – 7.25 (m, 2H), 7.23 – 7.15 (m, 2H), 6.59 (d, J = 9.5 Hz, 1H), 6.11 (d, J = 5.8 Hz, 1H), 4.72 – 4.61 (m, 1H), 4.19 (t, J = 4.9 Hz, 2H), 3.74 (t, J = 4.9 Hz, 2H), 3.68 – 3.58 (m, 1H), 3.49 (q, J = 7.0 Hz, 2H), 2.70 – 2.61 (m, 2H), 2.54 – 2.43 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Example 44 trans-N-[3-(4-Chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide (44) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 58 mg, 0.28 mmol) was dissolved indimethylformamide (1.5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 104 mg, 0.28 mmol) as well as diisopropyl ethylamine (0.16 mL,0.92 mmol) were added. After stirring for 10 min at 25 °C, trans-3-(4-chlorophenyl)cyclobutanamine hydrochloride (Int-185, 50 mg, 0.23 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a white solid (55 mg, 0.15mmol, 64% yield). MS m / z (ESI): 375.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.14 (d, J= 2.1 Hz, 1H), 7.65 (dd, J = 2.3, 9.4 Hz, 1H), 7.31 (d, J = 8.4 Hz, 2H), 7.22 (d, J = 8.4 Hz, 2H), 6.57 (d, J = 9.4 Hz, 1H), 6.08 (d, J = 6.2 Hz, 1H), 4.71 – 4.61 (m, 1H), 4.18 (t, J = 4.9 Hz, 2H), 3.73 (t, J = 4.9 Hz, 2H), 3.66 – 3.57 (m, 1H), 3.48 (q, J = 7.0 Hz, 2H), 2.67 – 2.59 (m, 2H), 2.52 – 2.43 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Example 45 trans-1-(2-Ethoxyethyl)-N-[3-(o-tolyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (45) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 80 mg, 0.38 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 173 mg, 0.45 mmol) as well as diisopropyl ethylamine (0.33 mL,1.89 mmol) were added. After stirring for 10 min at 20 °C, trans-3-(o-tolyl)cyclobutanaminehydrobromide (Int-186, 92 mg, 0.38 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 65:35 to 35:65 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a colorless gum (43 mg, 0.12 mmol, 31% yield). MS m / z (ESI):355.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J = 2.4 Hz, 1H), 7.68 (dd, J = 2.5,9.5 Hz, 1H), 7.23 – 7.09 (m, 4H), 6.50 (d, J = 9.5 Hz, 1H), 6.43 (d, J = 7.4 Hz, 1H), 4.64 – 4.52 (m, 1H), 4.11 (t, J = 4.9 Hz, 2H), 3.67 (t, J = 4.9 Hz, 2H), 3.45 (q, J = 7.0 Hz, 2H), 3.39 – 3.28 (m, 1H), 2.95 – 2.85 (m, 2H), 2.26 (s, 3H), 2.11 – 1.99 (m, 2H), 1.13 (t, J = 7.0 Hz, 3H). Example 46 trans-1-(2-Ethoxyethyl)-6-oxo-N-[3-[4-(1H-1,2,4-triazol-5-yl)phenyl]cyclobutyl]pyridine-3- carboxamide (46)1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 19 mg, 0.09 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 41 mg, 0.11 mmol) as well as diisopropyl ethylamine (93 mg, 126 uL, 0.72 mmol) were added. After stirring for 15 min at 25 °C, trans-3-[4-(1H-1,2,4-triazol-5- yl)phenyl]cyclobutanamine (Int-187, 31 mg, 0.14 mmol) was added and the resulting mixture was stirred at 25 °C for 18 h. Then, it was purified directly by preparative HPLC (Gemini NX, 100 x 30 mm x 5 um, (water + 0.1% formic acid) / acetonitrile, gradient 80:20 to 2:98 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (16.4 mg, 0.04 mmol, 45% yield). MS m / z (ESI): 408.3 [M+H]+. Example 47 trans-1-(2-Ethoxyethyl)-N-[3-[3-(1-methylpyrazol-3-yl)phenyl]cyclobutyl]-6-oxo-pyridine- 3-carboxamide (47) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 19 mg, 0.09 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 41 mg, 0.11 mmol) as well as diisopropyl ethylamine (93 mg, 126 uL, 0.72 mmol) were added. After stirring for 15 min at 25 °C, trans-3-[3-(1-methylpyrazol-3- yl)phenyl]cyclobutanamine (Int-188, 33 mg, 0.14 mmol) was added and the resulting mixture was stirred at 25 °C for 18 h. Then, it was purified directly by preparative HPLC (Gemini NX, 100 x 30 mm x 5 um, (water + 0.1% formic acid) / acetonitrile, gradient 80:20 to 2:98 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (21.3 mg, 0.05 mmol, 56% yield). MS m / z (ESI): 421.3 [M+H]+. Example 48 1-(2-Ethoxyethyl)-6-oxo-N-[3-[4-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide (48) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 19 mg, 0.09 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 41 mg, 0.11 mmol) as well as diisopropyl ethylamine (93 mg, 126 uL, 0.72 mmol) were added. After stirring for 15 min at 25 °C, 3-[4- (trifluoromethyl)phenyl]cyclobutanamine (Int-189, 31 mg, 0.14 mmol) was added and the resulting mixture was stirred at 25 °C for 18 h. Then, it was purified directly by preparative HPLC (Gemini NX, 100 x 30 mm x 5 um, (water + 0.1% formic acid) / acetonitrile, gradient 80:20 to 2:98 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (19.1 mg, 0.05 mmol, 52% yield). MS m / z (ESI): 409.1 [M+H]+. In analogy to the procedure described for the preparation of example 48, the following examples were prepared using the respective amines instead of starting material (amine) Int-189: Ex.-Structure Name Amine m / zNo. (ESI) 49 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-425.1 (5,6-dichloro-2-pyridyl)pyrrolidin-3- [M+H]+yl]pyridine-3-carboxamide Int-19050 N-[1-(2-cyano-3-pyridyl)pyrrolidin-3-382.2 yl]-1-(2-ethoxyethyl)-6-oxo-pyridine- [M+H]+3-carboxamide Int-191 51 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(6-391.1 chloro-2-pyridyl)pyrrolidin-3-yl]pyri- [M+H]+dine-3-carboxamide Int-192 52 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(5-391.1 chloro-2-pyridyl)pyrrolidin-3-yl]pyri- [M+H]+dine-3-carboxamide Int-82 53 1-(2-ethoxyethyl)-N-(3-methylcyclo-307.2 hexyl)-6-oxo-pyridine-3-carboxamide [M+H]+Int-193 54 1-(2-ethoxyethyl)-6-oxo-N-[4-(3-370.2 pyridyl)cyclohexyl]pyridine-3- [M+H]+carboxamide Int-194 Example 55 cis-1-(2-Ethoxyethyl)-N-[3-(hydroxymethyl)-3-phenyl-cyclobutyl]-6-oxo-pyridine-3- carboxamide (55)1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 129 mg, 0.61 mmol) was dissolvedin dimethylformamide (2 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 233 mg, 0.61 mmol) as well as diisopropyl ethylamine (0.41 mL,2.34 mmol) were added. After stirring for 10 min at 25 °C, cis-(3-amino-1-phenyl-cyclobutyl)methanol (Int-46, 115 mg, 0.58 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 78:22 to 48:52 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the titlecompound as a light green oil (97 mg, 45% yield). MS m / z (ESI): 371.2 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.12 - 8.06 (m, 1H), 7.70 - 7.59 (m, 2H), 7.31 - 7.22 (m, 2H), 7.19 - 7.09 (m, 3H), 6.41 (d, J = 9.4 Hz, 1H), 4.46 - 4.34 (m, 1H), 4.05 (br t, J = 4.8 Hz, 2H), 3.62 (br t, J = 4.8 Hz, 2H), 3.48 (s, 2H), 3.37 (q, J = 7.1 Hz, 2H), 2.81 (br dd, J = 8.9, 12.4 Hz, 2H), 2.40 (br dd, J = 5.3, 12.8 Hz, 2H), 1.05 (t, J = 7.0 Hz, 3H). Example 56 trans-1-(2-Ethoxyethyl)-N-[3-(hydroxymethyl)-3-phenyl-cyclobutyl]-6-oxo-pyridine-3- carboxamide (56) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 54 mg, 0.25 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 97 mg, 0.25 mmol) as well as diisopropyl ethylamine (0.17 mL,0.97 mmol) were added. After stirring for 10 min at 25 °C, trans-(3-amino-1-phenyl-cyclobutyl)methanol (Int-47, 43 mg, 0.24 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 79:21 to 49:51 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the titlecompound as a light green oil (25 mg, 27% yield). MS m / z (ESI): 371.2 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.09 (d, J = 2.6 Hz, 1H), 7.66 (dd, J = 2.6, 9.5 Hz, 1H), 7.35 – 7.29 (m, 1H), 7.24 - 7.18 (m, 1H), 7.14 - 7.08 (m, 2H), 6.59 (d, J = 7.3 Hz, 1H), 6.47 (d, J = 9.5 Hz, 1H), 4.74 - 4.62 (m, 1H), 4.06 (t, J = 4.9 Hz, 2H), 3.71 (s, 2H), 3.63 (t, J = 4.9 Hz, 2H), 3.42 (q, J = 7.0 Hz, 2H), 2.91 – 2.82 (m, 2H), 2.29 – 2.20 (m, 2H), 1.10 (t, J = 7.0 Hz, 3H). Example 57 trans-1-(2-Ethoxyethyl)-N-[3-(4-methoxyphenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (57) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 30 mg, 0.14 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 81 mg, 0.21 mmol) as well as diisopropyl ethylamine (0.10 mL,0.57 mmol) were added. After stirring for 30 min at 0 – 4 °C (ice bath), trans-3-(4-methoxyphenyl)cyclobutanamine (Int-195, 25 mg, 0.14 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 40:60 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a white solid (9.6 mg, 18% yield). MS m / z (ESI): 371.3 [M+H]+.1H NMR (400 MHz, CDCl3) δ ppm 8.14 (s, 1H), 7.71 - 7.63 (m, 1H), 7.21 (d, J = 8.4 Hz, 2H), 6.88 (d, J = 8.6 Hz, 2H), 6.56 (d, J = 9.4 Hz, 1H), 6.27 - 6.09 (m, 1H), 4.72 - 4.59 (m, 1H), 4.17 (t, J = 5.0 Hz, 2H), 3.81 (s, 3H), 3.73 (t, J = 5.0 Hz, 2H), 3.65 - 3.54 (m, 1H), 3.48 (q, J = 7.0 Hz, 2H), 2.68 - 2.56 (m, 2H), 2.50 - 2.38 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 58 1-(2-Ethoxyethyl)-6-oxo-N-[(3-phenyl-1-bicyclo[1.1.1]pentanyl)methyl]pyridine-3- carboxamide (58) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 73 mg, 0.35 mmol) was dissolved indimethylformamide (2 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 132 mg, 0.35 mmol) as well as diisopropyl ethylamine (0.25 mL, 1.44 mmol) were added. After stirring for 5 min at 0 – 4 °C (ice bath), (3-phenyl-1- bicyclo[1.1.1]pentanyl)methanamine (Int-33, 50 mg, 0.29 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 60:40 to 33:67 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a colorless oil (26 mg, 25% yield). MS m / z (ESI): 367.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.15 (s, 1H), 7.67 (d, J = 7.2 Hz, 1H), 7.35 – 7.18 (m, 5H), 6.58 (d, J = 9.3 Hz, 1H), 5.89 – 5.81 (m, 1H), 4.23 – 4.15 (m, 2H), 3.76 – 3.70 (m, 2H), 3.61 (d, J = 5.5 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 2.02 (s, 6H), 1.16 (t, J = 7.0 Hz, 3H). Example 59 and example 60 trans-1-(2-Ethoxyethyl)-6-oxo-N-[(3-phenylcyclobutyl)methyl]pyridine-3-carboxamide (59)and cis-1-(2-ethoxyethyl)-6-oxo-N-[(3-phenylcyclobutyl)methyl]pyridine-3-carboxamide(60) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 40 mg, 0.19 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 72 mg, 0.19 mmol) as well as diisopropyl ethylamine (0.16 mL, 0.95 mmol) were added. After stirring for 5 min at 0 – 4 °C (ice bath), (3- phenylcyclobutyl)methanamine (Int-36, 30 mg, 0.19 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 62:38 to 32:68 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OJ-H, 250 mm x 30 mm x 5 um, supercritical carbon dioxide / (methanol + 0.1% ammonia), isocratic 80:20 (v / v)). The product containing fractions were concentrated in vacuo to yield example 59 as second eluting stereoisomer as a white solid (6.4mg, 9% yield). MS m / z (ESI): 355.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J =2.6 Hz, 1H), 7.63 (dd, J = 2.5, 9.5 Hz, 1H), 7.35 – 7.29 (m, 2H), 7.26 – 7.18 (m, 3H), 6.57 (d, J = 9.6 Hz, 1H), 5.87 – 5.81 (m, 1H), 4.17 (t, J = 4.9 Hz, 2H), 3.72 (t, J = 4.9 Hz, 2H), 3.71 – 3.64 (m, 3H), 3.48 (q, J = 7.0 Hz, 2H), 2.61 – 2.51 ( m, 1H), 2.40 – 2.30 (m, 2H), 2.27 – 2.19 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 60 was obtained as first elutingstereoisomer as a white solid (15.2 mg, 21% yield). MS m / z (ESI): 355.2 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.10 (d, J = 2.4 Hz, 1H), 7.58 (dd, J = 2.6, 9.5 Hz, 1H), 7.34 – 7.25 (m, 2H), 7.22 – 7.17 (m, 3H), 6.55 (d, J = 9.5 Hz, 1H), 5.81 (br s, 1H), 4.16 (t, J = 4.9 Hz, 2H), 3.72 (t, J = 4.9 Hz, 2H), 3.51 – 3.39 (m, 5H), 3.48 (q, J = 7.0 Hz, 2H), 2.61 – 2.49 ( m, 3H), 1.94 – 1.84 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 61 and example 62 trans-1-(2-Ethoxyethyl)-6-oxo-N-(3-thiazol-2-ylcyclobutyl)pyridine-3-carboxamide (61) and cis-1-(2-ethoxyethyl)-6-oxo-N-(3-thiazol-2-ylcyclobutyl)pyridine-3-carboxamide (62) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 80 mg, 0.38 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 107 mg, 0.45 mmol) as well as diisopropyl ethylamine (147 mg, 1.14 mmol) were added. After stirring for 30 min at 0 – 4 °C (ice bath), 3-thiazol-2- ylcyclobutanamine (Int-54, 88 mg, 0.57 mmol) was added at 20 °C and the resulting mixture was stirred at 20 °C for 30 min. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.225% formic acid) / acetonitrile, gradient 40:60 to 10:90 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture (ca.65 mg). The mixture was separated into its diastereoisomers by preparative chiral SFC (Daicel Chiralcel OX-3, 50 mm x 4.6 mm x 3 um, supercritical carbon dioxide / (2-propanol + 0.05% diethylamine), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 61 as second eluting stereoisomer as a brown oil (18 mg, 14% yield). MS m / z (ESI): 347.9 [M+H]+. Analogously, example 62 was obtained as first eluting stereoisomer as a brown oil (35 mg, 26% yield). MS m / z (ESI): 347.9 [M+H]+. Example 63 cis-1-(2-Ethoxyethyl)-N-(3-hydroxy-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide (63) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 85 mg, 0.40 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 228 mg, 0.60 mmol) as well as diisopropyl ethylamine (0.35 mL, 2.00 mmol) were added. After stirring for 30 min at 0 – 4 °C (ice bath), cis-3-amino-1-phenyl- cyclobutanol hydrochloride (Int-196, 80 mg, 0.40 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 83:17 to 53:47 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compound as a white solid (57 mg, 40% yield). MS m / z (ESI): 357.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.15 (d, J = 2.3 Hz, 1H), 7.70 (dd, J = 2.5, 9.4 Hz, 1H), 7.53 – 7.49 (m, 2H), 7.44 – 7.38 (m, 2H), 7.35 – 7.30 (m, 1H), 6.58 (d, J = 9.5 Hz, 1H), 6.51 (d, J = 7.5 Hz, 1H), 4.39 – 4.29 (m, 1H), 4.18 (t, J = 4.9 Hz, 2H), 3.72 (t, J = 4.9 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 3.17 – 3.09 (m, 2H), 2.50 – 2.43 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 64 and example 65 trans-1-(2-Ethoxyethyl)-N-[3-(1-methylpyrazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (64) and cis-1-(2-ethoxyethyl)-N-[3-(1-methylpyrazol-4-yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide (65) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 102 mg, 0.48 mmol) was dissolvedin dimethylformamide (3 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 277 mg, 0.73 mmol) as well as diisopropyl ethylamine (218 mg, 1.68 mmol) were added. After stirring for 5 min at 25 °C, 3-(1-methylpyrazol-4- yl)cyclobutanamine hydrobromide (Int-59, 130 mg, 0.56 mmol) was added and the resulting mixture was stirred at 25 °C for 25 min. Then, it was concentrated in vacuo. The residue, a white solid, was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 88:12 to 58:42 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture (80 mg). The mixture was separated into its diastereoisomers by preparative chiral SFC (Daicel Chiralpak AD-H, 250 mm x 30 mm x 5 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 80:20 (v / v)). The product containing fractions were concentrated in vacuo to yield example 64 as second eluting stereoisomer as a light brown gum (38 mg, 23% yield). MS m / z(ESI): 345.4 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.12 (d, J = 2.4 Hz, 1H), 7.64 (dd, J= 9.5, 2.6 Hz, 1H), 7.39 (s, 1H), 7.27 – 7.26 (m, 1H), 6.55 (d, J = 9.5 Hz, 1H), 6.14 (br d, J = 7.1 Hz, 1H), 4.71 (sxt, J = 7.5 Hz, 1H), 4.16 (t, J = 5.0 Hz, 2H), 3.89 (s, 3H), 3.72 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.45 – 3.38 (m, 1H), 2.53 – 2.35 (m, 4H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 65 was obtained as first eluting stereoisomer as a grey solid (11 mg, 6%yield). MS m / z (ESI): 345.4 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.12 (d, J = 2.6 Hz,1H), 7.63 (dd, J = 9.5, 2.6 Hz, 1H), 7.37 (s, 1H), 7.18 (s, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.05 (br s, 1H), 4.55 – 4.43 (m, 1H), 4.16 (t, J = 5.0 Hz, 2H), 3.87 (s, 3H), 3.72 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.17 – 3.06 (m, 1H), 2.89 – 2.80 (m, 2H), 1.99 – 1.89 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 66 and example 67 trans-1-(2-Ethoxyethyl)-6-oxo-N-[3-(2,2,2-trifluoroethyl)cyclobutyl]pyridine-3-carboxamide (66) and cis 1-(2-ethoxyethyl)-6-oxo-N-[3-(2,2,2-trifluoroethyl)cyclobutyl]pyridine-3-carboxamide (67) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 67 mg, 0.32 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 180 mg, 0.47 mmol) as well as diisopropyl ethylamine (0.22 mL, 1.27 mmol) were added. After stirring for 30 min at 0 – 4 °C (ice bath), 3-(2,2,2- trifluoroethyl)cyclobutanamine hydrochloride (Int-197, 60 mg, 0.32 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 40:60 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture (82 mg). The mixture was separated into its diastereoisomers by preparative chiral SFC (Daicel Chiralpak IG, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (methanol + 0.1% ammonia), isocratic 80:20 (v / v)). The product containing fractions were concentrated in vacuo to yield example 66 as second eluting stereoisomer as a brown oil (24.5 mg, 22% yield). MS m / z (ESI): 347.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.11 (d, J = 2.5 Hz, 1H), 7.63 (dd, J = 2.6, 9.5 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.07 (br d, J = 6.4 Hz, 1H), 4.65 - 4.54 (m, 1H), 4.16 (t, J = 4.9 Hz, 2H), 3.72 (t, J = 4.8 Hz, 2H), 3.48 (q, J = 6.9 Hz, 2H), 2.74 - 2.59 (m, 1H), 2.40 - 2.29 (m, 4H), 2.29 - 2.18 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 67 was obtained as firsteluting stereoisomer as a brown oil (43 mg, 39% yield). MS m / z (ESI): 347.2 [M+H]+. 1H NMR(400 MHz, CDCl3): δ ppm 8.10 (d, J = 2.5 Hz, 1H), 7.61 (dd, J = 2.6, 9.5 Hz, 1H), 6.54 (d, J = 9.5 Hz, 1H), 6.04 (d, J = 7.1 Hz, 1H), 4.49 - 4.37 (m, 1H), 4.15 (t, J = 5.0 Hz, 2H), 3.72 (t, J = 5.0 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 2.73 - 2.65 (m, 2H), 2.40 - 2.28 (m, 1H), 2.28 – 2.16 (m, 2H), 1.78 – 1.68 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 68 and example 69 trans-1-(2-Ethoxyethyl)-6-oxo-N-[3-(trifluoromethyl)cyclobutyl]pyridine-3-carboxamide(68) and cis-1-(2-ethoxyethyl)-6-oxo-N-[3-(trifluoromethyl)cyclobutyl]pyridine-3-carboxamide (69) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 65 mg, 0.31 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 175 mg, 0.46 mmol) as well as diisopropyl ethylamine (200 mg, 1.54 mmol) were added. After stirring for 20 min at 0 – 4 °C (ice bath), 3- (trifluoromethyl)cyclobutanamine hydrochloride (Int-198, 54 mg, 0.31 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, it was concentrated in vacuo. The residue was purified by preparative HPLC (Waters Xbridge, 150 x 25 mm x 5 um, (water + 0.1% ammonia) / acetonitrile, gradient 94:6 to 64:36 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative chiral SFC (Daicel Chiralcel OD-H, 250 mm x 30 mm x 5 um, supercritical carbon dioxide / (2-propanol + 0.1% ammonia), isocratic 70:30 (v / v)). The product containing fractions were concentrated in vacuo to yield example 68 as second elutingstereoisomer as a colorless oil (13 mg, 13% yield). MS m / z (ESI): 333.1 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.12 (d, J = 2.6 Hz, 1H), 7.61 (dd, J = 2.5, 9.5 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.02 (br s, 1H), 4.72 – 4.60 (m, 1H), 4.16 (t, J = 5.0 Hz, 2H), 3.72 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.01 – 2.88 (m, 1H), 2.73 – 2.64 (m, 2H), 2.39 – 2.28 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 69 was obtained as first eluting stereoisomer as a colorlessoil (44 mg, 43% yield). MS m / z (ESI): 333.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.12(d, J = 2.5 Hz, 1H), 7.64 (dd, J = 2.7, 9.5 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.08 (br s, 1H), 4.63 – 4.50 (m, 1H), 4.16 (t, J = 5.0 Hz, 2H), 3.72 (t, J = 5.0 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 2.80 – 2.62 (m, 3H), 2.17 – 2.02 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 70 and example 71 trans-1-(2-Ethoxyethyl)-6-oxo-N-[3-(3-pyridyl)cyclobutyl]pyridine-3-carboxamide (70) and cis-1-(2-ethoxyethyl)-6-oxo-N-[3-(3-pyridyl)cyclobutyl]pyridine-3-carboxamide (71)1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 70 mg, 0.33 mmol) was dissolved indimethylformamide (0.5 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 93 mg, 0.40 mmol) as well as diisopropyl ethylamine (128 mg, 0.99 mmol) were added. After stirring for 30 min at 0 – 4 °C (ice bath), 3-(3- pyridyl)cyclobutanamine (Int-62, 74 mg, 0.50 mmol) was added at 20 °C and the resulting mixture was stirred at 20 °C for 30 min. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.225% formic acid) / acetonitrile, gradient 40:60 to 10:90 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a brown oil (90 mg). The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak IF-3, 50 mm x 4.6 mm x 3 um, supercritical carbon dioxide / (ethanol + 0.05% diethylamine), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 70 as first eluting stereoisomer as a brown oil (35 mg, 31% yield). MS m / z (ESI): 342.1 [M+H]+. Analogously, example 71 was obtained as second eluting stereoisomer as a brown oil (15 mg, 13% yield). MS m / z (ESI): 342.1 [M+H]+. Example 72 and example 73 trans-1-(2-Ethoxyethyl)-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3-carboxamide (72) and cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3-carboxamide (73) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 33 mg, 0.16 mmol) was dissolved indimethylformamide (2 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 90 mg, 0.24 mmol) as well as diisopropyl ethylamine (0.11 mL, 0.62 mmol) were added. After stirring for 5 min at 25 °C, 3-[6-(trifluoromethyl)-2-pyridyl]- cyclobutanamine 2,2,2-trifluoroacetate salt (Int-16, 58 mg, 0.16 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a green oil. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralcel OD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (2-propanol + 0.1% ammonia), isocratic 70:30 (v / v)). The product containing fractions were concentrated in vacuo to yield example 72 as second eluting stereoisomer as a light green oil (14 mg, 21% yield). MS m / z(ESI): 410.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J = 2.5 Hz, 1H), 7.81 (dd, J= 7.7, 7.8 Hz, 1H), 7.65 (dd, J = 2.6, 9.4 Hz, 1H), 7.54 (d, J = 7.5 Hz, 1H), 7.42 (d, J = 8.0 Hz, 1H), 6.57 (d, J = 9.4 Hz, 1H), 6.14 – 6.07 (m, 1H), 4.82 – 4.71 (m, 1H), 4.17 (t, J = 5.0 Hz, 2H), 3.82 – 3.70 (m, 3H), 3.48 (q, J = 7.0 Hz, 2H), 2.90 – 2.80 (m, 2H), 2.57 – 2.47 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 73 was obtained as first eluting stereoisomer as a lightgreen oil (7 mg, 11% yield). MS m / z (ESI): 410.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm8.14 (d, J = 2.5 Hz, 1H), 7.78 (dd, J = 7.5, 7.7 Hz, 1H), 7.71 (dd, J = 2.6, 9.4 Hz, 1H), 7.55 (d, J = 7.8 Hz, 1H), 7.33 (d, J = 7.7 Hz, 1H), 6.73 – 6.67 (m, 1H), 6.58 (d, J = 9.5 Hz, 1H), 4.76 – 4.66 (m, 1H), 4.18 (t, J = 5.0 Hz, 2H), 3.73 (t, J = 5.0 Hz, 2H), 3.52 – 3.41 (m, 3H), 2.99 – 2.89 (m, 2H), 2.39 – 2.29 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). Example 74 and example 75 trans-1-(2-Ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3-carboxamide (74) and cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3-carboxamide (75) 1-(2-Ethoxyethyl)--6-oxo-pyridine-3-carboxylic acid (Int-4, 48 mg, 0.23 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 86 mg, 0.23 mmol) as well as diisopropyl ethylamine (0.14 mL, 0.82 mmol) were added. After stirring for 10 min at 25 °C, 3-[2-(trifluoromethyl)-3-pyridyl]- cyclobutanamine 2,2,2-trifluoroacetate salt (Int-17, 68 mg, 0.21 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 72:28 to 42:58 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to give the title compounds as mixture as a light green oil. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak IK, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 74 as first eluting stereoisomeras a light yellow gum (9 mg, 10% yield). MS m / z (ESI): 410.2 [M+H]+. 1H NMR (400 MHz,CDCl3): δ ppm 8.66 - 8.48 (m, 1H), 8.26 - 8.13 (m, 1H), 8.11 - 7.97 (m, 1H), 7.80 - 7.67 (m, 1H), 7.61 - 7.47 (m, 1H), 6.67 - 6.39 (m, 2H), 4.78 - 4.61 (m, 1H), 4.25 - 4.11 (m, 2H), 4.12 - 3.96 (m, 1H), 3.81 - 3.61 (m, 2H), 3.54 - 3.40 (m, 2H), 2.76 - 2.60 (m, 2H), 2.59 - 2.47 (m, 2H), 1.20 - 1.08 (m, 3H). Analogously, example 75 was obtained as second eluting stereoisomer as alight green oil (6 mg, 7% yield). MS m / z (ESI): 410.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δppm 8.65 - 8.48 (m, 1H), 8.20 - 8.08 (m, 1H), 7.95 - 7.83 (m, 1H), 7.69 - 7.57 (m, 1H), 7.54 - 7.45 (m, 1H), 6.59 - 6.48 (m, 1H), 6.29 - 6.13 (m, 1H), 4.61 - 4.44 (m, 1H), 4.18 - 4.07 (m, 2H), 3.77 - 3.69 (m, 2H), 3.67 - 3.56 (m, 1H), 3.54 - 3.40 (m, 2H), 3.01 - 2.87 (m, 2H), 2.32 - 2.11 (m, 2H), 1.20 - 1.05 (m, 3H). Example 76 and example 77 trans-1-(2-Ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-7-ylcyclobutyl)pyridine-3-carboxamide (76) and cis-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-7-ylcyclobutyl)pyridine-3-carboxamide (77) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 42 mg, 0.20 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 76 mg, 0.20 mmol) as well as diisopropyl ethylamine (0.14 mL, 0.83 mmol) were added. After stirring for 10 min at 25 °C, 3-pyrazolo[1,5-a]pyridin-7- ylcyclobutanamine 2,2,2-trifluoroacetate salt (Int-28, 50 mg, 0.17 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 42:58 to 10:90 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak AY-H, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 70:30 (v / v)). The product containing fractions were concentrated in vacuo to yield example 76 as first eluting stereoisomer as a light brownsolid (24 mg, 38% yield). MS m / z (ESI): 381.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm8.15 (d, J = 2.6 Hz, 1H), 7.98 (d, J = 2.2 Hz, 1H), 7.69 (dd, J = 9.5, 2.6 Hz, 1H), 7.52 (d, J = 8.7 Hz, 1H), 7.18 (dd, J = 8.7, 7.0 Hz, 1H), 6.83 (d, J = 7.0 Hz, 1H), 6.60 – 6.56 (m, 2H), 6.28 (br d, J = 7.0 Hz, 1H), 4.73 – 4.62 (m, 1H), 4.37 – 4.28 (m, 1H), 4.18 (t, J = 5.0 Hz, 2H), 3.74 (t, J = 5.0 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 2.80 – 2.72 (m, 2H), 2.68 – 2.59 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 77 was obtained as second eluting stereoisomer as a light brownsolid (13 mg, 20% yield). MS m / z (ESI): 381.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm8.15 (d, J = 2.4 Hz, 1H), 8.02 (d, J = 2.2 Hz, 1H), 7.67 (dd, J = 2.6, 9.5 Hz, 1H), 7.50 (d, J = 8.3 Hz, 1H), 7.12 (dd, J = 7.0, 8.8 Hz, 1H), 6.65 – 6.51 (m, 4H), 4.81 – 4.69 (m, 1H), 4.17 (t, J = 4.9 Hz, 2H), 3.95 – 3.84 (m, 1H), 3.73 (t, J = 4.9 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.15 – 3.05 (m, 2H), 2.45 – 2.35 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 78 and example 79 trans-1-(2-Ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3-carboxamide (78) and cis-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3-carboxamide (79) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 42 mg, 0.20 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 76 mg, 0.20 mmol) as well as diisopropyl ethylamine (0.14 mL, 0.83 mmol) were added. After stirring for 10 min at 25 °C, 3-imidazo[1,2-a]pyridin-5- ylcyclobutanamine 2,2,2-trifluoroacetate salt (Int-29, 50 mg, 0.17 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Waters Xbridge, 150 x 25 mm x 10 um, (water + 0.1% ammonia) / acetonitrile, gradient 80:20 to 60:40 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak IG, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 50:50 (v / v)). The product containing fractions were concentrated in vacuo to obtain example 78 as second eluting stereoisomer as a light green gum(15 mg, 23% yield). MS m / z (ESI): 381.3 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.16 (d,J = 2.4 Hz, 1H), 8.12 (s, 1H), 7.72 – 7.66 (m, 2H), 7.39 – 7.32 (m, 2H), 6.58 (d, J = 9.5 Hz, 1H), 6.30 (br d, J = 6.4 Hz, 1H), 4.79 (sxt, J = 6.9 Hz, 1H), 4.18 (t, J = 4.9 Hz, 2H), 4.06 – 3.95 (m, 1H), 3.74 (t, J = 4.9 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 2.90 – 2.81 (m, 2H), 2.64 – 2.54 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 79 was obtained as first eluting stereoisomer as alight green gum (8 mg, 13% yield). MS m / z (ESI): 381.3 [M+H]+. 1H NMR (400 MHz, CDCl3):δ ppm 8.23 (d, J = 2.5 Hz, 1H), 7.73 (dd, J = 9.6, 2.6 Hz, 1H), 7.68 (s, 1H), 7.55 (br d, J = 8.9 Hz, 1H), 7.41 (s, 1H), 7.24 – 7.18 (m, 1H), 6.66 (br d, J = 6.9 Hz, 1H), 6.61 (d, J = 6.9 Hz, 1H), 6.52 (d, J = 9.5 Hz, 1H), 4.75 (sxt, J = 8.2 Hz, 1H), 4.15 (t, J = 4.9 Hz, 2H), 3.71 (t, J = 4.9 Hz, 2H), 3.49 – 3.43 (m, 3H), 3.12 – 3.03 (m, 2H), 2.16 – 2.06 (m, 2H), 1.14 (t, J = 7.0 Hz, 3H). Example 80 and example 81 trans-1-(2-Ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-4-ylcyclobutyl)pyridine-3-carboxamide (80) and cis-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-4-ylcyclobutyl)pyridine-3-carboxamide (81) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 59 mg, 0.28 mmol) was dissolved indimethylformamide (1 mL) and hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 106 mg, 0.28 mmol) as well as diisopropyl ethylamine (0.20 mL, 1.16 mmol) were added. After stirring for 10 min at 25 °C, 3-pyrazolo[1,5-a]pyridin-4- ylcyclobutanamine 2,2,2-trifluoroacetate salt (Int-30, 70 mg, 0.23 mmol) was added at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 79:21 to 49:51 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its diastereoisomers by preparative SFC (Daicel Chiralpak AY-H, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 70:30 (v / v)). The product containing fractions were concentrated in vacuo to yield example 80 as second eluting stereoisomer as a light greengum (21 mg, 24% yield). MS m / z (ESI): 381.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm8.43 (d, J = 6.8 Hz, 1H), 8.15 (d, J = 2.6 Hz, 1H), 7.95 (d, J = 2.2 Hz, 1H), 7.68 (dd, J = 9.5, 2.6 Hz, 1H), 7.10 (d, J = 7.0 Hz, 1H), 6.81 (t, J = 6.9 Hz, 1H), 6.58 (d, J = 9.4 Hz, 1H), 6.41 (dd, J = 2.3, 0.6 Hz, 1H), 6.20 (br d, J = 6.6 Hz, 1H), 4.71 – 4.60 (m, 1H), 4.18 (t, J = 5.0 Hz, 2H), 3.89 – 3.80 (m, 1H), 3.74 (t, J = 5.0 Hz, 2H), 3.49 (q, J = 7.0 Hz, 2H), 2.82 – 2.72 (m, 2H), 2.60 – 2.51 (m, 2H), 1.17 (t, J = 7.0 Hz, 3H). Analogously, example 81 was obtained as first elutingstereoisomer as a grey solid (9 mg, 10% yield). MS m / z (ESI): 381.2 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.38 (d, J = 6.6 Hz, 1H), 8.12 (d, J = 2.6 Hz, 1H), 7.95 (d, J = 2.3 Hz, 1H), 7.61 (dd, J = 9.5, 2.6 Hz, 1H), 6.88 (d, J = 7.0 Hz, 1H), 6.75 (t, J = 6.8 Hz, 1H), 6.54 (d, J = 9.5 Hz, 1H), 6.46 (dd, J = 2.2, 0.7 Hz, 1H), 5.97 (br d, J = 6.8 Hz, 1H), 4.74 – 4.62 (m, 1H), 4.16 (t, J = 5.0 Hz, 2H), 3.72 (t, J = 5.3 Hz, 2H), 3.55 – 3.50 (m, 1H), 3.47 (q, J = 7.0 Hz, 2H), 3.07 – 2.99 (m, 2H), 2.20 – 2.10 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H). Example 82 trans-6-Oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-morpholin-2-yl]methyl]pyridine-3- carboxamide (82) Step 1: tert-Butyl (2R)-2-[[2-oxo-5-[(trans-3-phenylcyclobutyl)carbamoyl]-1-pyridyl]methyl]morpholine-4-carboxylate (Int-199) tert-Butyl (2R)-2-[(5-methoxycarbonyl-2-oxo-1-pyridyl)methyl]morpholine-4-carboxylate (Int- 98, 105 mg, 0.30 mmol) was dissolved in methanol (0.5 mL) and water (1 mL), and sodium hydroxide (14 mg, 0.35 mmol) was added. The mixture was stirred at 80 °C for 30 min. After cooling, it was concentrated in vacuo. The residue was dissolved in dimethylformamide (2 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 126 mg, 0.33 mmol) as well as diisopropyl ethylamine (0.21 mL, 1.18 mmol) were added. Afterstirring for 10 min at 25 °C, trans-3-phenylcyclobutanamine (Int-178, 45.5 mg, 0.31 mmol) wasadded at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 57:43 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (100 mg, 0.21 mmol, 71% yield). MS m / z (ESI): 468.2 [M+H]+.Step 2: trans-6-Oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-morpholin-2-yl]methyl]pyridine-3-carboxamide (82) tert-Butyl (2R)-2-[[2-oxo-5-[(trans-3-phenylcyclobutyl)carbamoyl]-1- pyridyl]methyl]morpholine-4-carboxylate (Int-199, 90 mg, 0.19 mmol) was dissolved in 1,4- dioxane (1 mL) and a solution of hydrogen chloride in dioxane (ca.4 M, 3 mL, 1.20 mmol) was added. The mixture reaction was stirred at 25 °C for 5 h. After that, it was concentrated and was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a yellow solid (53 mg, 0.14mmol, 76% yield). MS m / z (ESI): 368.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.09 (d, J= 2.3 Hz, 1H), 7.66 (dd, J = 2.5, 9.5 Hz, 1H), 7.38 - 7.28 (m, 4H), 7.26 - 7.19 (m, 1H), 6.57 (d, J = 9.5 Hz, 1H), 6.15 (br d, J = 6.5 Hz, 1H), 4.73 - 4.62 (m, 1H), 4.36 - 4.30 (m, 1H), 3.90 - 3.76 (m, 2H), 3.72 - 3.60 (m, 2H), 3.57 - 3.46 (m, 1H), 3.04 (br d, J = 11.9 Hz, 1H), 2.90 - 2.77 (m, 2H), 2.71 - 2.63 (m, 2H), 2.63 - 2.54 (m, 1H), 2.53 - 2.42 (m, 2H). In analogy to the procedure described for the preparation of example 82, the following examples were prepared using the respective starting materials SM: Ex.-Structure Name SM 1H NMR (400 MHz,m / z No. CDCl3) (ESI) δ ppmtrans-6-oxo-N-Int- 8.10 (d, J = 2.6 Hz, 1H), 368.2 (3- 99 7.67 (dd, J = 9.5, 2.6 Hz, [M+H]+phenylcyclobut 1H), 7.38 – 7.28 (m, 4H), yl)-1-[[(2R)- 7.25 – 7.20 (m, 1H), 6.57 (d, morpholin-2- J = 9.4 Hz, 1H), 6.22 (br d, J yl]methyl]pyri = 6.6 Hz, 1H), 4.72 – 4.62 dine-3- (m, 1H), 4.32 (dd, J = 13.3, carboxamide 2.7 Hz, 1H), 3.90 – 3.77 (m, 2H), 3.72 – 3.61 (m, 2H), 3.57 – 3.48 (m, 1H), 3.05 (dd, J = 12.3, 1.7 Hz, 1H), 2.90 – 2.79 (m, 2H), 2.71 – 2.63 (m, 2H), 2.59 (dd, J = 12.1, 10.4 Hz, 1H), 2.53 – 2.44 (m, 2H).trans-6-oxo-N-Int- 8.16 (d, J = 2.4 Hz, 1H), 366.3 (3- 100 7.65 (dd, J = 9.5, 2.6 Hz, [M+H]+phenylcyclobut 1H), 7.37 – 7.28 (m, 4H), yl)-1-[[(3S)-3- 7.25 – 7.20 (m, 1H), 6.55 (d, piperidyl]- J = 9.5 Hz, 1H), 6.51 (br d, J methyl]- = 6.1 Hz, 1H), 4.71 – 4.61 pyridine-3- (m, 1H), 4.02 (dd, J = 13.0, carboxamide 8.4 Hz, 1H), 3.85 (dd, J = 13.1, 6.3 Hz, 1H), 3.71 – 3.61 (m, 1H), 3.06 – 2.96 (m, 2H), 2.76 – 2.61 (m, 3H), 2.56 – 2.47 (m, 3H), 2.25 – 2.12 (m, 1H), 1.78 - 1.63 (m, 2H), 1.59 – 1.49 (m, 1H), 1.38 – 1.29 (m, 1H).trans-6-oxo-N-Int- 8.13 (d, J = 2.3 Hz, 1H), 366.3 (3- 101 7.65 (dd, J = 9.5, 2.6 Hz, [M+H]+phenylcyclo- 1H), 7.38 –7.20 (m, 5H), butyl)-1- 6.55 (d, J = 9.4 Hz, 2H), [[(3R)-3- 4.71 – 4.61 (m, 1H), 4.01 piperidyl]- (dd, J = 13.1, 8.4 Hz, 1H), methyl]- 3.84 (dd, J = 13.1, 6.4 Hz, pyridine-3- 1H), 3.71 – 3.62 (m, 1H), carboxamide 3.05 – 2.96 (m, 2H), 2.73 – 2.61 (m, 3H), 2.56 – 2.45 (m, 3H), 2.22 – 2.08 (m, 1H), 1.85 – 1.70 (m, 2H), 1.59 – 1.46 (m, 1H), 1.37 – 1.25 (m, 1H).trans-6-oxo-N-Int- 8.06 (d, J = 2.4 Hz, 1H), 368.3 (3- 102 7.65 (dd, J = 9.5, 2.6 Hz, [M+H]+phenylcyclo- 1H), 7.38 – 7.28 (m, 4H), butyl)-1- 7.26 – 7.20 (m, 1H), 6.58 (d, [[(3R)- J = 9.5 Hz, 1H), 6.24 (br d, J morpholin-3- = 6.6 Hz, 1H), 4.66 (sxt, J = yl]methyl]pyri 7.0 Hz, 1H), 4.04 (dd, J = dine-3- 13.3, 4.7 Hz, 1H), 3.90 – carboxamide 3.83 (m, 2H), 3.77 (dt, J = 11.3, 3.1 Hz, 1H), 3.71 – 3.61 (m, 1H), 3.58 – 3.50 (m, 1H), 3.37 – 3.29 (m, 1H), 3.31 – 3.25 (m, 1H), 2.98 – 2.84 (m, 2H), 2.73 – 2.63 (m, 2H), 2.53 – 2.43 (m, 2H).87 trans-6-oxo-N-Int- 8.21 (br s, 1H), 7.69 (dd, J = 368.3 (3- 103 9.5, 2.3 Hz, 1H), 7.37 – 7.28 [M+H]+phenylcyclo- (m, 4H), 7.25 – 7.21 (m, butyl)-1- 1H), 6.77 (br s, 1H), 6.56 (d, [[(3S)- J = 9.5 Hz, 1H), 4.64 – 4.52 morpholin-3- (m, 1H), 4.16 – 4.08 (m, yl]methyl]pyri 1H), 3.98 – 3.89 (m, 2H), dine-3- 3.87 – 3.80 (m, 1H), 3.71 – carboxamide 3.60 (m, 2H), 3.48 – 3.41 (m, 2H), 3.09 – 3.02 (m, 1H), 3.00 – 2.91 (m, 1H), 2.69 – 2.59 (m, 2H), 2.55 – 2.44 (m, 2H). Example 88 trans-6-Oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-4-methylmorpholin-2-yl]methyl]pyridine-3- carboxamide formiate salt (88) trans-6-Oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-morpholin-2-yl]methyl]pyridine-3-carboxamide (82, 35 mg, 0.10 mmol) was dissolved in methanol (1 mL), acetic acid (0.01 mL, 0.10 mmol) and paraformaldehyde (11 mg, 0.38 mmol) were added and the mixture was stirred for 0.5 h at 45 °C. Then, sodium triacetoxyborohydride (101 mg, 0.48 mmol) was added and it was stirred for 0.5 h at 45 °C. After cooling, the mixture was filtered and the filtrate concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 70:30 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a white solid (19 mg,0.05 mmol, 47% yield). MS m / z (ESI): 382.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.08 (d, J = 2.4 Hz, 1H), 7.68 (dd, J = 2.6, 9.6 Hz, 1H), 7.38 - 7.28 (m, 4H), 7.26 - 7.19 (m, 1H), 6.57 (d, J = 9.5 Hz, 1H), 6.54 - 6.46 (m, 1H), 4.72 - 4.61 (m, 1H), 4.33 (dd, J = 3.8, 13.5 Hz, 1H), 4.05 - 3.97 (m, 1H), 3.94 - 3.80 (m, 2H), 3.73 - 3.61 (m, 2H), 2.94 (br d, J = 11.1 Hz, 1H), 2.76 (br d, J = 11.8 Hz, 1H), 2.71 - 2.62 (m, 2H), 2.54 - 2.44 (m, 2H), 2.36 (s, 3H), 2.27 - 2.18 (m, 1H), 1.97 (t, J = 10.9 Hz, 1H). Example 89 trans-1-(2-Acetamidoethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (89) Step 1: tert-Butyl N-[2-[2-oxo-5-[(3-phenylcyclobutyl)carbamoyl]-1-pyridyl]ethyl]carbamate(Int-200) Methyl 1-[2-(tert-butoxycarbonylamino)ethyl]-6-oxo-pyridine-3-carboxylate (Int-104, 150 mg, 0.51 mmol) was dissolved in methanol (0.6 mL) and water (1.5 mL), and sodium hydroxide (24 mg, 0.61 mmol) was added. The mixture was stirred at 80 °C for 30 min. After cooling, it was concentrated in vacuo. The residue was dissolved in dimethylformamide (1 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 206 mg, 0.54 mmol) as well as diisopropyl ethylamine (0.34 mL, 1.97 mmol) were added. Afterstirring for 10 min at 25 °C, trans-3-phenylcyclobutanamine (Int-178, 73 mg, 0.49 mmol) wasadded at 25 °C and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 64:36 to 34:66 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a light brown solid (80 mg, 0.19 mmol, 40% yield). MS m / z (ESI): 412.2 [M+H]+.Step 2: trans-1-(2-Aminoethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (Int-201)tert-Butyl N-[2-[2-oxo-5-[(3-phenylcyclobutyl)carbamoyl]-1-pyridyl]ethyl]carbamate (Int-200,40 mg, 0.10 mmol) was dissolved in 1,4-dioxane (2 mL) and a solution of hydrogen chloride in dioxane (ca.4 M, 4 mL, 1.60 mmol) was added. The mixture reaction was stirred at 25 °C for 2 h. After that, it was concentrated, the residue was redissolved in methanol (5 mL) and ion exchange resin amberlyst® A21 (500 mg) was added. The mixture was stirred at 25 °C for 1 h, filtered, and the filtrate was concentrated in vacuo to afford the title compound as a light brown oil (32 mg, quant. yield). MS m / z (ESI): 312.2 [M+H]+. Step 3: trans-1-(2-Acetamidoethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (89) trans-1-(2-Aminoethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (Int-201, 32 mg, 0.10 mmol) was dissolved in dichloromethane (1 mL), and triethylamine (0.07 mL, 0.47 mmol) followed by acetic anhydride (13 mg, 0.12 mmol) were added dropwise. The mixture was stirred at 25 °C for 2 h. After that, it was concentrated in vacuo and the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 78:22 to 48:52 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a white solid (20 mg, 0.06 mmol, 54% yield). MS m / z (ESI): 354.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.08 (d, J = 2.5 Hz, 1H), 7.74 (dd, J = 2.5, 9.5 Hz, 1H), 7.38 – 7.20 (m, 5H), 6.57 (d, J = 9.5 Hz, 2H), 6.43 – 6.37 (m, 1H), 4.71 – 4.61 (m, 1H), 4.17 (t, J = 5.9 Hz, 2H), 3.70 – 3.61 (m, 3H), 2.71 – 2.62 (m, 2H), 2.54 – 2.44 (m, 2H), 1.98 (s, 3H). Example 90 trans-1-[1-(Hydroxymethyl)cyclopropyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3- carboxamide (90) Methyl 1-[1-(hydroxymethyl)cyclopropyl]-6-oxo-pyridine-3-carboxylate (Int-136, 37.5 mg, 0.13 mmol) was dissolved in methanol (1 mL), and sodium hydroxide (5.4 mg, 0.13 mmol) was added. The mixture was stirred at 60 °C for 6 h. After cooling, it was concentrated in vacuo. Theresidue was dissolved in dimethylformamide (1 mL), trans-3-phenylcyclobutanamine (Int-178, 21 mg, 0.14 mmol), diisopropyl ethylamine (0.12 mL, 0.72 mmol), and 2,4,6-tributyl- 1,3,5,2λ⁵,4λ⁵,6λ⁵-trioxatriphosphinane 2,4,6-trioxide (T4P, CAS [163755-62-2], 50% m / m in dimethylacetamide, 206 mg, 0.29 mmol) were added. The resulting mixture was stirred at 25 °C for 1.5 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 72:28 to 52:48 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as acolorless oil (2 mg, 0.01 mmol, 4% yield). MS m / z (ESI): 339.1 [M+H]+. 1H NMR (400 MHz,CDCl3): δ ppm 8.18 (d, J = 2.5 Hz, 1H), 7.62 (dd, J = 2.6, 9.5 Hz, 1H), 7.38 – 7.21 (m, 5H), 6.57 (d, J = 9.5 Hz, 1H), 6.20 (d, J = 6.5 Hz, 1H), 4.73 – 4.61 (m, 1H), 3.81 (s, 2H), 3.71 – 3.61 (m, 1H), 2.73 – 2.62 (m, 2H), 2.54 – 2.44 (m, 2H), 2.08 – 1.98 (m, 1H), 1.38 – 1.23 (m, 4H). Example 91 trans-5-Chloro-6-oxo-N-(3-phenylcyclobutyl)-1-thiazol-2-yl-pyridine-3-carboxamide (91) Step 1: 5-Chloro-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylic acid (Int-202) Methyl 5-chloro-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylate (Int-141, 98 mg, 0.36 mmol) was dissolved in tetrahydrofuran (1 mL) and water (0.5 mL), and sodium hydroxide (4 M in water, 0.18 mL, 0.72 mmol) was added. The mixture solution was stirred at 34 °C for 16 h. After that, the pH was adjusted to pH 5 by addition of hydrochloric acid (1 M in water), and the mixture was extracted with ethyl acetate (3 x 10 mL). The combined organic layers were dried over sodium sulfate, filtered, and the filtrate was concentrated in vacuo to obtain the title compound as a brown solid (57 mg, 0.22 mmol, 62% yield). MS m / z (ESI): 254.8 [M–H]–.Step 2: trans-5-Chloro-6-oxo-N-(3-phenylcyclobutyl)-1-thiazol-2-yl-pyridine-3-carboxamide(91) 5-Chloro-6-oxo-1-thiazol-2-yl-pyridine-3-carboxylic acid (Int-202, 57 mg, 0.22 mmol) was dissolved in dimethylformamide (2 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 125 mg, 0.33 mmol) as well as diisopropyl ethylamine(0.08 mL, 0.44 mmol) were added. After stirring for 5 min at 20 °C, trans-3- phenylcyclobutanamine (Int-178, 33 mg, 0.22 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, the reaction mixture was concentrated and purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 58:42 to 28:72 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a white solid (31 mg, 0.08 mmol, 36% yield). MS m / z (ESI): 386.1 [M+H]+.1H NMR (400 MHz, d6-DMSO): δ ppm 9.41 (d, J = 2.2 Hz, 1H), 9.03 (d, J = 6.7 Hz, 1H), 8.43 (d, J = 2.3 Hz, 1H), 7.88 ( d, J = 3.4 Hz, 1H), 7.79 (d, J = 3.5 Hz, 1H), 7.37 – 7.31 (m, 4H), 7.25 – 7.18 (m, 1H), 4.56 – 4.46 (m, 1H), 3.69 – 3.59 (m, 1H), 2.59 – 2.41 (m, 4H). In analogy to the procedure described for the preparation of example 91, the following examples were prepared using the respective starting material SM: Ex.Structure Name SM 1H NMR (400 MHz,m / z - CDCl3) (ESI) No δ ppm . 92 trans-5-methyl-Int- 9.26 (d, J = 2.2 Hz, 1H), 366.1 6-oxo-N-(3- 144 7.81 – 7.78 (m, 1H), 7.74 (d, [M+H]+phenylcyclo- J = 3.4 Hz, 1H), 7.39 – 7.29 butyl)-1-thiazol- (m, 5H), 7.27 – 7.21 (m, 2-yl-pyridine-3- 1H), 6.35 (d, J = 6.0 Hz, carboxamide 1H), 4.77 – 4.66 (m, 1H), 3.75 – 3.64 (m, 1H), 2.75 – 2.66 (m, 2H), 2.59 – 2.49 (m, 2H), 2.32 (s, 3H). 93 trans-1-(2-Int- 8.03 (d, J = 2.0 Hz, 1H), 355.1 ethoxyethyl)-5- 146 7.56 (s, 1H), 7.38 – 7.20 (m, [M+H]+methyl-6-oxo- 5H), 6.16 (d, J = 5.6 Hz, N-(3- 1H), 4.73 – 4.63 (m, 1H), phenylcyclobuty 4.19 (t, J = 5.0 Hz, 2H), l)pyridine-3- 3.74 (t, J = 5.0 Hz, 2H), carboxamide 3.70 – 3.61 (m, 1H), 3.49 (q, J = 7.0 Hz, 2H), 2.72 – 2.63 (m, 2H), 2.53 – 2.43 (m, 2H), 2.21 (s, 3H), 1.17 (t, J = 7.0 Hz, 3H). 94 trans-5-fluoro-Int- 7.89 (s, 1H), 7.54 (dd, J = 385.2 1-[2-(1- 176 2.2, 9.7 Hz, 1H), 7.38 – 7.20 [M+H]+methylcyclopro- (m, 5H), 6.37 (d, J = 6.2 Hz, poxy)ethyl]-6- 1H), 4.72 – 4.61 (m, 1H), oxo-N-(3- 4.16 (t, J = 4.9 Hz, 2H), phenylcyclobuty 3.79 (t, J = 4.9 Hz, 2H), l)pyridine-3- 3.70 – 3.60 (m, 1H), 2.71 – carboxamide 2.62 (m, 2H), 2.54 – 2.44 (m, 2H), 1.29 (s, 3H), 0.62 – 0.56 (m, 2H), 0.41 – 0.34 (m, 2H). 95 trans-1-[2-(1-Int- 8.07 (d, J = 2.5 Hz, 1H), 367.3 methylcyclopro 175 7.71 (dd, J = 2.6, 9.4 Hz, [M+H]+poxy)ethyl]-6- 1H), 7.38 – 7.20 (m, 5H), oxo-N-(3- 6.58 (d, J = 9.5 Hz, 1H), phenylcyclobuty 6.28 (d, J = 6.4 Hz, 1H), l)pyridine-3- 4.73 – 4.62 (m, 1H), 4.11 (t, carboxamide J = 4.9 Hz, 2H), 3.78 (t, J = 4.9 Hz, 2H), 3.70 – 3.61 (m, 1H), 2.71 – 2.63 (m, 2H), 2.53 – 2.44 (m, 2H), 1.29 (s, 3H), 0.61 – 0.55 (m, 2H), 0.39 – 0.33 (m, 2H). Example 96 1-[2-(1-Methylcyclopropoxy)ethyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide (96) Step 1: 1-[2-(1-Methylcyclopropoxy)ethyl]-6-oxo-pyridine-3-carboxylic acid (Int-203) Methyl 1-[2-(1-Methylcyclopropoxy)ethyl]-6-oxo-pyridine-3-carboxylate (Int-175, 100 mg, 0.40 mmol) was dissolved in tetrahydrofuran (1 mL) and a solution of lithium hydroxide hydrate (67 mg, 1.59 mmol) in water (1 mL) was added. The solution was stirred at 20 °C for 20 h. After that, the pH was adjusted to pH 5 by addition of hydrochloric acid (1 M in water), and the mixture was extracted with ethyl acetate (3 x 20 mL). The combined organic layers were dried over sodium sulfate, filtered, and the filtrate was concentrated in vacuo to obtain the title compound as a colorless solid (92 mg, 0.39 mmol, 97% yield). MS m / z (ESI): 236.0 [M–H]–. Step 2: 1-[2-(1-Methylcyclopropoxy)ethyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide (96) 1-[2-(1-Methylcyclopropoxy)ethyl]-6-oxo-pyridine-3-carboxylic acid (Int-203, 92 mg, 0.39 mmol) was dissolved in dimethylformamide (2 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 221 mg, 0.58 mmol) as well as diisopropyl ethylamine (0.14 mL, 0.78 mmol) were added. After stirring for 5 min at 20 °C, (1R,2S)-2- phenylcyclopropanamine (52 mg, 0.39 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, the reaction mixture was concentrated and purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compound as a white solid (75 mg, 0.21 mmol, 55% yield). MS m / z (ESI):353.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.06 (d, J = 2.5 Hz, 1H), 7.67 (dd, J = 2.6,9.5 Hz, 1H), 7.33 – 7.26 (m, 2H), 7.23 – 7.16 (m, 3H), 6.57 (d, J = 9.4 Hz, 1H), 6.31 (br s, 1H), 4.15 – 4.03 (m, 2H), 3.76 (t, J = 5.0 Hz, 2H), 3.07 – 3.00 (m, 1H), 2.19 – 2.12 (m, 1H), 1.38 – 1.22 (m, 2H), 1.28 (s, 3H), 0.60 – 0.54 (m, 2H), 0.38 – 0.32 (m, 2H). Example 97 1-(2-Ethoxyethyl)-5-fluoro-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide (97) Methyl 1-(2-ethoxyethyl)-5-fluoro-6-oxo-pyridine-3-carboxylate (Int-6, 30 mg, 0.12 mmol) was dissolved in tetrahydrofuran (1 mL) and (1R,2S)-2-phenylcyclopropanamine (20 mg, 0.15 mmol) followed by 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD, CAS [5807-14-7], 17 mg, 0.12 mmol) were added. The mixture was stirred at 60 °C for 32 h. After that, the reaction mixture was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 66:34 to 36:64 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the titlecompound as a colorless gum (11 mg, 0.03 mmol, 27% yield). MS m / z (ESI): 345.2 [M+H]+. 1HNMR (400 MHz, CDCl3): δ ppm 7.95 (s, 1H), 7.48 (dd, J = 2.3, 9.7 Hz, 1H), 7.34 – 7.27 (m, 2H), 7.24 – 7.14 (m, 1H), 6.32 (br s, 1H), 4.26 – 4.16 (m, 2H), 3.73 (t, J = 5.0 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.03 (qd, J = 3.6, 7.4 Hz, 1H), 2.15 (ddd, J = 3.4, 6.3, 9.7 Hz, 1H), 1.38 – 1.21 (m, 3H), 1.15 (t, J = 7.0 Hz, 3H). In analogy to the procedure described for the preparation of example 97, the following examples were prepared using the respective starting material SM: Ex.-Structure Name SM 1H NMR (400 MHz,m / z No. CDCl3) (ESI) δ ppm 98 5-chloro-1-(2-Int- 8.08 (d, J = 2.4 Hz, 1H), 361.0 ethoxyethyl)- 10 7.87 (d, J = 2.4 Hz, 1H), [M+H]+6-oxo-N- 7.32 – 7.27 (m, 2H), 7.24 – [(1R,2S)-2- 7.14 (m, 3H), 6.27 (br, 1H), phenylcyclo- 4.29 – 4.11 (m, 2H), 3.80 – propyl]pyri- 3.61 (m, 2H), 3.47 (q, J = dine-3- 6.8 Hz, 2H), 3.10 – 2.97 (m, carboxamide 1H), 2.19 – 2.08 (m, 1H), 1.38 – 1.31 (m, 1H), 1.30 – 1.21 (m, 1H), 1.15 (q, J = 6.8 Hz, 3H).1-(2-Int- 8.13 – 8.07 (d , J = 2.4 341.1 ethoxyethyl)- 146 MHz, 1H), 7.65 – 7.58 (m, [M+H]+5-methyl-6- 1H), 7.42 – 7.33 (m, 3H), oxo-N- 7.27 (s, 3H), 6.49 – 6.38 (m, [(1R,2S)-2- 1H), 4.31 – 4.15 (m, 2H), phenylcyclo- 3.80 (t, J = 5.2 MHz, 2H), propyl]pyri- 3.59 – 3.50 (t, J = 6.8 MHz, dine-3- 2H), 3.16 – 3.06 (m, 1H), carboxamide 2.31 – 2.17 (m, 4H), 1.47 – 1.38 (m, 1H), 1.37 – 1.29 (m, 1H), 1.27 – 1.18 (m, 3H).1-(2-Int-3 8.14 (s, 1H), 7.66 (d, J = 8.8 327.1 ethoxyethyl)- Hz, 1H), 7.33 – 7.25 (m, [M+H]+6-oxo-N- 2H), 7.23 – 7.09 (m, 3H), [(1R,2S)-2- 6.59 – 6.35 (m, 2H), 4.32 – phenylcyclopr 3.98 (m, 2H), 3.76 – 3.58 opyl]pyridine- (m, 2H), 3.47 (q, J = 6.8 Hz, 3-carboxamide 2H), 3.08 – 2.95 (m, 1H), 2.22 – 2.06 (m, 1H), 1.40 – 1.20 (m, 2H), 1.15 (t, J = 6.8 Hz, 3H).1-benzyl-6-Int- 8.13 (d, J = 2.5 Hz, 1H), 345.1 oxo-N- 159 7.53 (dd, J = 2.5, 9.5 Hz, [M+H]+[(1R,2S)-2- 1H), 7.38 – 7.28 (m, 7H), phenylcyclo- 7.26 – 7.14 (m, 4H), 6.59 (d, propyl]- J = 9.5 Hz, 1H), 6.11 (br s, pyridine-3- 1H), 5.17 (s, 2H), 2.99 (br d, carboxamide J = 3.3 Hz, 1H), 2.13 (ddd, J = 3.6, 6.3, 9.6 Hz, 1H), 1.36 – 1.20 (m, 3H).6-oxo-1-(1-Int- 8.34 (d, J = 2.6 Hz, 1H), 371.1 phenyl- 166 7.52 (dd, J = 2.4, 9.7 Hz, [M+H]+cyclopropyl)- 1H), 7.36 – 7.28 (m, 4H), N-[(1R,2S)-2- 7.26 – 7.19 (m, 6H), 6.52 (d, phenylcyclo- J = 9.5 Hz, 1H), 6.15 (br s, propyl]pyridi- 1H), 3.04 – 2.99 (m, 1H), ne-3- 2.16 (ddd, J = 3.5, 6.4, 9.6 carboxamide Hz, 1H), 1.68 – 1.61 (m, 3H), 1.56 – 1.54 (m, 1H), 1.40 – 1.30 (m, 1H), 1.30 – 1.20 (m, 1H).6-oxo-1-Int- 8.12 (s, 1H), 7.70 – 7.62 (m, 331.1 phenyl-N-[ 204 1H), 7.56 – 7.44 (m, 3H), [M+H]+(1R,2S)-2- 7.38 (br d, J = 7.5 Hz, 2H), phenylcyclo- 7.32 – 7.27 (m, 2H), 7.24 – propyl]- 7.15 (m, 3H), 6.75 (d, J = pyridine-3- 9.6 Hz, 1H), 6.20 (br, 1H), carboxamide 3.06 – 2.98 (m, 1H), 2.19 – 2.10 (m, 1H), 1.39 – 1.31 (m, 1H), 1.28 – 1.20 (m, 1H).6-oxo-1-(2-Int- 7.63 – 7.56 (m, 2H), 7.37 – 359.1 phenylethyl)- 160 7.27 (m, 5H), 7.24 – 7.13 [M+H]+N-[(1R,2S)-2- (m, 5H), 6.59 – 6.52 (m, phenylcyclo- 1H), 5.98 – 5.93 (m, 1H), propyl]- 4.24 – 4.12 (m, 2H), 3.06 (t, pyridine-3- J = 7.2 Hz, 2H), 3.00 – 2.92 carboxamide (m, 1H), 2.12 – 2.04 (m, 1H), 1.36 – 1.28 (m, 1H), 1.23 – 1.15 (m, 1H).105 1-isobutyl-6-Int- 8.10 – 8.04 (m, 1H), 7.61 – 311.2 oxo-N- 161 7.48 (m, 1H), 7.33 – 7.25 [M+H]+[(1R,2S)-2- (m, 2H), 7.24 – 7.18 (m, phenyl- 3H), 6.54 (d, J = 9.4 Hz, cyclopropyl]- 1H), 6.26 (br s, 1H), 3.79 pyridine-3- (br d, J = 7.1 Hz, 2H), 3.02 carboxamide (br d, J = 3.2 Hz, 1H), 2.23 – 2.12 (m, 2H), 1.39 – 1.22 (m, 2H), 0.95 (d, J = 5.9 Hz, 6H). Example 106 1-(2-Ethoxyethyl)-6-oxo-N-[(1S,2R)-2-phenylcyclopropyl]pyridine-3-carboxamide (106) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 50 mg, 0.24 mmol) was dissolved in dimethylformamide (2 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 117 mg, 0.31 mmol) as well as diisopropyl ethylamine (92 mg, 0.71 mmol) were added. After stirring for 5 min at 25 °C, (1S,2R)-2-phenylcyclopropanamine (25 mg, 0.19 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, the reaction mixture was concentrated and purified by preparative HPLC (Waters Xbridge, 150 x 25 mm x 5 um, (water + 0.1% ammonia) / acetonitrile, gradient 74:26 to 45:55 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a lightbrown gum (4.4 mg, 0.01 mmol, 6% yield). MS m / z (ESI): 327.2 [M+H]+. 1H NMR (400 MHz,DMSO–d6): δ ppm 8.44 (br d, J = 3.9 Hz, 1H), 8.26 (d, J = 2.3 Hz, 1H), 7.86 (dd, J = 2.4, 9.5 Hz, 1H), 7.32 – 7.21 (m, 2H), 7.21 – 7.09 (m, 3H), 6.41 (d, J = 9.5 Hz, 1H), 4.08 (t, J = 5.3 Hz, 2H), 3.61 (t, J = 5.3 Hz, 2H), 3.45 – 3.39 (m, 2H), 3.32 – 3.32 (m, 1H), 3.04 – 2.88 (m, 1H), 2.03 (ddd, J = 3.5, 6.0, 9.2 Hz, 1H), 1.35 – 1.17 (m, 2H), 1.05 (t, J = 7.0 Hz, 3H). Example 107 and example 108 1-(2-Ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]pyridine-3- carboxamide (107) and 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-(3- chlorophenyl)cyclopropyl]pyridine-3-carboxamide (108) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 50 mg, 0.24 mmol) was dissolved indimethylformamide (1.5 mL) and the solution was cooled to 0 – 4 °C (ice bath). Hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 135 mg, 0.36 mmol) as well as diisopropyl ethylamine (0.17 mL, 0.95 mmol) were added. Afterstirring for 30 min at 0 – 4 °C, trans-2-(3-chlorophenyl)cyclopropanamine (Int-205, 40 mg, 0.24mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 64:36 to 34:66 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compounds as a mixture (50 mg). The mixture was separated into its enantiomers by preparative SFC (Regis (S,S) Whelk-O1, 250 mm x 25 mm x 10 um, supercritical carbon dioxide / (methanol + 0.1% ammonia), isocratic 40:60 (v / v)). The product containing fractions were concentrated in vacuo to yield example 107 as first eluting enantiomer as a colorless oil (14 mg, 17% yield). MS m / z(ESI): 361.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J = 1.8 Hz, 1H), 7.25 – 7.17(m, 3H), 7.11 (br d, J = 7.1 Hz, 1H), 6.56 (d, J = 9.4 Hz, 1H), 6.11 (br s, 1H), 4.21 – 4.12 (m, 2H), 3.72 (t, J = 4.9 Hz, 2H), 3.48 (q, J = 7.0 Hz, 2H), 3.01 (br d, J = 2.9 Hz, 1H), 2.16 – 2.09 (m, 1H), 1.38 – 1.24 (m, 3H), 1.16 (t, J = 7.0 Hz, 3H). Analogously, example 108 was obtained as second eluting enantiomer as a colorless oil (16 mg, 19% yield). MS m / z (ESI): 361.2[M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J = 2.2 Hz, 1H), 7.63 – 7.58 (m, 1H), 7.25– 7.16 (m, 3H), 7.11 (br d, J = 7.1 Hz, 1H), 6.55 (d, J = 9.4 Hz, 1H), 6.11 (br s, 1H), 4.21 – 4.11 (m, 2H), 3.72 (t, J = 4.9 Hz, 2H), 3.48 (q, J = 7.1 Hz, 2H), 3.01 (br d, J = 2.9 Hz, 1H), 2.15 – 2.08 (m, 1H), 1.38 – 1.23 (m, 3H), 1.16 (t, J = 7.0 Hz, 3H). Example 109 and example 110 1-(2-Ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(2-chlorophenyl)cyclopropyl]pyridine-3- carboxamide (109) and 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-(2- chlorophenyl)cyclopropyl]pyridine-3-carboxamide (110) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 50 mg, 0.24 mmol) was dissolved indimethylformamide (1 mL) and the solution was cooled to 0 – 4 °C (ice bath). Hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 135 mg, 0.36 mmol) as well as diisopropyl ethylamine (123 mg, 0.95 mmol) were added. Afterstirring for 10 min at 0 – 4 °C, trans-2-(2-chlorophenyl)cyclopropanamine hydrochloride (Int-206, 48 mg, 0.24 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was concentrated in vacuo, the residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 68:32 to 38:62 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to obtain the title compounds as a mixture (50 mg). The mixture was separated into its enantiomers by preparative SFC (Regis (S,S) Whelk-O1, 250 mm x 25 mm x 10 um, supercritical carbon dioxide / (methanol + 0.1% ammonia), isocratic 40:60 (v / v)). The product containing fractions were concentrated in vacuo to yield example 109 as second eluting enantiomer as a light yellow oil(25 mg, 29% yield). MS m / z (ESI): 361.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.16 (d,J = 2.4 Hz, 1H), 7.77 – 7.65 (m, 1H), 7.39 – 7.31 (m, 1H), 7.23 – 6.99 (m, 3H), 6.89 – 6.76 (m, 1H), 6.56 – 6.46 (m, 1H), 4.18 – 4.07 (m, 2H), 4.04 – 3.96 (m, 1H), 3.77 – 3.64 (m, 2H), 3.51 – 3.34 (m, 2H), 3.16 – 3.02 (m, 1H), 2.43 – 2.28 (m, 1H), 1.37 – 1.23 (m, 2H), 1.20 – 1.07 (m, 3H). Analogously, example 110 was obtained as first eluting enantiomer as a light yellow oil (15mg, 17% yield). MS m / z (ESI): 361.2 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.15 (d, J =2.4 Hz, 1H), 7.78 – 7.65 (m, 1H), 7.39 – 7.32 (m, 1H), 7.22 – 6.99 (m, 3H), 6.89 – 6.77 (m, 1H), 6.55 – 6.46 (m, 1H), 4.17 – 4.07 (m, 2H), 4.04 – 3.96 (m, 1H), 3.77 – 3.64 (m, 2H), 3.53 – 3.34 (m, 2H), 3.16 – 3.03 (m, 1H), 2.43 – 2.27 (m, 1H), 1.38 – 1.24 (m, 2H), 1.20 – 1.06 (m, 3H). Example 111 rac-6-Oxo-N-[(1R,2S)-2-phenylcyclopropyl]-1-(tetrahydrofuran-2-ylmethyl)pyridine-3- carboxamide (111) Step 1: 6-Oxo-1-(tetrahydrofuran-2-ylmethyl)pyridine-3-carboxylic acid (Int-207) Methyl 6-oxo-1-(tetrahydrofuran-2-ylmethyl)pyridine-3-carboxylate (Int-124, 170 mg, 0.72 mmol) was dissolved in methanol (2 mL), and an aqueous sodium hydroxide solution (2 M, 4.0 mL, 8.0 mmol) was added. The mixture was stirred at 25 °C for 1 h. After that, the pH was adjusted to pH 5 by addition of hydrochloric acid (1 M in water), and the mixture was extracted with ethyl acetate (3 x 20 mL). The combined organic layers were dried over sodium sulfate, filtered, and the filtrate was concentrated in vacuo to obtain the title compound as a colorless oil (86 mg, 0.39 mmol, 54% yield). MS m / z (ESI): 224.1 [M+H]+. Step 2: 6-Oxo-N-[(1R,2S)-2-phenylcyclopropyl]-1-(tetrahydrofuran-2-ylmethyl)pyridine-3- carboxamide (111) 6-Oxo-1-(tetrahydrofuran-2-ylmethyl)pyridine-3-carboxylic acid (Int-207, 70 mg, 0.31 mmol) was dissolved in dimethylformamide (1.5 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 179 mg, 0.47 mmol) as well as diisopropyl ethylamine (0.27 mL, 1.57 mmol) were added and the solution was cooled to 0 – 4 °C (ice bath). After stirring for 30 min at 0 – 4 °C, (1R,2S)-2-phenylcyclopropanamine (42 mg, 0.31 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, the reaction mixture was filtered and the filtrate concentrated in vacuo. The residue was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 72:28 to 42:58 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a white solid (80 mg, 0.24 mmol, 76% yield). MS m / z (ESI):339.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.16 (d, J = 2.1 Hz, 1H), 7.61 (d, J = 9.6 Hz,1H), 7.34 – 7.25 (m, 2H), 7.24 – 7.17 (m, 3H), 6.54 (d, J = 9.5 Hz, 1H), 6.30 – 6.19 (m, 1H), 4.46 – 4.36 (m, 1H), 4.27 – 4.17 (m, 1H), 3.92 – 3.83 (m, 1H), 3.80 – 3.64 (m, 2H), 3.06 – 2.98 ( m, 1H), 2.20 – 2.05 (m, 2H), 1.96 – 1.84 (m, 2H), 1.67 – 1.54 (m, 1H), 1.38 – 1.30 (m, 1H), 1.29 – 1.22 (m, 1H). Example 112 1-(2-Ethoxyethyl)-6-oxo-N-(1-phenyl-4-piperidyl)pyridine-3-carboxamide (112) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 49 mg, 0.23 mmol) was dissolved in dimethylformamide (1 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 106 mg, 0.28 mmol) as well as diisopropyl ethylamine (0.12 mL, 0.70 mmol) were added. After stirring for 10 min at 25 °C, phenylpiperidin-4-ylamine (Int-208, 41 mg, 0.23 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, the reaction mixture was concentrated and purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 89:11 to 59:41 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compoundas a white solid (30 mg, 0.08 mmol, 35% yield). MS m / z (ESI): 370.3 [M+H]+. 1H NMR (400MHz, CDCl3): δ ppm 8.12 (d, J = 2.2 Hz, 1H), 7.65 (dd, J = 2.2, 9.4 Hz, 1H), 7.34 (dd, J = 7.5, 8.2 Hz, 1H), 7.09 (d, J = 8.0 Hz, 2H), 7.02 (d, J = 7.1 Hz, 1H), 6.56 (d, J = 9.4 Hz, 1H), 5.91 (d, J = 8.9 Hz, 1H), 4.18 (t, J = 4.9 Hz, 2H), 3.76 – 3.66 (m, 4H), 3.48 (q, J = 7.0 Hz, 2H), 3.12 – 3.01 (m, 2H), 2.38 – 2.08 (m, 3H), 1.87 – 1.74 (m, 2H), 1.16 (t, J = 7.0 Hz, 3H). In analogy to the procedure described for the preparation of example 112, the following examples were prepared using the respective amines instead of amine Int-208: Ex.-Structure Name Amine 1H NMR (400 MHz,m / z No. CDCl3) (ESI) δ ppm 113 1-(2-8.15 – 8.11 (m, 1H), 7.65 361.2 ethoxyethyl)- – 7.58 (m, 1H), 7.29 – [M+H]+Int-209 6-oxo-N- 7.27 (m, 1H), 7.18 – 7.13 [(1R,2S)-2- (m, 2H), 6.59 – 6.52 (m, (4- 1H), 6.17 – 6.10 (m, 1H), chlorophenyl 4.25 – 4.10 (m, 2H), 3.76 )cyclo- – 3.69 (m, 2H), 3.52 – propyl]pyri- 3.43 (m, 2H), 3.01 – 2.92 dine-3- (m, 1H), 2.16 – 2.08 (m, carboxamide 1H), 1.36 – 1.23 (m, 2H), 1.19 – 1.11 (m, 3H). 114 1-(2-8.14 (s, 1H), 7.63 (br d, J 345.2 ethoxyethyl)- = 9.3 Hz, 1H), 7.27 – [M+H]+Int-210 6-oxo-N- 7.27 (m, 1H), 7.25 – 7.16 [(1R,2S)-2- (m, 2H), 7.02 – 6.96 (m, (4- 2H), 6.56 (br d, J = 9.0 fluorophenyl) Hz, 1H), 6.14 (br s, 1H), cyclo- 4.17 (br d, J = 4.3 Hz, propyl]pyridi 2H), 3.72 (br t, J = 4.6 ne-3- Hz, 3H), 3.48 (q, J = 7.2 carboxamide Hz, 2H), 2.96 (br s, 1H), 2.14 (br s, 1H), 1.34 – 1.13 (m, 7H). Example 115 6-Oxo-1-(1H-pyrazol-5-yl)-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide (115) Step 1: Sodium 6-oxo-1-(1H-pyrazol-5-yl)pyridine-3-carboxylate (Int-211) Methyl 6-oxo-1-(1H-pyrazol-5-yl)pyridine-3-carboxylate (Int-133, 65 mg, 0.30 mmol) was dissolved in methanol (10 mL) and water (0.1 mL), and sodium hydroxide (59 mg, 1.48 mmol) was added. The mixture was stirred at 80 °C for 0.5 h. After cooling, it was concentrated in vacuo to obtain the title compound as a light yellow oil (57 mg, 0.25 mmol, 83%), that was used in the next step without further purification. MS m / z (ESI): 206.1 [M+H]+. Step 2: 6-Oxo-1-(1H-pyrazol-5-yl)-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide (115) Sodium 6-oxo-1-(1H-pyrazol-5-yl)pyridine-3-carboxylate (Int-211, 57 mg, 0.25 mmol) was dissolved in dimethylformamide (2 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 114 mg, 0.30 mmol) as well as diisopropyl ethylamine (0.13 mL, 0.75 mmol) were added. After stirring for 10 min at 20 °C, (1R,2S)-2- phenylcyclopropanamine (40 mg, 0.30 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 60:40 to 30:70 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a whitesolid (28 mg, 0.09 mmol, 35% yield). MS m / z (ESI): 321.1 [M+H]+. 1H NMR (400 MHz,DMSO-d6) δ ppm 13.14 (s, 1H), 8.61 (d, J = 4.0 Hz, 1H), 8.57 (d, J = 2.5 Hz, 1H), 7.91 (dd, J = 2.6, 9.5 Hz, 1H), 7.87 (d, J = 2.2 Hz, 1H), 7.30 – 7.24 (m, 2H), 7.19 – 7.11 (m, 3H), 6.68 (d, J = 2.2 Hz, 1H), 6.54 (d, J = 9.5 Hz, 1H), 3.01 – 2.94 (m, 1H), 2.09 – 2.02 (m, 1H), 1.34 – 1.17 (m, 2H). Example 116 and example 117 1-(2-Ethoxyethyl)-6-oxo-N-[(3R)-1-phenylpyrrolidin-3-yl]pyridine-3-carboxamide (116) and 1-(2-ethoxyethyl)-6-oxo-N-[(3S)-1-phenylpyrrolidin-3-yl]pyridine-3-carboxamide (117) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 70 mg, 0.33 mmol) was dissolved indimethylformamide (2 mL) and the solution was cooled to 0 – 4 °C (ice bath). Hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 189 mg, 0.50 mmol) as well as diisopropyl ethylamine (0.23 mL, 1.33 mmol) were added. After stirring for 30 min at 0 – 4 °C, 1-phenylpyrrolidin-3-amine (Int-215, 54 mg, 0.33 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 64:36 to 44:56 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compounds as mixture. The mixture was separated into its enantiomers by preparative SFC (Daicel Chiralpak AD, 250 mm x 30 mm x 10 um, supercritical carbon dioxide / (ethanol + 0.1% ammonia), isocratic 60:40 (v / v)). The product containing fractions were concentrated in vacuo to yield example 116 as first eluting enantiomer as a yellowoil (24 mg, 21% yield). MS m / z (ESI): 356.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13(d, J = 1.6 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 7.31 – 7.25 (m, 3H), 6.83 – 6.74 (m, 1H), 6.70 – 6.60 (m, 2H), 6.54 (d, J = 9.5 Hz, 1H), 6.08 (br s, 1H), 4.88 – 4.76 (m, 1H), 4.16 (t, J = 5.0 Hz, 2H), 3.71 (t, J = 5.0 Hz, 2H), 3.62 (dd, J = 5.9, 10.1 Hz, 1H), 3.60 – 3.50 (m, 1H), 3.46 (q, J = 7.0 Hz, 2H), 3.42 – 3.30 (m, 2H), 2.47 – 2.34 (m, 1H), 2.17 – 2.06 (m, 1H), 1.13 (t, J = 7.0 Hz, 3H). Analogously, example 117 was obtained as second eluting enantiomer as a yellow oil (36mg, 29% yield). MS m / z (ESI): 356.1 [M+H]+. 1H NMR (400 MHz, CDCl3): δ ppm 8.13 (d, J =2.4 Hz, 1H), 7.68 – 7.62 (m, 1H), 7.33 – 7.27 (m, 3H), 6.84 – 6.75 (m, 1H), 6.72 – 6.61 (m, 2H), 6.54 (d, J = 9.5 Hz, 1H), 6.18 (br s, 1H), 4.87 – 4.78 (m, 1H), 4.15 (t, J = 5.0 Hz, 2H), 3.70 (t, J = 5.0 Hz, 2H), 3.62 (dd, J = 5.8, 10.1 Hz, 1H), 3.60 – 3.50 (m, 1H), 3.46 (q, J = 7.0 Hz, 2H), 3.42 – 3.31 (m, 2H), 2.46 – 2.35 (m, 1H), 2.16 – 2.06 (m, 1H), 1.13 (t, J = 7.0 Hz, 3H). Example 118 1-(2-Ethoxyethyl)-6-oxo-N-[(6R)-4-phenyl-4-azaspiro[2.4]heptan-6-yl]pyridine-3- carboxamide (118) 1-(2-Ethoxyethyl)-6-oxo-pyridine-3-carboxylic acid (Int-4, 60 mg, 0.28 mmol) was dissolved in dimethylformamide (2 mL), and the solution was cooled to 0 – 4 °C (ice bath). Hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 162 mg, 0.43 mmol) as well as diisopropyl ethylamine (0.20 mL, 1.14 mmol) were added. After stirring for 30 min at 0 – 4 °C, (6R)-4-phenyl-4-azaspiro[2.4]heptan-6-amine 2,2,2-trifluoro- acetate (Int-95, 53 mg, 0.18 mmol) was added and the resulting mixture was stirred at 25 °C for 1 h. Then, the reaction mixture was filtered and the filtrate was purified by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 72:28 to 52:48 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to afford the title compound as a colorless gum (16 mg, 0.04 mmol, 23% yield). MS m / z (ESI): 382.2 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 7.89 (s, 1H), 7.32 (d, J = 9.5 Hz, 1H), 7.29 – 7.24 (m, 2H), 7.00 (d, J = 7.9 Hz, 2H), 6.93 (t, J = 7.3 Hz, 1H), 6.47 (d, J = 9.5 Hz, 1H), 5.94 (br d, J = 6.0 Hz, 1H), 4.86 – 4.76 (m, 1H), 4.16 – 4.07 (m, 2H), 3.78 (dd, J = 11.2, 6.1 Hz, 1H), 3.69 (t, J = 4.8 Hz, 2H), 3.49 – 3.41 (m, 3H), 2.35 (dd, J = 13.3, 8.1 Hz, 1H), 1.92 (br d, J = 12.9 Hz, 1H), 1.14 (t, J = 6.9 Hz, 3H), 1.12 – 1.04 (m, 1H), 0.96 – 0.84 (m, 2H), 0.67 – 0.58 (m, 1H). In analogy to the procedure described for the preparation of example 118, the following examples were prepared using the respective amines instead of amine salt Int-95: Ex.-Structure Name Amine1H NMR (400 MHz) m / z No. salt δ ppm (ESI) 119 1-(2-(CDCl3): 8.54 (s, 1H), 358.2 * TFA ethoxyethyl)- 8.21 (d, J = 2.2 Hz, 1H), [M+H]+6-oxo-N- 8.00 – 7.91 (m, 2H), 7.83 [(3R)-1-pyri- Int-73 – 7.75 (m, 1H), 6.48 (d, J midin-5- = 9.5 Hz, 1H), 4.90 – 4.81 ylpyrrolidin- (m, 1H), 4.15 – 4.06 (m, 3- 2H), 3.75 – 3.62 (m, 3H), yl]pyridine- 3.51 – 3.35 (m, 4H), 3.32 3- – 3.24 (m, 1H), 2.45 – carboxamide 2.33 (m, 1H), 2.25 – 2.15 (m, 1H), 2.10 – 1.91 (m, 2H), 1.12 (t, J = 7.0 Hz, 3H). 120 1-(2-(CDCl3): 8.15 (d, J = 2.1 360.1 * TFA ethoxyethyl)- Hz, 1H), 7.66 (d, J = 7.9 [M+H]+6-oxo-N- Hz, 1H), 7.15 (s, 1H), 6.97 [(3R)-1-(1- Int-74 (br s, 1H), 6.55 (d, J = 9.5 methylpyrazo Hz, 1H), 4.86 – 4.76 (m, l-4- 1H), 4.16 (t, J = 5.0 Hz, yl)pyrrolidin- 2H), 3.85 (s, 3H), 3.72 (t, J 3-yl]pyri- = 5.0 Hz, 2H), 3.47 (q, J = dine-3- 7.0 Hz, 2H), 3.28 – 3.18 carboxamide (m, 2H), 3.03 – 2.93 (m, 1H), 2.53 – 2.42 (m, 1H), 2.06 – 1.94 (m, 1H), 1.75 – 1.48 (m, 2H), 1.15 (t, J = 7.0 Hz, 3H).1-(2-(d4-MeOH): 8.29 (s, 1H), 358.2 * HCl ethoxyethyl)- 8.07 (s, 1H), 8.00 – 7.92 [M+H]+6-oxo-N- (m, 2H), 7.76 (s, 1H), 6.52 [(3R)-1- Int-81 (d, J = 9.4 Hz, 1H), 4.73 – pyrazin-2- 4.66 (m, 1H), 4.19 (t, J = ylpyrrolidin- 4.9 Hz, 2H), 3.87 (dd, J = 3- 6.6, 11.0 Hz, 2H), 3.76 – yl]pyridine- 3.67 (m, 3H), 3.66 – 3.58 3- (m, 1H), 3.55 – 3.43 (m, carboxamide 3H), 2.45 – 2.35 (m, 1H), 2.24 – 2.14 (m, 1H), 1.10 (t, J = 7.0 Hz, 3H).1-(2-(CDCl3): 8.12 (d, J = 2.2 390.2 * TFA ethoxyethyl)- Hz, 1H), 7.67 – 7.60 (m, [M+H]+6-oxo-N- 1H), 7.23 – 7.16 (m, 2H), [(3R)-1-(4- 6.58 – 6.48 (m, 3H), 6.28 chlorophenyl Int-70 – 6.07 (m, 1H), 4.85 – )pyrrolidin-3- 4.75 (m, 1H), 4.20 – 4.10 yl]pyridine- (m, 2H), 3.75 – 3.67 (m, 3- 2H), 3.65 – 3.57 (m, 1H), carboxamide 3.54 – 3.41 (m, 2H), 3.39 – 3.24 (m, 2H), 2.47 – 2.35 (m, 1H), 2.15 – 2.05 (m, 1H), 1.13 (t, J = 7.0 Hz, 3H).1-(2-(CDCl3): 8.12 (d, J = 2.4 390.2 * TFA ethoxyethyl)- Hz, 1H), 7.62 (dd, J = 2.3, [M+H]+6-oxo-N- 9.3 Hz, 1H), 7.19 – 7.12 [(3R)-1-(3- Int-71 (m, 1H), 6.71 (d, J = 8.0 chlorophe- Hz, 1H), 6.61 – 6.52 (m, nyl)- 2H), 6.50 – 6.45 (m, 1H), pyrrolidin-3- 6.04 (br s, 1H), 4.83 – yl]pyridine- 4.75 (m, 1H), 4.16 (t, J = 3- 4.8 Hz, 2H), 3.71 (t, J = carboxamide 4.9 Hz, 2H), 3.64 (dd, J = 5.9, 10.1 Hz, 1H), 3.54 – 3.43 (m, 3H), 3.42 – 3.34 (m, 1H), 3.32 – 3.26 (m, 1H), 2.47 – 2.36 (m, 1H), 2.15 – 2.05 (m, 1H), 1.13 (t, J = 7.0 Hz, 3H).1-(2-(CDCl3): 8.15 (s, 1H), 390.2 * TFA ethoxyethyl)- 7.74 – 7.60 (m, 1H), 7.43 [M+H]+6-oxo-N- – 7.33 (m, 1H), 7.31 – [(3R)-1-(2- Int-72 7.17 (m, 1H), 7.08 – 6.87 chlorophe- (m, 2H), 6.56 (d, J = 9.4 nyl)pyrrolidi Hz, 1H), 6.44 – 6.19 (m, n-3- 1H), 4.85 – 4.73 (m, 1H), yl]pyridine- 4.17 (t, J = 5.0 Hz, 2H), 3- 3.83 – 3.66 (m, 1H), 3.72 carboxamide (t, J = 5.0 Hz, 2H), 3.57 – 3.38 (m, 2H), 3.47 (q, J = 7.0 Hz, 2H), 3.30 – 3.13 (m, 1H), 2.53 – 2.36 (m, 1H), 2.11 – 1.95 (m, 1H), 1.14 (t, J = 7.0 Hz, 3H). Example 125 trans-1-[2-Ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3- carboxamide (125) Step 1: Sodium 1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-pyridine-3-carboxylate (Int-212) Methyl 1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-pyridine-3-carboxylate (Int-155, 38 mg, 0.13 mmol) was dissolved in methanol (1 mL) and water (0.2 mL), and an aqueous sodium hydroxide solution (2 M, 100 uL, 0.20 mmol) was added. The mixture was stirred at 80 °C for 4 h. After cooling, it was concentrated in vacuo to obtain the title compound as a light yellow oil (40 mg), that was used in the next step without further purification. MS m / z (ESI): 270.1 [M+H]+.Step 2: trans-1-[2-Ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide (125) Sodium 1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-pyridine-3-carboxylate (Int-212, 40 mg, 0.13 mmol) was dissolved in dimethylformamide (1 mL), hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU, CAS [148893-10-1], 40 mg, 0.11 mmol) as well as diisopropylethylamine (0.07 mL, 0.41 mmol) were added. After stirring for 5 min at 20 °C, trans-3-phenylcyclobutanamine (Int-178, 17 mg, 0.11 mmol) was added and the resulting mixture was stirred at 20 °C for 1 h. Then, it was purified directly by preparative HPLC (Phenomenex luna C18, 150 x 25 mm x 10 um, (water + 0.1% formic acid) / acetonitrile, gradient 59:41 to 29:71 (v / v), flow 25 mL / min). The product containing fraction was lyophilized to yield the title compound as a light brown gum (29 mg, 0.07 mmol, 65% yield). MS m / z (ESI): 399.3 [M+H]+.1H NMR (400 MHz, CDCl3): δ ppm 8.36 (d, J = 2.6 Hz, 1H), 7.66 (dd, J = 2.6, 9.4 Hz, 1H), 7.38 - 7.28 (m, 4H), 7.26 - 7.20 (m, 1H), 6.59 (d, J = 9.5 Hz, 1H), 6.19 (br d, J = 6.5 Hz, 1H), 5.33 - 5.22 (m, 1H), 4.73 - 4.61 (m, 1H), 3.86 (dd, J = 5.9, 10.5 Hz, 2H), 3.76 (dd, J = 4.9, 10.5 Hz, 2H), 3.71 - 3.60 (m, 1H), 3.51 (q, J = 7.0 Hz, 4H), 2.73 - 2.62 (m, 2H), 2.54 - 2.42 (m, 2H), 1.18 (t, J = 7.0 Hz, 6H). In analogy to the procedure described for the preparation of example 125, the following examples were prepared using the respective amines instead of starting material (SM) Int-155: Ex.-Structure Name SM 1H NMR (400 MHz) δm / z No. ppm (ESI) 126 trans-1-(2-(DMSO-d6): 8.53 (br d, J 313.1 hydroxy- = 6.7 Hz, 1H), 8.28 (d, J [M+H]+ethyl)-6-oxo- = 2.6 Hz, 1H), 7.92 (dd, J N-(3- Int-112 = 9.5, 2.6 Hz, 1H), 7.36 – phenylcyclo- 7.30 (m, 4H), 7.24 – 7.17 butyl)- (m, 1H), 6.42 (d, J = 9.5 pyridine-3- Hz, 1H), 4.93 (t, J = 5.4 carboxamide Hz, 1H), 4.52 – 4.41 (m, 1H), 3.98 (br t, J = 5.3 Hz, 2H), 3.67 – 3.62 (m, 2H), 3.62 – 3.55 (m, 1H), 2.49 – 2.38 (m, 4H) 127 trans-1-[2- (DMSO-d6): 8.34 - 8.24 340.2 O (dimethyl- (m, 1H), 7.93 (br d, J = [M+H]+N H amino)ethyl]- 9.4 Hz, 1H), 7.38 - 7.24 N O 6-oxo-N-(3- (m, 4H), 7.23 - 7.13 (m, N phenylcyclo- Int-114 1H), 6.52 (d, J = 9.5 Hz, butyl)- 1H), 4.50 - 4.37 (m, 1H), pyridine-3- 4.33 - 4.23 (m, 2H), 3.64 carboxamide - 3.50 (m, 1H), 3.46 - 3.35 (m, 2H), 2.84 (s, 6H), 2.48 - 2.34 (m, 4H)trans-1-[3-(CDCl3): 8.29 (d, J = 2.4 368.2 (dimethyl- Hz, 1H), 7.80 (dd, J = [M+H]+amino)-3- 2.5, 9.4 Hz, 1H), 7.38 - oxo-propyl]- 7.28 (m, 4H), 7.25 - 7.18 6-oxo-N-(3- Int-115 (m, 1H), 6.60 - 6.52 (m, phenylcyclo- 2H), 4.72 - 4.61 (m, 1H), butyl)- 4.30 (t, J = 5.8 Hz, 2H), pyridine-3- 3.71 - 3.60 (m, 1H), 2.99 carboxamide (s, 3H), 2.95 (s, 3H), 2.91 (t, J = 5.8 Hz, 2H), 2.70 - 2.60 (m, 2H), 2.57 - 2.45 (m, 2H)trans-6-oxo-(CDCl3): δ ppm 8.12 (s, 381.2 N-(3- 1H), 7.75 (dd, J = 2.3, [M+H]+phenylcyclo- 9.5 Hz, 1H), 7.39 - 7.28 butyl)-1- (m, 4H), 7.26 - 7.20 (m, (3,3,3- Int-113 1H), 6.68 - 6.60 (m, 1H), trifluoro-2- 6.44 - 6.31 (m, 1H), 4.71 hydroxy- - 4.59 (m, 1H), 4.53 (br propyl)pyri- d, J = 13.8 Hz, 1H), 4.47 dine-3- - 4.37 (m, 1H), 4.13 - carboxamide 4.01 (m, 1H), 3.72 - 3.61 (m, 1H), 2.73 - 2.62 (m, 2H), 2.55 - 2.44 (m, 2H)trans-1-[2-(2-(CDCl3): 8.08 (d, J = 2.4 359.1 fluoroetho- Hz, 1H), 7.74 (dd, J = [M+H]+xy)ethyl]-6- 9.5, 2.6 Hz, 1H), 7.38 – oxo-N-(3- 7.28 (m, 4H), 7.25 – 7.20 phenylcy...

Claims

1. CLAIMS1. A compound of formula (I)or a pharmaceutically acceptable salt thereof, wherein: X is –(CH2)n–, wherein n is 0, 1 or 2; A is C3-8-cycloalkyl, or 3- to 10-membered heterocyclyl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; RA1is a group; RA2and RA3are each independently hydrogen, hydroxy, halogen, cyano, C1-6-alkyl, halo- C1-6-alkyl, or hydroxy-C1-6-alkyl; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl; B is C6-10-aryl or 5- to 14-membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- to 10- membered heteroaryl comprising 1 to 3 heteroatoms independently selected from N, O, and S, and the remaining atoms being carbon; wherein said 5- to 10-membered heteroaryl is optionally substituted with 1 to 3 C1-6-alkyl substituents; and RB2is hydrogen, halogen, C1-6-alkyl, C1-6-alkoxy, or halo-C1-6-alkyl;R1is a group , C2-6-alkyl, or C1-6-alkyl substituted with one or two substituents R1a; each R1ais independently hydroxy, halogen, cyano, halo-C1-6-alkyl, C1-6-alkoxy, amino, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-8-cycloalkyl,(ii) C6-10-aryl,(iii) 5- to 10-membered heteroaryl comprising 1 to 3 heteroatoms independentlyselected from N, O, and S, and the remaining atoms being carbon, or (iv) 3- to 10-membered heterocyclyl comprising 1 to 3 heteroatoms independentlyselected from N, O, and S, and the remaining atoms being carbon; RCis hydrogen, hydroxy-C1-6-alkyl, C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C6- 10-aryl, halo-C1-6-alkoxy, hydroxy, halogen, or cyano; and R2is selected from hydrogen, halogen, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, and halo-C1-6-alkoxy; wherein the term “cycloalkyl” refers to a saturated mono- or bicyclic hydrocarbon group; and the term “heterocyclyl” refers to a saturated mono- or bicyclic ring system.

2. The compound of formula (I) according to claim 1, or a pharmaceutically acceptable saltthereof, wherein n is 0 or 1.

3. The compound of formula (I) according to any one of claims 1 or 2, or a pharmaceuticallyacceptable salt thereof, wherein n is 0.

4. The compound of formula (I) according to any one of claims 1 to 3, or a pharmaceuticallyacceptable salt thereof, wherein A is C3-6-cycloalkyl or 5- to 6-membered heterocyclyl comprising nitrogen and the remaining atoms being carbon.

5. The compound of formula (I) according to any one of claims 1 to 4, or a pharmaceuticallyacceptable salt thereof, wherein A is C3-6-cycloalkyl.

6. The compound of formula (I) according to any one of claims 1 to 5, or a pharmaceuticallyacceptable salt thereof, wherein A is C3-4-cycloalkyl.

7. The compound of formula (I) according to any one of claims 1 to 4, or a pharmaceuticallyacceptable salt thereof, wherein A is:,8. The compound of formula (I) according to any one of claims 1 to 7, or a pharmaceuticallyacceptable salt thereof, wherein A is:.

9. The compound of formula (I) according to any one of claims 1 to 8, or a pharmaceuticallyacceptable salt thereof, wherein: RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl.

10. The compound of formula (I) according to any one of claims 1 to 8, or a pharmaceuticallyacceptable salt thereof, wherein: RA2is hydrogen, hydroxy, fluoro, methyl, trifluoromethyl, 2,2,2-trifluoroethyl, or hydroxymethyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form cyclopropyl.

11. The compound of formula (I) according to any one of claims 1 to 8, or a pharmaceuticallyacceptable salt thereof, wherein RA2and RA3are both hydrogen.

12. The compound of formula (I) according to any one of claims 1 to 11, or apharmaceutically acceptable salt thereof, wherein B is phenyl, 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, and the remaining atoms being carbon, or 9- to 12-membered bi- or tricyclic heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon.

13. The compound of formula (I) according to any one of claims 1 to 11, or apharmaceutically acceptable salt thereof, wherein B is phenyl or 9-membered fused bicyclic heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon.

14. The compound of formula (I) according to any one of claims 1 to 11, or apharmaceutically acceptable salt thereof, wherein B is,, , , .

15. The compound of formula (I) according to any one of claims 1 to 11, or apharmaceutically acceptable salt thereof, wherein B is:, , , .

16. The compound of formula (I) according to any one of claims 1 to 15, or apharmaceutically acceptable salt thereof, wherein: RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- membered heteroaryl comprising 2 or 3 nitrogen atoms, the remaining atoms being carbon; wherein said 5-membered heteroaryl is optionally substituted with one or two C1-6-alkyl substituents; and RB2is hydrogen, halogen, or C1-6-alkyl.

17. The compound of formula (I) according to any one of claims 1 to 15, or apharmaceutically acceptable salt thereof, wherein:RB1is hydrogen, halogen, or C1-6-alkyl; and RB2is hydrogen or C1-6< / sub>-alkyl.

18. The compound of formula (I) according to claim 16, or a pharmaceutically acceptable saltthereof, wherein: RB1is hydrogen, fluoro, chloro, methyl, trifluoroalkyl, methoxy, cyano, oxo, 1- methylpyrazol-3-yl, 3,5-dimethyl-1H-pyrazol-4-yl or, 1H-1,2,4-triazol-5-yl; and RB2is hydrogen, chloro, methyl.

19. The compound of formula (I) according to any one of claims 1 to 15, or apharmaceutically acceptable salt thereof, wherein: RB1is hydrogen, fluoro, or methyl; and RB2is hydrogen or methyl.

20. The compound of formula (I) according to any one of claims 1 to 19, or apharmaceutically acceptable salt thereof, wherein: 1R is a group , C2-6-alkyl, or C1-6-alkyl substituted with one or two substituents R1a; one R1ais hydroxy, halo-C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; and another R1a, if present, is hydroxy or C1-6-alkoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is (i) C3-4-cycloalkyl,(ii) phenyl,(iii) 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selectedfrom N and S, the remaining atoms being carbon, or (iv) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; and RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl.

21. The compound of formula (I) according to any one of claims 1 to 19, or apharmaceutically acceptable salt thereof, wherein: R1is a group or C1-6-alkyl substituted with one R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy; L is *–O(CH2)2– or -CH2-, wherein * denotes the point of attachment of L to ring C; C is (i) C3-4-cycloalkyl, or(ii) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; and RCis C1-6< / sub>-alkyl.

22. The compound of formula (I) according to claim 20, or a pharmaceutically acceptable saltthereof, wherein:R1is a group C2-4-alkyl or C2-4-alkyl substituted with one or two substituents R1a; wherein one R1ais hydroxy, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoroethoxy, difluoroethoxy, trifluoroethoxy, (CH3)2N-, CH3-C(O)NH-, (CH3)2N- C(O)-, methylsulfonyl; another R1a, if present, is hydroxy or ethoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2;C is cyclopropyl; cyclobuthyl; phenyl, ,RCis hydrogen, methyl, hydroxymethyl, ethoxy, ethoxymethyl, phenyl.

23. The compound of formula (I) according to any one of claims 1 to 19, or apharmaceutically acceptable salt thereof, wherein: 1R is ethyl or a group , wherein said ethyl substituted with one R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy; L is *–O(CH2)2–, or -CH2-, wherein * denotes the point of attachment of L to ring C; Cis cyclopropyl or;andRC< / sup>is methyl.

24. The compound of formula (I) according to any one of claims 1 to 23, or apharmaceutically acceptable salt thereof, wherein R2is hydrogen, halogen or C1-6-alkyl.

25. The compound of formula (I) according to any one of claims 1 to 23, or apharmaceutically acceptable salt thereof, wherein R2is hydrogen or halogen.

26. The compound of formula (I) according to claim 24, or a pharmaceutically acceptable saltthereof, wherein R2is hydrogen, chloro, fluoro or methyl.

27. The compound of formula (I) according to any one of claims 1 to 23, or apharmaceutically acceptable salt thereof, wherein R2is hydrogen or fluoro.

28. The compound of formula (I) according to claim 1, or a pharmaceutically acceptable saltthereof, wherein: X is –(CH2)n–, wherein n is 0 or 1 A is C3-6-cycloalkyl or 5- to 6-membered heterocyclyl comprising nitrogen and the remaining atoms being carbon; RA1is a group; RA2is hydrogen, hydroxy, halogen, C1-6-alkyl, halo-C1-6-alkyl, or hydroxy-C1-6-alkyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form a C3-4-cycloalkyl; B is phenyl, 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selected from N and S, and the remaining atoms being carbon, or 9- to 12-membered bi- or tricyclic heteroaryl comprising 1 to 3 heteroatoms independently selected from N and O, and the remaining atoms being carbon; RB1is hydrogen, halogen, cyano, C1-6-alkyl, halo-C1-6-alkyl, C1-6-alkoxy, oxo, or 5- membered heteroaryl comprising 2 or 3 nitrogen atoms, the remaining atoms being carbon; wherein said 5-membered heteroaryl is optionally substituted with one or two C1-6-alkyl substituents; and RB2is hydrogen, halogen, or C1-6-alkyl; 1R is a group , C2-6-alkyl or C1-6-alkyl substituted with one or two substituents R1a; one R1ais hydroxy, halo-C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-amino, (C1-6-alkyl)2-amino, C1-6-alkyl-C(O)NH-, (C1-6-alkyl)2N-C(O), halo-C1-6-alkoxy, methylsulfonyl; and another R1a, if present, is hydroxy or C1-6-alkoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2; C is(i) C3-4-cycloalkyl,(ii) phenyl,(iii) 5- to 6-membered heteroaryl comprising 1 or 2 heteroatoms independently selectedfrom N and S, the remaining atoms being carbon, or (iv) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis hydrogen, C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, phenyl; and R2is hydrogen, halogen, C1-6< / sub>-alkyl.

29. The compound of formula (I) according to claim 28, or a pharmaceutically acceptable saltthereof, wherein: n is 0; A is C3-6-cycloalkyl;; RA2and RA3are both hydrogen; B is phenyl or 9-membered fused bicyclic heteroaryl comprising two nitrogen atoms, the remaining atoms being carbon; RB1is hydrogen, halogen, or C1-6-alkyl; and RB2is hydrogen or C1-6-alkyl; C R1is a group , C2-6-alkyl, or C1-6-alkyl substituted with one R1a; R1ais C1-6-alkoxy or halo-C1-6-alkoxy; L is *–O(CH2)2– or -CH2-, wherein * denotes the point of attachment of L to ring C; C is (i) C3-4-cycloalkyl, or(ii) 5- to 6-membered heterocyclyl comprising 1 or 2 heteroatoms independentlyselected from N and O, the remaining atoms being carbon; RCis C1-6-alkyl; and R2is hydrogen or halogen.

30. The compound of formula (I) according to claim 28, or a pharmaceutically acceptable saltthereof, wherein: X is –(CH2)n–, wherein n is 0 or 1 A is: ;RA2is hydrogen, hydroxy, fluoro, methyl, trifluoromethyl, 2,2,2-trifluoroethyl, or hydroxymethyl; and RA3is hydrogen; or RA2and RA3are geminal substituents on a carbon atom and, together with the carbon atom to which they are attached, form cyclopropyl; B is:,, RB1is hydrogen, fluoro, chloro, methyl, trifluoroalkyl, methoxy, cyano, oxo, 1- methylpyrazol-3-yl, 3,5-dimethyl-1H-pyrazol-4-yl or, 1H-1,2,4-triazol-5-yl; and RB2is hydrogen, chloro, methyl; 1R is a group , C2-4-alkyl, or C1-4-alkyl substituted with one or two substituents R1a; wherein one R1ais hydroxy, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoroethoxy, difluoroethoxy, trifluoroethoxy, (CH3)2N-, CH3-C(O)NH-, (CH3)2N- C(O)-, methylsulfonyl;another R1a, if present, is hydroxy or ethoxy;L is *–O(CH2)2–, or -(CH2)m-, wherein * denotes the point of attachment of L to ring C; m is 0, 1 or 2;C is cyclopropyl, cyclobuthyl, phenyl,,,RCis hydrogen, methyl, hydroxymethyl, ethoxy, ethoxymethyl, phenyl; and R2is hydrogen, chloro, fluoro, or methyl.

31. The compound of formula (I) according to claim 29, or a pharmaceutically acceptable saltthereof, wherein: X is –(CH2)n–, wherein n is 0 Ais:; RA1is a group; RA2and RA3are both hydrogen; B is:, , , ;RB1is hydrogen, fluoro, or methyl; and RB2is hydrogen or methyl; 1R is ethyl or a group , wherein said ethyl substituted with one R1a; R1ais ethoxy or 2,2,2-trifluoroethoxy; L is *–O(CH2)2–, or -CH2-, wherein * denotes the point of attachment of L to ring C; Cis cyclopropyl or; RCis methyl; and R2is hydrogen, chloro, fluoro, or methyl.

32. The compound of formula (I) according to claim 1, or a pharmaceutically acceptable saltthereof, wherein said compound of formula (I) is selected from the group consisting of:trans-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; cis-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[6-(trifluoromethyl)-2- pyridyl]cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[6-(trifluoromethyl)-2- pyridyl]cyclobutyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[2-(trifluoromethyl)-3- pyridyl]cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[3-[2-(trifluoromethyl)-3- pyridyl]cyclobutyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-[2-(3,5-dimethyl-1H-pyrazol-4- yl)phenyl]cyclopropyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide;cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(2-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(2-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylbenzotriazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylbenzotriazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(4-methylquinazolin-8-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(4-methylquinazolin-8-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-(3-phenyl-1-bicyclo[1.1.1]pentanyl)pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[3-[3-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-N-[3-(1,3-benzoxazol-7-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; cis-N-[3-(1,3-benzoxazol-7-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-(3-fluoro-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-(3-fluoro-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide trans-1-(2-ethoxyethyl)-N-[3-(3-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide;cis-1-(2-ethoxyethyl)-N-[3-(3-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1'-methyl-2'-oxo-spiro[cyclopropane-1,3'-indoline]-7'- yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1'-methyl-2'-oxo-spiro[cyclopropane-1,3'-indoline]-7'- yl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; trans-N-[3-(2-chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(2-fluorophenyl)cyclobutyl]-6-oxo-pyridine-3-carboxamide; trans-N-[3-(3-chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide; trans-N-[3-(4-chlorophenyl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(o-tolyl)cyclobutyl]-6-oxo-pyridine-3-carboxami; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[4-(1H-1,2,4-triazol-5-yl)phenyl]cyclobutyl]pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-[3-(1-methylpyrazol-3-yl)phenyl]cyclobutyl]-6-oxo- pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[3-[4-(trifluoromethyl)phenyl]cyclobutyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(5,6-dichloro-2-pyridyl)-pyrrolidin-3-yl]pyri-dine-3- carboxamide; N-[1-(2-cyano-3-pyridyl)pyrrolidin-3-yl]-1-(2-ethoxy-ethyl)-6-oxo-pyri-dine-3- carboxamide; N-[1-(2-cyano-3-pyridyl)pyrrolidin-3-yl]-1-(2-ethoxy-ethyl)-6-oxo-pyri-dine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(5-chloro-2-pyridyl)-pyrro-li-din-3-yl]pyri-dine-3- carboxamide; 1-(2-ethoxyethyl)-N-(3-methylcyclo-hexyl)-6-oxo-pyri-dine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[4-(3-pyridyl)cyclohexyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(hydroxymethyl)-3-phenyl-cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(hydroxymethyl)-3-phenyl-cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(4-methoxyphenyl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3-phenyl-1-bicyclo[1.1.1]pentanyl)methyl]pyridine-3- carboxamide;trans-1-(2-ethoxyethyl)-6-oxo-N-[(3-phenylcyclobutyl)methyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[(3-phenylcyclobutyl)methyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-thiazol-2-ylcyclobutyl)pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-thiazol-2-ylcyclobutyl)pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-N-(3-hydroxy-3-phenyl-cyclobutyl)-6-oxo-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylpyrazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-[3-(1-methylpyrazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-(2,2,2-trifluoroethyl)cyclobutyl]pyridine-3- carboxamide; cis 1-(2-ethoxyethyl)-6-oxo-N-[3-(2,2,2-trifluoroethyl)cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-(trifluoromethyl)cyclobutyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-(trifluoromethyl)cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-(3-pyridyl)cyclobutyl]pyridine-3-carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-(3-pyridyl)cyclobutyl]pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[6-(trifluoromethyl)-2-pyridyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-[3-[2-(trifluoromethyl)-3-pyridyl]cyclobutyl]pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-7-ylcyclobutyl)pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-7-ylcyclobutyl)pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3- carboxamide; cis-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-4-ylcyclobutyl)pyridine-3- carboxamide;cis-1-(2-ethoxyethyl)-6-oxo-N-(3-pyrazolo[1,5-a]pyridin-4-ylcyclobutyl)pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-morpholin-2-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2R)-morpholin-2-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3S)-3-piperidyl]-methyl]-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3R)-3-piperidyl]-methyl]-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3R)-morpholin-3-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(3S)-morpholin-3-yl]methyl]pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-4-methylmorpholin-2-yl]methyl]pyridine-3- carboxamide; trans-1-(2-acetamidoethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide trans-1-[1-(hydroxymethyl)cyclopropyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3- carboxamide; trans-5-chloro-6-oxo-N-(3-phenylcyclobutyl)-1-thiazol-2-yl-pyridine-3-carboxamide; trans-5-methyl-6-oxo-N-(3-phenyl-cyclo-butyl)-1-thiazol-2-yl-pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-5-methyl-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-5-fluoro-1-[2-(1-methylcyclopro-po-xy)ethyl]-6-oxo-N-(3- phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[2-(1-methylcycloprop-oxy)ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3- carboxamide; 1-[2-(1-methylcyclopropoxy)ethyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 5-chloro-1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-5-methyl-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide;1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-benzyl-6-oxo-N-[(1R,2S)-2-phenylcyclo-propyl]-pyridine-3-carboxamide; 6-oxo-1-(1-phenyl-cyclopropyl)-N-[(1R,2S)-2-phenyl-cyclo-propyl]pyridi-ne-3- carboxamide; 6-oxo-1-phenyl-N-[ (1R,2S)-2-phenyl-cyclo-propyl]-pyridine-3-carboxamide; 6-oxo-1-(2-phenyl-ethyl)-N-[(1R,2S)-2-phenylcyclopropyl]-pyridine-3-carboxamide; 1-isobutyl-6-oxo-N-[(1R,2S)-2-phenyl-cyclopropyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(2-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1S,2R)-2-(2-chlorophenyl)cyclopropyl]pyridine-3- carboxamide; 6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]-1-(tetrahydrofuran-2-ylmethyl)pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-(1-phenyl-4-piperidyl)pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(4-chlorophenyl)-cyclo-propyl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(1R,2S)-2-(4-fluorophenyl)cyclo-propyl]pyridine-3- carboxamide; 6-oxo-1-(1H-pyrazol-5-yl)-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-phenylpyrrolidin-3-yl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3S)-1-phenylpyrrolidin-3-yl]pyridine-3-carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(6R)-4-phenyl-4-azaspiro[2.4]heptan-6-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-pyri-midin-5-ylpyrrolidin-3-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(1-methylpyrazol-4-yl)pyrrolidin-3-yl]-pyri-dine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-pyrazin-2-ylpyrroli-din-3-yl]pyridine-3-carboxamide;1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(4-chlorophenyl)pyrrolidin-3-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(3-chlorophenyl)pyrrolidin-3-yl]pyridine-3- carboxamide; 1-(2-ethoxyethyl)-6-oxo-N-[(3R)-1-(2-chlorophenyl)pyrrolidin-3-yl]pyridine-3- carboxamide; trans-1-[2-ethoxy-1-(ethoxymethyl)ethyl]-6-oxo-N-(3-phenylcyclobutyl)pyridine-3- carboxamide ; trans-1-(2-hydroxy-ethyl)-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[2-(dimethylamino)-ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[3-(dimethylamino)-3-oxo-propyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-(3,3,3-trifluoro-2-hydroxy-propyl)pyridine-3- carboxamide; trans-1-[2-(2-fluoroethoxy)ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3-carboxamide; trans-1-[2-(2,2-difluoroethoxy)-ethyl]-6-oxo-N-(3-phenylcyclobutyl)-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[2-(2,2,2-trifluoroethoxy)-ethyl]pyridine-3- carboxamide; cis-1-(3-ethoxycyclo-butyl)-6-oxo-N-(trans-3-phenylcyclo-butyl)pyridine-3-carboxamide; trans-1-(methylsulfonylmethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; 6-Oxo-1-(2-phenoxyethyl)-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-(2-methoxyethyl)-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3-carboxamide; 1-[2-(difluorometho-xy)-ethyl]-6-oxo-N-[(1R,2S)-2-phenyl-cyclopropyl]pyridine-3- carboxamide; 1-[2-(trifluorometho-xy)-ethyl]-6-oxo-N-[(1R,2S)-2-phenyl-cyclopropyl]pyridine-3- carboxamide; 1-[(1-ethoxycyclo-pro-pyl)methyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 1-[1-(ethoxymethyl)-cyclopropyl]-6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]pyridine-3- carboxamide; 6-oxo-N-[(1R,2S)-2-phenylcyclopropyl]-1-thiazol-2-yl-pyridine-3-carboxamide; and 6-oxo-1-(2-pyridyl-methyl)-N-[(1R,2S)-2-phenylcyclopro-pyl]-pyridine-3-carboxamide.

33. The compound of formula (I) according to claim 1, or a pharmaceutically acceptable saltthereof, wherein said compound of formula (I) is selected from the group consisting of: trans-N-[3-(1,3-dimethylindazol-4-yl)cyclobutyl]-1-(2-ethoxyethyl)-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-7-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-5-fluoro-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(5-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(6-fluoro-1-methyl-indazol-4-yl)cyclobutyl]-6-oxo-pyridine- 3-carboxamide; trans-1-(2-ethoxyethyl)-6-oxo-N-(3-phenylcyclobutyl)pyridine-3-carboxamide; trans-1-(2-ethoxyethyl)-N-[3-(1-methylindazol-4-yl)cyclobutyl]-6-oxo-pyridine-3- carboxamide; trans-1-(2-ethoxyethyl)-N-(3-imidazo[1,2-a]pyridin-5-ylcyclobutyl)-6-oxo-pyridine-3- carboxamide; trans-6-oxo-N-(3-phenylcyclobutyl)-1-[[(2S)-4-methylmorpholin-2-yl]methyl]pyridine-3- carboxamide; trans-5-fluoro-1-[2-(1-methylcyclopro-po-xy)ethyl]-6-oxo-N-(3- phenylcyclobutyl)-pyridine-3-carboxamide; and trans-6-oxo-N-(3-phenylcyclobutyl)-1-[2-(2,2,2-trifluoroethoxy)-ethyl]pyridine-3- carboxamide.

34. A process of preparation of a compound of formula (I) according to any one of claims 1 to33, or a pharmaceutically acceptable salt thereof, comprising reacting a compound of formula (II), wherein A, X, RA1, RA2, and RA3, are as defined in any one of claims 1 to 34<img src='' class="img-anchor img-center" img-id="IMGF000193_0001" / >(i) with a compound of formula (III), wherein R1 and R2 are as defined in anyone of claims 1 to 33in the presence of a stoichiometric amount of an appropriate coupling agent, e.g. hexafluorophosphate azabenzotriazole tetramethyl uronium (HATU), further in the presence of an over-stoichiometric amount of an appropriate non-nucleophlic base, e.g. triethylamine or diisopropyl ethylamine, in an aprotic solvent, such as dimethylformamide, or dichloromethaneor; or (ii) with a compound of formula (IV), wherein R1 and R2 are as defined in anyone of claims 1 to 33, and R is methyl or ethylin the presence of catalytic or stoichiometric amounts of a suitable strong base, such as 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD), in a suitable aprotic solvent, e.g. tetrahydrofuran, at elevated temperatures, such as 40 – 80 °C; to form said compound of formula (I).

35. A compound of formula (I) according to any one of claims 1 to 33 for use astherapeutically active substance.

36. A pharmaceutical composition comprising a compound of formula (I) according to anyone of claims 1 to 33 and a therapeutically inert carrier.

37. Use of a compound of formula (I) according to any one of claims 1 to 33 for the treatmentor prophylaxis of diseases and disorders that are associated with sEH.

38. A compound of formula (I) according to any one of claims 1 to 33 for use in the treatmentor prophylaxis of diseases and disorders that are associated with sEH.

39. Use of a compound of formula (I) according to any one of claims 1 to 33 in the preparationof a medicament for the treatment or prophylaxis of diseases and disorders that are associated with sEH.

40. A method for the treatment or prophylaxis of diseases and disorders that are associatedwith sEH in a human, which method comprises administering an effective amount of a compound of formula (I) according to any one of claims 1 to 33 to the human.

41. The invention as described hereinbefore.

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