COMPOUNDS OF SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZOL [1,2-a]-3-CARBOXAMIDE AS cFMS INHIBITORS Russian patent published in 2015 - IPC C07D471/04 A61K31/437 A61K31/4162 A61P9/00 A61P19/08 A61P29/00 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel formula I compounds and their pharmaceutically acceptable salts, which are cFMS inhibitors and are useful in treatment of bone diseases, cancer, autoimmune disorders, inflammatory diseases, cardio-vascular diseases and anaesthetics. Invention relates to versions of method of obtaining said compounds, pharmaceutical composition and method of treating bone diseases on their basis. In general formula

R¹ represents hetAr¹CH₂-, hetAr²CH₂-, (3-6Ccycloalkyl)-CH₂-, benzyl, which is optionally substituted with (1-4C)alkoxy, or N-(1-3Calkyl)pyridinonyl-CH₂-, which is optionally substituted with one or more substituents, independently selected from (1-6C)alkyl; hetAr¹ is pyridyl, optionally substituted with one or more substituents, independently selected from (1-6C)alkyl, (1-4C)alkoxy, halogen, hetCyc¹, hetCyc¹-CH₂-, amino(2-4C)alkoxy, [di(1-3Calkyl)amino](2-4C)alkoxy, dihydroxy(3-4C)alkoxy, hetCyc²O-, hetCyc^2a(l-2C)alkoxy and OH; hetCyc¹ is 6-membered heterocycle, which has 1-2 N atoms in ring and optionally substituted with NH₂; hetCyc² and hetCyc^2a independently are 5-6-membered heterocycles, which have 1-2 N atoms in ring and are optionally substituted with one or more substituents, independently selected from (1-6C)alkyl, OH and halogen; hetAr² is 5-membered heteroaryl ring, which has 2-3 heteroatoms in ring, independently selected from N, S and O, where, at least, one of said heteroatoms is N, where said ring is optionally substituted with one or more substituents, independently selected from (1-6C)alkyl, (2-4C)hydroxyalkyl, (3-4C)dihydroxyalkyl, (3-6Ccycloalkyl)CH₂-, hetCyc³, hetCyc^3a(1-2C)alkyl and benzyl, optionally substituted with (1-4C)alkoxy; hetCyc³ and hetCyc^3a independently are 6-membered heterocyclic rings, which have 1-2 N atoms in ring and optionally substituted with halogen; R² is (2-4C)alkyl, cyclopropyl, OMe, I or Br; R³ is H or Cl; R⁴ is H or CN; R⁵ is H, halogen, OH, hetAr³, hetAr⁴, hetAr⁵, hetCyc⁴, hetCyc⁵C(=O)-, hetCyc⁶(1-4Calkyl)-, hetCyc⁷(1-4C)alkoxy, (hetCyc⁸)-O-, hetCyc⁹(l-4C)alkoxy, (1-3Calkoxy)(1-4C)alkoxy, hydroxy(1-4C)alkoxy, dihydroxy(2-4C)alkoxy, difluoramino(1-4C)alkoxy, [(1-4Calkoxy)carbonylamide]difluoro(1-4C)alkoxy, (1-4Calkyl)C(=O)NH[(2-4C)alkylthio-, (1-4Calkyl)OC(=O)-, [di(1-4Calkyl)amino](1-4C)alkyl, R′R″NC(=O)-, 1-6Calkylthio, benzyloxy, [hydroxy(1-4C)alkoxy](1-4C)alkoxy or [(2-4Calkenyloxy)(1-4C)alkoxy](1-4C)alkoxy. Values of other substituents are given in invention formula.

EFFECT: obtaining compounds, which are inhibitors of cFMS and are useful in treatment of bone diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, and anaesthetics.

35 cl, 3 tbl, 162 ex