MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS Russian patent published in 2016 - IPC C07D471/22 C07D498/22 C07D487/22 A61K31/519 A61P35/00 A61P33/02 A61P25/28 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula I or its pharmaceutically acceptable salts, which are inhibitors of Trk kinases and are useful for treating pain, malignant oncological disease, inflammation, neurodegenerative diseases and Trypanasoma Crusi infections. Invention also describes versions of methods of producing compound of formula I. In Formula I (I) ring A is selected from A-1, A-2, A-3, having structure , where wavy line marked 1 indicates connection point of ring A to ring B, and wavy line marked 2 indicates point of connection ring A to W; X is N or CH; Y is H or F; R¹ is H or halogen; ring B is selected from rings B-1 and B-2, having structure , where wavy line marked 3 indicates point of connection to ring A, and wavy line marked 4 indicates point of connection to pyrazolo[1,5-a]pyrimidine ring of formula I; W is O, NH or CH₂, wherein, when ring A is A-2, then W is CH₂; m is 0, 1 or 2; D is carbon, R² and R^2a independently represent H, F, (1-3C)alkyl or OH (provided that R² and R^2a are not simultaneously OH), and R³ and R^3a are independently H or (1-3C)alkyl, or (D) is carbon or nitrogen, R² and R³ are absent, and R^2a and R^3a together with atoms to which they are bonded, form 5-6-member heteroaryl ring containing 1-2 heteroatoms ring; Z is *-NR^4aC(=O)-, *-ONHC(=O)-, *-NR^4bCH₂- or *-OC(=O)-, where asterix indicates connection point of Z to containing carbon R³; R^4a is H or (1-6C)alkyl; R^4b is H, (1-6C)alkyl, ((1-6C)alkyl)C(O)-, HOCH₂C(O)-, ((1-6 C)alkyl) sulfonyl, HO₂CCH₂- or ((1-6C)alkyl)NH(CO)-; and R-⁵ and R⁶ independently represent H, halogen, OH or (1-6C)alkyl.

EFFECT: useful for treating pain, malignant oncological disease, inflammation, neurodegenerative diseases and Trypanasoma Crusi infections.

73 cl, 1 tbl, 45 ex