AMINOPYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS Russian patent published in 2017 - IPC C07D417/14 C07F5/02 C07F9/38 A61K31/4439 A61K31/69 A61K31/662 A61P11/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula IA or a pharmaceutically acceptable salt thereof, where R⁴ represents -CO₂R^4a, -C(O)NH₂ or -CH₂OH; where R^4a is selected from a group consisting of H and CH₃; R⁵ represents H or fluorine; R⁶ is selected from a group consisting of: (i) C₁-C₄ alkyl; (ii) C₁-C₃ fluoroalkyl; (iii) -O-(C₁-C₆ alkyl); (iv) -R^6a, where R^6a selected from a group consisting of: (a) C₃-C₆ cycloalkyl, (b) a group of formula (1b), where R^6a1 represents H or -CH₂CH₂NH₂; and (c) 5-member heteroaryl containing 1–3 heteroatoms selected from a group consisting of N, O and S; where R^6a is unsubstituted or substituted with 1–3 fragments R^6a2, selected from a group consisting of halogen and C₁-C₃ alkyl; (v) -O-R^6b; where R^6b selected from a group consisting of: (a) C₃-C₆ cycloalkyl; and (b) a group of formula (2b), where p equals 1 or 2 and q equals 1 or 2; where R^6b is unsubstituted; and R⁷ represents H or halogen. Invention also relates to a pharmaceutical composition possessing inhibitory activity on Syk, containing an effective amount of compound of formula IA or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier. Disclosed compounds are intended for treating a disease or condition mediated by spleen tyrosine kinase (Syk), selected from a group consisting of asthma or chronic obstructive pulmonary disease.

EFFECT: aminopyridine-containing compounds, which are inhibitors of spleen tyrosine kinase (Syk).

12 cl, 1 dwg, 3 tbl, 44 ex

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(1b), (2b)