BRUTON'S TYROSINE KINASE INHIBITORS Russian patent published in 2017 - IPC C07D487/04 A61K31/519 A61P19/02 A61P11/06 A61P29/00 A61P37/00 

FIELD: pharmacology.

SUBSTANCE: compounds can be used as therapeutically active substances for the treatment of inflammatory and/or autoimmune conditions selected from rheumatoid arthritis and asthma. In formula I

A is phenyl, n is 1 or 2, R¹ is CH₂NHC(=O)R^1' or CH₂NHC(=O)CH₂NHR^1', where n is 1. And one R¹ is halogen, and the other R¹ represents CH₂NHC(=O)R^1' or CH₂N(CH₃)C(=O)R^1', when n is 2. R^1' represents a lower alkoxy group, phenyl, an unsaturated or partially unsaturated 8-9-membered bicyclic heterocycle containing 1-2 heteroatoms in the bicyclic system selected from nitrogen and sulfur, or a 4-6-membered monocyclic heteroaryl with 1-3 heteroatoms selected from nitrogen, oxygen and sulfur, or a 4-5-membered heterocycloalkyl containing oxygen or nitrogen atoms as heteroatoms, optionally substituted by one or more R^1". Each radical R^1" is an independent lower alkyl, halogen, 3-6-membered cycloalkyl, 4-membered heterocycloalkyl with an oxygen atom as a heteroatom, lower alkyl-4-membered heterocycloalkyl with an oxygen atom as a heteroatom, oxo group, cyano-lower alkyl, hydroxyl-lower alkyl or lower alkoxy group. R² is H, R³ or R⁴. R³ represents C(=O)OR^3', C(=O)R^3' or C(=O)NH(CH₂)₂R^3'. R^3' is H, a lower alkyl, 6-membered heterocycloalkyl with 1-2 heteroatoms selected from nitrogen and oxygen, an amino group or OH. R^4' is a pyrasolyl possibly substituted with R^4'. And R^4' is a methyl, CH₂-CH₂N(CH₃)₂, CH₂C(=O)OCH₂CH₃, CH₂C(=O)OH or CH₂CH₂OH.

EFFECT: increased efficiency of treatment.

18 cl, 2 tbl, 51 ex