P38 KINASE-INHIBITING ISOQUINOLINE DERIVATIVES Russian patent published in 2014 - IPC C07D401/06 A61K31/472 A61K31/4725 A61K31/496 A61K31/55 A61P11/06 

FIELD: chemistry.

SUBSTANCE: claimed invention relates to isoquinolinone derivatives of formula (I) or to its pharmaceutically acceptable salt, where R1 represents (C₁-C₅)alkyl, possibly substituted with 1, 2 or 3 groups, independently selected from groups -(C₁-C₆)alkyl, -(C₁-C₆)alkyloxy, -OH or -(C₁-C₆)alkyl-hydroxy, and where one independent substituent of R1 radical, representing -(C₁-C₆)alkyl, can be possibly condensed with other independent substituent of R1 radical, representing -(C₁-C₆)alkyl, with formation of saturated (C₃-C₄)cycloalkyl; R2 represents H; R3 represents (CH₂)_d-Y and R3 is independently possibly substituted with one or two groups -(C₁-C₆)alkyl, -NH₂, -HN(C₁-C₆)alkyl, -N-di-(C₁-C₆)alkyl, -(C₁-C₆)alkyl-NH₂, -(C₁-C₆)alkyl-hydroxy; Y us selected from heterocycloalkyl, S-(O)_e-heterocycloalkyl, S-(O)_e-(C₁-C₆)alkyl- heterocycloalkyl, -SO₂NH-(C₁-C₆)alkyl; d equal 0, 1 and 2; e equals o, 1 or 2; R4 and R5 are independently selected from (C₁-C₆)alkyl and halogeno; R6 represents H; heterocycloalkyl represents C- or N-bound 5-7-membered non-aromatic cyclic ring, which, when it is C-bound, contains one NR7 atom, and when it is N-bound, contains one N-atom, or one N-atom and one NR7 atom, R7 represents H or (C₁-C₆)alkyl. Invention also relates to application of formula (I) compound in treatment of chronic obstructive pulmonary disease (COPD) and asthma.

EFFECT: obtained are novel isoquinoline derivatives, possessing useful biological properties.

21 cl, 9 tbl, 67 ex