BI- AND POLYCYCLIC SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES, USEFUL AS RHO-KINASE INHIBITORS Russian patent published in 2014 - IPC C07D217/24 C07D493/08 C07D495/08 A61K31/472 A61P27/06 A61P9/00 A61P25/28 A61P11/06 A61P13/12 A61P7/00 

FIELD: chemistry.

SUBSTANCE: invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of formula (I), or to its stereoisomeric and/or tautomeric forms and/or to its pharmaceutically acceptable salts, where R₁ represents OH; R₃, R₄, R₅ and R₈ represents H; R₇ represents halogen or (C₁-C₆) alkyl; R₆ represents one (C₁-C₄)alkylene, bound to a cycloalkyl ring, in which (C₁-C₄)alkylene forms the second bond with the other carbon atom of the cycloalkyl ring with the formation of a bicyclic ring system, where in the bicyclic ring system one carbon atom is substituted with a group, independently selected from O, S or SO₂; and if m and s equal 2 or m equals 3 and s equals 1, R₆ represents a group CH₂-CH-(CH₂)₂, which via one group CH₂ is bound to the cycloalkyl ring, and two other CH₂ groups are bound to different carbon atoms of the cycloalkyl ring, and if m equals 3 and s equals 3, R₆ represents two methylene groups, bound to different carbon atoms of the cycloalkyl ring, where the methylene groups or group CH₂-CH-(CH₂)₂ are bound to the carbon atoms of the cycloalkyl ring and form an adamantane system of formula (XX) , where L can be bound to any secondary or tertiary carbon atom, or R₆ together with R₁₁ and an N atom form (C₅) heterocycloalkyl, bound with the cycloalkyl residue in the form of a spirocyclic ring system, where the bicyclic ring system, or the adamantane system, or a ring system, containing (C₅) heterocycloalkyl, represent non-substituted or optionally substituted with substituent R₉; R₉ represents (C₁-C₆)alkyl, (C₂-C₆)alkenyl, (C₆)aryl or cyclopropyl R₁₁ and R₁₂ independently on each other represent H or (C₁-C₆)alkylene-(C₆)aryl; n equals 0 or 1; m equals 2 or 3; s equals 1, 2 or 3; L represents O; its stereoisomeric and/or tautomeric forms and/or its pharmaceutically acceptable salts. The invention also relates to the application of a formula (I) compound.

EFFECT: novel bi- and polycyclic isoquinoline and isoquinolinone derivatives, useful as inhibitors of Rho-kinase, are obtained.

22 cl, 22 ex