CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES Russian patent published in 2012 - IPC C07D217/24 C07D217/22 A61K31/472 A61P9/12 A61P9/10 A61P27/02 A61P25/28 A61P35/00 A61P31/20 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: present invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of formula or stereoisomer and/or tautomer forms thereof, and/or pharmaceutically acceptable salts thereof, where R₁ is H or OH; R₂ is R', (C₇-C₈)alkyl, (C₁-C₆)alkylene-R', (C₂-C₆)alkenyl; or R₂ is (C₁-C₆)alkyl, under the condition that in said alkyl residue, at least one hydrogen is substituted with OH or OCH₃; or R₂ is (C₁-C₆)alkylene, bonded with cycloalkylamine, where (C₁-C₄)alkylene forms a second bond with another carbon atom of the cycloalkylamine ring and, together with carbon atoms of the cycloalkyalmine, forms a second 5-8-member ring; R₃, R₅ and R₈ denote H; R₄ is H, (C₁-C₆)alkyl or (C₁-C₆)alkylene-R'; R₆ and R₆' independently denote H, (C₁-C₈)alkyl, (C₁-C₆)alkylene-R' or C(O)O-(C₁-C₆)alkyl; R₇ is H, halogen or (C₁-C₆)alkyl; n equals 1; m equals 3 or 5; r equals 0 or 1 and L is O(CH₂)_p, where p=0; where R' is (C₃-C₈)cycloalkyl, (C₆)aryl; where in residues R₂-R₈ (C₆)aryl is unsubstituted or substituted with one or more suitable groups independently selected from halogen, (C₁-C₆)alkyl, O-(C₁-C₆)alkyl, where the alkyl group can be substituted with 1-3 halogen atoms. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the compound of formula (I).

EFFECT: obtaining novel 6-substituted isoquinoline and isoquinolinone derivatives suitable for treating and/or preventing diseases associated with Rho-kinase and/or Rho-kinase-mediated myosin light chain phosphatase phosphorylation.

36 cl, 5 tbl