CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLONE DERIVATIVES Russian patent published in 2012 - IPC C07D217/24 C07D401/12 A61K31/472 A61K31/4725 A61K31/5377 A61P9/00 A61P25/28 A61P11/06 A61P3/10 

Abstract RU 2457203 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to novel 6-substituted isoquinolone derivatives of formula

or , or stereoisomeric forms and/or pharmaceutically acceptable salts thereof, where R2 denotes H or (C1-C6)alkyl; R3, R4 and R5 denote H; R6 and R6' independently denote H, (C1-C8)alkyl, (C1-C6)alkylene-R', (C1-C6)alkylene-C(O)O-(C1-C6)alkyl, C(O)-(C1-C6)alkylene-R', or R6 and R6', together with a N atom with which they are bonded form a (C5-C6)heterocyclyl group in which one or more carbon atoms can be substituted with 1, 2 or 3 nitrogen atoms, 1 or 2 oxygen atoms or a combination of different heteroatoms; R7 denotes H, halogen, (C1-C6)alkyl; R8 denotes H; n equals 1; m equals 1, 2, 3, 4 or 5, and L denotes O or O-(C1-C6)alkylene; where, R' denotes (C3-C8)cycloalkyl, (C5-C10)heterocyclyl, (C6-C10)aryl; where in residues R6 and R6' alkyl or alkylene can optionally be substituted one or more times with COOH groups; and where in residues R6 and R6' (C6-C10)aryl and (C5-C10)heterocyclyl are unsubstituted or substituted one or more times with suitable groups independently selected from a group comprising CONH2 and (C1-C6)alkyl; where if m equals 3, R6 cannot denote H; where if m equals 3 and R6 denotes (C1-C8)alkyl, then the alkyl is substituted once or more times, preferably one to three times, with a COOH group. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the disclosed compounds.

EFFECT: novel isoquinolone derivatives which inhibit Rho-kinase and/or Rho-kinase mediated phosphorylation of the myosin light-chain phosphate.

31 cl, 6 tbl

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RU 2 457 203 C2

Authors

Plettenburg Oliver

Khofmajster Armin

Lorents Katrin

Brendel' Joakhim

Len Mattias

Veston Dzhon

Dates

2012-07-27Published

2007-12-19Filed