SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES AS Rho-KINASE INHIBITORS Russian patent published in 2012 - IPC C07D401/12 C07D401/14 A61K31/4725 A61P11/00 

Abstract RU 2455302 C2

FIELD: chemistry.

SUBSTANCE: invention relates to 6-substituted isoquinoline and isoquinolone derivatives of formula (I) where R1 denotes OH; R2 denotes H; R3 denotes H; R4 denotes H, (C1-C6)alkyl; R5 denotes H, halogen; R6 denotes H, (C1-C8)alkyl, (C1-C6)alkyleneR', (C1-C6)alkylene-C(O)NH-(C1-C6)alkyl, (C1-C6)alkylene-C(O)O-(C1-C6)alkyl, C(O) (C1-C6)alkyl, C(O)R1 or C(O)-(C1-C6)alkyleneR'; R7 denotes H, halogen, (C1-C6)alkyl; R8 denotes H; n equals 1, 2, 3 or 4; 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 R4, R6 and R7 alkyl or alkylene can optionally be substituted once or several times with OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONHCH3 or CON(CH3)2; where in residues R4, R6 and R7 alkyl or alkylene can optionally be substituted once or several times with halogen; where in residue R6(C6-C10)aryl and (C5-C10)heterocyclyl are unsubstituted or substituted once or several times with suitable groups independently selected from halogen; where, if m equals 3, R6 does not denote H; and where, if m equals 3 and R6 denotes a residue selected from (C1-C8)alkyl, (C1-C6)alkylene-R'; alkyl, alkylene in said residue is substituted with once or several times, preferably once to three times, with OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONHCH3 or CON(CH3)2; or stereoisomeric forms thereof and/or tautomeric forms thereof and/or pharmaceutically acceptable salts thereof. The invention also relates to use of compounds of formula I to prepare a medicinal agent which inhibits Rho-kinase, as well as to the medicinal agent itself.

EFFECT: novel compounds which can be useful when treating and/or preventing diseases associated with Rho-kinase and/or Rho-kinase-mediated myosin light chain phosphatase phosphorylation are obtained and described.

34 cl, 75 ex, 5 tbl

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RU 2 455 302 C2

Authors

Plettenburg Oliver

Khofmajster Armin

Brendel' Joakhim

Len Mattias

Dates

2012-07-10Published

2007-12-19Filed