6-SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES EFFECTIVE AS Rho-KINASE INHIBITORS Russian patent published in 2014 - IPC C07D217/24 C07D217/22 C07D405/12 C07D409/12 C07D417/12 A61K31/472 A61K31/4725 A61P9/04 A61P9/12 A61P11/06 A61P13/12 A61P27/06 A61P7/00 A61P25/28 

Abstract RU 2528229 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 6-substituted isoquinoline and isoquinolinone derivatives of formula or to its stereoisomer and/or tautomer forms and/or a pharmaceutically acceptable salt, wherein R1 represents H, OH or NH2; R3 represents H; R4 represents H, a halogen atom, CN or (C1-C6)alkylene-(C6-C10)aryl; R5 represents H, a halogen atom, (C1-C6)alkyl; R7 represents H, a halogen atom, (C1-C6)alkyl, O-(C1-C6)alkyl; R8 represents H; R9 and R6 are absent; R10 represents (C1-C6)alkyl, (C1-C8)heteroalkyl, (C3-C8)cycloalkyl, (C6)hetrocycloalkyl, (C1-C6)alkylene-(C3-C8)cycloalkyl, (C1-C6)alkylene-(C6-C10)aryl, (C1-C6)alkylene-(C6)heterocycloalkyl; R11 represents H; R12 represents (C1-C6)alkyl, (C3-C8)cycloalkyl, (C5)heteroaryl or (C6-C10)aryl; R13 and R14 independently represent H, (C1-C6)alkyl, (C1-C6)alkylene-R'; n is equal to 0; m is equal to 2 or 3; s is equal to 1 or 2; r is equal to 1; L represents O or NH; R' represents (C3-C8)cycloalkyl, (C6-C10)aryl; wherein in the rests, R10, R12-R14 alkyl or alkylene are unsubstituted or optionally substituted by one or more OCH3; wherein in the rests, R10, R12-R14 alkyl or alkylene are unsubstituted or optionally substituted by one or more halogen atoms; wherein (C1-C8)heteroaryl group means (C1-C8)alkyl groups, wherein at least one carbon atom is substituted by O;. (C6)heterocycloalkyl group means a monocyclic carbon ring system containing 6 ring atoms wherein one carbon atom can be substituted by 1 oxygen atom or 1 sulphur atom which can be optionally oxidated; (C5)heteroaryl means a monoring system wherein one or more carbon atoms can be substituted by 1 nitrogen atom or 1 sulphur atom or a combination of various heteroatoms. Also, the invention refers to using the compound of formula (I) and to a therapeutic agent based on the compound of formula (I).

EFFECT: there are prepared new compounds effective for treating and/or preventing diseases associated with Rho-kinase and/or mediated by Rho-kinase by phosphorylation of myosin light chain phosphatase, and the compositions containing these compounds.

32 cl, 111 ex

Similar patents RU2528229C2

Title Year Author Number
SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES AS Rho-KINASE INHIBITORS 2009
  • Plettenburg Oliver
  • Lorents Katrin
  • Veston Dzhon
  • Len Mattias
  • Kleemann Khajnts-Verner
  • Djuklo Oliv'E
  • Zhanno Frederik
RU2538588C2
CYCLOHEXYLAMINIZOQUINOLONE AS Rho-KINASE INHIBITORS 2006
  • Plettenburg Oliver
  • Khofmajster Armin
  • Kaderajt Diter
  • Brendel' Joakhim
  • Len Mattias
RU2440988C2
CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLONE DERIVATIVES 2007
  • Plettenburg Oliver
  • Khofmajster Armin
  • Lorents Katrin
  • Brendel' Joakhim
  • Len Mattias
  • Veston Dzhon
RU2457203C2
SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES AS Rho-KINASE INHIBITORS 2007
  • Plettenburg Oliver
  • Khofmajster Armin
  • Brendel' Joakhim
  • Len Mattias
RU2455302C2
BI- AND POLYCYCLIC SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES, USEFUL AS RHO-KINASE INHIBITORS 2009
  • Plettenburg Oliver
  • Lorents Katrin
  • Len Mattias
  • Djuklo Oliv'E
  • Biskarra Sandrin
RU2532481C2
CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES 2007
  • Plettenburg Oliver
  • Lorents Katrin
  • Gerlittser Jokhen
  • Len Mattias
  • Biskarra Sandrin
  • Zhanno Frederik
  • Djuklo Oliv'E
RU2468011C2
PIPERADINYL-SUBSTITUTED ISOQUINOLONE DERIVATIVES AS Rho-KINASE INHIBITORS 2006
  • Plettenburg Oliver
  • Khofmajster Armin
  • Kaderajt Diter
  • Brendel' Joakhim
  • Len Mattias
RU2414467C2
ISOQUINOLINE DERIVATIVES AS Rho-KINASE INHIBITORS 2006
  • Plettenburg Oliver
  • Khofmajster Armin
  • Kaderajt Diter
  • Pojkert Shtefan
  • Ruf Sven
  • Ritter Kurt
  • Len Mattias
  • Ivashchenko Jurij
  • Moneke Peter
  • Drejer Mattias
  • Kannt Ajmo
RU2443688C2
SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE 2014
  • Xi Ning
  • Wang Liang
  • Wang Tingjin
RU2683793C2
TRICYCLIC COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM AND USING THEM FOR TREATING IMMUNOLOGICAL AND ONCOLOGICAL COMPOUNDS 2009
  • Uishart Nejl
  • Ardzhiriadi Mariya A.
  • Koldervud Devid Dzh.
  • Eriksson Anna M.
  • Fiamengo Brajan A.
  • Frenk Kristin E.
  • Fridman Majkl
  • Dzhordzh Don M.
  • Godken Erik R.
  • Dzhozefson Natan S.
  • Li Bitsin S.
  • Morytko Majkl Dzh.
  • Styuart Kent D.
  • Voss Dzheffri V.
  • Uollejs Grir A.
  • Van Lu
  • Voller Kevin R.
RU2545023C9

RU 2 528 229 C2

Authors

Plettenburg Oliver

Lorents Katrin

Len Mattias

Veston Dzhon

Kleemann Khajnts-Verner

Dates

2014-09-10Published

2009-06-19Filed