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6-SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES EFFECTIVE AS Rho-KINASE INHIBITORS
专利权人:
SANOFI-AVENTIS
发明人:
PLETTENBURG Oliver (DE),ПЛЕТТЕНБУРГ Оливер (DE),LORENTs Katrin (DE),ЛОРЕНЦ Катрин (DE),LEN Mattias (DE),ЛЕН Маттиас (DE),VESTON Dzhon (DE),ВЕСТОН Джон (DE),KLEEMANN Khajnts-Verner (DE),КЛЕЕМАНН Хайнц-,PLETTENBURG OLIVER,ПЛЕТТЕНБУРГ Оливер,LORENTS KATRIN,ЛОРЕНЦ Катрин,LEN MATTIAS,ЛЕН Маттиас,VESTON DZHON,ВЕСТОН Джон,KLEEMANN KHAJNTS-VERNER,КЛЕЕМАНН Хайнц-Вернер
申请号:
RU2011102376/04
公开号:
RU0002528229C2
申请日:
2009.06.19
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
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-k
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