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BI- AND POLYCYCLIC SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES, USEFUL 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),DJuKLO Oliv'e (FR),ДЮКЛО Оливье (FR),BISKARRA Sandrin (FR),БИСКАРРА Сандрин (FR,PLETTENBURG OLIVER,ПЛЕТТЕНБУРГ Оливер,LORENTS KATRIN,ЛОРЕНЦ Катрин,LEN MATTIAS,ЛЕН Маттиас,DJUKLO OLIVE,ДЮКЛО Оливье,BISKARRA SANDRIN,БИСКАРРА Сандрин
申请号:
RU2011102460/04
公开号:
RU0002532481C2
申请日:
2009.06.18
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of formula (I), or to its stereoisomeric and/or tautomeric forms and/or to its pharmaceutically acceptable salts, where R1 represents OH; R3, R4, R5 and R8 represents H; R7 represents halogen or (C1-C6) alkyl; R6 represents one (C1-C4)alkylene, bound to a cycloalkyl ring, in which (C1-C4)alkylene forms the second bond with the other carbon atom of the cycloalkyl ring with the formation of a bicyclic ring system, where in the bicyclic ring system one carbon atom is substituted with a group, independently selected from O, S or SO2; and if m and s equal 2 or m equals 3 and s equals 1, R6 represents a group CH2-CH-(CH2)2, which via one group CH2 is bound to the cycloalkyl ring, and two other CH2 groups are bound to different carbon atoms of the cycloalkyl ring, and if m equals 3 and s equals 3, R6 represents two methylene groups, bound to different carbon atoms of the cycloalkyl ring, where the methylene groups or group CH2-CH-(CH2)2 are bound to the carbon atoms of the cycloalkyl ring and form an adamantane system of formula (XX) , where L can be bound to any secondary or tertiary carbon atom, or R6 together with R11 and an N atom form (C5) heterocycloalkyl, bound with the cycloalkyl residue in the form of a spirocyclic ring system, where the bicyclic ring system, or the adamantane system, or a ring system, containing (C5) heterocycloalkyl, represent non-substituted or optionally substituted with substituent R9; R9 represents (C1-C6)alkyl, (C2-C6)alkenyl, (C6)aryl or cyclopropyl R11 and R12 independently on each other represent H or (C1-C6)alkylene-(C6)aryl; n equals 0 or 1; m equals 2 or 3; s equals 1, 2 or 3; L represents O; its stereoisomeric and/or tautomeric forms and/or its pharmaceutically acceptable salts. The invention also relates to the application of a formula (I) compound.EFFECT: novel bi- and polycyclic isoquinoline and isoquinolinone derivati
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