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SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES 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),VESTON Dzhon (DE),ВЕСТОН Джон (DE),LEN Mattias (DE),ЛЕН Маттиас (DE),KLEEMANN Khajnts-Verner (DE),КЛЕЕМАНН Хайнц-,PLETTENBURG OLIVER,ПЛЕТТЕНБУРГ Оливер,LORENTS KATRIN,ЛОРЕНЦ Катрин,VESTON DZHON,ВЕСТОН Джон,LEN MATTIAS,ЛЕН Маттиас,KLEEMANN KHAJNTS-VERNER,КЛЕЕМАНН Хайнц-Вернер,DJUKLO OLIVE,ДЮКЛО Оливье,ZHANNO FREDE
申请号:
RU2011102456/04
公开号:
RU0002538588C2
申请日:
2009.06.19
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to substituted isoquinolines and isoquinolinones of formula (I) and to their stereoisomer and/or tautomer forms and/or pharmaceutically acceptable salts, wherein R1 is H, OH or NH2; R3 is H; R4 is H, halogen or (C1-C6)alkylene-R'; R5 is H, halogen, (C1-C6)alkyl; R7 is H, halogen, (C1-C6)alkyl, O-(C1-C6)alkyl; R8 is H; R6 is absent; or is one of (C1-C4)alkylene related to a cycloalkyl ring related to a cycloalkyl ring, wherein (C1-C4)alkylene forms a second bond to another carbon atom of the cycloalkyl ring to form a bicyclic ring system, R10 is H, phenyl, or pyridine, wherein phenyl is unsubstituted or substituted; R11 is H, (C1-C6)alkyl; or R11 and R12 together with the carbon atom to which they are attached form (C3)cycloalkyl; R12 is (C1-C6)alkyl, (C3-C8)cycloalkyl or phenyl; or R12 is H, provided r=2 and another R12 is other than H; or R11 and R12 together with the carbon atom to which they are attached form (C3)cycloalkyl; R13 and R14 are independently H, (C1-C6)alkyl, (C1-C6)alkylene-R', C(O)O-(C1-C6)alkyl, n is equal to 0; m is equal to 1 or 2; s is equal to 1 or 2; r is equal to 1 or 2; L is O, NH; R' is (C3-C8)cycloalkyl, (C6-C10)aryl; wherein in R11 and R12 residues, alkyl is unsubstituted or optionally substituted by one OCH3; wherein in R11 and R12 residues, alkyl is unsubstituted or optionally substituted by one or more halogens; wherein in R10 and R12 residues, (C6-C10)aryl is unsubstituted or optionally substituted by one or two groups optionally specified in halogen, CN, (C1-C6)alkyl, O-(C1-C6)alkyl, SO2-(C1-C6)alkyl, CF3 and OCF3. Also, the invention refers to using a compound of formula (I).EFFECT: there are prepared new isoquinoline and isoquinolinone derivatives effective in treating and preventing the diseases related to Rho-kinase inhibition.38 cl, 132 exИзобретение относится к замещенным изохинолинам и изохинолинонам формулы (I) и к их стереоизомерным и/или таутомерным формам и/или
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