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CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES
专利权人:
SANOFI-AVENTIS
发明人:
PLETTENBURG Oliver (DE),ПЛЕТТЕНБУРГ Оливер (DE),LORENTs Katrin (DE),ЛОРЕНЦ Катрин (DE),GERLITTsER Jokhen (DE),ГЕРЛИТЦЕР Йохен (DE),LEN Mattias (DE),ЛЕН Маттиас (DE),BISKARRA Sandrin (FR),БИСКАРРА Санд,PLETTENBURG OLIVER,ПЛЕТТЕНБУРГ Оливер,LORENTS KATRIN,ЛОРЕНЦ Катрин,GERLITTSER JOKHEN,ГЕРЛИТЦЕР Йохен,LEN MATTIAS,ЛЕН Маттиас,BISKARRA SANDRIN,БИСКАРРА Сандрин,ZHANNO FREDERIK,ЖАННО Фредерик,DJUKLO OLI
申请号:
RU2009128652/04
公开号:
RU0002468011C2
申请日:
2007.12.19
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
FIELD: chemistry; pharmaceutics.SUBSTANCE: present invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of formula or stereoisomer and/or tautomer forms thereof, and/or pharmaceutically acceptable salts thereof, where R1 is H or OH; R2 is R', (C7-C8)alkyl, (C1-C6)alkylene-R', (C2-C6)alkenyl; or R2 is (C1-C6)alkyl, under the condition that in said alkyl residue, at least one hydrogen is substituted with OH or OCH3; or R2 is (C1-C6)alkylene, bonded with cycloalkylamine, where (C1-C4)alkylene forms a second bond with another carbon atom of the cycloalkylamine ring and, together with carbon atoms of the cycloalkyalmine, forms a second 5-8-member ring; R3, R5 and R8 denote H; R4 is H, (C1-C6)alkyl or (C1-C6)alkylene-R'; R6 and R6' independently denote H, (C1-C8)alkyl, (C1-C6)alkylene-R' or C(O)O-(C1-C6)alkyl; R7 is H, halogen or (C1-C6)alkyl; n equals 1; m equals 3 or 5; r equals 0 or 1 and L is O(CH2)p, where p=0; where R' is (C3-C8)cycloalkyl, (C6)aryl; where in residues R2-R8 (C6)aryl is unsubstituted or substituted with one or more suitable groups independently selected from halogen, (C1-C6)alkyl, O-(C1-C6)alkyl, where the alkyl group can be substituted with 1-3 halogen atoms. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the compound of formula (I).EFFECT: obtaining novel 6-substituted isoquinoline and isoquinolinone derivatives suitable for treating and/or preventing diseases associated with Rho-kinase and/or Rho-kinase-mediated myosin light chain phosphatase phosphorylation.36 cl, 5 tblНастоящее изобретение относится к 6-замещенным производным изохинолина и изохинолинона формулы (I) или к его стереоизомерным и/или таутомерным формам, и/или к их фармацевтически приемлемым солям, где R1 представляет собой Н или ОН; R2 представляет собой R', (С7-С8)алкил, (С1-С)алкилен-R', (С2-С6)алкенил; или R2 представляет собой (С1-С6)алкил, при условии, что в указанном алкильном остатке по меньшей мере
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