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3. 发明授权

US5686477A 5-(arloxymethyl)oxazolines 失效
标题翻译： 5-（芳氧基甲基）恶唑啉
公开(公告)号：US5686477A
公开(公告)日：1997-11-11
申请号：US556797
申请日：1995-11-02
申请人： Christian Jarry , Isabelle Forfar , Jean-Jacques Bosc , Pierre Renard , Elizabeth Scalbert , Beatrice Guardiola
发明人： Christian Jarry , Isabelle Forfar , Jean-Jacques Bosc , Pierre Renard , Elizabeth Scalbert , Beatrice Guardiola
IPC分类号： A61K31/42 , A61K31/421 , A61K31/44 , A61P9/12 , A61P43/00 , C07D263/28 , C07D413/12 , C07D263/00 , A01N43/76 , C07D263/06
CPC分类号： C07D413/12 , C07D263/28
摘要： The invention relates to compounds of formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are selected, each independently of the other, from hydrogen and an alkyl radical, A is selected from the radicals: ##STR2## wherein: R.sub.3 represents a radical selected from halogen, alkyl, alkoxy, amino, 2-acetyl, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, trifluoromethyl and cyano, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are selected, each independently of the others, from hydrogen, a halogen, an alkyl, alkoxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, cyano and a trifluoromethyl radical, R.sub.9 represents the nitro radical, with the proviso that A cannot represent a grouping selected from: dihalophenyl, trihalophenyl, 4-methylphenyl, 4-chlorophenyl, 4-methoxyphenyl, 4-tert-butylphenyl and 3-(dimethylamino)phenyl, optical isomers thereof in pure form or in the form of a mixture, and pharmaceutically acceptable addition salts thereof with an acid or base, it being understood that: the terms "alkyl" and "alkoxy" represent straight-chained or branched radicals having from 1 to 6 carbon atoms. The compounds of the invention and the pharmaceutical compositions comprising them are proving to be useful in the treatment of disorders associated with I.sub.1 -receptors.
摘要翻译：本发明涉及式（I）化合物：其中：R 1和R 2各自独立地选自氢和烷基，A选自以下基团：其中：R3表示选自卤素，烷基，烷氧基，氨基，2-乙酰基，烷基氨基，二烷基氨基，羧基，烷氧基羰基，三氟甲基和氰基的基团，R4，R5， R6，R7和R8各自独立地选自氢，卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羧基，烷氧基羰基，氰基和三氟甲基，R9表示硝基，条件是 A不能代表选自二卤代苯基，三卤代苯基，4-甲基苯基，4-氯苯基，4-甲氧基苯基，4-叔丁基苯基和3-（二甲基氨基）苯基的基团，其纯的形式或其形式为混合物及其药学上可接受的加成盐与酸或碱反应要求：术语“烷基”和“烷氧基”表示具有1至6个碳原子的直链或支链基团。证明本发明的化合物和包含它们的药物组合物可用于治疗与I1受体相关的病症。

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