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    5-(arloxymethyl)oxazolines
    3.
    发明授权
    5-(arloxymethyl)oxazolines 失效
    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。