申请人:Rhone-Poulenc Sante
公开号:US04783472A1
公开(公告)日:1988-11-08
A compound of the general formula I; ##STR1## in which R is hydrogen or a halogen or an alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, phenoxy or phenylthio group, X is oxygen or sulphur or an imino, alkylimino, phenylimino, benzylimino, sulphinyl, sulphonyl, carbonyl, carbonylmethylene, methylenecarbonyl, carbonylvinylene or vinylenecarbonyl group, or X represents a valency bond or a straight-chain alkylene group containing 1 to 4 carbon atoms and Ar is a phenyl, naphthyl, pyridyl, quinolinyl, isoquinolinyl, thienyl, benzothienyl, thieno[3,2-b]thien-2-yl or thieno[2,3-b]thien-2-yl group, it being possible for the group Ar to be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino or benzamido group; each alkyl moiety containing 1 to 4 straight- or branched-chain carbon atoms; the compound being in separate enantiomeric form or mixtures thereof or a pharmaceutically acceptable salt thereof is useful in the treatment of all the pathological conditions in which PAF-acether may be directly or indirectly implicated.
通式为I的化合物;##STR1## 其中R是氢或卤素或烷基,烷氧基,烷
硫基,三
氟甲基,
氨基,烷基
氨基,二烷基
氨基,羟基,
氰基,羧基,烷基磺酰基,烷基磺酰基,磺酰胺基,烷基磺酰胺基,二烷基磺酰胺基,
氨基甲酰基,烷基
氨甲酰基,二烷基
氨甲酰基,苯基
氨甲酰基,二苯基
氨甲酰基,
吡啶基
氨甲酰基,二
吡啶基
氨甲酰基,苄基,烷基羰基,苯甲酰基,烷氧羰酰基,苯氧羰酰基,烷基羰酰氧基,苯甲酰氧基,烷基羰基
氨基,苯甲酰胺基,苯基,苯氧基或苯
硫基,X是氧或
硫或
亚胺基,烷基
亚胺基,苯基
亚胺基,苄基
亚胺基,磺酰基,磺酰基,羰基,羰基亚甲基,羰基
乙烯基或
乙烯基羰基基团,或X表示价键或含有1到4个碳原子的直链烷基基团,Ar是苯基,
萘基,
吡啶基,
喹啉基,
异喹啉基,
噻吩基,
苯并噻吩基,
噻吩[3,2-b]
噻吩-2-基或
噻吩[2,3-b]
噻吩-2-基团,其中Ar基团可能是未取代或取代一个或多个卤素或烷基,烷氧基,烷
硫基,三
氟甲基,
氨基,烷基
氨基,二烷基
氨基,羟基,
氰基,羧基,烷基磺酰基,烷基磺酰基,磺酰胺基,烷基磺酰胺基,二烷基磺酰胺基,
氨基甲酰基,烷基
氨甲酰基,二烷基
氨甲酰基,苯基
氨甲酰基,二苯基
氨甲酰基,
吡啶基
氨甲酰基,二
吡啶基
氨甲酰基,苄基,烷基羰基,苯甲酰基,烷氧羰酰基,苯氧羰酰基,烷基羰酰氧基,苯甲酰氧基,烷基羰基
氨基,苯甲酰胺基或苯基
氨基基团;每个烷基含有1到4个直链或支链碳原子;该化合物以分离的对映异构体形式或其混合物或其药学上可接受的盐形式在PAF-acether可能直接或间接涉及的所有病理情况的治疗中有用。