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    Diaryl sulphide derivatives
    25.
    发明授权
    Diaryl sulphide derivatives 失效
    二芳基硫化物衍生物

    公开(公告)号：US4771062A

    公开(公告)日：1988-09-13

    申请号：US18091

    申请日：1987-02-20

    申请人： Siegfried Raddatz ,  Hans Plumpe ,  Romanis Fruchtmann ,  Christian Kohlsdorfer ,  Bernhard Pelster

    发明人： Siegfried Raddatz ,  Hans Plumpe ,  Romanis Fruchtmann ,  Christian Kohlsdorfer ,  Bernhard Pelster

    IPC分类号： C07D277/18 ,  C07D277/38 ,  C07D277/42 ,  C07D279/06 ,  A61K31/425

    CPC分类号： C07D279/06 ,  C07D277/18 ,  C07D277/42

    摘要： A diaryl sulphide derivative of the formula ##STR1## in which R.sup.1 represents a thiazolamino radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, alkyl, aralkyl or acyl,R.sup.6 and R.sup.6 ' are identical or different and represent hydrogen, alkyl, aralkyl or aryl,R.sup.7 represents alkyl, cycloalkyl, aralkyl, acyl or aryl andn represents the number 1 or 2,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represent a group of the formula ##STR3## wherein R.sup.8 and R.sup.9 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, acyl, trifluoroacetyl, alkylsulphonyl, arylsulphonyl, trifluoromethylphenylsulphonyl or tolylsulphonyl andR.sup.4 has one of the abovementioned meanings or R.sup.1, or represents hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represents a group of the formula ##STR4## wherein R.sup.8 and R.sup.9 have the abovementioned meanings, and salts thereof. Such diaryl sulphide derivatives being useful as active compounds in the treatment and prevention of diseases of the respiratory tract and cardiovascular diseases.

    摘要翻译： 式（I）的二芳基硫化物衍生物，其中R 1表示下式的噻唑烷基：其中R 5表示氢，烷基，芳烷基或酰基，R 6和R 6'相同或不同 代表氢，烷基，芳烷基或芳基，R7代表烷基，环烷基，芳烷基，酰基或芳基，n代表数字1或2，R2和R3相同或不同，代表氢，烷基，烯基，环烷基，烷氧基，烷硫基 ，卤代烷基，卤代烷氧基，卤代烷硫基，芳基，芳烷基，芳氧基，芳烷氧基，芳烷硫基，酰基，羧基，烷氧基羰基，羧基烷基，烷氧基羰基烷基，硝基，氰基或卤素，或表示下式的基团：其中R8和R9相同或 代表氢，烷基，芳基，芳烷基，酰基，三氟乙酰基，烷基磺酰基，芳基磺酰基，三氟甲基苯磺酰基或甲苯磺酰基，R4具有上述含义之一或R 1，或表示氢，烷基，烯基，C 烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，芳基，芳烷基，芳氧基，芳烷氧基，芳烷硫基，酰基，羧基，烷氧基羰基，羧基烷基，烷氧基羰基烷基，硝基，氰基或卤素，或表示下式的基团其中R8 和R9具有上述含义及其盐。 这种二芳基硫化物衍生物可用作活性化合物，用于治疗和预防呼吸道疾病和心血管疾病。

    Enantiomerically pure intermediates for (quinolin-2-yl-methoxy) phenylacetic acids
    26.
    发明授权
    Enantiomerically pure intermediates for (quinolin-2-yl-methoxy) phenylacetic acids 失效
    （喹啉-2-基 - 甲氧基）苯乙酸的对映异构纯中间体

    公开(公告)号：US5473076A

    公开(公告)日：1995-12-05

    申请号：US164674

    申请日：1993-12-08

    申请人： Matthias Decker ,  Klaus-Helmut Mohrs ,  Siegfried Raddatz

    发明人： Matthias Decker ,  Klaus-Helmut Mohrs ,  Siegfried Raddatz

    IPC分类号： A61K31/47 ,  C07B53/00 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/38

    CPC分类号： C07D215/14

    摘要： (Quinolin-2-yl-methoxy)phenylacetic acids are known as inhibitors of enzymatic reactions in the context of arachidonic acid metabolism. Enantiomerically pure (quinolin-2-yl-methoxy)phenylacetic acids can be prepared in a simple manner and in high purity and yield by diastereoselective alkylation of corresponding (quinolin-2-yl-methoxy)phenylacetic acid menthyl esters and subsequent specific removal of the ester radical with acids.

    摘要翻译： （喹啉-2-基 - 甲氧基）苯乙酸在花生四烯酸代谢的情况下被称为酶反应的抑制剂。 对映异构纯的（喹啉-2-基 - 甲氧基）苯乙酸可以通过相应的（喹啉-2-基 - 甲氧基）苯乙酸薄荷酯的非对映选择性烷基化，以简单的方式制备，高纯度和收率，随后特异性地除去 酯基与酸。