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    Anthranilic acid analogs
    8.
    发明授权
    Anthranilic acid analogs 失效
    邻氨基苯甲酸类似物

    公开(公告)号：US6046239A

    公开(公告)日：2000-04-04

    申请号：US128493

    申请日：1998-08-03

    申请人： Joseph Richard Lennox ,  Schuyler Adam Antane ,  John Anthony Butera

    发明人： Joseph Richard Lennox ,  Schuyler Adam Antane ,  John Anthony Butera

    IPC分类号： A61K31/192 ,  A61K31/27 ,  A61K31/455 ,  A61K31/195

    CPC分类号： A61K31/27 ,  A61K31/192 ,  A61K31/455

    摘要： Compounds of the formula: ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 alkylsulfinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 alkylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.15 is hydrogen, metal cation, acetylamido, alkoxyacetoyl or a related moiety which delivers the carboxylate in vivo;the dotted line is an optional double bond; with the proviso that when R.sub.10 is an alkylidene moiety, the double bond is absent; andW is nitrogen or carbon bearing a hydrogen, or R.sub.4, R.sub.5 or R.sub.6 as hereinbefore defined; or pharmaceutical salts thereof, are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel and chloride channel modulation.

    摘要翻译： 下式的化合物：其中：R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8独立地是氢，COOR 15，卤素，硝基，氰基，C 1-10烷氧基，C 1-10卤代烷氧基，磺酸，C 1 -10烷基磺酰基，C6-12芳基磺酰基，C6-12芳烷基磺酰基，C1-10烷基亚磺酰基，C6-12烷基亚磺酰基，C6-12芳烷基亚磺酰基，氨磺酰基，C1-10烷基磺酰氨基，C6-12烷基磺酰氨基，C1-10烷酰基，C6-12芳基 ，C 6-12芳烷酰基，氨基，C 1-10烷基氨基，C 2-10二烷基氨基，C 6-12芳烷基氨基，C 6-12芳基氨基，甲酰氨基，C 1-10烷基羧酰氨基，C 6-12芳基羧酰胺基，C 1-10卤代烷基，C 1-10烷基， C2-12烯基，C6-12芳基，C6-12芳烷基; 条件是R4和R5中的至少一个是COOR15; R9是氢，C1-10烷基和C1-10卤代烷基; R10是氢，C1-10烷基，C1-10卤代烷基或C2-12亚烷基; R15是氢，金属阳离子，乙酰氨基，烷氧基乙酰基或在体内递送羧酸盐的相关部分; 虚线是可选的双键; 条件是当R 10是亚烷基部分时，双键不存在; 并且W是带有氢的氮或碳，或如上文所定义的R4，R5或R6; 或其药用盐可用于治疗通过钾通道和氯化物通道调节与平滑肌收缩相关的病症。