公开(公告)号：US5710152A

公开(公告)日：1998-01-20

申请号：US791269

申请日：1997-01-30

申请人： Yoshihiro Nagao ,  Yoshikuni Ito ,  Jiro Kotake ,  Tadayuki Kouda ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

发明人： Yoshihiro Nagao ,  Yoshikuni Ito ,  Jiro Kotake ,  Tadayuki Kouda ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D417/12 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54

CPC分类号： C07D417/12

摘要： A benzoazine derivative represented by the following formula (1), ##STR1## wherein R.sup.1 represents an alkyl group, alkoxy group, halogen atom, halogenoalkyl group, amino group, hydroxy group, benzyloxy group which may have a substituent, cyano group, carbamoyl group, acyl group, nitro group, carboxy group, or sulfonamide group; R.sup.2 and R.sup.3 may be the same or different and each individually represents a hydrogen atom or an alkyl group, or R.sup.2 and R.sup.3 indicate in combination an alkylene group having 2-7 carbon atoms; R.sup.4 and R.sup.5 may be the same or different and each individually represents a hydrogen atom or an alkyl group; X denotes O, S, or N--R.sup.6 (wherein R.sup.6 represents a hydrogen atom, an alkyl group, or an aryl group or pyridyl group which may have a substituent); m is an integer from 0 to 4; and n is an integer from 1 to 3, or a salt of the benzoazine derivative. The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity.

摘要翻译： 由下式（1）表示的苯并嗪衍生物，其中R1表示烷基，烷氧基，卤素原子，卤代烷基，氨基，羟基，可具有取代基的苄氧基，氰基 ，氨基甲酰基，酰基，硝基，羧基或磺酰胺基; R2和R3可以相同或不同，各自独立地表示氢原子或烷基，或R2和R3组合表示具有2-7个碳原子的亚烷基; R 4和R 5可以相同或不同，各自独立地表示氢原子或烷基; X表示O，S或N-R6（其中R6表示氢原子，烷基或可具有取代基的芳基或吡啶基）; m为0〜4的整数; n为1〜3的整数，或苯并嗪衍生物的盐。 该化合物对于降低血糖值，血浆胰岛素值和血浆甘油三酯值具有优异的效果，并且可用作预防或治疗糖尿病，高脂血症和肥胖症的药物。