申请人:American Home Products Corporation
公开号:US05914339A1
公开(公告)日:1999-06-22
The present invention provides new compounds having anti-diabetic and/or antihyperglycemia and/or anti-obesity activity, as well as pharmaceutical compositions and methods of treatment utilizing the compounds and processes for making the compounds, the compounds having the formula (II): ##STR1## wherein: R.sub.1 and R.sub.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen; R.sub.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl; R.sub.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl; or R.sub.2 and R.sub.3 are joined to form a ring: ##STR2## wherein R' is hydrogen, C.sub.1 to C.sub.6 alkyl, or aryl; R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl; R.sub.7 and R.sub.8 are independently OR.sub.9 or NR.sub.10 R.sub.11 ; R.sub.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, aryl, arylalkyl, alkoxyalkyl, heteroaryl, --CHR.sub.12 COOR.sub.13, --CHR.sub.12 C(O)R.sub.13, --CHR.sub.12 CONR.sub.1 R.sub.11, --CHR.sub.12 OCOOR.sub.13, or --CHR.sub.12 OC(O)R.sub.13, with the provision that R.sub.9 is not hydrogen in both R.sub.7 and R.sub.8 ; R.sub.10 and R.sub.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aralkyl, aryl, furanylalkyl, or alkoxycarbonylalkyl; R.sub.12 and R.sub.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aryl, or aralkyl; and the pharmaceutically acceptable salts thereof, the enantiomers thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.
该发明提供了具有抗糖尿病和/或抗高血糖和/或抗肥胖活性的新化合物,以及利用该化合物的制药组合物和治疗方法以及制备该化合物的方法,该化合物具有以下式子(II): ##STR1## 其中:R.sub.1和R.sub.6独立地为氢、C.sub.1到C.sub.6烷基、三氟甲基、氰基、C.sub.1到C.sub.6烷氧基或卤素;R.sub.2为氢或C.sub.1到C.sub.6三烷基硅基;R.sub.3为氢或C.sub.1到C.sub.6烷氧羰基;或者R.sub.2和R.sub.3连接形成环: ##STR2## 其中R'为氢、C.sub.1到C.sub.6烷基或芳基;R.sub.4和R.sub.5独立地为氢或C.sub.1到C.sub.6烷基;R.sub.7和R.sub.8独立地为OR.sub.9或NR.sub.10R.sub.11;R.sub.9为氢、C.sub.1到C.sub.12烷基、C.sub.1到C.sub.12环烷基、C.sub.1到C.sub.12硅基烷基、芳基、芳基烷基、烷氧基烷基、杂环芳基、--CHR.sub.12COOR.sub.13、--CHR.sub.12C(O)R.sub.13、--CHR.sub.12CONR.sub.1R.sub.11、--CHR.sub.12OCOOR.sub.13或--CHR.sub.12OC(O)R.sub.13,但R.sub.9在R.sub.7和R.sub.8中不同时为氢;R.sub.10和R.sub.11独立地为氢、C.sub.1到C.sub.12烷基、芳基烷基、芳基、呋喃基烷基或烷氧羰基烷基;R.sub.12和R.sub.13独立地为氢、C.sub.1到C.sub.12烷基、芳基或芳基烷基;以及其药学上可接受的盐、对映体、混合物和非对映异构体混合物。