申请人:American Home Products Corporation
公开号:US05438056A1
公开(公告)日:1995-08-01
The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.8 is alkyl containing 1 to 3 carbon atoms which possess blood-glucose lowering activity, to processes for preparation thereof, pharmaceutical compositions comprising the same, and to the method of using the same in the reduction of excess cholesterol in human beings and animals.
本发明的化合物具有以下结构式: ##STR1## 其中R.sup.1和R.sup.2分别独立为苯基,吡啶基,噻吩基,萘基,取代苯基,其中取代基选择自卤素,甲氧基和二烷基氨基,其中烷基含有1至3个碳原子;或R.sup.1和R.sup.2分别为以下结构的取代呋喃酮: ##STR2## 其中R.sup.5和R.sup.6分别独立为含有1至3个碳原子的烷基,含有5至7个碳原子的环烷基,苯基或取代苯基,其中取代基为含有1至5个碳原子的烷基或卤素;R.sup.7为氢或卤素;或R.sup.1和R.sup.2连接形成以下结构: ##STR3## 其中R.sup.3和R.sup.4分别独立为氢,含有4至20个支链、直链、环状、饱和或不饱和碳原子的烷基;或R.sup.3和R.sup.4连接形成以下结构: ##STR4## 其中R.sup.8为含有1至3个碳原子的烷基,具有降低血糖作用,本发明还涉及制备该化合物的方法,包含该化合物的制药组合物,以及在人体和动物中减少多余胆固醇的方法。