申请人:Nippon Zoki Pharmaceutical Co., Ltd.
公开号:US05900426A1
公开(公告)日:1999-05-04
Benzothiazole derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component possess a lipid lowering activity and are useful pharmaceuticals for the treatment of hyperlipemia. The lipid lowering agents are of the formula: ##STR1## wherein R.sub.1 is halogen, trifluoromethyl, acetamido or --OX.sub.1 ; X.sub.1 is hydrogen, alkyl or acyl; R.sub.2 is hydrogen, halogen, alkyl, hydroxyalkyl, trifluoromethyl, nitro, amino which may be substituted with alkyl or acyl, carboxy which may be esterified with alkyl, or --OX.sub.2 ; X.sub.2 is hydrogen, alkyl, acyl, carboxyalkyl which may be esterified with alkyl; n is an integer from 1 to 3 denoting the number of substituents R.sub.2 ; and plural R.sub.2 may be the same or different when n is 2 or 3; with the proviso that R.sub.1 is a group other than halogen when R.sub.2 is hydrogen. The benzothiazole derivatives and their pharmaceutically acceptable salts significantly decrease cholesterol, triglyceride and low-density lipoprotein in blood.
苯并噻唑衍生物及其药学上可接受的盐,以及含有该化合物作为有效成分的治疗剂具有降脂作用,是治疗高脂血症的有用药物。降脂剂的化学式为:##STR1## 其中R.sub.1是卤素,三氟甲基,乙酰胺或--OX.sub.1; X.sub.1是氢,烷基或酰基; R.sub.2是氢,卤素,烷基,羟基烷基,三氟甲基,硝基,氨基(可能被烷基或酰基取代),羧基(可能被烷基酯化),或--OX.sub.2; X.sub.2是氢,烷基,酰基,羧基烷基(可能被烷基酯化); n是1至3的整数,表示取代基R.sub.2的数量; 当n为2或3时,多个R.sub.2可以相同或不同; 假设当R.sub.2为氢时,R.sub.1是除卤素以外的其他基团。苯并噻唑衍生物及其药学上可接受的盐显著降低血液中的胆固醇、甘油三酯和低密度脂蛋白。