3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME
申请人:Japan Tobacco Inc.
公开号:EP0970954A1
公开(公告)日:2000-01-12
3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I):
wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 4, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.
提供了3-哌啶基-4-氧代喹唑啉衍生物,由式(I)表示:
其中 R 代表氨基或环状氨基,如二苯并氮杂卓,它们各自被取代或未被取代的芳基、取代或未被取代的杂芳基或类似基团取代,n 是 1 至 4 的整数,R3 和 R4 独立地代表氢原子、低级烷基或类似基团,或其药学上可接受的盐。本发明的化合物(I)具有优异的 MTP 抑制活性。因此,这些化合物不仅能抑制导致动脉硬化疾病的低密度脂蛋白的形成,还能调节血液中的总胆固醇、胆固醇和脂蛋白(如低密度脂蛋白),并通过调节 MTP 活性来调节细胞脂质。它们还可用作高脂血症或动脉硬化疾病的新型预防或治疗药物。此外,它们还可用作胰腺炎、肥胖症、高胆固醇血症和高甘油三酯血症的治疗或预防药物。