申请人:Bach Thomas Andrew
公开号:US20070135502A1
公开(公告)日:2007-06-14
Compounds of the formula
provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.
该公式化合物提供了对过氧化物酶体增殖物激活受体(PPARs)具有强效激动剂作用的药理制剂。因此,本发明的化合物对于治疗哺乳动物PPAR受体活性介导的疾病是有用的。这些疾病包括:血脂异常、高血脂、高胆固醇血症、动脉粥样硬化、高三酰甘油血症、心力衰竭、心肌梗塞、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸道疾病、眼科疾病、炎症性肠病、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖剂特别有用,用于治疗和预防出现受损的葡萄糖耐受性、高血糖和胰岛素抵抗的疾病,例如1型和2型糖尿病和X综合症。本发明的化合物中,对于同时激活PPARα和PPARγ受体的双重激动剂,更为优选。