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Noncyclic 1,3-Dicarbonyl compounds as dual PPAR agonists with potent antihyperglycemic and antihyperlipidemic activity

机译:非环状1,3-二羰基化合物作为双重PPAR激动剂,具有有效的降血糖和降血脂活性

摘要

Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification. These compounds, as peroxisome proliferator-activated receptor (PPAR) dual agonists for both RXR/PPARgamma and RXR/PPARalpha heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders. embedded image
机译:公开了式I的新型非环状1,3-二羰基化合物的制备和药物用途,其中环A,环B,R 1 ,R 2 ,R 3 ,R 4 ,R 5 ,X,Y,Z,Q,Ar和n如规范中所定义。这些化合物作为RXR / PPARgamma和RXR / PPARalpha异二聚体的过氧化物酶体增殖物激活受体(PPAR)双激动剂,可用于治疗和/或预防2型糖尿病和相关的代谢综合征,例如高血压,肥胖,胰岛素抵抗,高脂血症,高血糖症,高胆固醇血症,动脉粥样硬化,冠状动脉疾病和其他心血管疾病。 <图像alt =“嵌入式图像” file =“ US20070142427A1-20070621-C00001.GIF” he =“ 26.50mm” imgContent =“ chem” imgFormat =“ GIF” wi =“ 70.95mm“ />

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