Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity

US7268157B2 · kind B2 · utility

Assignees

• SHENZHEN CHIPSCREEN BIOSCIENCES CO., LTD. · CN
• Research Institute of Tsinghua University · CN

Inventors

• Xian-Ping Lu · San Diego, US
• Zhibin Li · Yuanjiang Hani, Yi and Dai Autonomous County, CN
• Chenzhong Liao · Tangxia, CN
• Leming Shi · Shanghai, CN
• Zhende Liu · Hangzhou City, CN
• Baoshun Ma · Tangxia, CN
• Zhiqiang Ning · Tangxia, CN
• Song Shan · Nanhu, CN
• Tuo Deng · Tangxia, CN

Key dates

• Filing date: Nov 18, 2003
• Grant date: Sep 11, 2007
• Expiry date: Jul 8, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D213/50
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta 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 with improved side effects profile commonly associated with conventional PPARgamma agonists.