公开(公告)号：US20100063065A1

公开(公告)日：2010-03-11

申请号：US12088333

申请日：2006-09-28

Applicant: Andrew Ayscough ,  David Rodyney Owen ,  Paul Meo ,  David James Pearson ,  Yvonne Walker ,  Richard Justin Boyce ,  Fabio Zuccotto

Inventor： Andrew Ayscough ,  David Rodyney Owen ,  Paul Meo ,  David James Pearson ,  Yvonne Walker ,  Richard Justin Boyce ,  Fabio Zuccotto

IPC: A61K31/381 ,  C07D333/36 ,  C07D409/10 ,  A61K31/506 ,  A61K31/4436 ,  A61P3/10 ,  A61P3/04 ,  A61P17/02 ,  A61P29/00 ,  A61P25/00

CPC classification number: C07D333/36

Abstract: The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, halo or trihalomethyl; R2 is aryl, heteroaryl, arylalkyl or heteroarylalkyl; R3 is H or F; and L is a linking group comprising a chain of from 2 to 8 atoms linking R and the carbonyl group (A); and pharmaceutically acceptable derivatives thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype δ (PPARδ). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.

Abstract translation: 本发明公开了式（I）的化合物; 其中：R是羧酸或其衍生物; R1是烷基，烯基，炔基，环烷基，烷氧基，烷硫基，卤代或三卤代甲基; R2是芳基，杂芳基，芳基烷基或杂芳基烷基; R3为H或F; L是包含连接R和羰基（A）的2至8个原子的链的连接基团; 和其药学上可接受的衍生物，其可用于治疗由过氧化物酶体增殖物激活受体（PPAR）亚型δ（PPARδ）介导的病症。 因此，本发明的化合物可用于治疗代谢综合征，肥胖症，II型糖尿病，血脂异常，伤口愈合，炎症，神经变性疾病和多发性硬化。