[EN] ANTIDIABETIC AZAINDOLES AND DIAZAINDOLES<br/>[FR] AZAINDOLES ET DIAZAINDOLES ANTIDIABÉTIQUES
申请人:MERCK & CO INC
公开号:WO2009005672A1
公开(公告)日:2009-01-08
Azaindoles and diazaindoles having aromatic substituents on the 5-membered ring are agonists or partial agonists of the PPAR receptor and are useful in the treatment and control of type 2 diabetes and of symptoms of diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Highly functionalized 7-azaindoles as selective PPARγ modulators
作者:Sheryl D. Debenham、Audrey Chan、Fiona WaiYu Lau、Weiguo Liu、Harold B. Wood、Karen Lemme、Lawrence Colwell、Bahanu Habulihaz、Taro E. Akiyama、Monica Einstein、Thomas W. Doebber、Neelam Sharma、Chaunlin F. Wang、Margaret Wu、Joel P. Berger、Peter T. Meinke
DOI:10.1016/j.bmcl.2008.07.103
日期:2008.9
A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPAR gamma modulators (SPPAR gamma Ms). Addition of substituents at the 6-position of the 7-azaindoles improves in vitro potency and pharmacokinetics. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series. (C) 2008 Elsevier Ltd. All rights reserved.