- ANTIDIABETIC AZAINDOLES AND DIAZAINDOLES
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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.
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Page/Page column 66-67
(2009/03/07)
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- Highly functionalized 7-azaindoles as selective PPARγ modulators
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A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARγ modulators (SPPARγMs). 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.
- Debenham, Sheryl D.,Chan, Audrey,Lau, Fiona WaiYu,Liu, Weiguo,Wood, Harold B.,Lemme, Karen,Colwell, Lawrence,Habulihaz, Bahanu,Akiyama, Taro E.,Einstein, Monica,Doebber, Thomas W.,Sharma, Neelam,Wang, Chaunlin F.,Wu, Margaret,Berger, Joel P.,Meinke, Peter T.
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supporting information; experimental part
p. 4798 - 4801
(2009/06/17)
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