671215-76-2Relevant articles and documents
Synthesis and structure-activity relationships of novel zwitterionic compounds as peroxisome proliferator activated receptor α/γ dual agonists with improved physicochemical properties
Shibata, Yoshihiro,Kagechika, Katsuji,Yamaguchi, Mitsuhiro,Yoshikawa, Kenji,Chiba, Kiyoshi,Takano, Hiromichi,Akiyama, Chiyuki,Ono, Mayumi,Nishi, Mina,Kubo, Hideo,Kobayashi, Yoshimasa,Usui, Hiroyuki
, p. 1248 - 1263 (2014/01/06)
We describe herein the design, syntheses and structure-activity relationships (SAR) of novel zwitter-ionic compounds as non-thiazolidinedion (TZD) based peroxisome proliferator activated receptor (PPAR) α/γ dual agonists. In the previous report, we obtained compound 1 showing potent PPARα/γ dual agonistic activities, together with a great glucose lowering effect in the db/db mice. However, this compound possessed fatal issues such as potent cytochrome P450 (CYP)3A4 direct inhibitory activity. Thus, we carried out the medicinal optimization to improve these while maintaining the potent PPAR agonistic activity. As a result, the issues were addressed by changing the furan ring to a low lipophilic 1,3,4-oxadiazole ring. Additionally, these oxadiazole derivatives exhibited a significant decrease in plasma glucose and plasma triglyceride levels without marked weight gain.
SUBSTITUTED ARYLOXAZOLES AND THEIR USE
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Page/Page column 56, (2011/06/23)
The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
Structure-based design of indole propionic acids as novel PPARα/γ co-agonists
Kuhn, Bernd,Hilpert, Hans,Benz, Joerg,Binggeli, Alfred,Grether, Uwe,Humm, Roland,Maerki, Hans Peter,Meyer, Markus,Mohr, Peter
, p. 4016 - 4020 (2007/10/03)
In the quest for novel PPARα/γ co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent PPARα/γ activ
Indolyl derivatives as liver-X-receptor (LXR) modulators
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Page/Page column 23, (2008/06/13)
The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.