56984-32-8Relevant articles and documents
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 1327, (2018/04/17)
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
Discovery and structure-activity relationship study of 4-phenoxythiazol-5-carboxamides as highly potent TGR5 agonists
Chen, Zhixiang,Ning, Mengmeng,Zou, Qingan,Cao, Hua,Ye, Yangliang,Leng, Ying,Shen, Jianhua
, p. 326 - 339 (2016/05/19)
A novel therapy that stimulates endogenous glucagon-like peptide-1 (GLP-1) secretion by Takeda G-protein-coupled receptor 5 (TGR5) agonists might be a superior alternative for the treatment of type 2 diabetes mellitus. A series of 4-phenoxythiazol-5-carboxamides were developed as highly potent TGR5 agonists using a bioisosteric replacement strategy based on the scaffold of 4-phenoxynicotinamides. The structure-activity relationship on the bottom phenyl ring and the thiazole ring was extensively studied, and the 2-methylthiazole derivatives 30c and e displayed the best in vitro potency toward human TGR5, with EC50 values of approximately 1 nM. While endowed with excellent in vitro potency, the 2-methyl-thiazoles were flawed with high microsomal clearance.
Adamantyl-pyrazole carboxamides as inhibitors of 11B-hydroxysteroid dehydrogenase
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Page/Page column 18, (2008/06/13)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.