903886-65-7Relevant academic research and scientific papers
Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy
Nishiura, Yuji,Matsumura, Akira,Kobayashi, Naotake,Shimazaki, Atsuyuki,Sakamoto, Shingo,Kitade, Naohisa,Tonomura, Yutaka,Ino, Akira,Okuno, Takayuki
, p. 2498 - 2503 (2018)
Novel acetyl-CoA carboxylase 2 (ACC2) selective inhibitors were identified by the conversion of the alkyne unit of A-908292 to the olefin linker. Modification of the center and left part of the lead compound 1b improved the ACC2 inhibitory activity and CY
NOVEL OLEFIN DERIVATIVE
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Paragraph 0557-0559, (2015/09/28)
The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound. A compound of formula (I′): wherein R1 is substituted or unsubstituted aryl etc., R2 is each independently hydrogen, substituted or unsubstituted alkyl etc., R3 is each independently hydrogen, substituted or unsubstituted alkyl etc., n is an integer from 0 to 3, R12 is hydrogen, substituted or unsubstituted alkyl etc., Ring A is aromatic carbocycle or aromatic heterocycle, R9 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., m is an integer from 0 to 4, R4 and R5 is each independently hydrogen, substituted or unsubstituted alkyl etc., R6 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., R13 is hydrogen, substituted or unsubstituted alkyl etc., X5 is bond etc., R7 is hydrogen or substituted or unsubstituted alkyl, R8 is substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted alkenylcarbonyl etc.
THIAZOLE COMPOUNDS USEFUL AS ACETYL-COA CARBOXYLASE (ACC) INHIBITORS
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Page/Page column 56, (2013/03/15)
The present invention provides thiazole compounds of Formula I or its pharmaceutically acceptable salts, prodrugs, solvates, N-oxide thereof; solvates of pharmaceutically acceptable salts and N-oxides; pharmaceutically acceptable salts of N-oxides, or prodrugs; or combination or mixtures thereof; (I) The present invention further provides a method for preventing or treating a condition that responds to an Acetyl-CoA Carboxylase (ACC) inhibitor by using compounds of formula (I) or ), its pharmaceutically acceptable salts, prodrugs, solvates, N-oxide thereof; solvates of pharmaceutically acceptable salts and N-oxides; pharmaceutically acceptable salts of N-oxides, or prodrugs; or combination or mixtures thereof.
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy) thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors
Gu, Yu Gui,Weitzberg, Moshe,Clark, Richard F.,Xu, Xiangdong,Li, Qun,Zhang, Tianyuan,Hansen, T. Matthew,Liu, Gang,Xin, Zhili,Wang, Xiaojun,Wang, Rongqi,McNally, Teresa,Camp, Heidi,Beutel, Bruce A.,Sham, Hing L.
, p. 3770 - 3773 (2007/10/03)
A structurally novel acetyl-CoA carboxylase (ACC) inhibitor is identified from high-throughput screening. A preliminary structure-activity relationship study led to the discovery of potent dual ACC1/ACC2 and ACC2 selective inhibitors against human recombinant ACC1 and ACC2. Selective ACC2 inhibitors exhibited IC50 1000-fold selectivity against ACC1. (S)-Enantiomer 9p exhibited high ACC2 activity and lowered muscle malonyl-CoA dose-dependently in acute rodent studies, whereas (R)-enantiomer 9o was weak and had no effect on the malonyl-CoA level.
Novel acetyl-CoA carboxylase (ACC) inhibitors and their use in diabetes, obesity and metabolic syndrome
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Page/Page column 40, (2008/06/13)
The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
