39223-32-0Relevant academic research and scientific papers
Discovery of SCH 900271, a potent nicotinic acid receptor agonist for the treatment of dyslipidemia
Palani, Anandan,Rao, Ashwin U.,Chen, Xiao,Huang, Xianhai,Su, Jing,Tang, Haiqun,Huang, Ying,Qin, Jun,Xiao, Dong,Degrado, Sylvia,Sofolarides, Michael,Zhu, Xiaohong,Liu, Zhidan,McKittrick, Brian,Zhou, Wei,Aslanian, Robert,Greenlee, William J.,Senior, Mary,Cheewatrakoolpong, Boonlert,Zhang, Hongtao,Farley, Constance,Cook, John,Kurowski, Stan,Li, Qiu,Van Heek, Margaret,Wang, Gangfeng,Hsieh, Yunsheng,Li, Fangbiao,Greenfeder, Scott,Chintala, Madhu
, p. 63 - 68 (2012)
Structure-guided optimization of a series of C-5 alkyl substituents led to the discovery of a potent nicotinic acid receptor agonist SCH 900271 (33) with an EC50 of 2 nM in the hu-GPR109a assay. Compound 33 demonstrated good oral bioavailability in all species. Compound 33 exhibited dose-dependent inhibition of plasma free fatty acid (FFA) with 50% FFA reduction at 1.0 mg/kg in fasted male beagle dogs. Compound 33 had no overt signs of flushing at doses up to 10 mg/kg with an improved therapeutic window to flushing as compared to nicotinic acid. Compound 33 was evaluated in human clinical trials.
Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
-
Page/Page column 79-80, (2008/06/13)
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.
