ACS Medicinal Chemistry Letters p. 414 - 418 (2013)
Update date:2022-08-05
Topics:
Qian, Yimin
Corbett, Wendy L.
Berthel, Steven J.
Choi, Duk Soon
Dvorozniak, Mark T.
Geng, Wanping
Gillespie, Paul
Guertin, Kevin R.
Haynes, Nancy-Ellen
Kester, Robert F.
Mennona, Francis A.
Moore, David
Racha, Jagdish
Radinov, Roumen
Sarabu, Ramakanth
Scott, Nathan R.
Grimsby, Joseph
Mallalieu, Navita L.
To resolve the metabolite redox cycling associated with our earlier clinical compound 2, we carried out lead optimization of lead molecule 1. Compound 4 showed improved lipophilic ligand efficiency and demonstrated robust glucose lowering in diet-induced obese mice without a liability in predictive preclinical drug safety studies. Thus, it was selected as a clinical candidate and further studied in type 2 diabetic patients. Clinical data suggests no evidence of metabolite cycling, which is consistent with the preclinical profiling of metabolism.
View MoreBAODING SINO-CHEM INDUSTRY CO.,LTD
Contact:0312-5956088
Address:NO.8 FUXING ROAD,CHINA
Zhangjiagang Golden Reach Fine Chemical Co.,LTD.
Contact:+86-512-6585 6968
Address:Changfu Road, Dongsha Chemical Industry Park, Zhangjiagang City, Jiangsu Province, China
Xinchang Yueding Chemical Co., Ltd.
Contact:86-571-56926323
Address:NO.90 BEIMENCHENGWAI CHENGGUAN TOWN XINCHANG
website:http://www.truewingroup.com
Contact:86-311-66699812
Address:NO.600 ZHONGSHAN EAST ROAD SHIJIAZHUANG
Jining tiansheng chemical co.,ltd.
Contact:+86-537-5158722
Address:ROOM 1011, BLOCK B, CUIDU INTERNATIOAL BUSINESS CENTER, JINING CITY, CHINA
Doi:10.1021/ja01599a042
(1956)Doi:10.1039/DT9790000547
()Doi:10.1021/jm00196a024
(1979)Doi:10.1002/cplu.201402390
(2015)Doi:10.1039/b203783c
(2002)Doi:10.1021/ja01863a051
(1940)