Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo
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- 作者：Pratik Devasthale ; Ying Wang ; Wei Wang ; John Fevig ; JianXin Feng ; Aiying Wang ; Tom Harrity ; Don Egan ; Nathan Morgan ; Michael Cap ; Aberra Fura ; Herbert E. Klei ; Kevin Kish ; Carolyn Weigelt ; Lucy Sun ; Paul Levesque ; Frederic Moulin ; Yi-Xin Li ; Robert Zahler ; Mark S. Kirby ; Lawrence G. Hamann
- 刊名：Journal of Medicinal Chemistry
- 出版年：2013
- 出版时间：September 26, 2013
- 年：2013
- 卷：56
- 期：18
- 页码：7343-7357
- 全文大小：646K
- 年卷期：v.56,no.18(September 26, 2013)
- ISSN：1520-4804
文摘
Optimization of a 5-oxopyrrolopyridine series based upon structure鈥揳ctivity relationships (SARs) developed from our previous efforts on a number of related bicyclic series yielded compound 2s (BMS-767778) with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. SAR in the series and characterization of 2s are described.