Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors:: Close analogs of JANUVIA™ (sitagliptin phosphate)

被引：47
作者：
Kim, Dooseop
Kowalchick, Jennifer E.
Edmondson, Scott D.
Mastracchio, Anthony
Xu, Jinyou
Eiermann, George J.
Leiting, Barbara
Wu, Joseph K.
Pryor, KellyAnn D.
Patel, Reshma A.
He, Huaibing
Lyons, Kathryn A.
Thornberry, Nancy A.
Weber, Ann E.
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 12期
关键词：
close analogs of Januvia; sitagliptin; type; 2; diabetes; triazolopiperazine-amides; dipeptidyl peptidase IV inhibitors; DPP-4; inhibitor; GLP-1; DPP-8; DPP-9;
D O I：
10.1016/j.bmcl.2007.03.098
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of beta-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the P-aminoamide series, which ultimately led to the discovery of JANUVIA (TM) (sitagliptin phosphate, Compound 1), are described. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3373 / 3377
页数：5
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