Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIA™ (sitagliptin phosphate)
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- 作者：Dooseop Kim ; Jennifer E. Kowalchick ; Scott D. Edmondson ; Anthony Mastracchio ; Jinyou Xu ; George J. Eiermann ; Barbara Leiting ; Joseph K. Wu ; KellyAnn D. Pryor ; Reshma A. Patel ; et al.
- 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
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：15 June 2007
- 年：2007
- 卷：17
- 期：12
- 页码：3373-3377
- 全文大小：159 K
文摘
A series of β-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the β-aminoamide series, which ultimately led to the discovery of JANUVIA™ (sitagliptin phosphate, compound 1), are described.