title: Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).
abstract: 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 beta-aminoamide series, which ultimately led to the discovery of JANUVIA (sitagliptin phosphate, compound 1), are described.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. dooseop_kim@merck.com
authors: Dooseop
authors: D
authors: Kim
authors: Jennifer E
authors: JE
authors: Kowalchick
authors: Scott D
authors: SD
authors: Edmondson
authors: Anthony
authors: A
authors: Mastracchio
authors: Jinyou
authors: J
authors: Xu
authors: George J
authors: GJ
authors: Eiermann
authors: Barbara
authors: B
authors: Leiting
authors: Joseph K
authors: JK
authors: Wu
authors: KellyAnn D
authors: KD
authors: Pryor
authors: Reshma A
authors: RA
authors: Patel
authors: Huaibing
authors: H
authors: He
authors: Kathryn A
authors: KA
authors: Lyons
authors: Nancy A
authors: NA
authors: Thornberry
authors: Ann E
authors: AE
authors: Weber
mesh_terms: D000577:Amides / Q000737:chemistry*; D000818:Animals; D054873:Dipeptidyl-Peptidase IV Inhibitors; D010879:Piperazines / Q000737:chemistry*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011719:Pyrazines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D000068900:Sitagliptin Phosphate; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000577:Amides; D054873:Dipeptidyl-Peptidase IV Inhibitors; D010879:Piperazines; D011480:Protease Inhibitors; D011719:Pyrazines; D014230:Triazoles; D000068900:Sitagliptin Phosphate