title: Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.
abstract: A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported.
authors.affiliation: Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. scott_edmondson@merck.com
authors.forename: Scott D
authors.initials: SD
authors.lastname: Edmondson
authors.forename: Anthony
authors.initials: A
authors.lastname: Mastracchio
authors.forename: Jason M
authors.initials: JM
authors.lastname: Cox
authors.forename: George J
authors.initials: GJ
authors.lastname: Eiermann
authors.forename: Huaibing
authors.initials: H
authors.lastname: He
authors.forename: Kathryn A
authors.initials: KA
authors.lastname: Lyons
authors.forename: Reshma A
authors.initials: RA
authors.lastname: Patel
authors.forename: Sangita B
authors.initials: SB
authors.lastname: Patel
authors.forename: Aleksandr
authors.initials: A
authors.lastname: Petrov
authors.forename: Giovanna
authors.initials: G
authors.lastname: Scapin
authors.forename: Joseph K
authors.initials: JK
authors.lastname: Wu
authors.forename: Shiyao
authors.initials: S
authors.lastname: Xu
authors.forename: Bing
authors.initials: B
authors.lastname: Zhu
authors.forename: Nancy A
authors.initials: NA
authors.lastname: Thornberry
authors.forename: Ranabir Sinha
authors.initials: RS
authors.lastname: Roy
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D004285:Dogs; D015195:Drug Design; D052216:Glucagon-Like Peptide 1 / Q000737:chemistry; D006801:Humans; D006868:Hydrolysis; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008253:Macaca mulatta; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D011719:Pyrazines / Q000138:chemical synthesis / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D000068900:Sitagliptin Phosphate; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D001562:Benzimidazoles; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007093:Imidazoles; D010880:Piperidines; D011719:Pyrazines; D011725:Pyridines; D014230:Triazoles; D052216:Glucagon-Like Peptide 1; C031000:benzimidazole; D000068900:Sitagliptin Phosphate