Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors

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. A...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (15), p.4097-4101
Main Authors: Edmondson, Scott D., Mastracchio, Anthony, Cox, Jason M., Eiermann, George J., He, Huaibing, Lyons, Kathryn A., Patel, Reshma A., Patel, Sangita B., Petrov, Aleksandr, Scapin, Giovanna, Wu, Joseph K., Xu, Shiyao, Zhu, Bing, Thornberry, Nancy A., Roy, Ranabir Sinha, Weber, Ann E.
Format: Article
Language:English
Subjects:
Animals
Benzimidazole
Benzimidazoles - chemical synthesis
Benzimidazoles - pharmacology
Biological and medical sciences
Buchwald coupling
Chemistry, Pharmaceutical - methods
Crystallography, X-Ray - methods
Dipeptidyl peptidase 8
Dipeptidyl peptidase-IV
Dipeptidyl-Peptidase IV Inhibitors - chemical synthesis
Dipeptidyl-Peptidase IV Inhibitors - pharmacology
Dogs
DPP-4
DPP-8
DPP-9
DPP-IV
Drug Design
General and cellular metabolism. Vitamins
GLP-1
Glucagon-like peptide 1
Glucagon-Like Peptide 1 - chemistry
Humans
Hydrolysis
Imidazoles - chemical synthesis
Imidazoles - pharmacology
Imidazopyridine
Inhibitory Concentration 50
Macaca mulatta
Medical sciences
Mice
Pharmacology. Drug treatments
Piperidines - chemical synthesis
Piperidines - chemistry
Piperidines - pharmacology
Pyrazines - chemical synthesis
Pyrazines - pharmacology
Pyridines - chemical synthesis
Pyridines - pharmacology
QPP
Quiescient peptidyl peptidase
Rats
Sitagliptin
Sitagliptin Phosphate
Triazoles - chemical synthesis
Triazoles - pharmacology
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.06.011