Discovery and structure - Activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors
Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulino
Pei, Zhonghua,Li, Xiaofeng,Von Geldern, Thomas W.,Longenecker, Kenton,Pireh, Daisy,Stewart, Kent D.,Backes, Bradley J.,Lai, Chunqiu,Lubben, Thomas H.,Ballaron, Stephen J.,Beno, David W. A.,Kempf-Grote, Anita J.,Sham, Hing L.,Trevillyan, James M.
p. 1983 - 1987
(2008/02/04)
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium ch
Cox, Jason M.,Harper, Bart,Mastracchio, Anthony,Leiting, Barbara,Sinha Roy, Ranabir,Patel, Reshma A.,Wu, Joseph K.,Lyons, Kathryn A.,He, Huaibing,Xu, Shiyao,Zhu, Bing,Thornberry, Nancy A.,Weber, Ann E.,Edmondson, Scott D.
p. 4579 - 4583
(2008/02/11)
AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 30; 38-39
(2010/10/20)
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