690258-03-8Relevant articles and documents
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1, 2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: A selective α-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Edmondson, Scott D.,Mastracchio, Anthony,Mathvink, Robert J.,He, Jiafang,Harper, Bart,Park, You-Jung,Beconi, Maria,Di Salvo, Jerry,Eiermann, George J.,He, Huaibing,Leiting, Barbara,Leone, Joseph F.,Levorse, Dorothy A.,Lyons, Kathryn,Patel, Reshma A.,Patel, Sangita B.,Petrov, Aleksandr,Scapin, Giovanna,Shang, Jackie,Roy, Ranabir Sinha,Smith, Aaron,Wu, Joseph K.,Xu, Shiyao,Zhu, Bing,Thornberry, Nancy A.,Weber, Ann E.
, p. 3614 - 3627 (2007/10/03)
A series of β-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2S
Discovery of potent and selective orally bioavailable β-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors
Edmondson, Scott D.,Mastracchio, Anthony,Duffy, Joseph L.,Eiermann, George J.,He, Huaibing,Ita, Ida,Leiting, Barbara,Leone, Joseph F.,Lyons, Kathryn A.,Makarewicz, Amanda M.,Patel, Reshma A.,Petrov, Aleksandr,Wu, Joseph K.,Thornberry, Nancy A.,Weber, Ann E.
, p. 3048 - 3052 (2007/10/03)
anti-Substituted biaryl β-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors that suffer from suboptimal selectivity and pharmacokinetics. This letter describes the substitution of the β-methyl substituent with β-polar subst