(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: Synthesis, in vitro, in vivo, and X-ray crystallographic characterization
A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.
Wright, Stephen W.,Ammirati, Mark J.,Andrews, Kim M.,Brodeur, Anne M.,Danley, Dennis E.,Doran, Shawn D.,Lillquist, Jay S.,Liu, Shenping,McClure, Lester D.,McPherson, R. Kirk,Olson, Thanh V.,Orena, Stephen J.,Parker, Janice C.,Rocke, Benjamin N.,Soeller, Walter C.,Soglia, Carolyn B.,Treadway, Judith L.,VanVolkenburg, Maria A.,Zhao, Zhengrong,Cox, Eric D.
p. 5638 - 5642
(2008/02/13)
Dihydro-benzo[b][1,4]diazepin-2-one derivatives
This invention relates to dihydro-benzo[b][1,4]diazepin-2-one derivatives of the formula wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
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(2008/06/13)
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