905274-03-5Relevant articles and documents
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2- (methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran- 3-amine (23)
Biftu, Tesfaye,Qian, Xiaoxia,Chen, Ping,Feng, Dennis,Scapin, Giovanna,Gao, Ying-Duo,Cox, Jason,Sinha Roy, Ranabir,Eiermann, George,He, Huabing,Lyons, Kathy,Salituro, Gino,Patel, Sangita,Petrov, Alexander,Xu, Feng,Xu, Shiyao Sherrie,Zhang, Bei,Caldwell, Charles,Wu, Joseph K.,Weber, Ann E.
, p. 5361 - 5366 (2013/09/23)
A series of novel tri-2,3,5-substituted tetrahydropyran analogs were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the series provided inhibitors with good DPP-4 potency and selectivity over other peptidases (QPP, DPP8, and FAP). Compound 23, which is very potent, selective, efficacious in the diabetes PD model, and has an excellent pharmacokinetic profile, is selected as a clinical candidate.
AMINOCYCLOHEXANES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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, (2008/06/13)
The present invention is directed to novel substituted aminocyclohexanes 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.