892113-81-4Relevant articles and documents
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Biftu, Tesfaye,Feng, Dennis,Qian, Xiaoxia,Liang, Gui-Bai,Kieczykowski, Gerard,Eiermann, George,He, Huaibing,Leiting, Barbara,Lyons, Kathy,Petrov, Aleksandr,Sinha-Roy, Ranabir,Zhang, Bei,Scapin, Giovanna,Patel, Sangita,Gao, Ying-Duo,Singh, Suresh,Wu, Joseph,Zhang, Xiaoping,Thornberry, Nancy A.,Weber, Ann E.
, p. 49 - 52 (2007)
Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC50 = 18 nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC50 = 2.6 nM), selective, and ef
PROCESS TO CHIRAL BETA AMINO ACID DERIVATIVES BY ASYMMETRIC HYDROGENATION
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Page/Page column 23; 24, (2010/11/08)
The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand with in situ protection of the primary amine product. The invention also relates to a novel process for the preparation of chiral beta-amino acid amides as inhibitors of the dipeptidyl peptidase-IV of structural formula III and the useful intermediates obtained therein. The products resulting from the instant process are inhibitors of dipeptidyl peptidase-IV and thereby useful for the treatment of Type 2 diabetes.
TARTARIC ACID SALTS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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Page/Page column 12-13, (2008/06/13)
Tartaric acid salts of (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl) butanoyl]hexahydro-3-(2,2,2-trifluoroethyl)-2H-1,4-diazepin-2-one are potent inhibitors of dipeptidyl peptidase-IV and are useful for the prevention and/or treatment of non-insulin depe