853934-64-2Relevant academic research and scientific papers
Discovery of β-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV
Nordhoff, Sonja,Cerezo-Galvez, Silvia,Deppe, Holger,Hill, Oliver,Lopez-Canet, Meritxell,Rummey, Christian,Thiemann, Meinolf,Matassa, Victor G.,Edwards, Paul J.,Feurer, Achim
scheme or table, p. 4201 - 4203 (2010/04/02)
Modifications of DPP-4 inhibitor 5, that was discovered by structure based design, are described and structure-activity relationships discussed. With analogue 7k one of the most potent non-covalent inhibitors of DPP-4 reported to date (IC50 = 0.38 nM) was discovered. X-ray structure of inhibitor 7k bound to DPP-4 revealed a hydrogen bonding interaction with Q553. First successful efforts in balancing overall properties, as demonstrated by improved metabolic stability, highlight the potential of this series.
Dpp-IV Inhibitors
-
Page/Page column 16, (2008/12/07)
The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the pre
The reversed binding of β-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors
Nordhoff, Sonja,Cerezo-Galvez, Silvia,Feurer, Achim,Hill, Oliver,Matassa, Victor G.,Metz, Guenther,Rummey, Christian,Thiemann, Meinolf,Edwards, Paul J.
, p. 1744 - 1748 (2007/10/03)
The co-crystal structure of β-phenethylamine fragment inhibitor 5 bound to DPP-IV revealed that the phenyl ring occupied the proline pocket of the enzyme. This finding provided the basis for a general hypothesis of a reverse binding mode for β-phenethylam
1-[(3R)-Amino-4-(2-fluoro-phenyl)-butyl]-pyrrolidine-(2R)-carboxylic acid benzyl amine derivatives and related compounds as dipeptidyl peptidase IV (DPP-IV) inhibitors for the treatment of type 2 diabetes mellitus
-
Page/Page column 20, (2010/02/14)
The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.
DPP-IV INHIBITORS
-
Page/Page column 16, (2010/02/11)
The invention relates to compounds of formula (I) wherein Z, R1-5, X, n, A1 and A2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to
