1246187-79-0Relevant articles and documents
IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS
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, (2011/06/19)
Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is -C(O)-O-R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano
Activation of the G-protein-coupled receptor 119: A conformation-base hypothesis for understanding agonist response
McClure, Kim F.,Darout, Etzer,Guimar?es, Cristiano R. W.,Deninno, Michael P.,Mascitti, Vincent,Munchhof, Michael J.,Robinson, Ralph P.,Kohrt, Jeffrey,Harris, Anthony R.,Moore, Dianna E.,Li, Bryan,Samp, Lacey,Lefker, Bruce A.,Futatsugi, Kentaro,Kung, Daniel,Bonin, Paul D.,Cornelius, Peter,Wang, Ruduan,Salter, Eben,Hornby, Sam,Kalgutkar, Amit S.,Chen, Yue
experimental part, p. 1948 - 1952 (2011/05/19)
The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.
3-OXA-7-AZABICYCLO[3.3.1]NONANES
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Page/Page column 25, (2010/10/03)
Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
GPR 119 MODULATORS
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Page/Page column 48, (2010/11/18)
Compounds of Formula (I) that modulate the activity of the G -protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
