SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
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(2011/02/24)
Design of potent and selective GPR119 agonists for type II diabetes
Screening of the Merck sample collection identified compound 1 as a weakly potent GPR119 agonist (hEC50 = 3600 nM). Dual termini optimization of 1 led to compound 36 having improved potency, selectivity, and formulation profile, however, modest
Szewczyk, Jason W.,Acton, John,Adams, Alan D.,Chicchi, Gary,Freeman, Stanley,Howard, Andrew D.,Huang, Yong,Li, Cai,Meinke, Peter T.,Mosely, Ralph,Murphy, Elizabeth,Samuel, Rachel,Santini, Conrad,Yang, Meng,Zhang, Yong,Zhao, Kake,Wood, Harold B.
p. 2665 - 2669
(2011/06/20)
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
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(2009/12/02)
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