1.
Bioorg Med Chem Lett
; 24(17): 4332-5, 2014 Sep 01.
Article
in English
| MEDLINE
| ID: mdl-25088191
ABSTRACT
A series of 5-fluoro-4,6-dialkoxypyrimidine GPR119 modulators were discovered and optimized for in vitro agonist activity. A lead molecule was identified that has improved agonist efficacy relative to our clinical compound (APD597) and possesses reduced CYP2C9 inhibitory potential. This optimized lead was found to be efficacious in rodent models of glucose control both alone and in combination with a Dipeptidyl peptidase-4 (DPP-4) inhibitor.
