Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists
New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demonstrated robust weight loss in a di
Cameron, Kimberly O.,Beretta, Elena E.,Chen, Yue,Chu-Moyer, Margaret,Fernando, Dilinie,Gao, Hua,Kohrt, Jeffrey,Lavergne, Sophie,Jardine, Paul Da Silva,Guzman-Perez, Angel,Hoth, Christopher,Perry, David A.,Hadcock, John R.,Gautreau, Denise,Makowski, Michael,Perez, Sylvie,Polivkova, Jana,Rogers, Lucy,Scott, Dennis O.,Swick, Andrew G.,Thiede, Lucinda,Trebino, Catherine E.,Trilles, Richard V.,Wilmowski, Julie,Zhang, Yingxin
p. 2943 - 2947
(2012/06/04)
1,2,4 TRIAZOLO [4, 3 -A] [1,5] BENZODIAZEPIN-5 (6H) -ONES AS AGONISTS OF THE CHOLECYSTOKININ-1 RECEPTOR (CCK-IR)
This invention relates to CCK-1 R agonists of Formula (I) wherein R1-R5 and X are as defined in the specificiation, as well as pharmaceutical compositions containing the compounds and methods of use of the compounds and compositions. The compounds are useful in treating obesity, type 2 diabetes and associated diseases.
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Page/Page column 105-106
(2010/07/02)
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Get Best Price for1228935-00-96-[2-(2-benzylpiperidin-1-yl)-2-oxoethyl]-4-(1H-indol-3-ylmethyl)-1-phenyl-4H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-5(6H)-one