77716-02-0Relevant articles and documents
Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes
Neelamkavil, Santhosh F.,Stamford, Andrew W.,Kowalski, Timothy,Biswas, Dipshikha,Boyle, Craig,Chackalamannil, Samuel,Xia, Yan,Jayne, Charles,Neustadt, Bernard,Hao, Jinsong,Liu, Hong,Dai, Xing,Baker, Hana,Hawes, Brian,O'Neill, Kim,Tang, Huadong,Greenlee, William J.
supporting information, p. 457 - 461 (2018/05/23)
The ever-growing prevalence of type 2 diabetes in the world has necessitated an urgent need for multiple orally effective agents that can regulate glucose homeostasis with a concurrent reduction in body weight. G-Protein coupled receptor 119 (GPR119) is a GPCR target at which agonists have demonstrated glucose-dependent insulin secretion and shows beneficial effects on glycemic control. Herein, we describe our efforts leading to the identification of a potent, oral GPR-119 agonist, MK-8282, which shows improved glucose tolerance in multiple animal models and has excellent off-target profile. The key design elements in the compounds involved a combination of a fluoro-pyrimidine and a conformationally constrained bridged piperidine to impart good potency and efficacy.
INDOLYLPYRIMIDINES AS MODULATORS OF GPR119
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Page/Page column 54, (2012/03/26)
The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions modulated by GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
BRIDGED CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
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Page/Page column 40-41, (2010/11/27)
A cyclic amine compound represented by the formula (1): [wherein Cy1 represents an (un)substituted aromatic ring; X represents oxygen, sulfur, (un)substituted nitrogen, sulfinyl, or sulfonyl; R1a and R2a/s