77716-01-9Relevant articles and documents
FXR receptor agonist
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Paragraph 0616; 0618; 0619; 0620, (2019/02/10)
The present invention discloses an FXR receptor agonist, belongs to the technical field of medicine, and particularly relates to a compound represented by a formula (I), a pharmaceutically acceptablesalt, an ester or a stereoisomer thereof, wherein R, R, R, M, L, L1, W, A , B, Q, m and n are defined in the specification. The present invention further relates to a preparation method of the compound, a pharmaceutical preparation, and applications in preparation of drugs for treatment and/or prevention of nonalcoholic fatty liver disease, primary biliary cirrhosis, lipid metabolism disorder, diabetic complication, malignant tumors and other related diseases mediated by FXR receptors. The formula I is defined in the specification.
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.
CROSS-LINKED CYCLIC AMINE COMPOUNDS AND AGENTS FOR PEST CONTROL
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Paragraph 0115; 0116, (2015/11/16)
Agents for pest control comprising cyclic amine compounds represented by the formula (1) or salts thereof or N-oxides thereof as an active ingredient, wherein Cy 1 represents an unsubstituted or substituted 5-membered heterocycle or unsubstituted or substituted group represented by the formula (a) below, wherein Y 1 and Y 2 each independently represents nitrogen or carbon and symbol * represents the bonding positions.