62519-54-4

Upstream product

• 943833-90-7 C₁₉H₁₇F₃O₃ 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 845-05-6 3-Trifluoromethylphenyl 4-methoxyphenyl ketone 
• 24393-56-4 ethyl (E)-3-(4-methoxyphenyl)prop-2-enoate 
• 401-78-5 3-bromo-1-trifluoromethylbenzene 

Downstream Products

• 943833-91-8 3-(4-hydroxy-phenyl)-3-(3-trifluoro-methyl-phenyl)-propionic acid ethyl ester 
• 943833-92-9 3-(4-butoxy-phenyl)-3-(3-trifluoro-methyl-phenyl)-propionic acid ethyl ester 

Relevant academic research and scientific papers

GPR40 AGONISTS

The invention is directed to compounds of Formula (I) useful as GPR40 agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, insulin resistance, hyperglycemia, obesity, diabetes such as NIDDM, and other disorders related to lipid metabolism, energy homeostasis, and complications thereof, using compounds of the invention are also described.

Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists

High-throughput screening of a subset of the J&J compound library containing the carboxylic acid functional group uncovered a bromophenyl derivative as a moderate potent GPR40 agonist. Chemical elaboration of this bromophenyl led to the discovery of a novel series of GPR40 agonists with submicromolar potency. Among them, 22 and 24 behaved as full agonists when compared to the endogenous GPR40 ligand linolenic acid in a functional Ca +2 flux assay in HEK cells expressing GPR40 receptor. Several GPR40 agonists have also demonstrated the ability to induce glucose-mediated insulin secretion in the mouse MIN6 pancreatic β-cell line. Our data supports the hypothesis that GPR40 may play an important role in fatty acid-mediated glucose-dependent insulin secretion. Compound 22 exhibited good pharmacokinetic profile in rat and may serve as a good candidate for in vivo study and may help to determine if GPR40 agonists would be beneficial in the treatment of type II diabetes.

Polycyclic compounds

Compounds of the formula (II): STR1 and pharmaceutically acceptable salts thereof, wherein R1 is phenyl or naphthyl or substituted phenyl or naphthyl group; R2 is: STR2 wherein R5 is hydrogen or C1-6 alkyl, R6 is hydrogen or C1-6 alkyl, phenyl, tolyl or benzyl and R7 is hydrogen; R3 and R4 are each hydrogen atom or C1-4 alkyl, and X is CO, CHOH, CHCI or C=C R8 R9 wherein R8 and R9 are each hydrogen or C1-4 alkyl; or CR10 OH or CHR10, wherein R10 is C1-4 alkyl, have been found to be mood-modifying agents and anorexic agents.