140841-05-0Relevant academic research and scientific papers
Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist
Sparks, Steven M.,Aquino, Christopher,Banker, Pierette,Collins, Jon L.,Cowan, David,Diaz, Caroline,Dock, Steven T.,Hertzog, Donald L.,Liang, Xi,Swiger, Erin D.,Yuen, Josephine,Chen, Grace,Jayawickreme, Channa,Moncol, David,Nystrom, Christopher,Rash, Vincent,Rimele, Thomas,Roller, Shane,Ross, Sean
, p. 1278 - 1283 (2017/06/19)
The long chain free fatty acid receptor 4 (FFA4/GPR120) has recently been recognized as lipid sensor playing important roles in nutrient sensing and inflammation and thus holds potential as a therapeutic target for type 2 diabetes and metabolic syndrome. To explore the effects of stimulating this receptor in animal models of metabolic disease, we initiated work to identify agonists with appropriate pharmacokinetic properties to support progression into in vivo studies. Extensive SAR studies of a series of phenylpropanoic acids led to the identification of compound 29, a FFA4 agonist which lowers plasma glucose in two preclinical models of type 2 diabetes.
AMIDE COMPOUND AND USE OF THE SAME
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Page/Page column 52, (2010/02/14)
PROBLEM TO BE SOLVED: To provide a compound having an excellent controlling effect against plant pests. SOLUTION: This amide compound expressed by formula (1) [wherein, R1 is H, a halogen atom, a 1-4C alkyl or the like; R2 is a 1-4C alkyl, a 1-4C haloalkyl or the like; R3 is H or a 1-3C alkyl; R4 is a halogen, a 1-4C alkylthio, a 2-5C alkylcarbonyloxy or the like; R5 is a 3-4C alkynyl; and X is O or S] has the excellent controlling effect against the plant pests. COPYRIGHT: (C)2006,JPOandNCIPI
Phenyl derivatives, their manufacture and use as pharmaceutical agents
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Page/Page column 56, (2010/02/11)
This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARδ and/or PPARα agonists.
Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors
O'Meara, Jeff A.,Yoakim, Christiane,Bonneau, Pierre R.,B?s, Michael,Cordingley, Michael G.,Déziel, Robert,Doyon, Louise,Duan, Jianmin,Garneau, Michel,Guse, Ingrid,Landry, Serge,Malenfant, Eric,Naud, Julie,Ogilvie, William W.,Thavonekham, Bounkham,Simoneau, Bruno
, p. 5580 - 5588 (2007/10/03)
A series of novel 8-substituted dipyridodiazepinone-based inhibitors were investigated for their antiviral activity against wild type human immunodeficiency virus (HIV-1) and the clinically prevalent K103N/Y181C mutant virus. Our efforts have resulted in a series of benzoic acid analogues that are potent inhibitors of HIV-1 replication against a panel of HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs). Furthermore, the combination of good antiviral potency, a broad spectrum of activity, and an excellent pharmacokinetic profile provides strong justification for the further development of compound 7 as a potential treatment for wild type and NNRT1-resistant HIV-1 infection.
