3277-04-1Relevant academic research and scientific papers
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists
Blanco, Maria-Jesus,Vetman, Tatiana,Chandrasekhar, Srinivasan,Fisher, Matthew J.,Harvey, Anita,Mudra, Daniel,Wang, Xu-Shan,Yu, Xiao-Peng,Schiffler, Matthew A.,Warshawsky, Alan M.
, p. 105 - 109 (2015/12/18)
A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was iden
Ammonium-salt-tagged IMesAuCl complexes and their application in gold-catalyzed cycloisomerization reactions in water
Belger, Katrin,Krause, Norbert
, p. 220 - 225 (2015/02/02)
The total synthesis and characterization of ammonium-salt-tagged IMesAuCl complexes is described. Moreover, we have demonstrated their catalytic activity and recyclability in cycloisomerization reactions of allenic and acetylenic alcohols in water. The water-soluble gold catalysts can be stabilized by the addition of LiCl.
DIMETHYLBENZOIC ACID COMPOUNDS
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Page/Page column 10, (2015/07/07)
The present invention provides a compound of the Formula I: wherein A is: and W, Y, X, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, for use as an inhibitor of the EP4 receptor.
DIMETHYL-BENZOIC ACID COMPOUNDS
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Page/Page column 18, (2014/01/17)
The present invention provides a compound of the Formula II: wherein A is: * R 1 is CH3, CF 3, or F; * R 2 is H, CH3, or F; * R 3 is CH3, OCH 3, OH, F; R 4 is OH or CH 20H; and *
Chemoselective reduction and self-immolation based FRET probes for detecting hydrogen sulfide in solution and in cells
Chen, Bifeng,Wang, Peng,Jin, Qingqing,Tang, Xinjing
supporting information, p. 5629 - 5633 (2014/07/22)
Hydrogen sulfide (H2S) has been regarded as the third gaseous transmitter. Based on the mechanism of chemoselective azido reduction and self-immolation, five fluorescence resonance energy transfer (FRET) probes for the detection of H2S were designed and synthesized. The effect of functional substitution of the self-immolative moiety on azido reduction and quinone-methide rearrangement were investigated. Their fluorescence responses and chemoselectivity for H2S detection were evaluated in solutions and in cells. This strategy may provide a general route for designing H 2S probes with many commercially available FRET pairs. the Partner Organisations 2014.
GPR40 RECEPTOR AGONIST, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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Paragraph 1156-1159; 1314-1317, (2014/05/24)
The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.
N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
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Page column 124, (2010/01/30)
Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
