121 articles for thisTarget
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Article Title
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Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP
Novartis Institutes For Biomedical Research
Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
Askat
A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.
Amgen
Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.
University of Pennsylvania
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Novartis Institutes For Biomedical Research
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
University of Pennsylvania
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Pfizer
SAR-based optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as highly potent EP1 receptor antagonists.
Asahi Kasei Pharma
Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.
Novartis Institutes For Biomedical Research
Synthesis and pharmacological evaluation of 2-aryloxy/arylamino-5-cyanobenzenesulfonylureas as novel thromboxane A2 receptor antagonists.
University of Liege
Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold.
Actelion Pharmaceuticals
Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist.
Actelion Pharmaceuticals
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.
Glaxosmithkline
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Glaxosmithkline
Synthesis and evaluation of trimetoquinol derivatives: novel thromboxane A2/prostaglandin H2 antagonists with diminished beta-adrenergic agonist activity.
Ohio State University
Synthesis of halogenated trimetoquinol derivatives and evaluation of their beta-agonist and thromboxane A2 (TXA2) antagonist activities.
Ohio State University
Synthesis and pharmacological evaluation of combined Thromboxane receptor antagonists/thromboxane synthase inhibitors: Pyridine-containing amino-prostanoids
TBA
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Pfizer
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.
Oxagen
Novel 2-(2-(benzylthio)-1H-benzo[d]imidazol-1-yl)acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype.
Actelion Pharmaceuticals
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.
Merck Frosst Canada
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.
Merck Frosst Centre For Therapeutic Research
Comparison between two classes of selective EP(3) antagonists and their biological activities.
Merck Frosst Centre For Therapeutic Research
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
Fujisawa Pharmaceutical
Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors.
Eli Lilly
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.
Merck Frosst Centre For Therapeutic Research
Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.
Amira Pharmaceuticals
Searching for new NO-donor aspirin-like molecules: Furoxanylacyl derivatives of salicylic acid and related furazans.
Universit£
Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.
University of Pennsylvania
Design and synthesis of new prostaglandin D2 receptor antagonists.
Minase Research Institute
Discovery of selective indole-based prostaglandin D2 receptor antagonist.
Minase Research Institute
Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Merck Research Laboratories
Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Amira Pharmaceuticals
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Merck Frosst Centre For Therapeutic Research
The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.
Merck Frosst Centre For Therapeutic Research
Azaindoles as potent CRTH2 receptor antagonists.
Merck Frosst Centre For Therapeutic Research
Potent and highly selective DP1 antagonists with 2,3,4,9-tetrahydro-1H-carbazole as pharmacophore.
Merck Frosst Centre For Therapeutic Research
3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists.
Glaxosmithkline
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
Merck Frosst Canada
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.
7Tm Pharma
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Merck Frosst Centre For Therapeutic Research
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Amira Pharmaceuticals
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Novartis Institutes of Biomedical Research
Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.
Glaxosmithkline
Synthesis of a novel series of 3-oxo-2,4-dioxobicyclo[3.2.1]octanes: additional evidence for two thromboxane receptor subtypes.
TBA
Oxa-prostanoid analogs. Identification of an orally effective, dual thromboxane receptor antagonist /thromboxane synthase inhibitor
TBA
Thia-prostanoid analogs with combined thromboxane receptor antagonist/thromboxane synthase inhibitor activities. Synthesis and pharmacological evaluation
TBA
Syntheses of Cyclopentane, Cyclohexene and Olefin Oxazoles as Thromboxane A2/Endoperoxide Receptor Antagonists
TBA
Interphenylene 7-oxabicyclo[2.2.1]heptanes. SQ33,961: a new potent, long-acting thromboxane antagonist
TBA
Structural homologies among thromboxane (TXA2) receptor antagonists: Minimal pharmacophoric requirements for high affinity interaction with TXA2 receptors
TBA
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Glaxosmithkline
Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Merck Frosst Centre For Therapeutic Research
Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain.
Glaxosmithkline
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPalpha and TPbeta isoforms of the human thromboxane A2 receptor.
University of LièGe
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Novartis Institutes of Biomedical Research
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Merck Frosst Canada
Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as antiplatelet agents acting on both the alpha and beta isoforms of the human thromboxane receptor.
University of LièGe
Identification of an indole series of prostaglandin D2 receptor antagonists.
Merck Frosst Canada
Development of dual-acting benzofurans for thromboxane A2 receptor antagonist and prostacyclin receptor agonist: synthesis, structure-activity relationship, and evaluation of benzofuran derivatives.
Toray Industries
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
Fujisawa Pharmaceutical
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
Fujisawa Pharmaceutical
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
7Tm Pharma
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Merck Frosst Centre For Therapeutic Research
Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.
Procter & Gamble Pharmaceuticals
Structure determination and comparison of BM567, a sulfonylurea, with terbogrel, two compounds with dual action, thromboxane receptor antagonism and thromboxane synthase inhibition.
FacultéS Universitaires N.D. De La Paix
Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry.
Merck Frosst Canada
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.
Procter & Gamble Pharmaceuticals
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.
Procter and Gamble Pharmaceuticals
Synthesis and biological characterization of sqbazide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A2 receptor.
Ecole Nationale SupéRieure De Chimie De Paris
New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.
Boehringer Ingelheim Pharma
Synthesis and thromboxane A2 antagonistic activity activity of indane derivatives.
Zeria Pharmaceutical
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounds.
Eli Lilly
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives.
Eli Lilly
Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.
Shionogi
On the bioisosteric potential of diazines: diazine analogues of the combined thromboxane A2 receptor antagonist and synthetase inhibitor Ridogrel.
University of Innsbruck
Interphenylene 7-oxabicyclo[2.2.1]heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-b]pyridine acid derivatives as thromboxane A2 receptor antagonists.
Carpibem
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.
Dr. Karl Thomae
Agents combining thromboxane receptor antagonism with thromboxane synthase inhibition: [[[2-(1H-imidazol-1-yl)ethylidene]amino]oxy]alkanoic acids.
Pharmacia-Farmitalia Carlo Erba
Quinones. 4. Novel eicosanoid antagonists: synthesis and pharmacological evaluation.
Takeda Chemical Industries
9,11-Epoxy-9-homo-14-thiaprost-5-enoic acid derivatives: potent thromboxane A2 antagonists.
Squibb Institute For Medical Research
7-Oxabicyclo[2.2.1]heptyl carboxylic acids as thromboxane A2 antagonists: aza omega-chain analogues.
Squibb Institute For Medical Research
Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2 antagonists. Semicarbazone omega-chains.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and thromboxane A2/prostaglandin H2 receptor antagonistic activity of phenol derivatives.
Takeda Chemical Industries
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 2.
Kyowa Hakko Kogyo
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 1.
Kyowa Hakko Kogyo
