69 articles for thisTarget
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Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Arena Pharmaceuticals
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP
Novartis Institutes For Biomedical Research
Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat.
Arena Pharmaceuticals
A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.
Amgen
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
Amgen
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
Isoquinoline derivatives as potent CRTH2 antagonists: design, synthesis and SAR.
Taisho Pharmaceutical
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
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
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
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
Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.
TBA
Isoquinoline derivatives as potent CRTH2 receptor antagonists: synthesis and SAR.
Taisho Pharmaceutical
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
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.
Merck Frosst Centre For Therapeutic Research
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
Amgen
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
Amgen
Discovery of new orally active prostaglandin D2 receptor antagonists.
Ono Pharmaceutical
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
Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
Merck Serono
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
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
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
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
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
Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Merck Frosst Centre For Therapeutic Research
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
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
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
7Tm Pharma
Identification of an indole series of prostaglandin D2 receptor antagonists.
Merck Frosst Canada
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
Discovery of orally active prostaglandin D2 receptor antagonists.
Minase Research Institute
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives.
Shionogi
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.
Shionogi
Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) 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
Potent and Selective Human Prostaglandin F (FP) Receptor Antagonist (BAY-6672) for the Treatment of Idiopathic Pulmonary Fibrosis (IPF).
Bayer
Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry.
Merck Frosst Canada
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
New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.
Shionogi
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Merck
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP
Glaxosmithkline