122 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 AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.
Askat
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.
Ono Pharmaceutical
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.
Eli Lilly
Structural optimization and structure-functional selectivity relationship studies of G protein-biased EP2 receptor agonists.
Ono Pharmaceutical
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.
Eli Lilly
Discovery of highly potent dual EP(2) and EP(3) agonists with subtype selectivity.
Ono Pharmaceutical
Discovery and characterization of a potent and selective EP4 receptor antagonist.
Eli Lilly
A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.
Amgen
From virtual to clinical: The discovery of PGN-1531, a novel antagonist of the prostanoid EP4 receptor.
Argenta Discovery
Selective EP4 Antagonist May Be Useful in Treating Arthritis and Arthritic Pain.
Therachem Research Medilab (India)
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
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¿-lactam analogs of PGE2 as EP4 and EP2/EP4 agonists.
Minase Research Institute
Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.
TBA
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.
Merck Frosst Canada
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Emd-Serono Research Institute
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
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
Emd-Serono Research Institute
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.
Emd-Serono Research Institute
Comparison between two classes of selective EP(3) antagonists and their biological activities.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
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 new chemical leads for prostaglandin D2 receptor antagonists.
Minase Research Institute
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.
Merck Frosst Centre For Therapeutic Research
Discovery of novel prostaglandin analogs as potent and selective EP2/EP4 dual agonists.
Minase Research Institute
Discovery of a novel EP2/EP4 dual agonist with high subtype-selectivity.
Minase Research Institute
Synthesis and evaluation of novel modified¿-lactam prostanoids as EP4 subtype-selective agonists.
Minase Research Institute
Efficient synthesis of a novel m-phenylene derivative as a selective EP4 agonist inducing follicular growth and maturation in the ovary.
Toray Industries
Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP4 receptor.
Rottapharm Madaus
Design and synthesis of new prostaglandin D2 receptor antagonists.
Minase Research Institute
Discovery of selective indole-based prostaglandin D2 receptor antagonist.
Minase Research Institute
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.
Merck Frosst Centre For Therapeutic Research
A novel series of potent and selective EP(4) receptor ligands: facile modulation of agonism and antagonism.
Merck Frosst Canada
The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.
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
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
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 3: Synthesis, metabolic stability, and biological evaluation of optically active analogs.
Minase Research Institute
Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists.
Minase Research Institute
1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists.
Decode Chemistry
Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.
Decode Chemistry
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 1: discovery and exploration of the carboxyamide side chain.
Minase Research Institute
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
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. part 2: optimization of the side chains to improve in vitro and in vivo potencies.
Minase Research Institute
Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that
Decode Chemistry
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 CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.
Pfizer
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
3-Acrylamide-4-aryloxyindoles: synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists.
Decode Chemistry
Peri-substituted hexahydro-indolones as novel, potent and selective human EP3 receptor antagonists.
Decode Chemistry
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
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
Scaffold Hopping Strategy to Identify Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy.
East China Normal University
Identification of an indole series of prostaglandin D2 receptor antagonists.
Merck Frosst Canada
Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.
Pfizer
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
Fujisawa Pharmaceutical
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.
Roche Palo Alto
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
Fujisawa Pharmaceutical
Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.
Roche Palo Alto
Discovery of orally active prostaglandin D2 receptor antagonists.
Minase Research Institute
Discovery and Optimization of 7-Alkylidenyltetrahydroindazole-Based Acylsulfonamide EP3 Antagonists.
Janssen Research & Development
Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.
Roche Palo Alto
Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
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
Design and synthesis of a highly selective EP4-receptor agonist. Part 2: 5-thia and 9beta-haloPG derivatives with improved stability.
Minase Research Institute
Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity.
Minase Research Institute
Design and synthesis of a highly selective EP2-receptor agonist.
Minase Research Institute
Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry.
Merck Frosst Canada
Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis.
Bayer
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
Difluoromethylene at the ?-Lactam ?-Position Improves 11-Deoxy-8-aza-PGE
Cayman Chemical
Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.
Ube Industries
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
Eli Lilly
Hit-to-lead optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as a novel class of EP1 receptor antagonists.
Asahi Kasei Pharma
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
Discovery of a novel 2-(1H-pyrazolo[3,4-b]pyridin-1-yl)thiazole derivative as an EP
Asahi Kasei Pharma
Tyrosinase inhibitory effect of benzoic acid derivatives and their structure-activity relationships.
Yonsei University
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Case Western Reserve University
Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.
Schering-Plough Research Institute
Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.
Aventis Pharma Deutschland
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).
Bristol-Myers Squibb
Ring Size effect in the PKC inhibitory activities of perhydroazepine analogs of balanol.
Sphinx Laboratories