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Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles.

Vanderbilt University Medical Center

Protease-Activated Receptor 1 (PAR-1) Antagonists as Potential Treatment for Acute Coronary Syndrome.

Therachem Research Medilab (India)

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.

Bayer Pharma

The chemistry and pharmacology of privileged pyrroloquinazolines.

Oregon Health & Science University

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

Northwest Agriculture & Forestry University

Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar.

Merck Research Laboratories

Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar.

Merck Research Laboratories

Discovery of Octahydroindenes as PAR1 Antagonists.

Korea Research Institute of Technology

Toward drugs for protease-activated receptor 2 (PAR2).

The University of Queensland

Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.

TBA

Discovery of nor-seco himbacine analogs as thrombin receptor antagonists.

Pfizer

Development of potent thrombin receptor antagonist peptides.

Bristol-Myers Squibb Pharmaceutical Research Institute

Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.

R. W. Johnson Pharmaceutical Research Institute

Discovery of a vorapaxar analog with increased aqueous solubility.

Merck Research Laboratories

Aplysillin A, a Thrombin Receptor Antagonist from the Marine Sponge Aplysina fistularis fulva

TBA

 

Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042

TBA

Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.

Schering-Plough Research Institute

Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.

Schering-Plough Research Institute

Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.

Schering-Plough Research Institute

Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.

Schering-Plough Research Institute

Metabolism-based identification of a potent thrombin receptor antagonist.

Schering-Plough Research Institute

Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring.

Schering-Plough Research Institute

Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.

Schering-Plough Research Institute

Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents.

Schering-Plough Research Institute

Direct evidence of edge-to-face CH/? interaction for PAR-1 thrombin receptor activation.

Kyushu University

Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.

TBA

Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold.

China Pharmaceutical University

High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.

Johnson & Johnson Pharmaceutical Research & Development

Protease activated receptor 4 (PAR4) antagonists: Research progress on small molecules in the field of antiplatelet agents.

China Pharmaceutical University

Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).

Merck Research Laboratories

Potent, low molecular weight thrombin receptor antagonists.

Schering-Plough Research Institute

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.

Merck Research Laboratories

Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.

The R. W. Johnson Pharmaceutical Research Institute

Design and synthesis of potent PAR-1 antagonists based on vorapaxar.

Hebei University of Technology

Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.

The R. W. Johnson Pharmaceutical Research Institute

Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against ?-Thrombin.

Northwest Agriculture & Forestry University

Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.

Bristol-Myers Squibb Research & Development

Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.

Schering-Plough Research Institute

Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).

The R. W. Johnson Pharmaceutical Research Institute

Thrombin inhibitors based on a propargylglycine template.

Biotech Research Institute

Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1).

University At Stony Brook

The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.

Marquette University

Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization.

Marquette University

Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug-Target Interactions.

Shanghai Jiao Tong University

Development of a potent thrombin receptor ligand.

Merck Research Laboratories

Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.

Marquette University

Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide.

Shandong University

6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.

Instituto De BiologÍA Celular

The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.

Johnson & Johnson Pharmaceutical