PMID

Data

Article Title

Organization

Development of Potent and Selective Antagonists for the UTP-Activated P2Y

University of Bonn

State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.

Galecto Biotech

GPCR crystal structures: Medicinal chemistry in the pocket.

Friedrich-Alexander University

Optimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y(12) antagonists for inhibition of platelet aggregation.

Actelion Pharmaceuticals

N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist.

Sanofi R & D

Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.

Bristol-Myers Squibb Research

Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations.

Astrazeneca

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.

Bristol-Myers Squibb

Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.

Bristol-Myers Squibb

Synthesis and biological evaluation of cyclopentyl-triazolol-pyrimidine (CPTP) based P2Y12 antagonists.

Shanghai Hengrui Pharmaceutical

Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.

Astrazeneca

Synthesis, structure-property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y12 receptor.

Astrazeneca

Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.

Bristol-Myers Squibb

Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.

Bristol-Myers Squibb Research and Development

From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.

Astrazeneca

Identification of high-affinity P2Y12 antagonists based on a phenylpyrazole glutamic acid piperazine backbone.

Sanofi-Aventis Deutschland

Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.

University of Bonn

High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.

University of Bonn

Adenosine analogues as inhibitors of P2Y12 receptor mediated platelet aggregation.

Inspire Pharmaceuticals

Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor.

Inspire Pharmaceuticals

Purine and pyrimidine (P2) receptors as drug targets.

National Institute of Diabetes

A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor.

Astrazeneca R&D

Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.

University of Pavia

Piperazinyl glutamate pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.

Pfizer

Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.

Pfizer

Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation.

Pfizer

Thienopyrimidine-based P2Y12 platelet aggregation inhibitors.

Pfizer

Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.

Pfizer

5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).

Amira Pharmaceuticals

6-Amino-2-mercapto-3H-pyrimidin-4-one derivatives as new candidates for the antagonism at the P2Y12 receptors.

Universit£

Discovery of a Series of 5-Amide-1

China Pharmaceutical University

The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.

Massachusetts General Hospital

Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors.

University of Bonn

Synthesis and biological evaluation of

Beijing University of Technology

P2Y

Al-Ahliyya Amman University

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.

Indian Institute of Technology (B.H.U.)

Strategies for targeting the P2Y

The University of Sydney

A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp.

Schering-Plough Research Institute

Switching a Xanthine Oxidase Inhibitor to a Dual-Target Antagonist of P2Y

Shenyang Pharmaceutical University

Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12)).

Cor Therapeutics

New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.

Glsynthesis

Synthesis and biological evaluation of antiplatelet 2-aminochromones.

Upjohn Laboratories

Reversible, orally available ADP receptor (P2Y

King Abdullah International Medical Research Center/King Saud Bin Abdulaziz University For Health Sciences

Facile alkylation of 4-nitrobenzotriazole and its platelet aggregation inhibitory activity.

Punjabi University

Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis and anticholinesterase activity of some new a-aminobisphosphonates.

Tarbiat Modares University