prasugrel and Acute-Coronary-Syndrome

prasugrel has been researched along with Acute-Coronary-Syndrome* in 1 studies

Other Studies

1 other study(ies) available for prasugrel and Acute-Coronary-Syndrome

Article	Year
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. Journal of medicinal chemistry, 2014, Sep-11, Volume: 57, Issue:17 In the search of a potential backup for clopidogrel, we have initiated a HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from a hit with low micromolar binding activity, we report here the main steps of the optimization process leading to the identification of the preclinical candidate SAR216471. It is a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists described in the literature. SAR216471 displays potent in vivo antiplatelet and antithrombotic activities and has the potential to differentiate from other antiplatelet agents. Topics: Acute Coronary Syndrome; Adenosine Diphosphate; Administration, Oral; Animals; Binding, Competitive; CHO Cells; Cricetinae; Cricetulus; Humans; Indoles; Injections, Intravenous; Male; Models, Chemical; Molecular Structure; Platelet Aggregation; Platelet Aggregation Inhibitors; Purinergic P2 Receptor Antagonists; Pyridazines; Rats; Rats, Sprague-Dawley; Receptors, Purinergic P2Y12; Thrombosis	2014

Article

Year

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.

Journal of medicinal chemistry, 2014, Sep-11, Volume: 57, Issue:17

In the search of a potential backup for clopidogrel, we have initiated a HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from a hit with low micromolar binding activity, we report here the main steps of the optimization process leading to the identification of the preclinical candidate SAR216471. It is a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists described in the literature. SAR216471 displays potent in vivo antiplatelet and antithrombotic activities and has the potential to differentiate from other antiplatelet agents.

Topics: Acute Coronary Syndrome; Adenosine Diphosphate; Administration, Oral; Animals; Binding, Competitive; CHO Cells; Cricetinae; Cricetulus; Humans; Indoles; Injections, Intravenous; Male; Models, Chemical; Molecular Structure; Platelet Aggregation; Platelet Aggregation Inhibitors; Purinergic P2 Receptor Antagonists; Pyridazines; Rats; Rats, Sprague-Dawley; Receptors, Purinergic P2Y12; Thrombosis

2014