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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6676-9. doi: 10.1016/j.bmcl.2010.09.009. Epub 2010 Sep 15.

Discovery of a vorapaxar analog with increased aqueous solubility.

Author information

1
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. yan.xia@merck.com

Abstract

An analog of the thrombin receptor antagonist vorapaxar (SCH 530348) with increased aqueous solubility, compound 9c (SCH 602539), was discovered through incorporation of polar substituents on the pyridine ring of the himbacine-derived lead series. This analog retained the excellent potency, pharmacokinetic and safety properties of vorapaxar while increasing the aqueous solubility by 20-fold. Also presented are in vivo evaluations of this compound in a cynomolgus monkey platelet aggregation assay and in a Folts model of thrombosis in anesthetized monkeys.

PMID:
20888225
DOI:
10.1016/j.bmcl.2010.09.009
[Indexed for MEDLINE]

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