Bioorganic & Medicinal Chemistry Letters 2006-07-15

Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.

John M Fevig, Joseph Cacciola, Joseph Buriak, Karen A Rossi, Robert M Knabb, Joseph M Luettgen, Pancras C Wong, Stephen A Bai, Ruth R Wexler, Patrick Y S Lam

Index: Bioorg. Med. Chem. Lett. 16 , 3755, (2006)

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Abstract

Previously, potent factor Xa inhibitors were described based on a pyrazole core. Modifications of the pyrazole core have provided additional novel, highly potent factor Xa inhibitors. This manuscript will describe the synthesis and biological activity of factor Xa inhibitors containing the 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one and related bicyclic cores. Many of these compounds are potent, selective, and orally bioavailable inhibitors of coagulation factor Xa.