Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
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.
Fevig
John M
JM
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. john.fevig@bms.com
Cacciola
Joseph
J
Buriak
Joseph
J
Rossi
Karen A
KA
Knabb
Robert M
RM
Luettgen
Joseph M
JM
Wong
Pancras C
PC
Bai
Stephen A
SA
Wexler
Ruth R
RR
Lam
Patrick Y S
PY