10276. Apixaban

Nomenclature

CAS number: 503612-47-3
4,5,6,7-Tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; BMS-562247.
C25H25N5O4; mol wt 459.50.
C 65.35%, H 5.48%, N 15.24%, O 13.93%.

Description and references

Direct factor Xa inhibitor. Prepn: D. Pinto et al., WO 03026652; eidem, US 6967208 (2003, 2005 both to Bristol-Myers Squibb). In vitro and in vivo antithrombotic and antihemostatic properties: P. C. Wong et al., J. Thromb. Haemost. 6, 820 (2008) DOI PubMed. Clinical evaluation in venous thromboembolism prophylaxis after total knee replacement: M. R. Lassen et al., ibid. 5, 2368 (2007) DOI PubMed. Review of discovery: D. J. P. Pinto et al., J. Med. Chem. 50, 5339-5356 (2007) DOI PubMed.

Chemical structure

Properties

Colorless solid. Aq soly (0.9% saline soln): 40-50 μg/ml.

Therapeutic Category

Antithrombotic.

Keywords

Antithrombotic