Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
The bicyclic dihydropyrazolopyridinone scaffold allowed for incorporation of multiple P1 moieties with subnanomolar binding affinities for blood coagulation factor Xa. The compound 3-[6-(2′-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoro-methyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-l-yl]-benzamide 6d shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability. Compound 6d was selected for further pre-clinical evaluations.
Pinto, Donald J.P.,Galemmo Jr., Robert A.,Quan, Mimi L.,Orwat, Michael J.,Clark, Charles,Li, Renhua,Wells, Brian,Woerner, Francis,Alexander, Richard S.,Rossi, Karen A.,Smallwood, Angela,Wong, Pancras C.,Luettgen, Joseph M.,Rendina, Alan R.,Knabb, Robert M.,He, Kan,Wexler, Ruth R.,Lam, Patrick Y.S.
p. 5584 - 5589
(2007/10/03)
Pyrazolobenzamides and derivatives as factor Xa inhibitors
The present application describes pyrazolobenzamides and derivatives thereof of Formula I: [in-line-formulae]P4-P-M-M4??I [/in-line-formulae] or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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Page/Page column 78; 82
(2010/11/08)
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