409082-02-6Relevant articles and documents
Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
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Page/Page column 68, (2013/06/27)
The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.
3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)
Islam, Imadul,Bryant, Judi,May, Karen,Mohan, Raju,Yuan, Shendong,Kent, Lorraine,Morser, John,Zhao, Lei,Vergona, Ron,White, Kathy,Adler, Marc,Whitlow, Marc,Buckman, Brad O.
, p. 1349 - 1354 (2007/10/03)
A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B. (-)2a displays TAFIa IC50 = 3 nM and 600-fold selectivity against CPN. Inhibition of TAFIa with (rac)2a resulted in dose dependent acceleration of human plasma clot lysis in vitro and was efficacious as an adjunct to tPA in an in vivo rabbit jugular vein thrombolysis model.