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

[1]  R. Knabb,et al.  Nonpeptide factor Xa inhibitors: DPC423, a highly potent and orally bioavailable pyrazole antithrombotic agent. , 2006, Cardiovascular drug reviews.

[2]  P. Lam,et al.  Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. , 2006, Bioorganic & medicinal chemistry letters.

[3]  P. Lam,et al.  Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor. , 2005, Journal of medicinal chemistry.

[4]  L. Drouet,et al.  Rationale for the use of antifactor Xa in the treatment and prevention of venous and arterial thromboembolic events , 2005, European journal of clinical investigation.

[5]  Deepak L. Bhatt,et al.  Factor Xa inhibitors in acute coronary syndromes: moving from mythology to reality , 2005, Journal of thrombosis and haemostasis : JTH.

[6]  P. Lam,et al.  Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1). , 2003, Journal of medicinal chemistry.

[7]  P. Lam,et al.  Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants. , 2003, Journal of medicinal chemistry.

[8]  P. Lam,et al.  Nonpeptide Factor Xa Inhibitors III: Effects of DPC423, an Orally-Active Pyrazole Antithrombotic Agent, on Arterial Thrombosis in Rabbits , 2002, Journal of Pharmacology and Experimental Therapeutics.

[9]  R. Leadley.  Coagulation factor Xa inhibition: biological background and rationale. , 2001, Current topics in medicinal chemistry.

[10]  P. Lam,et al.  Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa. , 2001, Journal of medicinal chemistry.

[11]  G M Pacifici,et al.  Methods of Determining Plasma and Tissue Binding of Drugs , 1992, Clinical pharmacokinetics.

[12]  TanakaKiyoshi,et al.  PREPARATION OF TRIFLUOROACETONITRILE PHENYLIMINE AND ITS REACTIONS WITH SOME DIPOLAROPHILES , 1982 .

[13]  V. Fuster,et al.  Clinical and Experimental Experience with Factor Xa Inhibitors , 2004, American journal of cardiovascular drugs : drugs, devices, and other interventions.

[14]  K. Mann,et al.  The dynamics of thrombin formation. , 2003, Arteriosclerosis, thrombosis, and vascular biology.

[15]  R. Knabb,et al.  Nonpeptide factor Xa inhibitors: I. Studies with SF303 and SK549, a new class of potent antithrombotics. , 2000, The Journal of pharmacology and experimental therapeutics.

[16]  A. Debnath,et al.  A QSAR investigation of the role of hydrophobicity in regulating mutagenicity in the ames test: 1. Mutagenicity of aromatic and heteroaromatic amines in Salmonella typhimurium TA98 and TA100 , 1992, Environmental and molecular mutagenesis.