Amidine inhibitors of serine proteases

Details Amidine inhibitors of serine proteases Amidine inhibitors of serine proteases

2005-01-04

2005-01-04

Aulakh, Charanjit S. (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S537000, C548S532000, C548S518000, C548S465000, C546S146000, C546S208000, C546S278400, C544S372000, C514S422000, C514S414000, C514S340000, C514S326000, C514S307000, C514S252010

Reexamination Certificate

active

06838479

ABSTRACT:
Inhibitors of serine proteases are provided having formula (I)wherein X, R1, R2, R3, R4and R5are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.

REFERENCES:
patent: 5504064 (1996-04-01), Morrissey et al.
patent: 5504067 (1996-04-01), Morrissey et al.
patent: 5580560 (1996-12-01), Nicolaisen et al.
patent: 5589173 (1996-12-01), O'Brien et al.
patent: 5646165 (1997-07-01), Abelman et al.
patent: 5656600 (1997-08-01), Abelman et al.
patent: 5656645 (1997-08-01), Tamura et al.
patent: 5658930 (1997-08-01), Tamura et al.
patent: 5658939 (1997-08-01), Abelman et al.
patent: 5670479 (1997-09-01), Abelman et al.
patent: 5679639 (1997-10-01), Griffin et al.
patent: 5726159 (1998-03-01), Schacht et al.
patent: 6057342 (2000-05-01), Fevig et al.
patent: 6410733 (2002-06-01), Pastor et al.
patent: WO 9315756 (1993-08-01), None
patent: WO 9413693 (1994-06-01), None
patent: WO 9610022 (1996-04-01), None
patent: WO 9616940 (1996-06-01), None
patent: WO 9640679 (1996-12-01), None
patent: WO 9730073 (1997-08-01), None
patent: WO 9964392 (1999-12-01), None
Broze, George J., “Tissue Factor Pathway Inhibitor”Thromb. Haemostas.74:90 (1995).
Dennis and Lazarus, “Kunitz Domain Inhibitors of Tissue Factor-Factor VIIa; II. Potent and Specific Inhibitors by Competitive Phage Selection”Journal of Biological Chemistry269(35):22137-22144 (1994).
Hagen et al., “Characterization of a cDNA coding for human factor VII”Proc. Natl. Acad. Sci. USA83:2412-2416 (1986).
Harker et al., “Antithrombotic benefits and hemorrhagic risks of direct thrombin antagonists”Thrombosis and Haemostasis74:464-472 (1995).
Jang et al., “Influence of blockade at specific levels of the coagulation cascade on restenosis in a rabbit atherosclerotic femoral artery injury model”Circulation92:3041-3050 (1995).
Katakura, S. et al., “A novel factor Xa inhibitor: structure-activity relationships and selectivity between factor Xa and thrombin”Biochem.&Biophys. Res. Comm.197:965-972 (1993).
Kelley et al., “A Soluble Tissue Factor Mutant Is a Selective Anticoagulant and Antithrombotic Agent”Blood89(9):3219-3227 (1997).
Kirchhofer et al., “Active Site-Blocked Factors VIIa and IXa Differentially Inhibit Fibrin Formation in a Human Ex Vivo Thrombosis Model”Arterioscler. Thromb. Vasc. Biol.15(8):1098-1106 (Aug. 1995).
Lawson, J.H. et al., “A model for the tissue factor pathway to thrombin”Journal of Biological Chemistry269:23357-23366 (1994).
Stanssens et al., “Anticoagulant repertoire of the hookworm ancylostoma caninum”Proc. Natl. Acad. Sci. USA93:2149-2154 (1996).
Stubbs and Bode, “Coagulation factors and their inhibitors”Current Opinion in Structural biology4:823-832 (1994).

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