Malonamid and malonamic ester derivatives with...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S357000, C546S291000, C546S300000

Reexamination Certificate

active

07153876

ABSTRACT:
Compounds of formula I,in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

REFERENCES:
patent: 2003/0027828 (2003-02-01), Schudok et al.
patent: 97/48706 (1997-12-01), None
patent: 97/49684 (1997-12-01), None
patent: 00/01704 (2000-01-01), None
H. Cole, “The tissue factor pathway of coagulation,”Aust. J. Med. Sci., 16:87-93 (1995).
G. J. Broze, Jr., “Tissue factor pathway inhibitor and the current concept of blood coagulation,”Blood Coagulation and Fibrinolysis, 6(Suppl. 1):S7-S13 (1995).
L. A. Harker et al., “Antithrombotic and Antilesion Benefits without Hemorrhagic Risks by Inhibiting Tissue Factor Pathway,”Haemostasis, 26 (Suppl. 1):76-82 (1996).
L. A. Harker et al., “Antithrombotic Benefits and Hemorrhagic Risks of Direct Thrombin Antagonists,”Thrombosis and Haemostasis, 74(1):464-472 (1995).
Y. Cheng and W. H. Prusoff, “Relationship Between the Inhibition Constant (K1) and the Concentration of Inhibitor Which Causes 50 Per Cent Inhibition (/50) of an Enzymatic Reaction,”Biochem. Pharmacol., 22:3099-3108 (1973).
I. H. Segel, Enzyme Kinetics: Behavior And Analysis Of Rapid Equilibrium And Steady-State Enzyme Systems 100-125 (John Wiley & Sons, New York 1975).
J. A. Ostrem et al., “Discovery of a Novel, Potent, and Specific Family of Factor Xa Inhibitors via Combinatorial Chemistry,”Biochemistry, 37:1053-1059 (1998).
J. E. Hall et al., “Anti-PneumocystisActivities of Aromatic Diamidoxime Prodrugs,”Antimicrobial Agents and Chemotherapy, 42(3):666-674 (1998).
G. E. Davies and J. S. Lowe, “The Inhibition of Guinea-Pig Plasma Kallikrein by Amidines,”Advances in Experimental Medicine and Biology, 8:453-460 (1970).
International Search Report for International Application No. PCT/EP 01/10845 (Nov. 27, 2001).
Geratz et al., “Diamidino-α,ω-diphenoxyalkanes. Structure-Activity Relationships for the Inhibition of Thrombin, Pancreatic Kallikrein, and Trypsin,”Journal of Medicinal Chemistry16(9):970-975 (1973).
Rauch et al., “Thrombus formation on atherosclerotic plaques: pathogenesis and clinical consequences,”Ann. Intern. Med., 134(3):224-238 (2001).
Van Aken et al., “Anticoagulation: the present and future,”Clin. Appl. Thromb. Hemost., 7(3):195-204 (2001).

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