Amidinoindoles, amidinoazoles, and analogs thereof

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

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5462757, 5462734, 5462737, 5483094, 5483625, 548491, 548484, 549467, 549 58, 514397, 514399, 514400, A01N 4340, A01N 4338, C07D40112, C07D23526

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active

060432578

ABSTRACT:
The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.

REFERENCES:
patent: 5328920 (1994-07-01), Effland et al.
Tidwell et al, Journal of Medicinal Chemistry, 1983, 26, 294-298, "Aromatic Amidines: Comparison of Their Ability to Block Respiratory Syncytial Virus Induced Cell Fusion and to Inhibit Plasmin, Urokinase, Thrombin, and Trypsin."
Fairley et al, Journal of Medicinal Chemistry, 1993, 36, 1746-1753, "Structure, DNA Minor Groove Binding, and Base Pair Specificity of Alkyl-and Aryl-Linked Bis (amidinobenzimidazoles) and Bis (amidinoindoles). "
Geratz et al, Thrombosis Research, 1981, 24, 73-83, "Inhibitory Effect of Amidino-Substituted Heterocyclic Compounds on The Amidase Activity of Plasmin and of High and Low Molecular Weight Urokinase and on Urokinase-Induced Plasminogen Activat ion. "

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