Amidinoindoles, amidinoazoles, and analogs thereof

Details Amidinoindoles, amidinoazoles, and analogs thereof Amidinoindoles, amidinoazoles, and analogs thereof

1997-08-18

1999-03-23

Richter, Johann

Chain, staple, and horseshoe making

548490, 548494, 548495, 548497, 548500, 548501, 548502, 548504, 548507, 548510, 548511, 548440, 548492, 548512, 549 29, 549 49, 549467, 549468, 549506, 544359, 544360, 546184, 546186, 546187, 546193, C07D20904, C07D20914, C07D20926, C07D33352

Patent

active

058861912

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.

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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 Activation".
Tidwell et al., Journal of Medicinal Chemistry, 1978, 21 (7), 613-623, "Diarylamidine Derivatives with One or Both of the Aryl Moieties Consisting of an Indole of Indole-like Ring. Inhibitors of Arginine-Specific Esteroproteases".

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