Aromatic amidine derivatives and salts thereof

Details Aromatic amidine derivatives and salts thereof Aromatic amidine derivatives and salts thereof

1995-06-06

1997-04-15

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514320, 514321, 514322, 514323, 514324, 546196, 546198, 546199, 546201, 546202, 546205, A61K 31445, C07D21106

Patent

active

056209916

ABSTRACT:
An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.
The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.

REFERENCES:
patent: 4634783 (1987-01-01), Fuji
patent: 4952562 (1990-08-01), Klein
patent: 5256812 (1993-10-01), Alig
patent: 5258398 (1993-11-01), Klein
Thrombosis Research, vol. 19, pp. 339-349, 1980, "Strategies for Anticoagulation With Synthetic Protease Inhibitors -Xa Inhibitors Versus Thrombin Inhibitors", R.R. Tidwell et al.

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