Aromatic amidine derivatives and salts 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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514367, 514373, 514375, 514379, 514393, 514394, 514395, 514408, 514423, 514424, 514428, 514429, 548148, 548165, 548178, 548179, 548180, 548207, 548209, 548217, 548221, 548222, 548223, 548224, 548241, 5483061, 5483615, 5483625, 548525, 548539, A61K 3140, C07D20709

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active

055763430

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: 4563527 (1986-01-01), Fuji
patent: 4634783 (1987-01-01), Fuji
patent: 4681886 (1987-07-01), Haugwitz et al.
patent: 4952562 (1990-08-01), Klein
patent: 5256812 (1993-10-01), Alig
patent: 5258398 (1993-11-01), Klein
Tidwell et al, "Strategies for Anticoagulation with Synthetic Protease Inhibitors-Xa Inhibitors Versus Thrombin Inhibitors", Thrombosis Research, 19:339-349 (1980).
Hauptmann et al, ACTA Biologica Et Medica Germanica, 35:635-644 (1976).
Markwardt, "Zur Wirkung Von Aromatischen Bisamidinen Auf Blutgerinnungs-Und Fibrinolysevorg ange".

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