Aromatic amidine derivatives and salts thereof

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

1997-09-05

1999-02-02

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

5142328, 5142338, 5142345, 5142352, 5142355, 514254, 514255, 514443, 514469, 544111, 544132, 544141, 544145, 544147, 544154, 544242, 544315, 544316, 544336, 544368, 544372, 544374, 549 58, 549467, A61K 3140, A61K 31445, A61K 31495, A61K 3150, A61K 31505, C07D40310, C07D23902, C07D24102

Patent

active

058665773

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: 4952562 (1990-08-01), Klein
patent: 5256812 (1993-10-01), Alig
patent: 5258398 (1993-11-01), Klein
Wagner et al. "Synthesis of 4-substituted 1-amidino and 6-substituted-2 aminonaphthyl derivatives . . . " CA 90:38710, 1978.
Balzarini et al. "Inhibitory activity of diarylamidine derivatives on murine leukemia . . . " CA 99:169063, 1983.
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 VonAromatischen Bisamidinen Auf Blutgerinnungs--Und Fibrinolysevorgange".
Balzarini et al. "Inhibitory activity of diarylamidine derivatives . . . " CA 99:169063, 1983.
Tidweli et al. "Diarylamidine Derivatives with one or both of the aryl moieties consisting of an indole or indole like ring. Inhibitors of arginin-specific esteroproteases" J. Med. Chem. v. 21 pp. 613-623, 1987.

Affiliated with

Also associated with

Rating

Aromatic amidine derivatives and salts thereof does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Aromatic amidine derivatives and salts thereof, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Aromatic amidine derivatives and salts thereof will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1117726