Claims
- 1. An aromatic amidine derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof: ##STR14## wherein R.sup.1 is a hydrogen atom or a lower alkoxy group; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group, a carboxyl group, an alkoxycarbonyl group, a carboxyalkyl group or an alkoxycarbonylalkyl group; R.sup.3 is a hydrogen atom, a carboxyl group, an alkoxycarbonyl group, a carboxyalkyl group, an alkoxycarbonylalkyl group, a carboxyalkoxy group or an alkoxycarbonylalkoxy group; R.sup.4 is a hydrogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; n is an integer of 0 to 4; A is an alkylene group having a carbon number of 1 to 4, which may have 1 or 2 substituents selected from the group consisting of hydroxyalkyl, carboxyl, alkoxycarbonyl, carboxyalkyl and alkoxycarbonylalkyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety selected from the group consisting of imidazoline, piperazine, tetrahydrofuran, hexahydropyrimidine, pyrrole, imidazole, pyrazine, pyrrolidinone, piperidinone and morpholine; or Y is a cyclic hydrocarbon moiety selected from cyclopentyl and cyclohexyl optionally substituted with a substituent; wherein the group represented by ##STR15## is a member selected from the group consisting of indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; and said lower alkyl or alkoxy group has a carbon number of 1 to 6.
- 2. The aromatic amidine derivative or salt thereof according to claim 1, wherein said group represented by ##STR16## is a member selected from the group consisting of indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzothiazolyl, naphthyl and tetrahydronaphthyl.
- 3. The aromatic amidine derivative or salt thereof according to claim 1, wherein Y is said saturated or unsaturated 5- or 6-membered heterocyclic moiety.
- 4. An anticoagulation composition comprising an anticoagulative effective amount of the compound of claim 1 or a salt thereof as an active ingredient and a pharmaceutically acceptable carrier.
- 5. An anticoagulation composition comprising an anticoagulative effective amount of the compound of claim 2 or a salt thereof as an active ingredient and a pharmaceutically acceptable carrier.
- 6. An anticoagulation composition comprising an anticoagulative effective amount of the compound of claim 3 or a salt thereof as an active ingredient and a pharmaceutically acceptable carrier.
Priority Claims (1)
Number |
Date |
Country |
Kind |
3-286088 |
Oct 1991 |
JPX |
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Parent Case Info
This is a Continuation of parent application Ser. No. 08/469,593, filed Jun. 6, 1995; which in turn is a Divisional of parent application Ser. No. 08/282,571, filed Jul. 29, 1994 (now abandoned); which is a Continuation of application Ser. No. 07/969,396, filed Oct. 30, 1992 (now abandoned).
US Referenced Citations (5)
Foreign Referenced Citations (3)
Number |
Date |
Country |
0048433 |
Mar 1982 |
EPX |
3402628 |
Aug 1984 |
DEX |
1050302 |
May 1965 |
GBX |
Non-Patent Literature Citations (7)
Entry |
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. |
Divisions (1)
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Number |
Date |
Country |
Parent |
282571 |
Jul 1994 |
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Continuations (2)
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Number |
Date |
Country |
Parent |
469593 |
Jun 1995 |
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Parent |
969369 |
Oct 1992 |
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