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 substituted or unsubstituted pyrrolidinyl group; 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. An aromatic amidine derivative, 2-[4-[(1-acetimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)propionic acid, or a salt thereof.
- 4. An aromatic amidine derivative, (+)-2-[4-[((3S)-1-acetimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)propionic acid, or a salt thereof.
- 5. An aromatic amidine derivative, (2S)-2-[4-[((3S)-1-acetimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)propionic acid, or a salt thereof.
- 6. An aromatic amidine derivative, (2R)-2-[4-[((3R)-1-acetimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)propionic acid, or a salt thereof.
- 7. An aromatic amidine derivative, 2-[4-[(1-acetimidoyl-2-pyrrolidinyl)methoxy]phenyl]-3-(5-amidinobenzo[b]thien-2-yl)propionic acid, or a salt thereof.
- 8. An aromatic amidine derivative, (+)-2-[4-[((2S)-1-acetimidoyl-2-pyrrolidinyl)methoxy]phenyl]-3-(5-amidinobenzo[b]thien-2-yl)propionic acid, or a salt thereof.
- 9. 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.
- 10. 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.
- 11. 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.
- 12. An anticoagulation composition comprising an anticoagulative effective amount of the compound of claim 4 or a salt thereof as an active ingredient and a pharmaceutically acceptable carrier.
- 13. An anticoagulation composition comprising an anticoagulative effective amount of the compound of claim 5 or a salt thereof as an active ingredient and a pharmaceutically acceptable carrier.
- 14. An anticoagulation composition comprising an anticoagulative effective amount of the compound of claim 8 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 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 (6)
Foreign Referenced Citations (3)
Number |
Date |
Country |
0048433 |
Mar 1982 |
EPX |
3402628 |
Aug 1984 |
DEX |
1050302 |
May 1965 |
GBX |
Non-Patent Literature Citations (3)
Entry |
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". |
Divisions (1)
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Number |
Date |
Country |
Parent |
282571 |
Jul 1994 |
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Continuations (1)
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Number |
Date |
Country |
Parent |
969396 |
Oct 1992 |
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