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 alkoxy group; R.sup.2 is a hydrogen atom, a alkyl group, a 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 alkyl group or a 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 piperidinyl group optionally substituted with a member selected from the group consisting of an alkyl group, an alkanoyl group, a carbamoyl group, a mono- or dialkylcarbamoyl group, a formimidoyl group, an alkanoimidoyl group, a benzimidoyl group, a carboxyl group, an alkoxycarbonyl group, a carboxyalkyl group, an alkylcarbonylalkyl group, an aminoalkyl group, an alkanoylamino group, an alkanoylaminoalkyl group, an imino group, and alkoxycarbonylimino 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 alkyl, alkoxy or akanoyl 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-4-piperidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)propionic acid, or a salt thereof.
- 4. An aromatic amidine derivative, (+)-2-[4-[(1-acetimidoyl-4-piperidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)propionic acid, or a salt thereof.
- 5. 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.
- 6. 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.
- 7. 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.
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. 08/282,571, 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 (4)
Non-Patent Literature Citations (1)
Entry |
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. |
Continuations (2)
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Number |
Date |
Country |
Parent |
282571 |
Jul 1994 |
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Parent |
969396 |
Oct 1992 |
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