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Claims for Patent: 8,404,703

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Claims for Patent: 8,404,703

Title:Medicinal compositions containing aspirin
Abstract: A combination of 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
Inventor(s): Asai; Fumitoshi (Nishitokyo, JP), Sugidachi; Atsuhiro (Kawasaki, JP), Ogawa; Taketoshi (Tokyo, JP), Inoue; Teruhiko (Ube, JP)
Assignee: Daiichi Sankyo Company, Limited (Tokyo, JP)
Application Number:11/520,168
Patent Claims: 1. A method for treatment of a disease caused by thrombus or embolus, said method consisting of: administering (i) 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c] pyridine or a pharmaceutically acceptable salt thereof, (ii) aspirin, and (iii) one or more pharmaceutically acceptable excipients, lubricants, binders, disintegrators, emulsifiers, stabilizers, corrigents and/or diluents, wherein (i) and (ii) are administered in pharmacologically effective amounts, to a human in need of reduction of thrombogenesis or reduction of platelet aggregation.

2. The method according to claim 1, wherein the pharmaceutically acceptable salt is a hydrochloride.

3. A method for the treatment of a patient undergoing stenting, angioplasty, and/or to prevent restenosis comprising administering a pharmaceutical composition comprising 2-acetoxy-5 -(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, as active ingredients, in their pharmacologically effective amounts, to a warm-blooded animal.

4. A method according to claim 3, in which the pharmaceutically acceptable salt is the hydrochloride or maleate.

5. A method according to claim 3 or claim 4, in which the warm-blooded animal is a human.

6. The method according to claim 1, wherein said disease caused by thrombus or embolus is selected from the group consisting of: stable angina pectoris, unstable angina pectoris, thromboembolism, cerebral ischemic insult, restenosis, and embolism.

7. A method for inhibiting thrombogenesis, platelet aggregation, or thromboembolization consisting of: administering (i) 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, (ii) aspirin, and (iii) one or more pharmaceutically acceptable excipients, lubricants, binders, disintegrators, emulsifiers, stabilizers, corrigents and/or diluents, wherein (i) and (ii) are administered in pharmacologically effective amounts, to a human having a cardiovascular disease.

8. The method according to claim 7, wherein the pharmacologically effective amounts are pharmacologically effective amounts for the components individually.

9. The method according to claim 7, wherein the pharmaceutically acceptable salt is a hydrochloride.

10. The method according to claim 7, wherein said human is a patient undergoing angioplasty, endarterectomy or stent therapy.

11. The method according to claim 7, wherein 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine and aspirin are administered.

12. The method according to claim 1, wherein the pharmacologically effective amounts are pharmacologically effective amounts for the components individually.

13. The method according to claim 1, wherein 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine and aspirin are administered.

14. A method for reducing thrombotic symptoms associated with cardiovascular or cerebrovascular disorders, said method consisting of: administering (i) 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c] pyridine or a pharmaceutically acceptable salt thereof, (ii) aspirin, and (iii) one or more pharmaceutically acceptable excipients, lubricants, binders, disintegrators, emulsifiers, stabilizers, corrigents and/or diluents, wherein (i) and (ii) are administered in pharmacologically effective amounts, to a human in need of reducing said symptoms.

15. The method according to claim 14, wherein the pharmaceutically acceptable salt is a hydrochloride.

16. The method according to claim 14, wherein said human has a cardiovascular disorder.

17. The method according to claim 16, wherein said human is a patient undergoing angioplasty, endarterectomy or stent therapy.

18. The method according to claim 14, wherein the pharmacologically effective amounts are pharmacologically effective amounts for the components individually.

19. The method according to claim 14, wherein 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine and aspirin are administered.

20. A method for reducing thrombotic cardiovascular events in a human, said method consisting of: administering (i) 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, (ii) aspirin, and (iii) one or more pharmaceutically acceptable excipients, lubricants, binders, disintegrators, emulsifiers, stabilizers, corrigents and/or diluents, wherein (i) and (ii) are administered in pharmacologically effective amounts, to said human in need of reduction of thrombogenesis or reduction of platelet aggregation.

21. The method according to claim 20, wherein the pharmaceutically acceptable salt is a hydrochloride.

22. The method according to claim 20, wherein the pharmacologically effective amounts are pharmacologically effective amounts for the components individually.

23. The method according to claim 20, wherein 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine and aspirin are administered.

24. A method for preventing a disease caused by thrombus or embolus, said method consisting of: administering (i) 2-acetoxy-5-(.alpha.-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahyd- rothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, (ii) aspirin, and (iii) one or more pharmaceutically acceptable excipients, lubricants, binders, disintegrators, emulsifiers, stabilizers, corrigents and/or diluents, wherein (i) and (ii) are administered in pharmacologically effective amounts, to a human in need of reduction of thrombogenesis or reduction of platelet aggregation.

25. The method according to claim 24, wherein the pharmaceutically acceptable salt is a hydrochloride.

26. The method according to claim 24, wherein said human has a cardiovascular disease.

27. The method according to claim 24, wherein said human has received or is undergoing angioplasty or stent therapy.
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