Benzamides and related inhibitors of factor XA

Patent metadata

Field	Value
Publication number	US-9629831-B2
Application number	US-201514742465-A
Country	US
Kind code	B2
Filing date	Jun 17, 2015
Priority date	Feb 29, 2000
Publication date	Apr 25, 2017
Grant date	Apr 25, 2017

Abstract

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

First claim

What is claimed is:

1. A method for preventing or treating venous thrombosis in a human patient in need thereof comprising administering to said patient a tablet comprising a maleate salt of the following compound:

2. A method for preventing or treating venous thrombosis in a human patient in need thereof comprising administering to said patient a capsule comprising a maleate salt of the following compound:

3. A method for preventing or treating deep venous thrombosis in a human patient in need thereof comprising administering to said patient a tablet comprising a maleate salt of the following compound:

4. A method for preventing or treating deep venous thrombosis in a human patient in need thereof comprising administering to said patient a capsule comprising a maleate salt of the following compound:

5. A method for preventing or treating pulmonary embolism in a human patient in need thereof comprising administering to said patient a tablet comprising a maleate salt of the following compound:

6. A method for preventing or treating pulmonary embolism in a human patient in need thereof comprising administering to said patient a capsule comprising a maleate salt of the following compound:

7. The method of claim 1 , wherein the method comprises administering the tablet once daily.

8. The method of claim 2 , wherein the method comprises administering the capsule once daily.

9. The method of claim 1 , wherein the tablet further comprises microcrystalline cellulose and magnesium stearate.

10. The method of claim 2 , wherein the capsule further comprises microcrystalline cellulose and magnesium stearate.

11. The method of claim 3 , wherein the method comprises administering the tablet once daily.

12. The method of claim 5 , wherein the method comprises administering the tablet once daily.

13. The method of claim 4 , wherein the method comprises administering the capsule once daily.

14. The method of claim 6 , wherein the method comprises administering the capsule once daily.

15. The method of claim 3 , wherein the tablet further comprises microcrystalline cellulose and magnesium stearate.

16. The method of claim 5 , wherein the tablet further comprises microcrystalline cellulose and magnesium stearate.

17. The method of claim 4 , wherein the capsule further comprises microcrystalline cellulose and magnesium stearate.

18. The method of claim 6 , wherein the capsule further comprises microcrystalline cellulose and magnesium stearate.

Assignees

• Millennium Pharm Inc

Inventors

• Zhu Bing-Yan
• Huang Wenrong

Classifications

• C07C237/42

  having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated · CPC title

• A61K31/616

  by carboxylic acids, e.g. acetylsalicylic acid · CPC title

• A61K9/48

  Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• C07C317/40

  Y being a hydrogen or a carbon atom · CPC title