Claims
- 1. A compound of formula (I):
- 2. A compound of claim 1 which is in substantially pure form.
- 3. A compound of claim 1 which is in the form of an acid addition salt.
- 4. A compound of claim 3 wherein said acid is selected from the group consisting of mineral acids and organic acids.
- 5. A compound of claim 4 wherein said acid is a mineral acid.
- 6. A compound of claim 5 wherein said mineral acid is selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid and sulfamic acid.
- 7. A compound of claim 5 wherein said mineral acid is hydrochloric acid.
- 8. A compound of claim 4 wherein said acid is an organic acid.
- 9. A compound of claim 4 wherein said organic acid is selected from the group consisting of acetic acid, citric acid, lactic acid, tartaric acid, malonic acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, cyclohexylsulfamic acid and quinic acid.
- 10. A compound of claim 1 which is in the form of a solvate.
- 11. A compound of claim 10 wherein said solvate is a hemisolvate.
- 12. A compound of claim 10 wherein said solvate is selected from the group consisting of alcohol solvates, ether solvates and nitrile solvates.
- 13. A compound of claim 12 wherein said solvate is an alcohol solvate.
- 14. A compound of claim 13 wherein said alcohol is selected from the group consisting of methyl alcohol, ethyl alcohol, propyl alcohols, butyl alcohols, and pentyl alcohols.
- 15. A compound of claim 14 wherein said alcohol is a secondary alcohol.
- 16. A compound of claim 15 wherein said secondary alcohol is selected from the group consisting of iso-propyl alcohol and sec-butyl alcohol.
- 17. A compound of claim 16 wherein said secondary alcohol is sec-butyl alcohol.
- 18. A compound of claim 12 wherein said solvate is an ether solvate.
- 19. A compound of claim 18 wherein said ether is selected from the group consisting of dimethoxymethane, tetrahydrofuran, dioxanes, furan, diethyl ether, ethylene glycol dimethyl ether, ethylene glycol diethyl ether, diethylene glycol dimethyl ether, diethylene glycol diethyl ether, triethylene glycol diisopropyl ether, anisole, and t-butyl methyl ether. Preferred among these ethers are diethyl ether, tetrahydrofuran and dioxane.
- 20. A compound of claim 12 wherein said solvate is a nitrile solvate.
- 21. A compound of claim 20 wherein said nitrile is acetonitrile.
- 22. A compound of claim 1 which has formula (I-i):
- 23. A compound of claim 10 which is prepared by recrystallizing from a solvent the compound of Formula (I).
- 24. A compound of claim 23 wherein said solvent is selected from the group consisting of alcohols, ethers and nitrites.
- 25. A compound of claim 24 wherein said solvent is an alcohol.
- 26. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier or excipient.
- 27. A pharmaceutical composition of claim 26 wherein said compound of Formula (I) is in the form of a hydrochloride salt.
- 28. A pharmaceutical composition of claim 27 wherein said compound of Formula (I) is the 2-butanol hemisolvate.
- 29. A pharmaceutical composition of claim 26 which is in a capsule or compressed tablet dosage form.
- 30. A pharmaceutical composition of claim 29 wherein said therapeutically effective amount is from about 1 mg to about 1000 mg per dose.
- 31. A pharmaceutical composition of claim 26 which is in liquid form.
- 32. A method of treating or preventing a pathological condition mediated by Factor Xa production in a patient, comprising administering to said patient a pharmaceutically effective amount of a compound according to claim 1.
- 33. A method of claim 32 wherein the pathological condition is selected from the group consisting of acute myocardial infarction (AMI), unstable angina, thromboembolism, acute vessel closure associated with thrombolytic therapy, percutaneous transluminal coronary angioplasty (PTCA), transient ischemic attacks, stroke, intermittent claudication, and restenosis.
- 34. A method of inhibiting Factor Xa production in a patient, comprising administering to said patient a pharmaceutically effective amount of a compound according to claim 1.
- 35. A compound of claim 22 which is characterized by a differential scanning calorimetry thermogram having a peak at about 185° C. to about 192° C.
- 36. A compound of claim 22 which is characterized by a differential scanning calorimetry thermogram substantially in accordance with that shown in FIG. 1.
- 37. A compound of claim 22 which is characterized by an x-ray powder diffraction pattern which comprises two or more 2θ values selected from 5.0±0.2, 14.8±0.2, 15.1±0.2, 15.8±0.2, 16.6±0.2, 17.7±0.2, 17.9±0.2, 19.6±0.2, 24.9±0.2, 25.0±0.2, and 27.0±0.2.
- 38. A compound of claim 22 which is characterized by an x-ray powder diffraction pattern substantially in accordance with that shown in FIG. 2.
- 39. A compound of claim 22 wherein 2-BuOH is (S)-(+)-2-butanol.
- 40. A compound of claim 22 wherein 2-BuOH is (R)-(−)-2-butanol.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0108903.6 |
Apr 2001 |
GB |
|
Parent Case Info
[0001] This application is a continuation application of International Application Number PCT/US01/31087, filed Oct. 4, 2001, which, in turn, is entitled to the benefit of, and claims priority from earlier filed U.S. Application No. 60/238,316, filed Oct. 5, 2000, and Great Britain Application Number 0108903.6, filed Apr. 10, 2001, the contents of all of which are incorporated herein by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60238316 |
Oct 2000 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/US01/31087 |
Oct 2001 |
US |
Child |
10404678 |
Apr 2003 |
US |