Claims
- 1. A compound of formula I and pharmaceutically acceptable salts and solvates thereof, characterized in that the compound is in particulate form, said particles having a mean particle size of less than about 25 microns, at least about 90% of said particles have a size of less than about 50 microns.
- 2. The compound of claim 1 wherein said particles have a mean particle size of between about 5 and about 20 microns.
- 3. The compound of claim 2 wherein at least 90% of said particles have a size of less than about 35 microns.
- 4. A compound of claim 1 which is the non-solvated crystalline 6-hydroxy-2-(4-hydroxy-phenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride having substantially the following X-ray diffraction pattern obtained with copper radiation:d-line spacingI/Io(Angstroms)(x100)13.386471.319.359833.168.4625 2.087.3888 7.576.9907 5.806.634651.046.171729.575.9975 5.675.9135 9.875.646738.475.477310.545.2994 4.744.8680 4.034.7910 5.984.661457.504.5052 5.754.3701 9.034.251669.994.205957.644.174065.074.081912.443.967322.533.9318100.00 3.8775 9.073.709633.383.656121.653.5576 3.363.5037 7.973.452218.023.4138 4.653.273810.233.1857 8.903.1333 6.243.0831 9.433.002512.132.9437 4.962.8642 7.702.790411.952.7246 3.052.6652 3.322.5882 7.30.
- 5. A pharmaceutical formulation comprising or formulated using the compound of claim 4 and one or more pharmaceutically acceptable carriers, diluents, or excipients.
- 6. A pharmaceutical composition comprising or formulated using a compound according to claim 1, or a pharmaceutically acceptable salt or solvate thereof, in combination with one or more pharmaceutically acceptable carriers, diluents or excipients.
- 7. A non-solvated crystalline hydrochloride salt of a compound of formula I characterized in that the compound is in particulate form, said particles having a mean particle size of between about 5 and about 20 microns, at least about 90% of said particles having a size of less than about 35 microns.
- 8. A compound of claim 7 which is the non-solvated crystalline 6-hydroxy-2-(4-hydroxy-phenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride, having substantially the following x-ray diffraction pattern obtained with copper radiation:d-line spacingI/Io(Angstroms)(x100)13.386471.319.359833.168.4625 2.087.3888 7.576.9907 5.806.634651.046.171729.575.9975 5.675.9135 9.875.646738.475.477310.545.2994 4.744.8680 4.034.7910 5.984.661457.504.5052 5.754.3701 9.034.251669.994.205957.644.174065.074.081912.443.967322.533.9318100.00 3.8775 9.073.709633.383.656121.653.5576 3.363.5037 7.973.452218.023.4138 4.653.273810.233.1857 8.903.1333 6.243.0831 9.433.002512.132.9437 4.962.8642 7.702.790411.952.7246 3.052.6652 3.322.5882 7.30.
- 9. A pharmaceutical formulation comprising or formulated using the compound of claim 8 and one or more pharmaceutically-acceptable carriers, diluents, or excipients.
- 10. A pharmaceutical composition comprising or formulated using a compound according to claim 7, or a pharmaceutically acceptable salt or solvate thereof, with one or more pharmaceutically acceptable carriers, diluents or excipients.
- 11. A compound of claim 1 which is non-solvated crystalline 6-hydroxy-2-(4-hydroxy-phenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride.
- 12. A method of inhibiting osteoporosis comprising administering an effective amount of a compound of claim 1 to a person in need thereof.
- 13. A method of lowering serum lipid levels comprising administering a compound of claim 1, or a pharmaceutically acceptable salt or solvate thereof, to a person in need thereof.
- 14. A method for preventing breast cancer comprising administering to a woman in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt or solvate thereof.
- 15. A method of inhibiting osteoporosis comprising administering an effective amount of a compound of claim 7 to a person in need thereof.
- 16. A method of lowering serum lipid levels comprising administering a compound of claim 7, or a pharmaceutically acceptable salt or solvate thereof, to a person in need thereof.
- 17. A method for preventing breast cancer comprising administering to a woman in need thereof an effective amount of a compound of claim 7, or a pharmaceutically acceptable salt or solvate thereof.
Parent Case Info
This patent application claims the benefit under Title 35, United States Code Section 119(e) of U.S. Provisional Patent Application No. 60/014,167 having a filing date of Mar. 26, 1996.
US Referenced Citations (13)
Foreign Referenced Citations (5)
Number |
Date |
Country |
108606 |
Nov 1983 |
EP |
605193 |
Dec 1993 |
EP |
670162 |
Feb 1995 |
EP |
674903 |
Oct 1995 |
EP |
2293382 |
Mar 1996 |
GB |
Non-Patent Literature Citations (5)
Entry |
West “Blocky diamond particles from diamond powder” CA 73:57576, 1970.* |
Search report, title of 19 references.* |
see copy in SN 09/063,478.* |
Lieberman et al. “Pharmaceutical dosage forms” Marcel Dekker Inc. p. 107-117, 186-187, 1980.* |
Omelczuk et al. “Influence of micronization on the compaction properties of an investigational drug using tableting index analysis” Eur. J. Pharm. Biopharm. v. 43, 95-100, 1997. |
Provisional Applications (1)
|
Number |
Date |
Country |
|
60/014167 |
Mar 1996 |
US |