You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Details for Patent: 6,458,811


✉ Email this page to a colleague

« Back to Dashboard


Title: Benzothiophenes formulations containing same and methods
Abstract:This invention provides compounds of formula I ##STR1## and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.
Inventor(s): Arbuthnot; Gordon Nelson (Indianapolis, IN), Dalder; Brian Weston (West Lafayette, IN), Hartauer; Kerry John (Indianapolis, IN), Luke; Wayne Douglas (West Lafayette, IN), Stratford, Jr.; Robert Eugene (Carmel, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Filing Date:Mar 10, 1997
Application Number:08/812,896
Claims:1. A compound of formula I ##STR8##

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]th iophene hydrochloride having substantially the following X-ray diffraction pattern obtained with copper radiation:

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 ##STR9##

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]th iophene hydrochloride, having substantially the following x-ray diffraction pattern obtained with copper radiation:

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]th iophene 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.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.