Patent EA-001257-B1 (EA)
Title: Benzothiiophenes, pharmaceutical compositions containing same, and methods of treating human pathology using same
Inventor: ARBUTHOT GORDON N
IPC: C07D333/58
Filed: 1997-03-20
Abstract: 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. 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 1 or 2 wherein at least about 90% of said particles have a size of less than about 50 microns. 4. The compound of claim 3 wherein at least 90% of said particles have a size of less than about 35 microns. 5. The compound of any of claims 1 to 4 wherein the compound of formula I is raloxifene hydrochloride. 6.The compound of claim 5 which is the non-solvated crystalline hydrochloride having substantially the following X-ray diffraction pattern obtained with copper radiation: d-line spacing (Angstroms)	I/I o (x100) 13,3864	71,31 9,3598	33,16 8,4625	2,08 7,3888	7,57 6,9907	5,80 6,6346	51,04 6,1717	29,57 5,9975	5,67 5,9135	9,87 5,6467	38,47 5,4773	10,54 5,2994	4,74 4,8680	4,03 4,7910	5,98 4,6614	57,50 4,5052	5,75 4,3701	9,03 4,2516	69,99 4,2059	57,64 4,1740	65,07 4,0819	12,44 3,9673	22,53 3,9318	100,00 3,8775	9,07 3,7096	33,38 3,6561	21,65 3,5576	3,36 3,5037	7,97 3,4522	18,02 3,4138	4,65 3,2738	10,23 3,1857	8,90 3,1333	6,24 3,0831	9,43 3,0025	12,13 2,9437	4,96 2,8642	7,70 2,7904	11,95 2,7246	3,05 2,6652	3,32 2,5882	7,30 13,3864	71,31 9,3598	33,16 8,4625	2,08 7,3888	7,57 6,9907	5,80 6,6346	51,04 6,1717	29,57 5,9975	5,67 5,9135	9,87 5,6467	38,47 5,4773	10,54 5,2994	4,74 4,8680	4,03 4,7910	5,98 4,6614	57,50 4,5052	5,75 4,3701	9,03 4,2516	69,99 4,2059	57,64 4,1740	65,07 4,0819	12,44 3,9673	22,53 3,9318	100,00 3,8775	9,07 3,7096	33,38 3,6561	21,65 3,5576	3,36 3,5037	7,97 3,4522	18,02 3,4138	4,65 3,2738	10,23 3,1857	8,90 3,1333	6,24 3,0831	9,43 3,0025	12,13 2,9437	4,96 2,8642	7,70 2,7904	11,95 2,7246	3,05 2,6652	3,32 2,5882	7,30 7. A pharmaceutical composition comprising or formulated using a compound as claimed in any one of claims 1 to 5 and one or more pharmaceutically acceptable carriers, diluents, or excipients. 8. A method of enhancing bioavailability in the treatment of osteoporosis with raloxifene comprising administering an effective amount of a compound of formula I as claimed in any one of claims 1 to 6, or a pharmaceutical composition as claimed in claims 7, to a person in need thereof. 9. A method of enhancing bioavailability in lowering serum lipid levels with raloxifene comprising administering an effective amount of a compound of formula I as claimed in any one of claims 1 to 6, or a pharmaceutical composition as claimed in claims 7, to a person in need thereof. 10. A method for enhancing bioavailability in preventing breast cancer with raloxifene comprising administering an effective amount of a compound of formula I as claimed in any one of claims 1 to 6, or a pharmaceutical composition as claimed in claims 7, to a person in need thereof. 11. An article of manufacture comprising packaging material containing a pharmaceutical composition, said packaging material further containing labeling indicating said pharmaceutical composition is useful for inhibiting a human pathology, said pharmaceutical composition comprising or formulated using a compound as claimed in any of claims 1-6.