Patent EA-002360-B1 (EA)
Title: Treatment of central nervous system disorders with selective estrogen receptor modulators
Inventor: BALES KELLY RENEE
IPC: A61P25/28
Filed: 1998-04-07
Abstract: 1. A method of treating, in a patient in need of such treatment, a central nervous system disorder selected from depression, mood swings, and Alzheimer's disease comprising administering a therapeutically effective amount of a compound having the structure   or a pharmaceutically acceptable salt or pro-drug thereof, wherein R<1> and R<2> are independently selected from the group consisting of hydroxy and alkoxy of one to four carbon atoms; and R<3> and R<4> are independently selected from methyl or ethyl, or R<3> and R<4>, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methylpyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring. 2. The method of Claim 1 wherein said method comprises treating, in a patient in need of such treatment, depression or mood swings. 3. The method of Claim 1 wherein said method comprises treating, in a patient in need of such treatment, Alzheimer' s disease. 4. The method of Claim 1 wherein R<1> and R<2> are both hydroxy. 5. The method of Claim 2 wherein R<1> and R<2> are both hydroxy. 6. The method of Claim 3 wherein R<1> and R<2> are both hydroxy. 7. The method of Claim 1 wherein R<1> is hydroxy and R<2> is alkoxy of one to four carbon atoms. 8. The method of Claim 2 wherein R<1> is hydroxy and R<2> is alkoxy of one to four carbon atoms. 9. The method of Claim 3 wherein R<1> is hydroxy and R<2> is alkoxy of one to four carbon atoms. 10. The method of Claim 1 wherein R<3> and R<4> combine with the nitrogen atom to which they are attached to form a piperidino ring. 11. The method of Claim 2 wherein R<3> and R<4> combine with the nitrogen atom to which they are attached to form a piperidino ring. 12. The method of Claim 3 wherein R<3> and R<4> combine with the nitrogen atom to which they are attached to form a piperidino ring. 13. A method of treating, in a patient in need of such treatment, depression or mood swings comprising administering a therapeutically effective amount of a compound having the structure   or a pharmaceutically acceptable salt or pro-drug thereof, wherein R<2> is hydroxy or methoxy. 14. The method of Claim 13 wherein said compound is 6-hydroxy-2-(4-methoxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 15. The method of Claim 13 wherein said compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 16. A method of treating, in a patient in need of such treatment, Alzheimer's disease comprising administering a therapeutically effective amount of a compound having the structure   or a pharmaceutically acceptable salt or pro-drug thereof, wherein R<2> is hydroxy or methoxy. 17. The method of Claim 16 wherein said compound is 6-hydroxy-2-(4-methoxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 18. The method of Claim 16 wherein said compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 19. The method of Claim 13 wherein said salt is the hydrochloride salt. 20. The method of Claim 16 wherein said salt is the hydrochloride salt.