Patent EA-005029-B1 (EA)
Title: Highly selective norepinephrine reuptake inhibitors and methods of using the same
Inventor: WONG ERIK H F
IPC: A61K31/00
Filed: 2000-06-22
Abstract: 1. Use an optically pure (S, S) reboxetine, or a pharmaceutically acceptable salt thereof, said compound being substantially free of (R, R) reboxetine in a manufacture of a medicament to treat or prevent a disease selected from chronic pain, incontinence, migraine headaches and fibromyalgia and other somatoform disorders and peripheral neuropathy. 2. Use according to claim 1 wherein the (S, S) reboxetine is administered in an amount of about 0.1 to about 10 mg/day. 3. Use according to claim 1 wherein the (S, S) reboxetine is administered in an amount of about 0.5 to about 8 mg/day, for example, of about 0.5 to about 5 mg/day, of about 0.5 to about 2.5 mg/day, of about 0.5 to about 0.9 mg/day, of about 0.5 to about 0.8 mg/day or of about 0.5 to about 0.75 mg/day. 4. Use according to any preceeding claim wherein the (S, S) reboxetine pharmaceutically acceptable salt is a methanesulfonate salt. 5. Use according to any preceeding claim wherein the optically pure (S, S) reboxetine or a pharmaceutically acceptable salt thereof comprises at least about 90 wt. % of (S, S) reboxetine, and less than about 10 wt. % of (R, R) reboxetine, based on the total weight of the (S, S) and (R, R) reboxetine present. 6. Use according to claim 5 wherein the optically pure (S, S) reboxetine or a pharmaceutically acceptable salt thereof comprises at least about 97 wt. % of (S, S) reboxetine and less than about 3 wt. % of (R, R) reboxetine, based on the total weight of the (S, S) and (R, R) reboxetine present. 7. Use according to claim 6 wherein the optically pure (S, S) reboxetine or a pharmaceutically acceptable salt thereof comprises at least about 99 wt. % of (S, S) reboxetine and less than about 1 wt. % of (R, R) reboxetine, based on the total weight of the (S, S) and (R, R) reboxetine present. 8. Use according to claim 1 wherein the incontinence comprises incontinence under stress, incontinence caused by overfull of urinary bladder or mixed incontinence. 9. Use according to claim 1 wherein the somatoform disorder comprises somatyzed disorder, conversion disorder, pain, hypochondriac syndrome, dismorphic disorder, non-differential somatoform disorder or NOS somatoform disorder. 10. A method of treating or preventing a disease selected from chronic pain, incontinence, migraine headaches and fibromyalgia and other somatoform disorders and peripheral neuropathy in mammels comprising administering a therapeutically effective amount of an optically pure (S, S) reboxetine, or a pharmaceutically acceptable salt thereof, said compound being substantially free of (R, R) reboxetine. 11. The method according to claim 10 wherein the (S, S) reboxetine is administered in an amount of about 0.1 to about 10 mg/day. 12. The method according to claim 11 wherein the (S, S) reboxetine is administered in an amount of about 0.5 to about 8 mg/day, for example, of about 0.5 to about 5 mg/day, of about 0.5 to about 2.5 mg/day, of about 0.5 to about 0.9 mg/day, of about 0.5 to about 0.8 mg/day or of about 0.5 to about 0.75 mg/day. 13. The method according to any one of claims 10-12 wherein the (S, S) reboxetine pharmaceutically acceptable salt is a methanesulfonate salt. 14. The method according to any one of claims 10-13 wherein the optically pure (S, S) reboxetine or a pharmaceutically acceptable salt thereof comprises at least about 90 wt. % of (S, S) reboxetine, and less than about 10 wt. % of (R, R) reboxetine, based on the total weight of the (S, S) and (R, R) reboxetine present. 15. The method according to claim 14 wherein the optically pure (S, S) reboxetine or a pharmaceutically acceptable salt thereof comprises at least about 97 wt. % of (S, S) reboxetine and less than about 3 wt. % of (R, R) reboxetine, based on the total weight of the (S, S) and (R, R) reboxetine present. 16. The method according to claim 15 wherein the optically pure (S, S) reboxetine or a pharmaceutically acceptable salt thereof comprises at least about 99 wt. % of (S, S) reboxetine and less than about 1 wt. % of (R, R) reboxetine, based on the total weight of the (S, S) and (R, R) reboxetine present. 17. The method according to claim 10 wherein the incontinence comprises incontinence under stress, incontinence caused by overfull of urinary bladder or mixed incontinence. 18. The method according to claim 10 wherein the somatoform disorder comprises somatyzed disorder, conversion disorder, pain, hypochondriac syndrome, dismorphic disorder, non-differential somatoform disorder or NOS somatoform disorder.