Title:
p-ヒドロキシ-ミルナシプランの立体異性体およびその使用方法
Document Type and Number:
Japanese Patent JP4288263
Kind Code:
B2
Abstract:
The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (-)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient. Finally, the present invention relates to methods of treating mammals suffering from various afflictions, e.g., depression, chronic pain, or fibromyalgia, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of the present invention.
Inventors:
Lerry, Roman, Buoy.
Hefernan, Michael
Backwalled, Stephen, Elle.
Swager, Timothy, M.
Hefernan, Michael
Backwalled, Stephen, Elle.
Swager, Timothy, M.
Application Number:
JP2005501895A
Publication Date:
July 01, 2009
Filing Date:
October 22, 2003
Export Citation:
Assignee:
COLLEGIUM PHARMACEUTICAL, INC.
International Classes:
C07C237/24; A61K9/22; A61K31/165; A61K31/195; A61K31/277; A61K31/655; A61K31/695; A61K45/00; A61P1/04; A61P1/06; A61P1/14; A61P3/10; A61P9/04; A61P9/10; A61P11/02; A61P11/06; A61P13/02; A61P13/10; A61P15/00; A61P17/00; A61P17/02; A61P17/06; A61P17/16; A61P19/02; A61P25/00; A61P25/04; A61P25/06; A61P25/14; A61P25/22; A61P25/24; A61P25/32; A61P29/00; A61P31/18; A61P31/22; A61P35/00; A61P37/00; A61P37/06; A61P43/00; C07C233/58; A61K
Domestic Patent References:
| JP58004752A | ||||
| JP3056415A |
Attorney, Agent or Firm:
Mizuno Yuuki
Junji Endo
Junji Endo