The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 02, 2006
Filed:
Oct. 22, 2003
Roman V. Rariy, Allston, MA (US);
Michael Heffernan, Hingham, MA (US);
Stephen L. Buchwald, Newton, MA (US);
Timothy M. Swager, Newton, MA (US);
Roman V. Rariy, Allston, MA (US);
Michael Heffernan, Hingham, MA (US);
Stephen L. Buchwald, Newton, MA (US);
Timothy M. Swager, Newton, MA (US);
Collegium Pharmaceutical, Inc., Cumberland, RI (US);
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 (IC=28.6 nM for norepinephrine, IC=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC=10.3 nM for norepinephrine, IC=22 nM for serotonin). In contrast, (−)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC=88.5 nM for norepinephrine, IC=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.