CN101081817A - Novel O-demethylated-venlafaxine maleate - Google Patents
Novel O-demethylated-venlafaxine maleate Download PDFInfo
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- CN101081817A CN101081817A CN 200610081567 CN200610081567A CN101081817A CN 101081817 A CN101081817 A CN 101081817A CN 200610081567 CN200610081567 CN 200610081567 CN 200610081567 A CN200610081567 A CN 200610081567A CN 101081817 A CN101081817 A CN 101081817A
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- Prior art keywords
- venlafaxine
- demethyl
- maleate
- demethylated
- novel
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
The present invention provides one new salt of O-demethyl-venlafaxine, O-demethyl-venlafaxine maleate, and its medicine composition.
Description
Technical field:
The invention provides the new salt of O-demethyl-Venlafaxine, O-demethyl-Venlafaxine maleate and pharmaceutical composition thereof.O-demethyl-Venlafaxine maleate is the pharmaceutically useful salt that is used for the treatment of the O-demethyl-Venlafaxine of various dysthymia disorders.
Background technology:
O-demethyl-Venlafaxine is the major metabolite of Venlafaxine, be serotonin and NRI, be used for the treatment of various dysthymia disorders, its chemical name is 4-[2-(dimethylamino)-1-(1-hydroxy-cyclohexyl) ethyl] phenol, U.S. Patent No. 4535186 has been enumerated its fumarate; U.S. Patent No. 2004044241 discloses its succinate; U.S. Patent No. 2003236309 discloses its formate.
Summary of the invention:
The present invention relates to the new salt of O-demethyl-Venlafaxine, i.e. O-demethyl-Venlafaxine maleate.Its structural formula is as follows:
Wherein X represents 0.5～2, and preferred X=1
O-demethyl-Venlafaxine comprise racemic mixture with and the pure form of stereoisomerism.
O-demethyl-Venlafaxine maleate has good solubility, perviousness and bioavailability.New salt of the present invention has the suitable character that is particularly suitable for as medicine.The maleate of O-demethyl-Venlafaxine or its mixing salt contain the maleate of the O-demethyl-Venlafaxine that can effectively treat animal such as the amount of human target indication with pharmaceutically acceptable carrier or mixing diluents in the pharmaceutical composition.
O-demethyl-Venlafaxine maleate can generate by toxilic acid and the reaction of O one desmethylvenlafaxine free alkali that makes metered amount, and toxilic acid and free alkali are all in solvent.
Embodiment:
The method for preparing O-demethyl-Venlafaxine maleate among the present invention illustrates with following indefiniteness embodiment.
Embodiment 1
O-demethyl-Venlafaxine free alkali is dissolved in the acetone-water solution, adds the toxilic acid of stoichiometry, stir about 15 minutes with the cooling of gained reaction solution, promptly obtains O-demethyl-Venlafaxine maleate.
Embodiment 2
O-demethyl-Venlafaxine free alkali is dissolved in the ethanol-water solution, adds the toxilic acid of stoichiometry, stir about 15 minutes with the cooling of gained reaction solution, promptly obtains O-demethyl-Venlafaxine maleate.
Claims (7)
1, the maleate compound of O-demethyl-Venlafaxine or its mixture
2, the described compound of claim 1, the ratio of its O-demethyl-Venlafaxine and toxilic acid is 1: 1
3, the described compound of claim 1, the ratio of its O-demethyl-Venlafaxine and toxilic acid is 1: 2
4, the described compound of claim 1, the ratio of its O-demethyl-Venlafaxine and toxilic acid is 2: 1
5, each described compound of claim 1 to 4, it is the anhydride of the maleate of O-demethyl-Venlafaxine
6, each described compound of claim 1 to 4, it is the hydrate of the maleate of O-demethyl-Venlafaxine
7, pharmaceutical composition wherein contains the maleate of each described O-demethyl-Venlafaxine of claim 1 to 6 or its mixing salt with pharmaceutically acceptable carrier or mixing diluents.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610081567 CN101081817A (en) | 2006-05-29 | 2006-05-29 | Novel O-demethylated-venlafaxine maleate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610081567 CN101081817A (en) | 2006-05-29 | 2006-05-29 | Novel O-demethylated-venlafaxine maleate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101081817A true CN101081817A (en) | 2007-12-05 |
Family
ID=38911640
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610081567 Pending CN101081817A (en) | 2006-05-29 | 2006-05-29 | Novel O-demethylated-venlafaxine maleate |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101081817A (en) |
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2006
- 2006-05-29 CN CN 200610081567 patent/CN101081817A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |