CN101081816A - 新的o－去甲基－文拉法辛的酒石酸盐 - Google Patents
新的o－去甲基－文拉法辛的酒石酸盐 Download PDFInfo
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- CN101081816A CN101081816A CN 200610081566 CN200610081566A CN101081816A CN 101081816 A CN101081816 A CN 101081816A CN 200610081566 CN200610081566 CN 200610081566 CN 200610081566 A CN200610081566 A CN 200610081566A CN 101081816 A CN101081816 A CN 101081816A
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- venlafaxine
- tartrate
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
本发明提供了新的O－去甲基－文拉法辛的盐，O－去甲基－文拉法辛的酒石酸盐及其药物组合物。
Description
技术领域：
本发明提供了O-去甲基-文拉法辛新的盐，O-去甲基-文拉法辛酒石酸盐及其药物组合物。O-去甲基-文拉法辛酒石酸盐是用于治疗各种抑郁症的O-去甲基-文拉法辛的可药用的盐。
背景技术：
O-去甲基-文拉法辛是文拉法辛的主要代谢物，为5-羟色胺和去甲肾上腺素再摄取抑制剂，用于治疗各种抑郁症，其化学名称为4-[2-(二甲基氨基)-1-(1-羟基环己基)乙基]苯酚，美国专利No.4535186列举了其富马酸盐；美国专利No.2004044241公开了其琥珀酸盐；美国专利No.2003236309公开了其甲酸盐。
发明内容：
本发明涉及O-去甲基-文拉法辛的新的盐，即O-去甲基-文拉法辛酒石酸盐。其结构式如下：
其中X代表0.5～2，优选X＝1
O-去甲基-文拉法辛包括外消旋混合物以及其立体异构纯的形式。
酒石酸包括酒石酸及其异构体重酒石酸
O-去甲基-文拉法辛酒石酸盐具有良好的溶解性、渗透性和生物利用度。本发明的新的盐具有特别适于作为药物的适宜性质。O-去甲基-文拉法辛的酒石酸盐或其混合盐与药物上可接受的载体或稀释剂混合，药物组合物中含有可有效治疗动物诸如人类目标适应症的量的O-去甲基-文拉法辛的酒石酸盐。
O-去甲基-文拉法辛酒石酸盐可以通过使计量量的酒石酸或重酒石酸与O一去甲文拉法辛游离碱相接触而生成，酒石酸和游离碱都在溶剂中。
具体实施方式：
本发明中制备O-去甲基-文拉法辛酒石酸盐的方法用下列非限定性实施例来说明。
实施例1
将O-去甲基-文拉法辛游离碱溶于丙酮-水溶液中，加入化学计量量的酒石酸，搅拌约15分钟，将所得反应液冷却，即获得O-去甲基-文拉法辛酒石酸盐。
实施例2
将O-去甲基-文拉法辛游离碱溶于乙醇-水溶液中，加入化学计量量的酒石酸，搅拌约15分钟，将所得反应液冷却，即获得O-去甲基-文拉法辛酒石酸盐。
Claims (7)
1、O-去甲基-文拉法辛的酒石酸盐化合物或其混合物
2、权利要求1所述的化合物，其O-去甲基-文拉法辛与酒石酸的比例为1∶1
3、权利要求1所述的化合物，其O-去甲基-文拉法辛与酒石酸的比例为1∶2
4、权利要求1所述的化合物，其O-去甲基-文拉法辛与酒石酸的比例为2∶1
5、权利要求1至4任一项所述化合物，其是O-去甲基-文拉法辛的酒石酸盐的无水物
6、权利要求1至4任一项所述化合物，其是O-去甲基-文拉法辛的酒石酸盐的水合物
7、药物组合物，其中含有权利要求1至6任一项所述的O-去甲基-文拉法辛的酒石酸盐或其混合盐与药物上可接受的载体或稀释剂混合。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610081566 CN101081816A (zh) | 2006-05-29 | 2006-05-29 | 新的o－去甲基－文拉法辛的酒石酸盐 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN 200610081566 CN101081816A (zh) | 2006-05-29 | 2006-05-29 | 新的o－去甲基－文拉法辛的酒石酸盐 |
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| Publication Number | Publication Date |
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| CN101081816A true CN101081816A (zh) | 2007-12-05 |
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| CN 200610081566 Pending CN101081816A (zh) | 2006-05-29 | 2006-05-29 | 新的o－去甲基－文拉法辛的酒石酸盐 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2085377A1 (en) * | 2008-01-29 | 2009-08-05 | LEK Pharmaceuticals D.D. | Novel salts of O-desmethyl-venlafaxine |
| WO2010008735A3 (en) * | 2008-06-16 | 2010-07-15 | Teva Pharmaceutical Industries Ltd. | Solid states of o-desmethylvenlaf axine salts |
-
2006
- 2006-05-29 CN CN 200610081566 patent/CN101081816A/zh active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2085377A1 (en) * | 2008-01-29 | 2009-08-05 | LEK Pharmaceuticals D.D. | Novel salts of O-desmethyl-venlafaxine |
| WO2009095431A1 (en) * | 2008-01-29 | 2009-08-06 | Lek Pharmaceuticals D.D. | Novel salts of o-desmethyl-venlafaxine |
| US20110082213A1 (en) * | 2008-01-29 | 2011-04-07 | Furlan Borut | Novel salts of o-desmethyl-venlafaxine |
| AU2009209666B2 (en) * | 2008-01-29 | 2013-05-02 | Lek Pharmaceuticals D.D. | Novel salts of O-desmethyl-venlafaxine |
| US8604194B2 (en) | 2008-01-29 | 2013-12-10 | Lek Pharmaceuticals D.D. | Salts of O-desmethyl-venlafaxine |
| WO2010008735A3 (en) * | 2008-06-16 | 2010-07-15 | Teva Pharmaceutical Industries Ltd. | Solid states of o-desmethylvenlaf axine salts |
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Open date: 20071205 |