EA201691538A1 - Способ получения солей вортиоксетина - Google Patents
Способ получения солей вортиоксетинаInfo
- Publication number
- EA201691538A1 EA201691538A1 EA201691538A EA201691538A EA201691538A1 EA 201691538 A1 EA201691538 A1 EA 201691538A1 EA 201691538 A EA201691538 A EA 201691538A EA 201691538 A EA201691538 A EA 201691538A EA 201691538 A1 EA201691538 A1 EA 201691538A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- salts
- vortioxetine
- preparation
- relates
- purity
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 4
- YQNWZWMKLDQSAC-UHFFFAOYSA-N vortioxetine Chemical compound CC1=CC(C)=CC=C1SC1=CC=CC=C1N1CCNCC1 YQNWZWMKLDQSAC-UHFFFAOYSA-N 0.000 abstract 3
- 229960002263 vortioxetine Drugs 0.000 abstract 3
- 239000002050 international nonproprietary name Substances 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- -1 vortioxetine L - (+) - mandelate salt Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/08—Acetic acid
- C07C53/10—Salts thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/06—Oxalic acid
- C07C55/07—Salts thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/08—Malonic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/10—Succinic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/265—Citric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
- C07C65/03—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
- C07C65/05—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
- C07C65/10—Salicylic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Изобретение относится к улучшенному способу получения фармацевтически активных ингредиентов и также к солям высокой чистоты и фармацевтическим композициям, полученным с помощью указанного способа. В частности, изобретение относится к экономически выгодному способу получения соединения, имеющего международное непатентованное наименование (МНН) вортиоксетин и название по химической номенклатуре 1-[2-(2,4-диметилфенилсульфанил)фенил]пиперазин. Вортиоксетин соответствует следующей формуле I. В частности, изобретение относится к получению L-(+)-манделатной соли вортиоксетина высокой чистоты формулы IX, превращению этой соли в другие соли высокой чистоты и также к формулированию указанных солей.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
HUP1400044 | 2014-01-31 | ||
HUP1400430 | 2014-09-17 | ||
PCT/HU2015/000007 WO2015114395A1 (en) | 2014-01-31 | 2015-01-30 | Process for the preparation of vortioxetine salts |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201691538A1 true EA201691538A1 (ru) | 2017-01-30 |
EA029060B1 EA029060B1 (ru) | 2018-02-28 |
Family
ID=89708196
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201691538A EA029060B1 (ru) | 2014-01-31 | 2015-01-30 | Способ получения солей вортиоксетина |
Country Status (5)
Country | Link |
---|---|
US (1) | US9822086B2 (ru) |
EP (1) | EP3099669A1 (ru) |
CN (1) | CN106103418A (ru) |
EA (1) | EA029060B1 (ru) |
WO (1) | WO2015114395A1 (ru) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016079751A2 (en) * | 2014-11-17 | 2016-05-26 | Megafine Pharma (P) Ltd. | A process for preparation of vortioxetine and polymorphs thereof |
WO2016125190A2 (en) | 2015-02-04 | 2016-08-11 | Mylan Laboratories Limited | Novel crystalline forms of vortioxetine, premixes, and processes for the preparation thereof |
WO2017167180A1 (zh) | 2016-03-29 | 2017-10-05 | 上海华汇拓医药科技有限公司 | 沃替西汀的帕莫酸盐及其晶型 |
US10519121B2 (en) | 2016-12-30 | 2019-12-31 | Apicore Us Llc | Process and novel polymorphic form of vortioxetine and its pharmaceutically acceptable salts |
US10428033B2 (en) | 2017-02-15 | 2019-10-01 | Piramal Enterprises Limited | Process for the preparation of vortioxetine and salts thereof |
LT3615518T (lt) * | 2017-04-25 | 2022-03-10 | H. Lundbeck A/S | Vortioksetino hbr alfa formos gamybos būdas |
KR102026337B1 (ko) | 2017-07-07 | 2019-09-27 | 영진약품 주식회사 | 1-[2-(2,4-디메틸페닐설파닐)페닐]피페라진의 신규염 및 이의 제조방법 |
CN109521102A (zh) * | 2017-09-18 | 2019-03-26 | 万全万特制药(厦门)有限公司 | 氢溴酸沃替西汀终产品有关物质的分离测定方法 |
CN108250064A (zh) * | 2018-04-20 | 2018-07-06 | 梧州学院 | 沃替西汀-二羟基苯甲酸新盐型及其制备方法 |
CN108912069A (zh) * | 2018-08-22 | 2018-11-30 | 梧州学院 | 一种沃替西汀与c2-c4二羧酸新盐型及其制备方法与应用 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA81749C2 (ru) | 2001-10-04 | 2008-02-11 | Х. Луннбек А/С | производные фенилпиперазина как ингибиторы обратного захвата серотонинА |
CN102617513B (zh) * | 2006-06-16 | 2015-09-23 | H.隆德贝克有限公司 | 作为用于治疗认知损伤的、具有结合的对血清素再吸收、5-ht3和5-ht1a活性的化合物的1-[2-(2,4-二甲基苯基硫烷基)-苯基]哌嗪 |
TW200848411A (en) | 2007-03-20 | 2008-12-16 | Lundbeck & Co As H | Novel therapeutic uses of 1-[2-(2, 4-dimethylphenylsulfanyl)phenyl]-piperazine |
TW200932233A (en) | 2007-11-13 | 2009-08-01 | Lundbeck & Co As H | Therapeutic uses of compounds having combined SERT, 5-HT3 and 5-HT1a activity |
TW201033181A (en) | 2009-02-17 | 2010-09-16 | Lundbeck & Co As H | Purification of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine |
CA2759456C (en) | 2009-04-24 | 2017-10-31 | H. Lundbeck A/S | Liquid formulations of salts of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine |
TW201212918A (en) | 2010-08-23 | 2012-04-01 | Lundbeck & Co As H | Therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]piperazine |
MX344144B (es) | 2012-01-03 | 2016-12-07 | H Lundbeck As | Proceso para la fabricacion de 1-[2-(2,4-dimetilfenilsulfanil)feni l] piperazina. |
US20160200698A1 (en) | 2013-09-12 | 2016-07-14 | Hangzhou Pushai Pharmaceutical Technology Co., Ltd | Vortioxetine salt and crystal thereof, their preparation method, pharmaceutical compositions and usage |
CN103788019B (zh) * | 2014-01-22 | 2015-10-07 | 苏州明锐医药科技有限公司 | 沃替西汀的制备方法 |
CN103788020B (zh) * | 2014-01-22 | 2015-11-04 | 苏州明锐医药科技有限公司 | 沃替西汀的制备方法 |
CN103936694A (zh) | 2014-04-23 | 2014-07-23 | 中国药科大学 | 一种抗抑郁药沃替西汀的制备方法 |
-
2015
- 2015-01-30 EP EP15709732.0A patent/EP3099669A1/en not_active Withdrawn
- 2015-01-30 WO PCT/HU2015/000007 patent/WO2015114395A1/en active Application Filing
- 2015-01-30 CN CN201580006423.7A patent/CN106103418A/zh active Pending
- 2015-01-30 EA EA201691538A patent/EA029060B1/ru not_active IP Right Cessation
- 2015-01-30 US US15/115,063 patent/US9822086B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
EP3099669A1 (en) | 2016-12-07 |
EA029060B1 (ru) | 2018-02-28 |
US9822086B2 (en) | 2017-11-21 |
US20170114034A1 (en) | 2017-04-27 |
WO2015114395A1 (en) | 2015-08-06 |
CN106103418A (zh) | 2016-11-09 |
WO2015114395A9 (en) | 2015-12-03 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM RU |