JP2019525900A - ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 - Google Patents
ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 Download PDFInfo
- Publication number
- JP2019525900A JP2019525900A JP2018565312A JP2018565312A JP2019525900A JP 2019525900 A JP2019525900 A JP 2019525900A JP 2018565312 A JP2018565312 A JP 2018565312A JP 2018565312 A JP2018565312 A JP 2018565312A JP 2019525900 A JP2019525900 A JP 2019525900A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- heteroaryl
- heterocyclyl
- independently
- Prior art date
- 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.)
- Pending
Links
- YQNWZWMKLDQSAC-UHFFFAOYSA-N Cc(cc1)cc(C)c1Sc(cccc1)c1N1CCNCC1 Chemical compound Cc(cc1)cc(C)c1Sc(cccc1)c1N1CCNCC1 YQNWZWMKLDQSAC-UHFFFAOYSA-N 0.000 description 3
- JCESALWPDRHVCW-UHFFFAOYSA-N CCCCCCCCCCCCCCCCCC(OCOC(N(CC1)CCN1c(cccc1)c1Sc1ccc(C)cc1C)=O)=O Chemical compound CCCCCCCCCCCCCCCCCC(OCOC(N(CC1)CCN1c(cccc1)c1Sc1ccc(C)cc1C)=O)=O JCESALWPDRHVCW-UHFFFAOYSA-N 0.000 description 1
- AVFXLZAAFMSLPX-UHFFFAOYSA-N Cc(cc1C)ccc1Sc(cccc1)c1N(CC1)CCN1C(OCCl)=O Chemical compound Cc(cc1C)ccc1Sc(cccc1)c1N(CC1)CCN1C(OCCl)=O AVFXLZAAFMSLPX-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
- C07D295/16—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 acylated on ring nitrogen atoms
- C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- 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
-
- 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
- C07D295/16—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 acylated on ring nitrogen atoms
- C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021069689A JP7123211B2 (ja) | 2016-06-16 | 2021-04-16 | ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610446737.5 | 2016-06-16 | ||
| CN201610446737 | 2016-06-16 | ||
| PCT/CN2017/088493 WO2017215636A1 (zh) | 2016-06-16 | 2017-06-15 | 二芳基硫醚哌嗪类化合物及其制备方法和用途 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021069689A Division JP7123211B2 (ja) | 2016-06-16 | 2021-04-16 | ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019525900A true JP2019525900A (ja) | 2019-09-12 |
| JP2019525900A5 JP2019525900A5 (https=) | 2020-05-28 |
Family
ID=60662997
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018565312A Pending JP2019525900A (ja) | 2016-06-16 | 2017-06-15 | ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 |
| JP2021069689A Active JP7123211B2 (ja) | 2016-06-16 | 2021-04-16 | ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021069689A Active JP7123211B2 (ja) | 2016-06-16 | 2021-04-16 | ジアリールチオエーテルピペラジン化合物、その調製方法及び使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10927089B2 (https=) |
| JP (2) | JP2019525900A (https=) |
| CN (1) | CN109311833B (https=) |
| WO (1) | WO2017215636A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021527705A (ja) * | 2018-06-20 | 2021-10-14 | バイオ アーゲー ファーマシューティカルズ エス.エー. | ボルチオキセチンおよびボルチオキセチン中間体を調製するためのワンポット有機擬触媒c−h活性化手法 |
| JP2024528732A (ja) * | 2021-08-05 | 2024-07-30 | 浙江華海薬業股▲フン▼有限公司 | ボルチオキセチンパモ酸塩の凍結乾燥粉末注射剤およびその調製方法 |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2021115372A1 (zh) * | 2019-12-10 | 2021-06-17 | 江苏恩华药业股份有限公司 | 一种沃替西汀前药及其应用 |
| CN115448895B (zh) * | 2021-06-09 | 2025-07-11 | 苏州恩华生物医药科技有限公司 | 一种沃替西汀前药的晶型、其制备方法和应用 |
| CN120424027B (zh) * | 2024-02-05 | 2026-03-24 | 石药集团中奇制药技术(石家庄)有限公司 | 一种伏硫西汀半帕莫酸盐晶型 |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009541216A (ja) * | 2006-06-16 | 2009-11-26 | ハー・ルンドベック・アクチエゼルスカベット | 認識機能障害(cognitiveimpairment)を治療するための、組み合わされたセロトニン再取り込み、5−HT3および5−HT1A活性を有する化合物としての1−[2−(2,4−ジメチルフェニルスルファニル)−フェニル]ピペラジン |
| CN104829558A (zh) * | 2014-02-10 | 2015-08-12 | 江苏豪森药业股份有限公司 | 二芳基硫醚胺类化合物的制备方法 |
| WO2016004908A1 (en) * | 2014-07-08 | 2016-01-14 | Zentiva, K.S. | Method of preparing vortioxetine |
| CN105461656A (zh) * | 2015-11-11 | 2016-04-06 | 北京万全德众医药生物技术有限公司 | 一种制备沃替西汀的新工艺 |
| EP3023417A1 (en) * | 2014-11-21 | 2016-05-25 | Dipharma Francis S.r.l. | Process for the preparation of an antidepressant and the intermediates thereof |
| WO2016079751A2 (en) * | 2014-11-17 | 2016-05-26 | Megafine Pharma (P) Ltd. | A process for preparation of vortioxetine and polymorphs thereof |
| JP2019515024A (ja) * | 2016-03-29 | 2019-06-06 | シャンハイ・シナジー・ファーマシューティカル・サイエンシーズ・カンパニー・リミテッド | ボルチオキセチンのパモ酸塩及びその結晶形 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB507565A (en) * | 1937-12-10 | 1939-06-12 | May & Baker Ltd | Process for the preparation of amidine derivatives |
| WO2003053942A1 (en) | 2001-12-20 | 2003-07-03 | H. Lundbeck A/S | Aryloxyphenyl and arylsulfanylphenyl derivatives |
| TW200848411A (en) | 2007-03-20 | 2008-12-16 | Lundbeck & Co As H | Novel therapeutic uses of 1-[2-(2, 4-dimethylphenylsulfanyl)phenyl]-piperazine |
| CN103087060B (zh) * | 2011-10-28 | 2016-08-03 | 华东理工大学 | 高活性哌虫啶异构体及其制备方法 |
| NZ722096A (en) | 2011-12-15 | 2016-11-25 | Alkermes Pharma Ireland Ltd | Prodrugs of secondary amine compounds |
| WO2014191548A1 (en) | 2013-05-31 | 2014-12-04 | Lek Pharmaceuticals D.D. | New process for the synthesis of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine |
| CN106170480B (zh) | 2014-05-09 | 2019-09-20 | 上海科胜药物研发有限公司 | 新的沃替西汀中间体及其合成方法 |
| WO2017125504A1 (en) * | 2016-01-20 | 2017-07-27 | Amneal Pharmaceuticals Company Gmbh | Polymorphic forms of vortioxetine hydrobromide tert-butanolate |
| WO2017162536A1 (en) | 2016-03-21 | 2017-09-28 | H. Lundbeck A/S | Vortioxetine prodrugs |
-
2017
- 2017-06-15 WO PCT/CN2017/088493 patent/WO2017215636A1/zh not_active Ceased
- 2017-06-15 CN CN201780032963.1A patent/CN109311833B/zh active Active
- 2017-06-15 US US16/308,462 patent/US10927089B2/en active Active
- 2017-06-15 JP JP2018565312A patent/JP2019525900A/ja active Pending
-
2021
- 2021-04-16 JP JP2021069689A patent/JP7123211B2/ja active Active
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009541216A (ja) * | 2006-06-16 | 2009-11-26 | ハー・ルンドベック・アクチエゼルスカベット | 認識機能障害(cognitiveimpairment)を治療するための、組み合わされたセロトニン再取り込み、5−HT3および5−HT1A活性を有する化合物としての1−[2−(2,4−ジメチルフェニルスルファニル)−フェニル]ピペラジン |
| CN104829558A (zh) * | 2014-02-10 | 2015-08-12 | 江苏豪森药业股份有限公司 | 二芳基硫醚胺类化合物的制备方法 |
| WO2016004908A1 (en) * | 2014-07-08 | 2016-01-14 | Zentiva, K.S. | Method of preparing vortioxetine |
| WO2016079751A2 (en) * | 2014-11-17 | 2016-05-26 | Megafine Pharma (P) Ltd. | A process for preparation of vortioxetine and polymorphs thereof |
| EP3023417A1 (en) * | 2014-11-21 | 2016-05-25 | Dipharma Francis S.r.l. | Process for the preparation of an antidepressant and the intermediates thereof |
| CN105461656A (zh) * | 2015-11-11 | 2016-04-06 | 北京万全德众医药生物技术有限公司 | 一种制备沃替西汀的新工艺 |
| JP2019515024A (ja) * | 2016-03-29 | 2019-06-06 | シャンハイ・シナジー・ファーマシューティカル・サイエンシーズ・カンパニー・リミテッド | ボルチオキセチンのパモ酸塩及びその結晶形 |
Non-Patent Citations (2)
| Title |
|---|
| BASTIN,R.J. ET AL: ""Salt selection and optimization procedures for pharmaceutical new chemical entities"", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 4, no. 5, JPN6009059058, 2000, pages 427 - 435, ISSN: 0004581327 * |
| C.G.WERMUTH編, 「最新 創薬化学 下巻」, vol. pp.347-365, JPN6014029314, 1999, ISSN: 0004581326 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021527705A (ja) * | 2018-06-20 | 2021-10-14 | バイオ アーゲー ファーマシューティカルズ エス.エー. | ボルチオキセチンおよびボルチオキセチン中間体を調製するためのワンポット有機擬触媒c−h活性化手法 |
| JP7389761B2 (ja) | 2018-06-20 | 2023-11-30 | バイオ アーゲー ファーマシューティカルズ エス.エー. | ボルチオキセチンおよびボルチオキセチン中間体を調製するためのワンポット有機擬触媒c-h活性化手法 |
| JP2024528732A (ja) * | 2021-08-05 | 2024-07-30 | 浙江華海薬業股▲フン▼有限公司 | ボルチオキセチンパモ酸塩の凍結乾燥粉末注射剤およびその調製方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20190256482A1 (en) | 2019-08-22 |
| US10927089B2 (en) | 2021-02-23 |
| CN109311833B (zh) | 2022-11-04 |
| WO2017215636A1 (zh) | 2017-12-21 |
| CN109311833A (zh) | 2019-02-05 |
| JP2021107432A (ja) | 2021-07-29 |
| JP7123211B2 (ja) | 2022-08-22 |
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