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 PDF

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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
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compound
alkyl
heteroaryl
heterocyclyl
independently
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JP2018565312A
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English (en)
Japanese (ja)
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JP2019525900A5 (enExample
Inventor
レイ、シン
リ、ドンミン
ルオ、ゾンフア
ヘ、ビフェイ
ワン、キアン
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Sunshine Lake Pharma Co Ltd
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Sunshine Lake Pharma Co Ltd
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Publication of JP2019525900A5 publication Critical patent/JP2019525900A5/ja
Priority to JP2021069689A priority Critical patent/JP7123211B2/ja
Pending legal-status Critical Current

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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
JP2018565312A 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 Pending JP2019525900A (ja)

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 2016-06-16
CN201610446737.5 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

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JP2019525900A true JP2019525900A (ja) 2019-09-12
JP2019525900A5 JP2019525900A5 (enExample) 2020-05-28

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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

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Country Link
US (1) US10927089B2 (enExample)
JP (2) JP2019525900A (enExample)
CN (1) CN109311833B (enExample)
WO (1) WO2017215636A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
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 (3)

* Cited by examiner, † Cited by third party
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CA3018402C (en) * 2016-03-29 2021-05-11 Shanghai Synergy Pharmaceutical Sciences Co., Ltd Vortioxetine pamoic acid salt and crystal form thereof
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

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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

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GB507565A (en) * 1937-12-10 1939-06-12 May & Baker Ltd Process for the preparation of amidine derivatives
MXPA04005989A (es) 2001-12-20 2004-09-27 Lundbeck & Co As H Derivados de ariloxifenilo y arilsulfanilfenilo.
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
JP5952912B2 (ja) 2011-12-15 2016-07-13 アルカーメス ファーマ アイルランド リミテッド 二級アミン化合物のプロドラッグ
CN105339361A (zh) 2013-05-31 2016-02-17 斯洛文尼亚莱柯制药股份有限公司 用于合成1-(2-((2，4-二甲基苯基)硫代)苯基)哌嗪的新方法
WO2015169130A1 (zh) 2014-05-09 2015-11-12 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
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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

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Cited By (3)

* Cited by examiner, † Cited by third party
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
WO2017215636A1 (zh) 2017-12-21
US20190256482A1 (en) 2019-08-22
CN109311833A (zh) 2019-02-05
CN109311833B (zh) 2022-11-04
JP7123211B2 (ja) 2022-08-22
JP2021107432A (ja) 2021-07-29
US10927089B2 (en) 2021-02-23

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