CN109311833B - 二芳基硫醚哌嗪类化合物及其制备方法和用途 - Google Patents

二芳基硫醚哌嗪类化合物及其制备方法和用途 Download PDF

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Publication number
CN109311833B
CN109311833B CN201780032963.1A CN201780032963A CN109311833B CN 109311833 B CN109311833 B CN 109311833B CN 201780032963 A CN201780032963 A CN 201780032963A CN 109311833 B CN109311833 B CN 109311833B
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CN109311833A (zh
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雷鑫
李东明
罗忠华
何必飞
王茜
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Guangdong HEC Pharmaceutical Co Ltd
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Sunshine Lake Pharma Co Ltd
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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)
  • 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)
CN201780032963.1A 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 Active CN109311833B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610446737 2016-06-16
CN2016104467375 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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CN109311833A CN109311833A (zh) 2019-02-05
CN109311833B true CN109311833B (zh) 2022-11-04

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US (1) US10927089B2 (https=)
JP (2) JP2019525900A (https=)
CN (1) CN109311833B (https=)
WO (1) WO2017215636A1 (https=)

Families Citing this family (6)

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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
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
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
EP4382096A4 (en) * 2021-08-05 2025-06-18 Zhejiang Huahai Pharmaceutical Co., Ltd. Lyophilized vortioxetine pamoate powder for injection and manufacturing process therefor
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

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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
EP2044043B2 (en) * 2006-06-16 2021-03-03 H. Lundbeck A/S 1- ý[- (2, 4-dimethylphenylsulfanyl) -phenyl]piperazine hydrobromide as a compound with combined serotonin reuptake, 5-ht3 and 5-ht1a activity for the treatment of cognitive impairment
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
CN104829558B (zh) * 2014-02-10 2020-03-03 江苏豪森药业集团有限公司 二芳基硫醚胺类化合物的制备方法
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
CZ2014471A3 (cs) * 2014-07-08 2016-01-20 Zentiva, K.S. Způsob přípravy vortioxetinu
WO2016079751A2 (en) * 2014-11-17 2016-05-26 Megafine Pharma (P) Ltd. A process for preparation of vortioxetine and polymorphs thereof
EP3023417B1 (en) 2014-11-21 2017-06-28 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
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
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

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US20190256482A1 (en) 2019-08-22
US10927089B2 (en) 2021-02-23
WO2017215636A1 (zh) 2017-12-21
CN109311833A (zh) 2019-02-05
JP2021107432A (ja) 2021-07-29
JP2019525900A (ja) 2019-09-12
JP7123211B2 (ja) 2022-08-22

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Address after: 523808 No.1, Gongye North Road, Songshanhu Park, Dongguan City, Guangdong Province

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