CN109311833A - 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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CN109311833A
CN109311833A CN201780032963.1A CN201780032963A CN109311833A CN 109311833 A CN109311833 A CN 109311833A CN 201780032963 A CN201780032963 A CN 201780032963A CN 109311833 A CN109311833 A CN 109311833A
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compound
alkyl
heterocycle
heteroaryl
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CN109311833B (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
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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
    • 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
    • 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

Abstract

本发明涉及二芳基硫醚哌嗪类化合物及其制备方法和用途，具体地，所述化合物为式(I)所示化合物，其中，HX为C10‑20脂肪酸或双羟萘酸。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
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)

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CN2016104467375 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

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JP (2) JP2019525900A (zh)
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WO (1) WO2017215636A1 (zh)

Cited By (1)

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CN109311832A (zh) * 2016-03-29 2019-02-05 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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WO2019242889A1 (en) * 2018-06-20 2019-12-26 Vio Ag Pharmaceuticals S.A. A one-pot organo-pseudocatalytic c-h activation approach for the preparation of vortioxetine and vortioxetine intermediate
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

Citations (6)

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GB507565A (en) * 1937-12-10 1939-06-12 May & Baker Ltd Process for the preparation of amidine derivatives
CN101472906A (zh) * 2006-06-16 2009-07-01 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
CN103087060A (zh) * 2011-10-28 2013-05-08 华东理工大学 高活性哌虫啶异构体及其制备方法
WO2016004908A1 (en) * 2014-07-08 2016-01-14 Zentiva, K.S. Method of preparing vortioxetine
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

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ES2280595T3 (es) 2001-12-20 2007-09-16 H. Lundbeck A/S 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
NZ722096A (en) 2011-12-15 2016-11-25 Alkermes Pharma Ireland Ltd Prodrugs of secondary amine compounds
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
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
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WO2017125504A1 (en) * 2016-01-20 2017-07-27 Amneal Pharmaceuticals Company Gmbh Polymorphic forms of vortioxetine hydrobromide tert-butanolate
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AU2017242867B9 (en) * 2016-03-29 2019-07-04 Shanghai Synergy Pharmaceutical Sciences Co., Ltd Vortioxetine pamoic acid salt and crystal form thereof

Patent Citations (6)

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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
CN101472906A (zh) * 2006-06-16 2009-07-01 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
CN103087060A (zh) * 2011-10-28 2013-05-08 华东理工大学 高活性哌虫啶异构体及其制备方法
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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109311832A (zh) * 2016-03-29 2019-02-05 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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JP2021107432A (ja) 2021-07-29
CN109311833B (zh) 2022-11-04
JP7123211B2 (ja) 2022-08-22
US10927089B2 (en) 2021-02-23
JP2019525900A (ja) 2019-09-12
US20190256482A1 (en) 2019-08-22
WO2017215636A1 (zh) 2017-12-21

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

Patentee after: Guangdong Dongyangguang Pharmaceutical Co.,Ltd.

Address before: 523808 No. 1 Industrial North Road, Songshan Industrial Park, Songshan, Guangdong, Dongguan, Hubei

Patentee before: SUNSHINE LAKE PHARMA Co.,Ltd.

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