CN109311832A - 沃替西汀的帕莫酸盐及其晶型 - Google Patents

沃替西汀的帕莫酸盐及其晶型 Download PDF

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CN109311832A
CN109311832A CN201780016707.3A CN201780016707A CN109311832A CN 109311832 A CN109311832 A CN 109311832A CN 201780016707 A CN201780016707 A CN 201780016707A CN 109311832 A CN109311832 A CN 109311832A
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crystal form
vortioxetine
powder diffraction
ray powder
hydrochlorate
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CN109311832B (zh
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李云飞
夏小二
许昕
张瑱
刘磊
张小娟
张立明
李东升
王艺瑾
葛建
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Shanghai Synergy Pharmaceutical Sciences Co Ltd
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Shanghai Synergy Pharmaceutical Sciences Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/08Heterocyclic 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
    • C07D295/096Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds 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
    • C07C65/01Compounds 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
    • C07C65/105Compounds 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 polycyclic
    • C07C65/11Compounds 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 polycyclic with carboxyl groups on a condensed ring system containing two rings
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    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

本发明提供了一种沃替西汀的帕莫酸盐,其包括沃替西汀帕莫酸盐的晶型物、溶剂化物或无定形物。本发明提供了所述沃替西汀的帕莫酸盐及其晶型的制备方法和应用。本发明所制备的沃替西汀帕莫酸盐延长了沃替西汀在体内的滞留时间,实现了沃替西汀在体内的缓慢释放,适用于长效药物剂型的制备。

Description

PCT国内申请,说明书已公开。

Claims (25)

  1. PCT国内申请,权利要求书已公开。
CN201780016707.3A 2016-03-29 2017-03-28 沃替西汀的帕莫酸盐及其晶型 Active CN109311832B (zh)

Applications Claiming Priority (3)

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CN2016101876394 2016-03-29
CN201610187639 2016-03-29
PCT/CN2017/078427 WO2017167180A1 (zh) 2016-03-29 2017-03-28 沃替西汀的帕莫酸盐及其晶型

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US (1) US10793536B2 (zh)
EP (1) EP3438099A1 (zh)
JP (1) JP6669932B2 (zh)
CN (1) CN109311832B (zh)
AU (1) AU2017242867B9 (zh)
CA (1) CA3018402C (zh)
WO (1) WO2017167180A1 (zh)

Cited By (1)

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CN111925294A (zh) * 2020-07-06 2020-11-13 济南大学 一种托特罗定帕莫酸盐及其制备方法

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WO2017215636A1 (zh) * 2016-06-16 2017-12-21 广东东阳光药业有限公司 二芳基硫醚哌嗪类化合物及其制备方法和用途
WO2018086534A1 (zh) * 2016-11-09 2018-05-17 广东东阳光药业有限公司 氢溴酸沃替西汀长效注射制剂
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
CN110934868A (zh) * 2018-09-21 2020-03-31 合肥合源药业有限公司 难溶性复合物、药物组合物及其应用
CN109134352A (zh) * 2018-09-21 2019-01-04 合肥锐思生物医药有限公司 一种制备难溶性复合物或其溶剂合物的方法
US20220119338A1 (en) * 2019-01-11 2022-04-21 Alar Pharmaceuticals Inc. Ketamine pamoate and use thereof
CN114965720B (zh) * 2021-02-20 2024-02-23 成都康弘药业集团股份有限公司 一种测定氢溴酸伏硫西汀有关物质的方法
WO2022199707A1 (zh) * 2021-03-26 2022-09-29 上海博志研新药物技术有限公司 哌马色林药用盐、制备方法、含其的药物组合物及应用
CN117597111A (zh) 2021-08-05 2024-02-23 浙江华海药业股份有限公司 一种沃替西汀帕莫酸盐冻干粉针剂及其制备方法
CN115702894A (zh) * 2021-08-11 2023-02-17 朱信红 一种用于止吐的缓释组合物及其制备方法

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US20140243278A1 (en) * 2011-07-05 2014-08-28 Sunil Sadanand Nadkarni Acid Addition Salt of Donepezil and Pharmaceutical Composition Thereof
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CN109311833A (zh) * 2016-06-16 2019-02-05 广东东阳光药业有限公司 二芳基硫醚哌嗪类化合物及其制备方法和用途

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US20140243278A1 (en) * 2011-07-05 2014-08-28 Sunil Sadanand Nadkarni Acid Addition Salt of Donepezil and Pharmaceutical Composition Thereof
CN104039765A (zh) * 2011-11-29 2014-09-10 顾自强 多奈哌齐双羟萘酸盐、制备方法及其应用
CN109311833A (zh) * 2016-06-16 2019-02-05 广东东阳光药业有限公司 二芳基硫醚哌嗪类化合物及其制备方法和用途

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CN111925294A (zh) * 2020-07-06 2020-11-13 济南大学 一种托特罗定帕莫酸盐及其制备方法

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CN109311832B (zh) 2023-01-06
AU2017242867A1 (en) 2018-10-11
CA3018402C (en) 2021-05-11
AU2017242867A8 (en) 2018-10-25
WO2017167180A1 (zh) 2017-10-05
US10793536B2 (en) 2020-10-06
EP3438099A4 (en) 2019-02-06
JP2019515024A (ja) 2019-06-06
AU2017242867B9 (en) 2019-07-04
EP3438099A1 (en) 2019-02-06
JP6669932B2 (ja) 2020-03-18
US20190169147A1 (en) 2019-06-06
CA3018402A1 (en) 2017-10-05
AU2017242867B2 (en) 2019-06-06

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