CN113677671A - 美利曲辛与氟哌噻吨共晶及其制备方法 - Google Patents

美利曲辛与氟哌噻吨共晶及其制备方法 Download PDF

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CN113677671A
CN113677671A CN202080024653.7A CN202080024653A CN113677671A CN 113677671 A CN113677671 A CN 113677671A CN 202080024653 A CN202080024653 A CN 202080024653A CN 113677671 A CN113677671 A CN 113677671A
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flupentixol
melitracen
hydrochloride
crystal
crystal form
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CN113677671B (zh
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罗欢
路苹
蒋钰
许向阳
张长青
周珺
钱桦江
赵振坤
刘志强
侯媛媛
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Suzhou Enhua Biomedical Technology 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/82—Purification; Separation; Stabilisation; Use of additives
    • C07C209/84—Purification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/31—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by at least three rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D335/10—Dibenzothiopyrans; Hydrogenated dibenzothiopyrans
    • C07D335/12—Thioxanthenes
    • C07D335/20—Thioxanthenes with hydrocarbon radicals, substituted by amino radicals, directly attached in position 9
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/22—Ortho- or ortho- and peri-condensed systems containing three rings containing only six-membered rings
    • C07C2603/24—Anthracenes; Hydrogenated anthracenes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明提供了盐酸氟哌噻吨和盐酸美利曲辛形成的共晶，所述共晶中盐酸氟哌噻吨和盐酸美利曲辛的摩尔比为1:1，该共晶稳定性好，溶解度高，药效优于市售黛力新片剂，副反应更少。

Description

PCT国内申请，说明书已公开。

Claims (11)

  1. PCT国内申请，权利要求书已公开。
CN202080024653.7A 2019-08-02 2020-07-31 美利曲辛与氟哌噻吨共晶及其制备方法 Active CN113677671B (zh)

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CN2019107199235 2019-08-02
CN201910719923.5A CN112300119B (zh) 2019-08-02 2019-08-02 美利曲辛与氟哌噻吨共晶及其制备方法
PCT/CN2020/106328 WO2021023119A1 (zh) 2019-08-02 2020-07-31 美利曲辛与氟哌噻吨共晶及其制备方法

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2374450A1 (en) * 2010-04-06 2011-10-12 H. Lundbeck A/S Flupentixol compositions
CN104177330A (zh) * 2014-09-10 2014-12-03 宁辉 盐酸氟哌噻吨结晶化合物及其药物组合物
CN104288153A (zh) * 2014-09-19 2015-01-21 四川海思科制药有限公司 一种氟哌噻吨美利曲辛药物组合物及其制备方法
CN105663062A (zh) * 2016-02-17 2016-06-15 南京卓泰医药科技有限公司 一种氟哌噻吨美利曲辛药物组合物及其制备方法
CN108498470A (zh) * 2017-02-24 2018-09-07 重庆圣华曦药业股份有限公司 一种氟哌噻吨美利曲辛药物组合物及其制备方法
CN109674754A (zh) * 2019-01-10 2019-04-26 广东赛烽医药科技有限公司 一种氟哌噻吨美利曲辛药物组合物及其制剂

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109771386B (zh) * 2019-01-10 2021-10-08 广东赛烽医药科技有限公司 一种氟哌噻吨美利曲辛片剂及其制备方法

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2374450A1 (en) * 2010-04-06 2011-10-12 H. Lundbeck A/S Flupentixol compositions
CN104177330A (zh) * 2014-09-10 2014-12-03 宁辉 盐酸氟哌噻吨结晶化合物及其药物组合物
CN104288153A (zh) * 2014-09-19 2015-01-21 四川海思科制药有限公司 一种氟哌噻吨美利曲辛药物组合物及其制备方法
CN105663062A (zh) * 2016-02-17 2016-06-15 南京卓泰医药科技有限公司 一种氟哌噻吨美利曲辛药物组合物及其制备方法
CN108498470A (zh) * 2017-02-24 2018-09-07 重庆圣华曦药业股份有限公司 一种氟哌噻吨美利曲辛药物组合物及其制备方法
CN109674754A (zh) * 2019-01-10 2019-04-26 广东赛烽医药科技有限公司 一种氟哌噻吨美利曲辛药物组合物及其制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SANDEEP KUMAR和ARUN NANDA: "Approaches to Design of Pharmaceutical Cocrystals:A Review", 《MOLECULAR CRYSTALS AND LIQUID CRYSTALS》 *

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WO2021023119A1 (zh) 2021-02-11
CN112300119B (zh) 2024-04-16
CN113677671B (zh) 2023-01-17
CN112300119A (zh) 2021-02-02

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