CN108112252B - 制备阿地溴铵的方法 - Google Patents

制备阿地溴铵的方法 Download PDF

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Publication number
CN108112252B
CN108112252B CN201680031574.2A CN201680031574A CN108112252B CN 108112252 B CN108112252 B CN 108112252B CN 201680031574 A CN201680031574 A CN 201680031574A CN 108112252 B CN108112252 B CN 108112252B
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CN
China
Prior art keywords
solvent
bromide
reaction
aclidinium bromide
aclidinium
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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CN201680031574.2A
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English (en)
Chinese (zh)
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CN108112252A (zh
Inventor
Z·门德斯
C·卡塞拉
A·C·康斯坦丁诺
B·桑托斯
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Hovione Scientia Ltd
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Hovione Scientia Ltd
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Publication of CN108112252A publication Critical patent/CN108112252A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/0018—Evaporation of components of the mixture to be separated
    • B01D9/0027—Evaporation of components of the mixture to be separated by means of conveying fluid, e.g. spray-crystallisation
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/005—Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Otolaryngology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Non-Silver Salt Photosensitive Materials And Non-Silver Salt Photography (AREA)
  • Catalysts (AREA)
CN201680031574.2A 2015-03-30 2016-03-30 制备阿地溴铵的方法 Expired - Fee Related CN108112252B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PT10837015A PT108370B (pt) 2015-03-30 2015-03-30 Processo de preparação de brometo de aclidínio
PT108370 2015-03-30
PCT/GB2016/050888 WO2016156836A1 (en) 2015-03-30 2016-03-30 Process for the preparation of aclidinium bromide

Publications (2)

Publication Number Publication Date
CN108112252A CN108112252A (zh) 2018-06-01
CN108112252B true CN108112252B (zh) 2020-11-24

Family

ID=55806548

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CN201680031574.2A Expired - Fee Related CN108112252B (zh) 2015-03-30 2016-03-30 制备阿地溴铵的方法

Country Status (9)

Country Link
US (2) US10087177B2 (enExample)
EP (1) EP3277679A1 (enExample)
JP (4) JP2018510189A (enExample)
CN (1) CN108112252B (enExample)
AU (1) AU2016240289B2 (enExample)
CA (2) CA3165243A1 (enExample)
IL (1) IL254712A0 (enExample)
PT (1) PT108370B (enExample)
WO (1) WO2016156836A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT108370B (pt) 2015-03-30 2018-10-25 Hovione Farm S A Processo de preparação de brometo de aclidínio
CN108586450B (zh) * 2017-12-15 2021-02-19 上海方予健康医药科技有限公司 一种胆碱m受体抗结剂的重结晶纯化方法
PT115583B (pt) * 2019-06-17 2022-05-02 Hovione Farm S A Processo contínuo para a preparação de medicamentos anticolinérgicos
CN114890997A (zh) * 2022-04-20 2022-08-12 江苏联环药业股份有限公司 一种抗胆碱能药物噻格溴铵的制备工艺

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1829534A (zh) * 2003-07-29 2006-09-06 贝林格尔.英格海姆国际有限公司 包括β模拟物和抗胆碱能药的吸入药剂
CN101490048A (zh) * 2006-07-21 2009-07-22 奥米罗实验室有限公司 制备3(r)-(2-羟基-2,2-二噻吩-2-基乙酰氧基)-1-(3-苯氧基丙基)-1-氮鎓二环[2.2.2]辛烷溴化物的方法
CN104619706A (zh) * 2012-08-15 2015-05-13 葛兰素集团有限公司 化学方法
CN105683186A (zh) * 2013-10-29 2016-06-15 赞蒂瓦有限合伙公司 工业上适用的用于制备高纯度阿地溴铵的方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
AU2930501A (en) * 2000-01-07 2001-07-24 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
US6482847B2 (en) * 2000-10-03 2002-11-19 Hoffmann-La Roche Inc. Amorphous form of cell cycle inhibitor having improved solubility and bioavailability
AR044134A1 (es) * 2003-05-02 2005-08-24 Novartis Ag Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas.
CA2635581C (en) * 2005-12-28 2017-02-28 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
WO2015071824A1 (en) * 2013-11-13 2015-05-21 Glenmark Pharmaceuticals Limited; Glenmark Generics Limited Process for the preparation of aclidinium bromide
PT108370B (pt) 2015-03-30 2018-10-25 Hovione Farm S A Processo de preparação de brometo de aclidínio

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1829534A (zh) * 2003-07-29 2006-09-06 贝林格尔.英格海姆国际有限公司 包括β模拟物和抗胆碱能药的吸入药剂
CN101490048A (zh) * 2006-07-21 2009-07-22 奥米罗实验室有限公司 制备3(r)-(2-羟基-2,2-二噻吩-2-基乙酰氧基)-1-(3-苯氧基丙基)-1-氮鎓二环[2.2.2]辛烷溴化物的方法
CN104619706A (zh) * 2012-08-15 2015-05-13 葛兰素集团有限公司 化学方法
CN105683186A (zh) * 2013-10-29 2016-06-15 赞蒂瓦有限合伙公司 工业上适用的用于制备高纯度阿地溴铵的方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Discovery of Novel Quaternary Ammonium Derivatives of (3R)-Quinuclidinol Esters as Potent and Long-Acting Muscarinic Antagonists with Potential for Minimal Systemic Exposure after Inhaled Administration;Maria Prat 等;《Journal of Medicinal Chemistry》;20090804;第52卷(第16期);第5076-5092页，尤其是第5090页化合物56的制备 *
Maria Prat 等.Discovery of Novel Quaternary Ammonium Derivatives of (3R)-Quinuclidinol Esters as Potent and Long-Acting Muscarinic Antagonists with Potential for Minimal Systemic Exposure after Inhaled Administration.《Journal of Medicinal Chemistry》.2009,第52卷(第16期),第5076-5092页，尤其是第5090页化合物56的制备. *

Also Published As

Publication number Publication date
US20180105517A1 (en) 2018-04-19
US10087177B2 (en) 2018-10-02
AU2016240289B2 (en) 2020-08-27
JP2020143160A (ja) 2020-09-10
PT108370B (pt) 2018-10-25
US10590124B2 (en) 2020-03-17
IL254712A0 (en) 2017-11-30
CN108112252A (zh) 2018-06-01
AU2016240289A1 (en) 2017-10-19
PT108370A (pt) 2016-09-30
JP7124035B2 (ja) 2022-08-23
EP3277679A1 (en) 2018-02-07
CA2980665A1 (en) 2016-10-06
US20180362523A1 (en) 2018-12-20
JP2021020965A (ja) 2021-02-18
JP2022160667A (ja) 2022-10-19
JP2018510189A (ja) 2018-04-12
CA3165243A1 (en) 2016-10-06
WO2016156836A1 (en) 2016-10-06

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