CN102639531B - 噻托溴铵的无水合物 - Google Patents

噻托溴铵的无水合物 Download PDF

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Publication number
CN102639531B
CN102639531B CN201080044044.4A CN201080044044A CN102639531B CN 102639531 B CN102639531 B CN 102639531B CN 201080044044 A CN201080044044 A CN 201080044044A CN 102639531 B CN102639531 B CN 102639531B
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CN
China
Prior art keywords
tiotropium bromide
anhydrous tiotropium
anhydrous
organic solvent
bromide
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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CN201080044044.4A
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English (en)
Chinese (zh)
Other versions
CN102639531A (zh
Inventor
维纳亚克·戈文德·戈雷
宾杜·马诺杰库马
达塔特拉亚·希恩德
达塔特雷·科卡内
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Generics UK Ltd
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Generics UK Ltd
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Publication of CN102639531A publication Critical patent/CN102639531A/zh
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • 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
    • 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
    • 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
    • A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • 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
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C07D451/10—Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pulmonology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dispersion Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201080044044.4A 2009-08-07 2010-08-06 噻托溴铵的无水合物 Expired - Fee Related CN102639531B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN1048/KOL/2009 2009-08-07
IN1048KO2009 2009-08-07
PCT/GB2010/051310 WO2011015882A2 (en) 2009-08-07 2010-08-06 Novel anhydrate

Publications (2)

Publication Number Publication Date
CN102639531A CN102639531A (zh) 2012-08-15
CN102639531B true CN102639531B (zh) 2016-01-20

Family

ID=42830336

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080044044.4A Expired - Fee Related CN102639531B (zh) 2009-08-07 2010-08-06 噻托溴铵的无水合物

Country Status (9)

Country Link
US (2) US8697719B2 (https=)
EP (1) EP2462140A2 (https=)
JP (2) JP5822831B2 (https=)
CN (1) CN102639531B (https=)
AU (1) AU2010280497B2 (https=)
CA (2) CA2768553C (https=)
IN (1) IN2012DN00968A (https=)
NZ (2) NZ597920A (https=)
WO (1) WO2011015882A2 (https=)

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Publication number Priority date Publication date Assignee Title
RS52663B2 (sr) 2005-12-19 2018-05-31 Sicor Inc Nova kristalna forma tiotropijum bromida i proces njene pripreme
US9108962B2 (en) 2005-12-19 2015-08-18 Sicor, Inc. Forms of tiotropium bromide and processes for preparation thereof
NZ597920A (en) 2009-08-07 2014-05-30 Generics Uk Ltd Anhydrate of tiotropium bromide
TR201111589A2 (tr) * 2011-03-03 2012-09-21 Bi̇lgi̇ç Mahmut Tiotropyum bromür susuz kristal formu.
PT106142B (pt) 2012-02-10 2014-07-18 Hovione Farmaci Ncia S A Processo para a preparação de brometo de tiotrópio
EP2897955B1 (en) * 2012-09-11 2019-11-06 Bilgic, Mahmut New tiotropium bromide crystalline form
CN104341413A (zh) * 2013-07-29 2015-02-11 天津金耀集团有限公司 一种无水噻托溴铵的新晶型
DK2897588T3 (da) * 2013-11-22 2019-08-12 Teva Branded Pharmaceutical Products R&D Inc Inhalerbart lægemiddel
EP2913332A1 (en) 2014-02-27 2015-09-02 Euticals S.P.A. Crystalline form of tiotropium bromide with lactose
WO2018069887A1 (en) * 2016-10-14 2018-04-19 Glenmark Specialty S.A. Nebulizable compositions of tiotropium and formoterol

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1861598A (zh) * 2006-03-07 2006-11-15 南昌弘益科技有限公司 噻托溴铵无水物制备方法
CN1875019A (zh) * 2003-11-03 2006-12-06 贝林格尔·英格海姆国际有限公司 具有抗胆碱能的新颖无水晶体
WO2007075858A2 (en) * 2005-12-19 2007-07-05 Sicor Inc. Novel forms of tiotropium bromide and processes for preparation thereof
CN101166738A (zh) * 2005-05-02 2008-04-23 贝林格尔·英格海姆国际有限公司 噻托溴铵的新晶型

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DE3931041C2 (de) 1989-09-16 2000-04-06 Boehringer Ingelheim Kg Ester von Thienylcarbonsäuren mit Aminoalkoholen, ihre Quaternierungsprodukte, Verfahren zu ihrer Herstellung und diese enthaltende Arzneimittel
US5610163A (en) 1989-09-16 1997-03-11 Boehringer Ingelheim Gmbh Esters of thienyl carboxylic acids and amino alcohols and their quaternization products
CN100519558C (zh) 2000-10-12 2009-07-29 贝林格尔英格海姆法玛两合公司 结晶单水合物、其制备方法及其在制备药物组合中的用途
US6908928B2 (en) 2000-10-12 2005-06-21 Bi Pharma Kg. Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions
DE10064816A1 (de) 2000-12-22 2002-06-27 Boehringer Ingelheim Pharma Verfahren zur Herstellung eines Anticholinergikums
US6506900B1 (en) 2001-01-31 2003-01-14 Boehringer Ingelheim Pharma Ag Process for preparing a scopine ester intermediate
AUPR315301A0 (en) 2001-02-19 2001-03-15 Silverbrook Research Pty. Ltd. An Apparatus (ART102)
US6608055B2 (en) 2001-06-22 2003-08-19 Boehringer Ingelheim Pharma Kg Crystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
US6610849B2 (en) 2001-06-28 2003-08-26 Boehringer Ingelheim Pharma Kg Process for the manufacture of tropenol
DE10200943A1 (de) 2002-01-12 2003-07-24 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Scopinestern
US6747153B2 (en) 2002-05-31 2004-06-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Industrial process for preparing tropenol
DE602004021921D1 (de) 2003-05-28 2009-08-20 Theravance Inc Azabicycloalkanverbindungen als muscarinrezeptor antagonisten
US7968717B2 (en) * 2003-11-03 2011-06-28 Boehringer Ingelhein International Gmbh Crystalline anhydrate with anticholinergic efficacy
CN1271073C (zh) * 2004-10-26 2006-08-23 江苏正大天晴药业股份有限公司 结晶性抗胆碱能药噻托溴铵晶体
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JP2008540367A (ja) * 2005-05-02 2008-11-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規結晶性臭化チオトロピウム
DE102005035112A1 (de) 2005-07-27 2007-02-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neues Verfahren zur Herstellung von Tiotropiumsalzen unter Anwendung von in organischen Lösungsmitteln löslichen N-Methylscopiniumsalzen
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US20080051582A1 (en) 2006-07-10 2008-02-28 Sicor Inc. Process for the preparation of tiotropium bromide
WO2008089852A1 (de) 2007-01-26 2008-07-31 Boehringer Ingelheim Pharma Gmbh & Co.Kg Neues verfahren zur herstellung von tiotropiumsalzen
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DK2240477T3 (en) 2008-01-10 2014-12-08 Generics Uk Ltd New process for the preparation of skopinestre
NZ597920A (en) 2009-08-07 2014-05-30 Generics Uk Ltd Anhydrate of tiotropium bromide
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CN1875019A (zh) * 2003-11-03 2006-12-06 贝林格尔·英格海姆国际有限公司 具有抗胆碱能的新颖无水晶体
CN101166738A (zh) * 2005-05-02 2008-04-23 贝林格尔·英格海姆国际有限公司 噻托溴铵的新晶型
WO2007075858A2 (en) * 2005-12-19 2007-07-05 Sicor Inc. Novel forms of tiotropium bromide and processes for preparation thereof
CN1861598A (zh) * 2006-03-07 2006-11-15 南昌弘益科技有限公司 噻托溴铵无水物制备方法

Also Published As

Publication number Publication date
WO2011015882A3 (en) 2011-09-01
CN102639531A (zh) 2012-08-15
US20120149725A1 (en) 2012-06-14
JP2013501041A (ja) 2013-01-10
CA2931876A1 (en) 2011-02-10
NZ624602A (en) 2015-11-27
US20140249175A1 (en) 2014-09-04
JP2015214574A (ja) 2015-12-03
CA2768553A1 (en) 2011-02-10
AU2010280497B2 (en) 2015-10-22
JP5822831B2 (ja) 2015-11-24
US9181268B2 (en) 2015-11-10
NZ597920A (en) 2014-05-30
CA2768553C (en) 2016-08-02
US20150051241A9 (en) 2015-02-19
AU2010280497A8 (en) 2012-03-08
EP2462140A2 (en) 2012-06-13
WO2011015882A2 (en) 2011-02-10
US8697719B2 (en) 2014-04-15
AU2010280497A1 (en) 2012-02-23
IN2012DN00968A (https=) 2015-04-10

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Granted publication date: 20160120

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