JP5086267B2 - 臭化チオトロピウムの新規な形態およびそれを製造する方法 - Google Patents

臭化チオトロピウムの新規な形態およびそれを製造する方法 Download PDF

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JP5086267B2
JP5086267B2 JP2008538130A JP2008538130A JP5086267B2 JP 5086267 B2 JP5086267 B2 JP 5086267B2 JP 2008538130 A JP2008538130 A JP 2008538130A JP 2008538130 A JP2008538130 A JP 2008538130A JP 5086267 B2 JP5086267 B2 JP 5086267B2
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tiotropium bromide
tiotropium
bromide
hours
solution
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JP2009513675A (ja
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ディウルゲロフ，ニコラ
スカルピッタ，フランチェスカ
ポンティロリ，アレッサンドロ
コバチネ−メゼイ，アドリエンヌ
アロンヒメ，ジュディス
イェゴロブ，アレクサンドル
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シコール インコーポレイティド
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    • 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
    • C07D451/12—Oxygen atoms acylated by aromatic or heteroaromatic carboxylic acids, e.g. cocaine
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2008538130A 2005-12-19 2006-12-19 臭化チオトロピウムの新規な形態およびそれを製造する方法 Active JP5086267B2 (ja)

Applications Claiming Priority (17)

Application Number Priority Date Filing Date Title
US75267205P 2005-12-19 2005-12-19
US60/752,672 2005-12-19
US75453005P 2005-12-27 2005-12-27
US60/754,530 2005-12-27
US76143706P 2006-01-23 2006-01-23
US60/761,437 2006-01-23
US77405106P 2006-02-15 2006-02-15
US60/774,051 2006-02-15
US78031006P 2006-03-07 2006-03-07
US60/780,310 2006-03-07
US83218906P 2006-07-20 2006-07-20
US60/832,189 2006-07-20
US85122306P 2006-10-12 2006-10-12
US60/851,223 2006-10-12
US85274006P 2006-10-18 2006-10-18
US60/852,740 2006-10-18
PCT/US2006/048734 WO2007075858A2 (en) 2005-12-19 2006-12-19 Novel forms of tiotropium bromide and processes for preparation thereof

Related Child Applications (2)

Application Number Title Priority Date Filing Date
JP2012037796A Division JP5567610B2 (ja) 2005-12-19 2012-02-23 臭化チオトロピウムの新規な形態およびそれを製造する方法
JP2012127232A Division JP2012176975A (ja) 2005-12-19 2012-06-04 臭化チオトロピウムの新規な形態およびそれを製造する方法

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JP2009513675A JP2009513675A (ja) 2009-04-02
JP5086267B2 true JP5086267B2 (ja) 2012-11-28

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JP2008538130A Active JP5086267B2 (ja) 2005-12-19 2006-12-19 臭化チオトロピウムの新規な形態およびそれを製造する方法
JP2012037796A Active JP5567610B2 (ja) 2005-12-19 2012-02-23 臭化チオトロピウムの新規な形態およびそれを製造する方法
JP2012127232A Pending JP2012176975A (ja) 2005-12-19 2012-06-04 臭化チオトロピウムの新規な形態およびそれを製造する方法

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JP2012127232A Pending JP2012176975A (ja) 2005-12-19 2012-06-04 臭化チオトロピウムの新規な形態およびそれを製造する方法

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US (4) US8163913B2 (enExample)
EP (2) EP1869035B2 (enExample)
JP (3) JP5086267B2 (enExample)
KR (1) KR101395881B1 (enExample)
CN (1) CN102731494A (enExample)
AT (1) ATE552256T1 (enExample)
BR (1) BRPI0608427A2 (enExample)
CA (1) CA2627729A1 (enExample)
DK (1) DK1869035T4 (enExample)
ES (2) ES2384486T3 (enExample)
IL (1) IL187947A0 (enExample)
MX (1) MX2007009988A (enExample)
PL (2) PL2123650T3 (enExample)
PT (1) PT1869035E (enExample)
RS (1) RS52663B2 (enExample)
TW (1) TW200732340A (enExample)
WO (1) WO2007075858A2 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012176975A (ja) * 2005-12-19 2012-09-13 Sicor Inc 臭化チオトロピウムの新規な形態およびそれを製造する方法
PT106142A (pt) * 2012-02-10 2013-08-12 Hovione Farmaciencia S A Processo para a preparação de brometo de tiotrópio

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US9108962B2 (en) * 2005-12-19 2015-08-18 Sicor, Inc. Forms of tiotropium bromide and processes for preparation thereof
GB0716026D0 (en) 2007-08-16 2007-09-26 Norton Healthcare Ltd An inhalable medicament
WO2009087419A1 (en) * 2008-01-10 2009-07-16 Generics [Uk] Limited Novel process for the preparation of scopine esters
EP2172190A1 (en) * 2008-10-02 2010-04-07 Laboratorios Liconsa, S.A. Inhalable particles comprising tiotropium
AU2009312582B2 (en) * 2008-11-04 2014-03-27 Cipla Limited Tiotropium bromide having a low degree of crystallinity
BRPI0916047A2 (pt) * 2008-11-04 2015-11-10 Cipla Ltd composição farmacêutica em aerossol, uso de uma composição farmacêutica em aerossol, método para tratamento de sintomas crônicos ou agudos severos, moderados ou leves, ou para tratamento profilático de um distúrbio respiratório, dispensador farmacêutico em aerossol, processo para fabricação de um dispensador farmacêutico em aerossol e processo para fabricação de um complexo de um agente ativo e um adjuvante
CA2768553C (en) 2009-08-07 2016-08-02 Generics [Uk] Limited Anhydrate of tiotropium bromide
WO2011015883A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Dichloromethane solvate of tiotropium bromide and its use
TR201111589A2 (tr) * 2011-03-03 2012-09-21 Bi̇lgi̇ç Mahmut Tiotropyum bromür susuz kristal formu.
CZ304368B6 (cs) 2011-11-28 2014-04-02 Zentiva, K.S. Směsný solvát tiotropium bromidu a způsob jeho přípravy
GB201200525D0 (en) 2011-12-19 2012-02-29 Teva Branded Pharmaceutical Prod R & D Inc An inhalable medicament
EP2705838A1 (en) * 2012-09-06 2014-03-12 Xspray Microparticles Ab Tiotropium preparations
EP2897955B1 (en) * 2012-09-11 2019-11-06 Bilgic, Mahmut New tiotropium bromide crystalline form
ES2620758T3 (es) 2012-11-05 2017-06-29 Zentiva K.S. Estabilización de solvatos de tiotropio
KR20150135328A (ko) 2013-04-01 2015-12-02 풀매트릭스 인코퍼레이티드 티오트로피움 건조 분말
EP2789611A1 (en) * 2013-04-08 2014-10-15 Cerbios-Pharma S.A. A crystalline form of tiotropium bromide
US10034866B2 (en) 2014-06-19 2018-07-31 Teva Branded Pharmaceutical Products R&D, Inc. Inhalable medicament comprising tiotropium
RU2567539C1 (ru) * 2015-02-04 2015-11-10 Индивидуальный предприниматель Михайлов Олег Ростиславович КРИСТАЛЛИЧЕСКАЯ γ-МОДИФИКАЦИЯ (1α,2β,4β,5α,7β-7)-[(ГИДРОКСИДИ-2-ТИЕНИЛАЦЕТИЛ)ОКСИ]-9,9-ДИМЕТИЛ-3-ОКСА-9-АЗОНИАТРИЦИКЛО[3.3.1.02,4]НОНАН БРОМИДА МОНОГИДРАТА, СПОСОБ ЕЁ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕЁ ОСНОВЕ
WO2017138896A1 (en) * 2016-02-11 2017-08-17 Sima Patent Ve Lisanslama Hizmetleri Ltd. Şti Crystalline form of tiotropium bromide anhydrate
US11365170B2 (en) 2018-07-13 2022-06-21 Kyowa Hakko Bio Co., Ltd. Non-solvate crystal of eucomic acid and method for producing same
PT115583B (pt) 2019-06-17 2022-05-02 Hovione Farm S A Processo contínuo para a preparação de medicamentos anticolinérgicos
EP4108230A1 (en) 2021-06-24 2022-12-28 Laboratoires SMB New dry powder composition of tiotropium for inhalation

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CN101331128B (zh) * 2005-12-19 2013-05-29 西科尔公司 噻托溴铵的形式及其制备方法
PT1869035E (pt) * 2005-12-19 2013-01-10 Sicor Inc Novas formas de brometo de tiotrópio e processos para sua preparação
EP1923393A1 (en) 2006-11-17 2008-05-21 Boehringer Ingelheim Pharma GmbH & Co. KG Crystalline form of tiotropium bromide and urea
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CA2768553C (en) 2009-08-07 2016-08-02 Generics [Uk] Limited Anhydrate of tiotropium bromide

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012176975A (ja) * 2005-12-19 2012-09-13 Sicor Inc 臭化チオトロピウムの新規な形態およびそれを製造する方法
PT106142A (pt) * 2012-02-10 2013-08-12 Hovione Farmaciencia S A Processo para a preparação de brometo de tiotrópio
PT106142B (pt) * 2012-02-10 2014-07-18 Hovione Farmaci Ncia S A Processo para a preparação de brometo de tiotrópio

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Publication number Publication date
ES2384486T3 (es) 2012-07-05
JP2012136538A (ja) 2012-07-19
JP5567610B2 (ja) 2014-08-06
CN102731494A (zh) 2012-10-17
DK1869035T3 (da) 2013-01-14
US8163913B2 (en) 2012-04-24
US8846926B2 (en) 2014-09-30
US20140057935A1 (en) 2014-02-27
EP1869035B2 (en) 2015-08-12
US20120165364A1 (en) 2012-06-28
CA2627729A1 (en) 2007-07-05
EP2123650B1 (en) 2012-04-04
ES2396978T3 (es) 2013-03-01
US20070225314A1 (en) 2007-09-27
PL1869035T3 (pl) 2013-04-30
RS52663B2 (sr) 2018-05-31
EP2123650A1 (en) 2009-11-25
PL2123650T3 (pl) 2012-09-28
PT1869035E (pt) 2013-01-10
WO2007075858A2 (en) 2007-07-05
DK1869035T4 (en) 2015-11-16
MX2007009988A (es) 2008-02-22
KR20080078779A (ko) 2008-08-28
ES2396978T5 (es) 2015-12-04
RS52663B (sr) 2013-06-28
PL1869035T5 (pl) 2016-01-29
JP2009513675A (ja) 2009-04-02
KR101395881B1 (ko) 2014-05-21
JP2012176975A (ja) 2012-09-13
BRPI0608427A2 (pt) 2009-12-29
US20120108625A1 (en) 2012-05-03
ATE552256T1 (de) 2012-04-15
IL187947A0 (en) 2008-03-20
EP1869035B1 (en) 2012-10-03
TW200732340A (en) 2007-09-01
EP1869035A2 (en) 2007-12-26
WO2007075858A3 (en) 2007-11-01

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