CN102731494A - 噻托溴铵的新形式及其制备方法 - Google Patents

噻托溴铵的新形式及其制备方法 Download PDF

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Publication number
CN102731494A
CN102731494A CN201210232788XA CN201210232788A CN102731494A CN 102731494 A CN102731494 A CN 102731494A CN 201210232788X A CN201210232788X A CN 201210232788XA CN 201210232788 A CN201210232788 A CN 201210232788A CN 102731494 A CN102731494 A CN 102731494A
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China
Prior art keywords
tiotropium bromide
powder
ray diffractogram
peak
crystalline
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.)
Pending
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CN201210232788XA
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English (en)
Chinese (zh)
Inventor
N·久尔赫洛夫
F·斯卡皮塔
A·蓬蒂罗利
A·科瓦奇尼-梅蔡
J·阿伦希姆
A·耶戈洛夫
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Sicor Inc
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Sicor Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38115166&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102731494(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sicor Inc filed Critical Sicor Inc
Publication of CN102731494A publication Critical patent/CN102731494A/zh
Pending legal-status Critical Current

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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)
CN201210232788XA 2005-12-19 2006-12-19 噻托溴铵的新形式及其制备方法 Pending CN102731494A (zh)

Applications Claiming Priority (16)

Application Number Priority Date Filing Date Title
US75267205P 2005-12-19 2005-12-19
US60/752672 2005-12-19
US75453005P 2005-12-27 2005-12-27
US60/754530 2005-12-27
US76143706P 2006-01-23 2006-01-23
US60/761437 2006-01-23
US77405106P 2006-02-15 2006-02-15
US60/774051 2006-02-15
US78031006P 2006-03-07 2006-03-07
US60/780310 2006-03-07
US83218906P 2006-07-20 2006-07-20
US60/832189 2006-07-20
US85122306P 2006-10-12 2006-10-12
US60/851223 2006-10-12
US85274006P 2006-10-18 2006-10-18
US60/852740 2006-10-18

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN200680047726.4A Division CN101331128B (zh) 2005-12-19 2006-12-19 噻托溴铵的形式及其制备方法

Publications (1)

Publication Number Publication Date
CN102731494A true CN102731494A (zh) 2012-10-17

Family

ID=38115166

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201210232788XA Pending CN102731494A (zh) 2005-12-19 2006-12-19 噻托溴铵的新形式及其制备方法

Country Status (17)

Country Link
US (4) US8163913B2 (https=)
EP (2) EP2123650B1 (https=)
JP (3) JP5086267B2 (https=)
KR (1) KR101395881B1 (https=)
CN (1) CN102731494A (https=)
AT (1) ATE552256T1 (https=)
BR (1) BRPI0608427A2 (https=)
CA (1) CA2627729A1 (https=)
DK (1) DK1869035T4 (https=)
ES (2) ES2384486T3 (https=)
IL (1) IL187947A0 (https=)
MX (1) MX2007009988A (https=)
PL (2) PL1869035T5 (https=)
PT (1) PT1869035E (https=)
RS (1) RS52663B2 (https=)
TW (1) TW200732340A (https=)
WO (1) WO2007075858A2 (https=)

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RS52663B2 (sr) * 2005-12-19 2018-05-31 Sicor Inc Nova kristalna forma tiotropijum bromida i proces njene pripreme
GB0716026D0 (en) * 2007-08-16 2007-09-26 Norton Healthcare Ltd An inhalable medicament
DK2240477T3 (en) * 2008-01-10 2014-12-08 Generics Uk Ltd New process for the preparation of skopinestre
EP2172190A1 (en) * 2008-10-02 2010-04-07 Laboratorios Liconsa, S.A. Inhalable particles comprising tiotropium
JP2012507574A (ja) * 2008-11-04 2012-03-29 シプラ・リミテッド 医薬エアロゾル組成物
WO2010052450A1 (en) * 2008-11-04 2010-05-14 Cipla Limited Tiotropium bromide having a low degree of crystallinity
WO2011015883A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Dichloromethane solvate of tiotropium bromide and its use
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.
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
PT106142B (pt) * 2012-02-10 2014-07-18 Hovione Farmaci Ncia S A Processo para a preparação de brometo de tiotrópio
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
UA115888C2 (uk) 2012-11-05 2018-01-10 Зентіва, К.С. Стабілізація сольватів тіотропію
JP6473738B2 (ja) 2013-04-01 2019-02-20 パルマトリックス，インコーポレイテッド チオトロピウム乾燥粉末
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

Citations (7)

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CN1392795A (zh) * 2000-10-12 2003-01-22 贝林格尔英格海姆法玛公司 含噻托品鎓的新颖可吸入粉末
CN1481383A (zh) * 2000-12-22 2004-03-10 ���ָ��Ӣ��ķ�������Ϲ�˾ 制备抗胆碱能剂替托品溴化物的方法
CN1520294A (zh) * 2001-06-22 2004-08-11 ���ָ��Ӣ��ķ�������Ϲ�˾ 结晶性抗胆碱能药,其制备方法及其在药物制备中的用途
WO2005042527A1 (de) * 2003-11-03 2005-05-12 Boehringer Ingelheim International Gmbh Neues kristallines anhydrat mit anticholinerger wirksamkeit
CN1642952A (zh) * 2002-03-20 2005-07-20 贝林格尔英格海姆法玛两合公司 溴化替托品的结晶微粉体
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

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BRPI0609295A2 (pt) 2005-05-02 2010-03-23 Boehringer Ingelheim Int formas cristalinas de brometo de tiotràpio, composiÇço farmacÊutica, uso e mÉtodo para preparar as mesmas
RS52663B2 (sr) * 2005-12-19 2018-05-31 Sicor Inc Nova kristalna forma tiotropijum bromida i proces njene pripreme
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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NZ597920A (en) 2009-08-07 2014-05-30 Generics Uk Ltd Anhydrate of tiotropium bromide
WO2011015883A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Dichloromethane solvate of tiotropium bromide and its use

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Publication number Priority date Publication date Assignee Title
US5610163A (en) * 1989-09-16 1997-03-11 Boehringer Ingelheim Gmbh Esters of thienyl carboxylic acids and amino alcohols and their quaternization products
CN1392795A (zh) * 2000-10-12 2003-01-22 贝林格尔英格海姆法玛公司 含噻托品鎓的新颖可吸入粉末
CN1481383A (zh) * 2000-12-22 2004-03-10 ���ָ��Ӣ��ķ�������Ϲ�˾ 制备抗胆碱能剂替托品溴化物的方法
CN1520294A (zh) * 2001-06-22 2004-08-11 ���ָ��Ӣ��ķ�������Ϲ�˾ 结晶性抗胆碱能药,其制备方法及其在药物制备中的用途
CN1642952A (zh) * 2002-03-20 2005-07-20 贝林格尔英格海姆法玛两合公司 溴化替托品的结晶微粉体
WO2005042527A1 (de) * 2003-11-03 2005-05-12 Boehringer Ingelheim International Gmbh Neues kristallines anhydrat mit anticholinerger wirksamkeit
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

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Publication number Publication date
TW200732340A (en) 2007-09-01
DK1869035T4 (en) 2015-11-16
EP2123650A1 (en) 2009-11-25
US20120165364A1 (en) 2012-06-28
PT1869035E (pt) 2013-01-10
PL1869035T3 (pl) 2013-04-30
ES2384486T3 (es) 2012-07-05
RS52663B2 (sr) 2018-05-31
US8163913B2 (en) 2012-04-24
ES2396978T3 (es) 2013-03-01
KR20080078779A (ko) 2008-08-28
WO2007075858A2 (en) 2007-07-05
EP2123650B1 (en) 2012-04-04
JP5567610B2 (ja) 2014-08-06
KR101395881B1 (ko) 2014-05-21
EP1869035B1 (en) 2012-10-03
PL1869035T5 (pl) 2016-01-29
JP2012136538A (ja) 2012-07-19
ATE552256T1 (de) 2012-04-15
US8846926B2 (en) 2014-09-30
WO2007075858A3 (en) 2007-11-01
JP2009513675A (ja) 2009-04-02
US20140057935A1 (en) 2014-02-27
JP2012176975A (ja) 2012-09-13
CA2627729A1 (en) 2007-07-05
PL2123650T3 (pl) 2012-09-28
ES2396978T5 (es) 2015-12-04
US20070225314A1 (en) 2007-09-27
JP5086267B2 (ja) 2012-11-28
EP1869035B2 (en) 2015-08-12
MX2007009988A (es) 2008-02-22
US20120108625A1 (en) 2012-05-03
IL187947A0 (en) 2008-03-20
EP1869035A2 (en) 2007-12-26
RS52663B (sr) 2013-06-28
BRPI0608427A2 (pt) 2009-12-29
DK1869035T3 (da) 2013-01-14

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