HUP0301457A2 - Eljárás tiotropium-bromid előállítására - Google Patents

Eljárás tiotropium-bromid előállítására

Info

Publication number
HUP0301457A2
HUP0301457A2 HU0301457A HUP0301457A HUP0301457A2 HU P0301457 A2 HUP0301457 A2 HU P0301457A2 HU 0301457 A HU0301457 A HU 0301457A HU P0301457 A HUP0301457 A HU P0301457A HU P0301457 A2 HUP0301457 A2 HU P0301457A2
Authority
HU
Hungary
Prior art keywords
tiotropium bromide
formula
producing tiotropium
producing
bromide
Prior art date
Application number
HU0301457A
Other languages
English (en)
Inventor
Rolf Banholzer
Wolfgang Broeder
Manfred Graulich
Sven Luettke
Andreas Mathes
Helmut Meissner
Peter Specht
Original Assignee
Boehringer Ingelheim Pharma Gmbh & Co. Kg
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7668836&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0301457(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Pharma Gmbh & Co. Kg filed Critical Boehringer Ingelheim Pharma Gmbh & Co. Kg
Publication of HUP0301457A2 publication Critical patent/HUP0301457A2/hu
Publication of HUP0301457A3 publication Critical patent/HUP0301457A3/hu
Publication of HU230320B1 publication Critical patent/HU230320B1/hu

Links

Classifications

    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Silicates, Zeolites, And Molecular Sieves (AREA)
  • Catalysts (AREA)

Abstract

A találmány tárgyát új eljárás képezi, az képletű tiotropium-bromidelőállítására a képletű tropenol-észter képletű szkopin-észterré valóepoxidálásával, majd metil-bromiddal az (I) képletű tiotropium-bromiddá való kvaternerezésével. Ó
HU0301457A 2000-12-22 2001-12-12 Eljárás az antikolinergikum tiotropium-bromid előállítására HU230320B1 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10064816A DE10064816A1 (de) 2000-12-22 2000-12-22 Verfahren zur Herstellung eines Anticholinergikums
DE10064816.9 2000-12-22
PCT/EP2001/014566 WO2002051840A1 (de) 2000-12-22 2001-12-12 Verfahren zur herstellung des anticholinergikums tiotropiumbromid

Publications (3)

Publication Number Publication Date
HUP0301457A2 true HUP0301457A2 (hu) 2003-10-28
HUP0301457A3 HUP0301457A3 (en) 2006-05-29
HU230320B1 HU230320B1 (hu) 2016-01-28

Family

ID=7668836

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0301457A HU230320B1 (hu) 2000-12-22 2001-12-12 Eljárás az antikolinergikum tiotropium-bromid előállítására

Country Status (42)

Country Link
US (1) US6486321B2 (hu)
EP (2) EP1426373B1 (hu)
JP (1) JP4198991B2 (hu)
KR (1) KR100853109B1 (hu)
CN (2) CN1244581C (hu)
AR (1) AR033599A1 (hu)
AT (2) ATE266661T1 (hu)
AU (1) AU2002229650B2 (hu)
BG (1) BG66373B1 (hu)
BR (1) BRPI0116444B8 (hu)
CA (1) CA2433518C (hu)
CY (1) CY1105210T1 (hu)
CZ (1) CZ294958B6 (hu)
DE (3) DE10064816A1 (hu)
DK (2) DK1345936T3 (hu)
EA (1) EA005533B1 (hu)
EC (1) ECSP034652A (hu)
EE (1) EE04495B1 (hu)
EG (1) EG23914A (hu)
ES (2) ES2271722T3 (hu)
HK (2) HK1060570A1 (hu)
HR (1) HRP20030502B1 (hu)
HU (1) HU230320B1 (hu)
IL (2) IL156351A0 (hu)
ME (1) MEP40608A (hu)
MX (1) MXPA03005426A (hu)
MY (1) MY129525A (hu)
NO (1) NO327739B1 (hu)
NZ (1) NZ527066A (hu)
PE (1) PE20020755A1 (hu)
PL (1) PL202478B1 (hu)
PT (2) PT1426373E (hu)
RS (1) RS50271B (hu)
SA (1) SA01220589B1 (hu)
SI (1) SI1345936T1 (hu)
SK (1) SK287318B6 (hu)
TR (1) TR200401127T4 (hu)
TW (1) TWI234564B (hu)
UA (1) UA74409C2 (hu)
UY (1) UY27079A1 (hu)
WO (1) WO2002051840A1 (hu)
ZA (1) ZA200304707B (hu)

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US20020111363A1 (en) * 2000-10-31 2002-08-15 Karin Drechsel Inhalable formulation of a solution containing a tiotropium salt
US20020151541A1 (en) * 2000-10-31 2002-10-17 Michel Pairet Pharmaceutical compositions containing tiotropium salts and antihistamines and their use
US20020137764A1 (en) 2000-10-31 2002-09-26 Karin Drechsel Inhalable formulation of a solution containing a tiotropium salt
US7776315B2 (en) * 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
US20020193392A1 (en) * 2000-11-13 2002-12-19 Christel Schmelzer Pharmaceutical compositions based on tiotropium salts of salts of salmeterol
US20100310477A1 (en) * 2000-11-28 2010-12-09 Boehringer Ingelheim Pharma Gmbh & Co. Kg. Pharmaceutical compositions based on anticholingerics and additional active ingredients
US20030013675A1 (en) * 2001-05-25 2003-01-16 Boehringer Ingelheim Pharma Kg Combination of an adenosine A2A-receptor agonist and tiotropium or a derivative thereof for treating obstructive airways and other inflammatory diseases
US20030070679A1 (en) * 2001-06-01 2003-04-17 Boehringer Ingelheim Pharma Kg Capsules containing inhalable tiotropium
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
KR101011353B1 (ko) * 2001-06-22 2011-01-28 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 결정질 항콜린제, 이의 제조방법 및 이를 포함하는 약제학적 조성물
US20030018019A1 (en) * 2001-06-23 2003-01-23 Boehringer Ingelheim Pharma Kg Pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics
DE10141377A1 (de) * 2001-08-23 2003-03-13 Boehringer Ingelheim Pharma Aufstreuverfahren zur Herstellung von Pulverformulierungen
US6919325B2 (en) * 2001-09-14 2005-07-19 Boehringer Ingelheim Pharma Kg Pharmaceutical compositions containing tiotropium salts and low-solubility salmeterol salts
DE10200943A1 (de) * 2002-01-12 2003-07-24 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Scopinestern
US7405224B2 (en) * 2002-01-31 2008-07-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthenecarboxylates, processes for preparing them, and their use as pharmaceutical compositions
US6790856B2 (en) * 2002-01-31 2004-09-14 Boehringer Ingelheim Pharma Kg Fluorenecarboxylic acid esters, process for the manufacture thereof, and use thereof as medicaments
US7309707B2 (en) * 2002-03-20 2007-12-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg Crystalline micronisate, process for the manufacture thereof and use thereof for the preparation of a medicament
US7311894B2 (en) * 2002-03-28 2007-12-25 Boehringer Ingelheim Pharma Gmbh & Co. Kg HFA suspension formulations containing an anticholinergic
US7244415B2 (en) 2002-03-28 2007-07-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg HFA suspension formulations of an anhydrate
CA2479919C (en) * 2002-04-04 2011-05-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Powder formulations suitable for inhalation
US20030235538A1 (en) 2002-04-09 2003-12-25 Boehringer Ingelheim Pharma Gmbh & Co. Kg Method for the administration of an anticholinergic by inhalation
US7084153B2 (en) * 2002-04-12 2006-08-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Medicaments comprising steroids and a novel anticholinergic
US7417051B2 (en) * 2002-04-12 2008-08-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Medicaments comprising betamimetics and a novel anticholinergic
US7763280B2 (en) * 2002-11-28 2010-07-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Tiotropium containing powder formulation for inhalation
DE10345065A1 (de) * 2003-09-26 2005-04-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Aerosolformulierung für die Inhalation enthaltend ein Anticholinergikum
PL2067779T3 (pl) * 2003-11-03 2013-09-30 Boehringer Ingelheim Int Sole tiotropium, sposoby ich wytwarzania oraz zawierające je kompozycje farmaceutyczne
KR20060102561A (ko) * 2003-11-03 2006-09-27 베링거 인겔하임 인터내셔날 게엠베하 신규한 티오트로피움염, 이의 제조 방법 및 이를 함유하는약제학적 제형
SE0303570L (sv) * 2003-12-03 2005-06-04 Microdrug Ag Fukt-känslig medicinsk produkt
KR20080007656A (ko) * 2005-05-02 2008-01-22 베링거 인겔하임 인터내셔날 게엠베하 티오트로피움 브로마이드의 신규한 결정질 형태
ES2393794T3 (es) 2005-05-02 2012-12-28 Boehringer Ingelheim International Gmbh Nuevas formas cristalinas de bromuro de tiotropio
NZ583872A (en) * 2005-06-15 2011-10-28 Boehringer Ingelheim Int Process for preparing tiotropium salts, tiotropium salts as such and pharmaceutical compositions thereof
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
CN1316245C (zh) * 2005-07-28 2007-05-16 山东齐都药业有限公司 托烷司琼合成中残留中间体托品醇的检测方法
TWI274641B (en) * 2005-08-30 2007-03-01 Rexon Ind Corp Ltd Cutting machine
DE102005059602A1 (de) 2005-12-14 2007-06-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Mikronisierung
EP1966196A2 (en) * 2005-12-19 2008-09-10 Sicor, Inc. Pure and stable tiotropium bromide
RU2453547C2 (ru) * 2005-12-19 2012-06-20 Сикор Инк. Новые формы тиотропия бромида и способы их получения
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DK1869035T4 (en) * 2005-12-19 2015-11-16 Sicor Inc HIS UNKNOWN CRYSTALLIC FORM OF THIOTROPIUM BROMIDE AND PROCEDURE FOR PREPARING THEREOF
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EP1882691A1 (en) * 2006-07-26 2008-01-30 CHIESI FARMACEUTICI S.p.A. Quinuclidine derivatives as M3 antagonists
EP1950196A1 (de) * 2007-01-29 2008-07-30 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung von Ammoniumhexafluorophosphaten
EP2036898A2 (de) * 2007-09-13 2009-03-18 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung von 1,3-Dioxolan-2Onen sowie von Carbonsäureestern durch Transacylierung unter Basischen Reaktionsbedingungen
SI2240477T1 (sl) * 2008-01-10 2015-02-27 Generics (Uk) Limited Nov postopek za pripravo estrov skopina
WO2011015884A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Process to prepare scopine esters
CA2931876A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Anhydrate of tiotropium bromide
CN101768158B (zh) * 2010-01-04 2013-05-29 南昌弘益科技有限公司 噻托溴铵无水物及其制备方法
CN101863885B (zh) * 2010-06-03 2012-05-30 南京金丹呈医药技术有限公司 一种噻托溴铵的制备方法
TR201007108A2 (tr) * 2010-08-25 2012-03-21 B�Lg�� Mahmut Yeni tiotropyum bromür kristali ve üretim yöntemi.@
ITRM20110508A1 (it) 2011-09-27 2013-03-28 Lusochimica Spa Processo per la preparazione degli esteri della scopina.
EP2607351B1 (en) * 2011-12-22 2017-03-15 Cerbios-Pharma S.A. Continuous process for the alkylation of cyclic tertiary amines
PT106142B (pt) 2012-02-10 2014-07-18 Hovione Farmaci Ncia S A Processo para a preparação de brometo de tiotrópio
CZ305012B6 (cs) * 2012-03-30 2015-03-25 Zentiva, K.S. Způsob přípravy skopinesteru kyseliny di(2-thienyl)glykolové, intermediátu v syntéze tiotropium bromidu
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
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WO2019129801A1 (en) 2017-12-28 2019-07-04 Linnea S.A. Process for the purification of methyl-2,2-dithienylglycolate
CN113264929B (zh) * 2021-05-02 2023-10-10 润生药业有限公司 一种噻托溴铵的制备方法

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Also Published As

Publication number Publication date
BRPI0116444B8 (pt) 2021-05-25
IL156351A0 (en) 2004-01-04
DK1345936T3 (da) 2004-07-19
BR0116444A (pt) 2003-12-23
ES2221658T3 (es) 2005-01-01
ATE337314T1 (de) 2006-09-15
WO2002051840A1 (de) 2002-07-04
US20020133010A1 (en) 2002-09-19
CA2433518A1 (en) 2002-07-04
HK1096683A1 (en) 2007-06-08
EG23914A (en) 2007-12-30
CY1105210T1 (el) 2010-03-03
CN1840529A (zh) 2006-10-04
EE04495B1 (et) 2005-06-15
PT1426373E (pt) 2006-11-30
PL361837A1 (en) 2004-10-04
DE10064816A1 (de) 2002-06-27
TR200401127T4 (tr) 2004-07-21
ZA200304707B (en) 2004-04-20
UY27079A1 (es) 2002-07-31
BRPI0116444B1 (pt) 2015-09-01
UA74409C2 (uk) 2005-12-15
PL202478B1 (pl) 2009-06-30
EA200300666A1 (ru) 2003-12-25
MXPA03005426A (es) 2005-04-20
JP2004525099A (ja) 2004-08-19
CZ20031685A3 (cs) 2003-10-15
MY129525A (en) 2007-04-30
CN100393719C (zh) 2008-06-11
NO327739B1 (no) 2009-09-14
EP1345936A1 (de) 2003-09-24
ATE266661T1 (de) 2004-05-15
SA01220589B1 (ar) 2006-10-31
CN1244581C (zh) 2006-03-08
EP1345936B1 (de) 2004-05-12
NO20032827L (no) 2003-06-20
SK287318B6 (sk) 2010-07-07
DE50110835D1 (de) 2006-10-05
HUP0301457A3 (en) 2006-05-29
NO20032827D0 (no) 2003-06-20
DK1426373T3 (da) 2006-12-18
HU230320B1 (hu) 2016-01-28
CZ294958B6 (cs) 2005-04-13
PT1345936E (pt) 2004-09-30
BG66373B1 (bg) 2013-10-31
KR100853109B1 (ko) 2008-08-21
KR20030062439A (ko) 2003-07-25
EA005533B1 (ru) 2005-04-28
CA2433518C (en) 2007-03-20
SI1345936T1 (en) 2004-08-31
EP1426373A1 (de) 2004-06-09
DE50102299D1 (de) 2004-06-17
ECSP034652A (es) 2003-07-25
AR033599A1 (es) 2003-12-26
MEP40608A (en) 2011-02-10
BG107910A (bg) 2004-02-27
HRP20030502B1 (en) 2011-09-30
IL156351A (en) 2011-09-27
YU50903A (sh) 2006-05-25
EE200300309A (et) 2003-10-15
ES2271722T3 (es) 2007-04-16
AU2002229650B2 (en) 2006-12-21
JP4198991B2 (ja) 2008-12-17
EP1426373B1 (de) 2006-08-23
US6486321B2 (en) 2002-11-26
SK9352003A3 (en) 2003-10-07
RS50271B (sr) 2009-07-15
TWI234564B (en) 2005-06-21
PE20020755A1 (es) 2002-09-24
HK1060570A1 (en) 2004-08-13
HRP20030502A2 (en) 2005-04-30
NZ527066A (en) 2004-12-24
CN1481383A (zh) 2004-03-10

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