CN100586948C - 结晶性抗胆碱能药,其制备方法及其在药物制备中的用途 - Google Patents

结晶性抗胆碱能药,其制备方法及其在药物制备中的用途 Download PDF

Info

Publication number
CN100586948C
CN100586948C CN02812303A CN02812303A CN100586948C CN 100586948 C CN100586948 C CN 100586948C CN 02812303 A CN02812303 A CN 02812303A CN 02812303 A CN02812303 A CN 02812303A CN 100586948 C CN100586948 C CN 100586948C
Authority
CN
China
Prior art keywords
tiotropium bromide
crystal
anhydrous
preparation
tiotropium
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 - Lifetime
Application number
CN02812303A
Other languages
English (en)
Chinese (zh)
Other versions
CN1520294A (zh
Inventor
彼得·西格
乌尔里克·沃思曼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH and Co KG
Original Assignee
Boehringer Ingelheim Pharma GmbH and 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
Application filed by Boehringer Ingelheim Pharma GmbH and Co KG filed Critical Boehringer Ingelheim Pharma GmbH and Co KG
Publication of CN1520294A publication Critical patent/CN1520294A/zh
Application granted granted Critical
Publication of CN100586948C publication Critical patent/CN100586948C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic 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
    • C07D451/02Heterocyclic 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
    • C07D451/04Heterocyclic 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
    • C07D451/06Oxygen atoms
    • C07D451/10Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pulmonology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
CN02812303A 2001-06-22 2002-06-08 结晶性抗胆碱能药,其制备方法及其在药物制备中的用途 Expired - Lifetime CN100586948C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10129710 2001-06-22
DE10129710.6 2001-06-22
DE10215436.8 2002-04-08
DE10215436 2002-04-08

Publications (2)

Publication Number Publication Date
CN1520294A CN1520294A (zh) 2004-08-11
CN100586948C true CN100586948C (zh) 2010-02-03

Family

ID=26009556

Family Applications (1)

Application Number Title Priority Date Filing Date
CN02812303A Expired - Lifetime CN100586948C (zh) 2001-06-22 2002-06-08 结晶性抗胆碱能药,其制备方法及其在药物制备中的用途

Country Status (37)

Country Link
EP (1) EP1401445B1 (enExample)
JP (1) JP2005504015A (enExample)
KR (2) KR100971616B1 (enExample)
CN (1) CN100586948C (enExample)
AR (1) AR037491A1 (enExample)
AT (1) ATE337006T1 (enExample)
AU (1) AU2002345016B2 (enExample)
BG (1) BG66303B1 (enExample)
BR (1) BR0210537A (enExample)
CA (1) CA2450961C (enExample)
CO (1) CO5550423A2 (enExample)
CY (1) CY1105223T1 (enExample)
CZ (1) CZ302786B6 (enExample)
DE (1) DE50207943D1 (enExample)
DK (1) DK1401445T3 (enExample)
EA (1) EA005813B1 (enExample)
EE (1) EE05316B1 (enExample)
EG (1) EG24851A (enExample)
ES (1) ES2271280T3 (enExample)
HR (1) HRP20031066B1 (enExample)
HU (1) HUP0400333A3 (enExample)
IL (2) IL159238A0 (enExample)
ME (1) ME00412B (enExample)
MX (1) MXPA03011718A (enExample)
MY (1) MY122779A (enExample)
NO (1) NO334301B1 (enExample)
NZ (1) NZ530690A (enExample)
PE (2) PE20081305A1 (enExample)
PL (1) PL208137B1 (enExample)
PT (1) PT1401445E (enExample)
RS (1) RS50441B (enExample)
SA (1) SA02230255B1 (enExample)
SI (1) SI1401445T1 (enExample)
SK (1) SK287262B6 (enExample)
TW (2) TW200617007A (enExample)
UY (1) UY27342A1 (enExample)
WO (1) WO2003000265A1 (enExample)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10212264A1 (de) 2002-03-20 2003-10-02 Boehringer Ingelheim Pharma Kristallines Mikronisat, Verfahren zu dessen Herstellung und dessen Verwendung zur Herstellung eines Arzneimittels
US7056916B2 (en) 2002-11-15 2006-06-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Medicaments for the treatment of chronic obstructive pulmonary disease
US20050038004A1 (en) * 2003-07-31 2005-02-17 Robinson Cynthia B. Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with an anticholinergic bronchodilator for treatment of asthma or chronic obstructive pulmonary disease
PT1682542E (pt) * 2003-11-03 2010-01-27 Boehringer Ingelheim Int Novo anidrato cristalino com actividade anticolinérgica
DE102004016179A1 (de) * 2004-03-30 2005-10-20 Boehringer Ingelheim Pharma Verbindungen zur Behandlung von proliferativen Prozessen
ES2523518T3 (es) 2004-04-22 2014-11-26 Boehringer Ingelheim International Gmbh Nuevas combinaciones farmacológicas para el tratamiento de enfermedades de las vías respiratorias
US7220742B2 (en) 2004-05-14 2007-05-22 Boehringer Ingelheim International Gmbh Enantiomerically pure beta agonists, process for the manufacture thereof and use thereof as medicaments
DE102004024454A1 (de) 2004-05-14 2005-12-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Enantiomerenreine Betaagonisten, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE602004020337D1 (de) 2004-08-11 2009-05-14 Boehringer Ingelheim Pharma Anticholinergika enthaltende Arzneimittel zur Behandlung von Krankheiten der ableitenden Harnwege
US20060079544A1 (en) * 2004-08-13 2006-04-13 Boehringer Ingelheim International Gmbh Medicaments for the prevention or treatment of alveolar pneumonia comprising an anticholinergic
DE102004048389A1 (de) 2004-10-01 2006-04-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Modifizierung von Oberflächen von Laktose als Hilfsstoff zur Verwendung für Pulverinhalativa
CN101163706A (zh) 2005-04-21 2008-04-16 贝林格尔·英格海姆国际有限公司 用于治疗炎性疾病的二氢噻吩并嘧啶
MX2007012907A (es) 2005-04-28 2008-03-14 Boehringer Ingelheim Int Nuevos compuestos para el tratamiento de enfermedades inflamatorias.
EP2085396A3 (en) * 2005-05-02 2009-11-25 Boehringer Ingelheim International Gmbh Novel crystalline forms of tiotropium bromide
KR20080007656A (ko) * 2005-05-02 2008-01-22 베링거 인겔하임 인터내셔날 게엠베하 티오트로피움 브로마이드의 신규한 결정질 형태
DE102005030733A1 (de) 2005-07-01 2007-01-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittelkombinationen zur Behandlung von Atemwegserkrankungen enthaltend langwirksame Beta-2-Agonisten und wenigstens einen weiteren Wirkstoff
ES2530991T3 (es) 2005-08-15 2015-03-09 Boehringer Ingelheim Int Procedimiento para la obtención de betamiméticos
TWI396541B (zh) 2005-10-10 2013-05-21 Boehringer Ingelheim Int 用於治療呼吸疾病之新穎藥物組合
US7423146B2 (en) 2005-11-09 2008-09-09 Boehringer Ingelheim International Gmbh Process for the manufacturing of pharmaceutically active 3,1-benzoxazine-2-ones
US9108962B2 (en) 2005-12-19 2015-08-18 Sicor, Inc. Forms of tiotropium bromide and processes for preparation thereof
MX2007009988A (es) 2005-12-19 2008-02-22 Sicor Inc Formas novedosas de bromuro de tiotropio y procesos para su preparacion.
CN100999521B (zh) * 2006-01-13 2010-12-08 江苏正大天晴药业股份有限公司 结晶性抗胆碱药噻托溴铵
EP1847543A1 (de) 2006-04-19 2007-10-24 Boehringer Ingelheim Pharma GmbH & Co. KG Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen
ATE505193T1 (de) 2006-08-07 2011-04-15 Boehringer Ingelheim Int Arzneimittelkombinationen zur behandlung von atemwegserkrankungen
UY30550A1 (es) 2006-08-22 2008-03-31 Boehringer Ingelheim Int Nuevos beta-agonistas enantioméricamente puros, procedimientos para su preparacion y su uso como medicamentos
GB0716026D0 (en) 2007-08-16 2007-09-26 Norton Healthcare Ltd An inhalable medicament
ES2524910T3 (es) 2007-10-19 2014-12-15 Boehringer Ingelheim International Gmbh Piperidino-dihidrotienopirimidinas sustituidas
EP2093219A1 (de) 2008-02-22 2009-08-26 Boehringer Ingelheim International Gmbh Kristalline, enantiomerenreine Salzform eines Betamimetikums und dessen Verwendung als Arzneimittel
CN102256963B (zh) 2008-12-19 2014-06-11 贝林格尔.英格海姆国际有限公司 作为ccr2受体拮抗剂用于治疗炎症、哮喘和copd的环状嘧啶-4-甲酰胺
WO2010101538A2 (en) 2009-03-06 2010-09-10 Bilgic Mahmut New crystal forms
MX346393B (es) 2009-12-17 2017-03-17 Centrexion Therapeutics Corp Nuevos antagonistas del receptor ccr2 y usos de los mismo.
US20130143905A1 (en) 2009-12-17 2013-06-06 Boehringer Ingelheim International Gmbh Novel antagonists for ccr2 and uses thereof
EP2528915B1 (en) 2010-01-29 2015-10-28 Boehringer Ingelheim International GmbH Substituted naphthyridines and their use as syk kinase inhibitors
JP2013526507A (ja) 2010-05-12 2013-06-24 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ccr2受容体アンタゴニスト、その製造方法及び薬物としてのその使用
WO2011141477A1 (en) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
WO2011144501A1 (en) 2010-05-17 2011-11-24 Boehringer Ingelheim International Gmbh Ccr2 antagonists and uses thereof
WO2011147772A1 (en) 2010-05-25 2011-12-01 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists
US8962656B2 (en) 2010-06-01 2015-02-24 Boehringer Ingelheim International Gmbh CCR2 antagonists
TR201007108A2 (tr) * 2010-08-25 2012-03-21 B�Lg�� Mahmut Yeni tiotropyum bromür kristali ve üretim yöntemi.@
WO2012101013A1 (en) 2011-01-28 2012-08-02 Boehringer Ingelheim International Gmbh Substituted pyridinyl-pyrimidines and their use as medicaments
TR201101897A2 (tr) 2011-02-28 2012-09-21 Bi̇lgi̇ç Mahmut Tiotropyum bromür içeren kristal madde
TR201111589A2 (tr) * 2011-03-03 2012-09-21 Bi̇lgi̇ç Mahmut Tiotropyum bromür susuz kristal formu.
TR201102068A2 (tr) 2011-03-03 2012-09-21 Bi̇lgi̇ç Mahmut Tiotropyum bromür içeren kristal maddeler
JP5786257B2 (ja) 2011-06-16 2015-09-30 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 新規の選択的ccr2拮抗薬
WO2013010839A1 (en) 2011-07-15 2013-01-24 Boehringer Ingelheim International Gmbh Novel and selective ccr2 antagonists
JP5860960B2 (ja) 2011-07-26 2016-02-16 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 置換キノリン類及び医薬としてのそれらの使用
US20130059866A1 (en) 2011-08-24 2013-03-07 Boehringer Ingelheim International Gmbh Novel piperidino-dihydrothienopyrimidine sulfoxides and their use for treating copd and asthma
PL2782914T3 (pl) 2011-11-25 2019-01-31 Adverio Pharma Gmbh Sposób wytwarzania podstawionych 5-fluoro-1H-pirazolopirydyn
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
US9096579B2 (en) 2012-04-20 2015-08-04 Boehringer Ingelheim International Gmbh Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
EP2897955B1 (en) * 2012-09-11 2019-11-06 Bilgic, Mahmut New tiotropium bromide crystalline form
WO2014067499A1 (en) 2012-11-05 2014-05-08 Zentiva, K.S. Stabilization of tiotropium solvates
CN104341412A (zh) * 2013-07-29 2015-02-11 天津金耀集团有限公司 一种无水噻托溴铵结晶的制备方法
SG11201607794QA (en) 2014-03-19 2016-10-28 Boehringer Ingelheim Int Heteroaryl syk inhibitors
US10034866B2 (en) 2014-06-19 2018-07-31 Teva Branded Pharmaceutical Products R&D, Inc. Inhalable medicament comprising tiotropium
RS60737B1 (sr) 2014-10-21 2020-09-30 Ariad Pharma Inc Kristalni oblici 5-hloro-n4-[-2-(dimetilfosforil)fenil]-n2-{2-metoksi-4-[4-(4-metilpiperazin-1-il)piperidin-1-il]pirimidin-2,4-diamina
EP3414243A1 (en) * 2016-02-11 2018-12-19 Sima Patent Ve Lisanslama Hizmetleri Ltd. STI Crystalline form of tiotropium bromide anhydrate

Citations (1)

* Cited by examiner, † Cited by third party
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DK1326862T3 (da) * 2000-10-12 2004-11-22 Boehringer Ingelheim Pharma Krystallinsk monohydrat af tiotropiumbromid, fremgangsmåde til fremstilling deraf og anvendelse deraf til fremstilling af et lægemiddel
DE10064816A1 (de) * 2000-12-22 2002-06-27 Boehringer Ingelheim Pharma Verfahren zur Herstellung eines Anticholinergikums

Patent Citations (1)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
AR037491A1 (es) 2004-11-17
NO20035696D0 (no) 2003-12-19
CZ2004120A3 (cs) 2004-05-12
KR100971616B1 (ko) 2010-07-22
IL159238A0 (en) 2004-06-01
CA2450961A1 (en) 2003-01-03
HRP20031066B1 (en) 2011-10-31
PL364489A1 (en) 2004-12-13
EE200400029A (et) 2004-04-15
MY122779A (en) 2006-05-31
EP1401445B1 (de) 2006-08-23
EP1401445A1 (de) 2004-03-31
DE50207943D1 (de) 2006-10-05
CN1520294A (zh) 2004-08-11
CO5550423A2 (es) 2005-08-31
ME00412B (me) 2011-10-10
MXPA03011718A (es) 2004-12-06
PL208137B1 (pl) 2011-03-31
JP2005504015A (ja) 2005-02-10
YU99703A (sh) 2006-05-25
EA005813B1 (ru) 2005-06-30
ATE337006T1 (de) 2006-09-15
CY1105223T1 (el) 2010-03-03
AU2002345016B2 (en) 2008-04-17
KR20090031638A (ko) 2009-03-26
SK522004A3 (en) 2004-06-08
KR20040018285A (ko) 2004-03-02
UY27342A1 (es) 2003-02-28
SA02230255B1 (ar) 2006-10-31
HK1068540A1 (zh) 2005-04-29
HRP20031066A2 (en) 2004-04-30
SI1401445T1 (sl) 2007-02-28
BG66303B1 (bg) 2013-03-29
WO2003000265A1 (de) 2003-01-03
KR101011353B1 (ko) 2011-01-28
SK287262B6 (sk) 2010-04-07
EA200301293A1 (ru) 2004-08-26
RS50441B (sr) 2010-03-02
PE20081305A1 (es) 2008-10-01
PT1401445E (pt) 2006-10-31
CZ302786B6 (cs) 2011-11-09
CA2450961C (en) 2010-03-30
BG108440A (bg) 2004-08-31
MEP62008A (en) 2011-05-10
DK1401445T3 (da) 2006-11-27
HUP0400333A2 (hu) 2004-12-28
PE20030130A1 (es) 2003-04-02
IL159238A (en) 2010-04-15
NZ530690A (en) 2005-05-27
TWI261589B (en) 2006-09-11
HUP0400333A3 (en) 2012-10-29
NO334301B1 (no) 2014-02-03
ES2271280T3 (es) 2007-04-16
EE05316B1 (et) 2010-08-16
BR0210537A (pt) 2004-06-22
EG24851A (en) 2010-10-27
TW200617007A (en) 2006-06-01

Similar Documents

Publication Publication Date Title
CN100586948C (zh) 结晶性抗胆碱能药,其制备方法及其在药物制备中的用途
CN100519558C (zh) 结晶单水合物、其制备方法及其在制备药物组合中的用途
US6608055B2 (en) Crystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
US6777423B2 (en) Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions
JP5227790B2 (ja) 新規結晶性臭化チオトロピウム
CA2479652C (en) Crystalline micronisate of tiotropium bromide
HK1068540B (en) Crystalline anticholinergic, method for its production, and use thereof in the production of a drug
HK1086557B (en) Crystalline monohydrate, method for producing the same and the use thereof in the production of a medicament
HK1060567B (en) Crystalline monohydrate, method for producing the same and the use thereof in the production of a medicament
HK1114856B (en) Novel crystalline forms of tiotropium bromide

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1068540

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1068540

Country of ref document: HK

CX01 Expiry of patent term

Granted publication date: 20100203

CX01 Expiry of patent term