JP2008540367A5 - - Google Patents
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- Publication number
- JP2008540367A5 JP2008540367A5 JP2008509409A JP2008509409A JP2008540367A5 JP 2008540367 A5 JP2008540367 A5 JP 2008540367A5 JP 2008509409 A JP2008509409 A JP 2008509409A JP 2008509409 A JP2008509409 A JP 2008509409A JP 2008540367 A5 JP2008540367 A5 JP 2008540367A5
- Authority
- JP
- Japan
- Prior art keywords
- tiotropium bromide
- crystalline
- solvate
- ray powder
- powder diagram
- 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
Links
- 229960000257 tiotropium bromide Drugs 0.000 claims 28
- LERNTVKEWCAPOY-VOGVJGKGSA-N C[N+]1(C)[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 Chemical compound C[N+]1(C)[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 LERNTVKEWCAPOY-VOGVJGKGSA-N 0.000 claims 24
- 239000012453 solvate Substances 0.000 claims 23
- 238000010586 diagram Methods 0.000 claims 18
- 239000000843 powder Substances 0.000 claims 18
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 12
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 12
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 11
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 10
- 239000013078 crystal Substances 0.000 claims 10
- MQLXPRBEAHBZTK-SEINRUQRSA-M tiotropium bromide hydrate Chemical compound O.[Br-].C[N+]1(C)[C@H]2C[C@@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 MQLXPRBEAHBZTK-SEINRUQRSA-M 0.000 claims 10
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Substances OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 9
- 238000004519 manufacturing process Methods 0.000 claims 7
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 5
- 239000002904 solvent Substances 0.000 claims 4
- 229940110309 tiotropium Drugs 0.000 claims 4
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical compound O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 claims 4
- -1 tiotropium bromide anhydride Chemical class 0.000 claims 4
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 2
- 239000007858 starting material Substances 0.000 claims 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000808 adrenergic beta-agonist Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 1
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 239000000021 stimulant Substances 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US67676005P | 2005-05-02 | 2005-05-02 | |
| PCT/EP2006/061765 WO2006117300A2 (en) | 2005-05-02 | 2006-04-21 | Crystalline forms of tiotropium bromide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008540367A JP2008540367A (ja) | 2008-11-20 |
| JP2008540367A5 true JP2008540367A5 (enExample) | 2009-06-18 |
Family
ID=36617384
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008509409A Pending JP2008540367A (ja) | 2005-05-02 | 2006-04-21 | 新規結晶性臭化チオトロピウム |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20060246009A1 (enExample) |
| EP (1) | EP1879888A2 (enExample) |
| JP (1) | JP2008540367A (enExample) |
| KR (1) | KR20080007656A (enExample) |
| CN (1) | CN101203513A (enExample) |
| AU (1) | AU2006243239A1 (enExample) |
| BR (1) | BRPI0611091A2 (enExample) |
| CA (1) | CA2606552A1 (enExample) |
| IL (1) | IL187054A0 (enExample) |
| MX (1) | MX2007013691A (enExample) |
| RU (1) | RU2007144531A (enExample) |
| WO (1) | WO2006117300A2 (enExample) |
| ZA (1) | ZA200708175B (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070167480A1 (en) * | 2005-12-19 | 2007-07-19 | Sicor Inc. | Pure and stable tiotropium bromide |
| KR101395881B1 (ko) | 2005-12-19 | 2014-05-21 | 시코르, 인크. | 브롬화 티오트로피움의 신규한 형태 및 이의 제조 방법 |
| CN101360744A (zh) * | 2005-12-19 | 2009-02-04 | 西科尔公司 | 纯和稳定的噻托溴铵 |
| US9108962B2 (en) | 2005-12-19 | 2015-08-18 | Sicor, Inc. | Forms of tiotropium bromide and processes for preparation thereof |
| 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 |
| US20080051582A1 (en) | 2006-07-10 | 2008-02-28 | Sicor Inc. | Process for the preparation of tiotropium bromide |
| EP1923393A1 (en) * | 2006-11-17 | 2008-05-21 | Boehringer Ingelheim Pharma GmbH & Co. KG | Crystalline form of tiotropium bromide and urea |
| GB0716026D0 (en) * | 2007-08-16 | 2007-09-26 | Norton Healthcare Ltd | An inhalable medicament |
| EP2403851B1 (en) | 2009-03-06 | 2015-06-17 | Mahmut Bilgic | New crystalline forms of tiotropium bromide |
| CA2931876A1 (en) | 2009-08-07 | 2011-02-10 | 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 |
| TR201007108A2 (tr) * | 2010-08-25 | 2012-03-21 | B�Lg�� Mahmut | Yeni tiotropyum bromür kristali ve üretim yöntemi.@ |
| TR201101897A2 (tr) * | 2011-02-28 | 2012-09-21 | Bi̇lgi̇ç Mahmut | Tiotropyum bromür içeren kristal madde |
| CZ304368B6 (cs) * | 2011-11-28 | 2014-04-02 | Zentiva, K.S. | Směsný solvát tiotropium bromidu a způsob jeho přípravy |
| CN103130798B (zh) * | 2011-11-30 | 2015-12-02 | 连云港润众制药有限公司 | 噻托溴铵的结晶 |
| 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 |
| WO2014042605A1 (en) * | 2012-09-11 | 2014-03-20 | Mahmut Bilgic | New tiotropium bromide crystalline form |
| ME02679B (me) * | 2012-11-05 | 2017-06-20 | Zentiva Ks | Stabilizacija tiotropij solvata |
| EP2789611A1 (en) * | 2013-04-08 | 2014-10-15 | Cerbios-Pharma S.A. | A crystalline form of tiotropium bromide |
| 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 |
| 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 |
| EP2913332A1 (en) | 2014-02-27 | 2015-09-02 | Euticals S.P.A. | Crystalline form of tiotropium bromide with lactose |
| US10034866B2 (en) | 2014-06-19 | 2018-07-31 | Teva Branded Pharmaceutical Products R&D, Inc. | Inhalable medicament comprising tiotropium |
| WO2017138896A1 (en) | 2016-02-11 | 2017-08-17 | Sima Patent Ve Lisanslama Hizmetleri Ltd. Şti | Crystalline form of tiotropium bromide anhydrate |
| PT115583B (pt) * | 2019-06-17 | 2022-05-02 | Hovione Farm S A | Processo contínuo para a preparação de medicamentos anticolinérgicos |
Family Cites Families (10)
| 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 |
| DE50103666D1 (de) * | 2000-10-12 | 2004-10-21 | Boehringer Ingelheim Pharma | Kristallines monohydrat von tiotropiumbromid, verfahren zu dessen herstellung und dessen verwendung zur herstellung eines arzneimittels |
| DE10064816A1 (de) * | 2000-12-22 | 2002-06-27 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung eines Anticholinergikums |
| PL208137B1 (pl) * | 2001-06-22 | 2011-03-31 | Boehringer Ingelheim Pharma | Bezwodny krystaliczny bromek tiotropium, sposób jego wytwarzania i zastosowanie krystalicznego monohydratu bromku tiotropium do wytwarzania krystalicznego bezwodnego bromku 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 |
| DE10212264A1 (de) * | 2002-03-20 | 2003-10-02 | Boehringer Ingelheim Pharma | Kristallines Mikronisat, Verfahren zu dessen Herstellung und dessen Verwendung zur Herstellung eines Arzneimittels |
| DE10214264A1 (de) * | 2002-03-28 | 2003-10-16 | Boehringer Ingelheim Pharma | HFA-Suspensionsformulierungen eines Anhydrats |
| US7244415B2 (en) * | 2002-03-28 | 2007-07-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | HFA suspension formulations of an anhydrate |
| EP1575588A1 (en) * | 2002-12-16 | 2005-09-21 | Boehringer Ingelheim Pharma GmbH & Co.KG | Tiotropium containing hfc solution formulations |
| CN100509809C (zh) * | 2003-11-03 | 2009-07-08 | 贝林格尔·英格海姆国际有限公司 | 具有抗胆碱能作用的新颖无水晶体 |
-
2006
- 2006-04-21 EP EP06763053A patent/EP1879888A2/en not_active Withdrawn
- 2006-04-21 RU RU2007144531/04A patent/RU2007144531A/ru not_active Application Discontinuation
- 2006-04-21 MX MX2007013691A patent/MX2007013691A/es not_active Application Discontinuation
- 2006-04-21 KR KR1020077028066A patent/KR20080007656A/ko not_active Withdrawn
- 2006-04-21 CN CNA2006800139215A patent/CN101203513A/zh active Pending
- 2006-04-21 BR BRPI0611091-6A patent/BRPI0611091A2/pt not_active IP Right Cessation
- 2006-04-21 JP JP2008509409A patent/JP2008540367A/ja active Pending
- 2006-04-21 WO PCT/EP2006/061765 patent/WO2006117300A2/en not_active Ceased
- 2006-04-21 CA CA002606552A patent/CA2606552A1/en not_active Abandoned
- 2006-04-21 AU AU2006243239A patent/AU2006243239A1/en not_active Abandoned
- 2006-05-01 US US11/381,079 patent/US20060246009A1/en not_active Abandoned
-
2007
- 2007-09-25 ZA ZA200708175A patent/ZA200708175B/xx unknown
- 2007-10-31 IL IL187054A patent/IL187054A0/en unknown
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