ATE540926T1 - Verbessertes verfahren zur herstellung von montelukastsäure natriumsalz in amorpher form - Google Patents
Verbessertes verfahren zur herstellung von montelukastsäure natriumsalz in amorpher formInfo
- Publication number
- ATE540926T1 ATE540926T1 AT03817134T AT03817134T ATE540926T1 AT E540926 T1 ATE540926 T1 AT E540926T1 AT 03817134 T AT03817134 T AT 03817134T AT 03817134 T AT03817134 T AT 03817134T AT E540926 T1 ATE540926 T1 AT E540926T1
- Authority
- AT
- Austria
- Prior art keywords
- acid
- sodium salt
- crude
- montelucastic
- producing
- Prior art date
Links
- 239000002253 acid Substances 0.000 title abstract 6
- 238000004519 manufacturing process Methods 0.000 title 1
- NOJNFULGOQGBKB-UHFFFAOYSA-M sodium;3-[3-tert-butylsulfanyl-1-[[4-(6-ethoxypyridin-3-yl)phenyl]methyl]-5-[(5-methylpyridin-2-yl)methoxy]indol-2-yl]-2,2-dimethylpropanoate Chemical compound [Na+].C1=NC(OCC)=CC=C1C(C=C1)=CC=C1CN1C2=CC=C(OCC=3N=CC(C)=CC=3)C=C2C(SC(C)(C)C)=C1CC(C)(C)C([O-])=O NOJNFULGOQGBKB-UHFFFAOYSA-M 0.000 title 1
- XBPCUCUWBYBCDP-UHFFFAOYSA-N Dicyclohexylamine Chemical class C1CCCCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 abstract 4
- UCHDWCPVSPXUMX-TZIWLTJVSA-N Montelukast Chemical compound CC(C)(O)C1=CC=CC=C1CC[C@H](C=1C=C(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)C=CC=1)SCC1(CC(O)=O)CC1 UCHDWCPVSPXUMX-TZIWLTJVSA-N 0.000 abstract 4
- 229960005127 montelukast Drugs 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 2
- 239000002904 solvent Substances 0.000 abstract 2
- VFAXPOVKNPTBTM-UHFFFAOYSA-N 2-[1-(sulfanylmethyl)cyclopropyl]acetic acid Chemical compound OC(=O)CC1(CS)CC1 VFAXPOVKNPTBTM-UHFFFAOYSA-N 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- FKNQFGJONOIPTF-UHFFFAOYSA-N Sodium cation Chemical compound [Na+] FKNQFGJONOIPTF-UHFFFAOYSA-N 0.000 abstract 1
- -1 alkyl lithium Chemical compound 0.000 abstract 1
- 230000008878 coupling Effects 0.000 abstract 1
- 238000010168 coupling process Methods 0.000 abstract 1
- 238000005859 coupling reaction Methods 0.000 abstract 1
- SMBQBQBNOXIFSF-UHFFFAOYSA-N dilithium Chemical compound [Li][Li] SMBQBQBNOXIFSF-UHFFFAOYSA-N 0.000 abstract 1
- 238000001704 evaporation Methods 0.000 abstract 1
- 229910052744 lithium Inorganic materials 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 239000003586 protic polar solvent Substances 0.000 abstract 1
- 229910001415 sodium ion Inorganic materials 0.000 abstract 1
- 159000000000 sodium salts Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/18—Halogen atoms or nitro radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Quinoline Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/IN2003/000214 WO2004108679A1 (en) | 2003-06-06 | 2003-06-06 | An improved method for the preparation of montelukast acid and sodium salt thereof in amorphous form |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE540926T1 true ATE540926T1 (de) | 2012-01-15 |
Family
ID=33495847
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03817134T ATE540926T1 (de) | 2003-06-06 | 2003-06-06 | Verbessertes verfahren zur herstellung von montelukastsäure natriumsalz in amorpher form |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8450491B2 (de) |
| EP (1) | EP1631550B1 (de) |
| AT (1) | ATE540926T1 (de) |
| AU (1) | AU2003253247A1 (de) |
| CA (1) | CA2528228C (de) |
| PT (1) | PT1631550E (de) |
| WO (1) | WO2004108679A1 (de) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050107612A1 (en) * | 2002-12-30 | 2005-05-19 | Dr. Reddy's Laboratories Limited | Process for preparation of montelukast and its salts |
| AU2004283832B2 (en) * | 2003-10-10 | 2011-04-07 | Synthon B.V. | Solid-state montelukast |
| EP1709001A2 (de) * | 2004-01-28 | 2006-10-11 | Pliva Istrazivanje i Razvoj d.o.o. | Feste formen von montelukastsäure |
| CA2554572A1 (en) * | 2004-01-30 | 2005-08-18 | Teva Pharmaceutical Industries Ltd. | Montelukast free acid polymorphs |
| EP1760077A1 (de) * | 2004-01-30 | 2007-03-07 | Teva Pharmaceutical Industries Ltd. | Polymorphe Formen vonMontelukast freie Säure |
| WO2005075427A2 (en) * | 2004-01-30 | 2005-08-18 | Teva Pharmaceutical Industries Ltd. | Montelukast sodium polymorphs |
| BRPI0506610A (pt) | 2004-02-03 | 2007-05-02 | Chemagis Ltd | montelucaste sódico amorfo, processo de preparação de montelucaste sódico amorfo, composição farmacêutica, método de tratamento utilizando a administração de montelucaste sódico amorfo, co-precipitado amorfo de montelucaste sódico e processo de preparação de co-precipitado amorfo de montelucaste sódico |
| EP1646612B1 (de) * | 2004-04-21 | 2009-07-01 | Teva Pharmaceutical Industries Ltd | Verfahren zur herstellung von montelukast-natrium |
| WO2006058545A1 (en) * | 2004-11-30 | 2006-06-08 | Medichem, S.A. | New process for the preparation of a leukotriene antagonist |
| CN101213177A (zh) * | 2005-07-05 | 2008-07-02 | 特瓦制药工业有限公司 | 孟鲁司特的纯化 |
| WO2007004237A2 (en) * | 2005-07-05 | 2007-01-11 | Matrix Laboratories Ltd | A process for the preparation of montelukast |
| EP1948612A2 (de) * | 2005-11-16 | 2008-07-30 | Teva Pharmaceutical Industries Ltd | Verfahren zum trocknen von montelukast-natrium durch azeotrope entfernung des lösungsmittels |
| US8178680B2 (en) | 2005-12-13 | 2012-05-15 | Msn Laboratories Limited | Process for the preparation of Montelukast and its pharmaceutically acceptable salts |
| EP1968942A4 (de) * | 2005-12-23 | 2010-06-02 | Glade Organics Private Ltd | Verbessertes verfahren zur herstellung von montelukast-natrium |
| PT1976522E (pt) | 2005-12-30 | 2013-09-09 | Krka Tovarna Zdravil D D Novo Mesto | Composição farmacêutica contendo montelucaste |
| CN101432267A (zh) | 2006-03-17 | 2009-05-13 | 斯索恩有限公司 | 孟鲁司特金刚烷胺盐 |
| EP2004608B1 (de) * | 2006-04-12 | 2011-09-14 | Glade Organics Private Limited | Verbessertes verfahren zur herstellung von montelukast-natrium |
| EP1886998A1 (de) | 2006-08-09 | 2008-02-13 | Esteve Quimica, S.A. | Verfahren zur Reinigung von Montelukast und dessen Aminesalzen |
| WO2008023044A1 (en) * | 2006-08-23 | 2008-02-28 | Sandoz Ag | Process for the preparation of montelukast free acid and its amine salts |
| US8115004B2 (en) | 2006-11-20 | 2012-02-14 | Msn Laboratories Limited | Process for pure montelukast sodium through pure intermediates as well as amine salts |
| CZ302518B6 (cs) * | 2007-07-09 | 2011-06-29 | Zentiva, A. S. | Zpusob izolace a cištení montelukastu |
| WO2009144742A2 (en) * | 2008-05-26 | 2009-12-03 | Aptuit Laurus Pvt Limited | An improved process for preparing montelukast and salts thereof |
| WO2010148209A2 (en) * | 2009-06-19 | 2010-12-23 | Dr. Reddy's Laboratories Ltd. | Preparation of montelukast |
| EP2287154A1 (de) | 2009-07-14 | 2011-02-23 | KRKA, D.D., Novo Mesto | Effiziente Synthese zur Herstellung von Montelukast |
| WO2011121091A1 (en) | 2010-03-31 | 2011-10-06 | Krka, D.D., Novo Mesto | Efficient synthesis for the preparation of montelukast and novel crystalline form of intermediates therein |
| WO2014012954A1 (en) | 2012-07-18 | 2014-01-23 | Takeda Gmbh | Treatment of partly controlled or uncontrolled severe asthma |
| WO2014118796A1 (en) | 2013-01-31 | 2014-08-07 | Melody Healthcare Pvt. Ltd. | An in-situ process for the preparation of highly pure montelukast sodium |
| JP2015007000A (ja) * | 2013-06-24 | 2015-01-15 | 株式会社トクヤマ | モンテルカスト遊離酸の結晶を製造する方法 |
| JP6173864B2 (ja) * | 2013-10-01 | 2017-08-02 | 株式会社トクヤマ | モンテルカストナトリウムのアモルファスを製造する方法 |
| CN103570619B (zh) * | 2013-11-08 | 2015-12-09 | 南京靖龙药物研发有限公司 | 一种孟鲁司特钠衍生物的制备方法 |
| EP3096760A1 (de) | 2014-01-22 | 2016-11-30 | Takeda GmbH | Behandlung von teilweise kontrolliertem oder unkontrolliertem schweren asthma mit einem pde4-inhibitor (und in kombination mit einem leukotrien-modifikator) |
| CN105585524B (zh) * | 2016-02-29 | 2018-03-02 | 山东新时代药业有限公司 | 一种由孟鲁司特酸制备孟鲁司特钠的方法 |
| CN105924392B (zh) * | 2016-02-29 | 2018-03-02 | 山东新时代药业有限公司 | 一种孟鲁司特钠制备方法 |
| CN107162969A (zh) * | 2017-07-05 | 2017-09-15 | 成都亿知科技有限公司 | 孟鲁司特钠晶体及其制备方法和药物组合物 |
| ES2876292T3 (es) * | 2017-07-24 | 2021-11-12 | Interquim Sa | Procedimiento de preparación y purificación del antagonista de LFA-1 lifitegrast |
| US10966943B2 (en) | 2018-09-06 | 2021-04-06 | Innopharmascreen Inc. | Methods and compositions for treatment of asthma or parkinson's disease |
| IT201900008340A1 (it) | 2019-06-07 | 2020-12-07 | Genetic S P A | Sali di montelukast e loro composizioni farmaceutiche |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2053209C (en) | 1990-10-12 | 1998-12-08 | Michel L. Belley | Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists |
| US5565473A (en) * | 1990-10-12 | 1996-10-15 | Merck Frosst Canada, Inc. | Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists |
| TW448160B (en) * | 1993-12-28 | 2001-08-01 | Merck & Co Inc | Novel dicyclohexylamine salt and process for the preparation of leukotriene antagonists |
| AU2003209043A1 (en) * | 2002-02-07 | 2003-09-02 | Dr. Reddy's Laboratories Ltd. | Novel anhydrous amorphous forms of montelukast sodium salt |
-
2003
- 2003-06-06 CA CA2528228A patent/CA2528228C/en not_active Expired - Lifetime
- 2003-06-06 PT PT03817134T patent/PT1631550E/pt unknown
- 2003-06-06 AU AU2003253247A patent/AU2003253247A1/en not_active Abandoned
- 2003-06-06 AT AT03817134T patent/ATE540926T1/de active
- 2003-06-06 WO PCT/IN2003/000214 patent/WO2004108679A1/en not_active Ceased
- 2003-06-06 US US10/576,971 patent/US8450491B2/en not_active Expired - Fee Related
- 2003-06-06 EP EP03817134A patent/EP1631550B1/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CA2528228C (en) | 2011-09-20 |
| EP1631550B1 (de) | 2012-01-11 |
| WO2004108679A1 (en) | 2004-12-16 |
| EP1631550A1 (de) | 2006-03-08 |
| AU2003253247A1 (en) | 2005-01-04 |
| US8450491B2 (en) | 2013-05-28 |
| PT1631550E (pt) | 2012-04-19 |
| CA2528228A1 (en) | 2004-12-16 |
| US20070082925A1 (en) | 2007-04-12 |
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