WO2005003104A3 - Monohydrate de lamotrigine - Google Patents

Monohydrate de lamotrigine Download PDF

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Publication number
WO2005003104A3
WO2005003104A3 PCT/IN2004/000186 IN2004000186W WO2005003104A3 WO 2005003104 A3 WO2005003104 A3 WO 2005003104A3 IN 2004000186 W IN2004000186 W IN 2004000186W WO 2005003104 A3 WO2005003104 A3 WO 2005003104A3
Authority
WO
WIPO (PCT)
Prior art keywords
lamotrigine
monohydrate
anhydrous
dichlorophenyl
preparation
Prior art date
Application number
PCT/IN2004/000186
Other languages
English (en)
Other versions
WO2005003104A2 (fr
Inventor
Charugundla Kishore
Bokka Ravisankar
Sulur G Manjunatha
Ashok Krishna Kulkarni
Original Assignee
Jubilant Organosys Ltd
Charugundla Kishore
Bokka Ravisankar
Sulur G Manjunatha
Ashok Krishna Kulkarni
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 Jubilant Organosys Ltd, Charugundla Kishore, Bokka Ravisankar, Sulur G Manjunatha, Ashok Krishna Kulkarni filed Critical Jubilant Organosys Ltd
Publication of WO2005003104A2 publication Critical patent/WO2005003104A2/fr
Publication of WO2005003104A3 publication Critical patent/WO2005003104A3/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne du monohydrate de (3,5-diamino-6-(2,3-dichlorophényl)-1,2,4-triazine) lamotrigine (Ia) et de la lamotrigine anhydre, ainsi qu'un procédé de préparation associé. L'invention concerne également un procédé amélioré de production de lamotrigine (I). Ce procédé consiste à mettre en réaction du 2,3-dichlorobenzoyl cyanure (II) et du bicarbonate d'aminoguanidine dans un acide minéral aqueux, facultativement avec un solvant organique miscible dans l'eau, à une température comprise entre 30 et 80 °C, de sorte à produire du 2-(2,3-dichlorophényl)-2-(guanidinylamino)acétonitrile (base de Schiff). La base de Schiff est ensuite cyclisée dans un alcool aqueux, de sorte à produire de la lamotrigine pure de qualité pharmaceutiquement acceptable qui, pendant un séchage à vide à une température comprise entre 45 et 50 °C, produit du monohydrate de lamotrigine et/ou, pendant un autre séchage à une température comprise entre 100 et 110 °C, produit de la lamotrigine anhydre. Le monohydrate de lamotrigine ou la lamotrigine anhydre ainsi produit(e) peut ensuite être associé(e) à un excipient pharmaceutiquement acceptable pour être administré(e) à un patient.
PCT/IN2004/000186 2003-07-03 2004-06-28 Monohydrate de lamotrigine WO2005003104A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0315608.0 2003-07-03
GB0315608A GB2395483A (en) 2003-07-03 2003-07-03 Crystalline lamotrigine and its monohydrate

Publications (2)

Publication Number Publication Date
WO2005003104A2 WO2005003104A2 (fr) 2005-01-13
WO2005003104A3 true WO2005003104A3 (fr) 2005-09-22

Family

ID=27741536

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2004/000186 WO2005003104A2 (fr) 2003-07-03 2004-06-28 Monohydrate de lamotrigine

Country Status (2)

Country Link
GB (1) GB2395483A (fr)
WO (1) WO2005003104A2 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102005027149A1 (de) * 2005-06-11 2006-12-14 Lanxess Deutschland Gmbh Verfahren zur Herstellung von substituierten Benzoylcyaniden
US20120142919A1 (en) * 2006-08-02 2012-06-07 Medichem, S.A. Method for synthesizing lamotrigine
CN103570637A (zh) * 2013-09-13 2014-02-12 盐城凯利药业有限公司 一种拉莫三嗪的制备方法
CN106083753B (zh) * 2016-06-07 2019-04-02 浙江奇彩环境科技股份有限公司 一种改进的拉莫三嗪合成工艺
CN113214177B (zh) * 2021-04-16 2022-05-03 上海奥科达生物医药科技有限公司 一种拉莫三嗪水合物的晶体形式、其制备方法及包含其的组合物
CN115068422B (zh) * 2022-08-19 2022-11-29 上海奥科达生物医药科技有限公司 一种拉莫三嗪湿混悬剂及其制备方法和应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0247892A1 (fr) * 1986-05-30 1987-12-02 The Wellcome Foundation Limited Sels de triazine
EP0963980A2 (fr) * 1998-06-10 1999-12-15 The Wellcome Foundation Limited Dérivé de 1,2,4-triazine, la preparation et l'utilisation comme marqueur de référence pour verifié la pureté et la stabilité de "lamotrigine"
WO2000035888A1 (fr) * 1998-12-14 2000-06-22 Sharad Kumar Vyas Procede et appareil ameliore de preparation de 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine
EP1127873A2 (fr) * 2000-02-25 2001-08-29 Chemagis Ltd. Procédé pour la préparation de benzoylcyanide amidinohydrazones
WO2002068398A1 (fr) * 2001-02-27 2002-09-06 Teva Pharmaceutical Industries Ltd. Nouvelles formes cristallines de lamotrigine et leurs procedes de preparation
WO2003078407A1 (fr) * 2001-12-24 2003-09-25 Apotex Pharmachem Inc. Nouveau procede efficace pour preparer de la lamotrigine et des 3,5-diamino-6-substitutees-1,2,4-triazines associees
WO2004083191A1 (fr) * 2003-03-17 2004-09-30 Hetero Drugs Limited Nouvelles formes cristallines de lamotrigine

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS234018B2 (en) * 1979-06-01 1985-03-14 Wellcome Found Method of 3,5-diammino-6-1,2,4-triazine derivatives making

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0247892A1 (fr) * 1986-05-30 1987-12-02 The Wellcome Foundation Limited Sels de triazine
EP0963980A2 (fr) * 1998-06-10 1999-12-15 The Wellcome Foundation Limited Dérivé de 1,2,4-triazine, la preparation et l'utilisation comme marqueur de référence pour verifié la pureté et la stabilité de "lamotrigine"
WO2000035888A1 (fr) * 1998-12-14 2000-06-22 Sharad Kumar Vyas Procede et appareil ameliore de preparation de 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine
EP1127873A2 (fr) * 2000-02-25 2001-08-29 Chemagis Ltd. Procédé pour la préparation de benzoylcyanide amidinohydrazones
WO2002068398A1 (fr) * 2001-02-27 2002-09-06 Teva Pharmaceutical Industries Ltd. Nouvelles formes cristallines de lamotrigine et leurs procedes de preparation
WO2003078407A1 (fr) * 2001-12-24 2003-09-25 Apotex Pharmachem Inc. Nouveau procede efficace pour preparer de la lamotrigine et des 3,5-diamino-6-substitutees-1,2,4-triazines associees
WO2004083191A1 (fr) * 2003-03-17 2004-09-30 Hetero Drugs Limited Nouvelles formes cristallines de lamotrigine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KUBICKI, M. ET AL: "Hydrogen bonding patterns in 3,5-diamino-6-aryl triazines", JOURNAL OF MOLECULAR STRUCTURE , 570(1-3), 53-60 CODEN: JMOSB4; ISSN: 0022-2860, 2001, XP002308632 *

Also Published As

Publication number Publication date
GB0315608D0 (en) 2003-08-13
GB2395483A (en) 2004-05-26
WO2005003104A2 (fr) 2005-01-13

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