BRPI0407672A - processos para preparar imatinib e um sal de adição ácida deste, sais de adição ácida de imatinib, composição farmaceuticamente aceitável deste, imatinib e uso deste - Google Patents

processos para preparar imatinib e um sal de adição ácida deste, sais de adição ácida de imatinib, composição farmaceuticamente aceitável deste, imatinib e uso deste

Info

Publication number
BRPI0407672A
BRPI0407672A BRPI0407672-9A BRPI0407672A BRPI0407672A BR PI0407672 A BRPI0407672 A BR PI0407672A BR PI0407672 A BRPI0407672 A BR PI0407672A BR PI0407672 A BRPI0407672 A BR PI0407672A
Authority
BR
Brazil
Prior art keywords
imatinib
acid addition
addition salt
preparing
pharmaceutically acceptable
Prior art date
Application number
BRPI0407672-9A
Other languages
English (en)
Inventor
Rajendra Narayanrao Kankan
Dharmaraj Ramachandra Rao
Original Assignee
Cipla Ltd
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 Cipla Ltd filed Critical Cipla Ltd
Publication of BRPI0407672A publication Critical patent/BRPI0407672A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

"PROCESSOS PARA PREPARAR IMATINIB E UM SAL DE ADIçãO áCIDA DESTE, SAIS DE ADIçãO áCIDA DE IMATINIB, COMPOSIçãO FARMACEUTICAMENTE ACEITáVEL DESTE, IMATINIB E USO DESTE". A presente invenção refere-se a um processo para preparar imatinib, quer como base livre, quer como sal de adição ácida, o qual processo compreende reagir N-(2-metil-5aminofenil-4-(3-piridil)-2-pirimidina amina da fórmula (II) com haleto de 4-(4-metil-piperazino metil)benzoíla de fórmula (III) na presença de um solvente orgânico inerte, de maneira a produzir um sal de hidrohaleto de imatinib de fórmula (I) onde n representa 1, 2 ou 3 e Hal representa bromo, cloro, flúoro ou iodo, quer na forma anidra, quer na forma hidratada que pode, conforme desejado, opcionalmente ser adicionalmente convertido quer na base livre, quer em um sal de adição ácida adicional. A presente invenção também se refere ao imatinib preparado de acordo com o processo acima.
BRPI0407672-9A 2003-02-18 2004-01-08 processos para preparar imatinib e um sal de adição ácida deste, sais de adição ácida de imatinib, composição farmaceuticamente aceitável deste, imatinib e uso deste BRPI0407672A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0303730A GB2398565A (en) 2003-02-18 2003-02-18 Imatinib preparation and salts
PCT/GB2004/000018 WO2004074502A2 (en) 2003-02-18 2004-01-08 A process of preparing imatinib

Publications (1)

Publication Number Publication Date
BRPI0407672A true BRPI0407672A (pt) 2006-03-01

Family

ID=9953245

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0407672-9A BRPI0407672A (pt) 2003-02-18 2004-01-08 processos para preparar imatinib e um sal de adição ácida deste, sais de adição ácida de imatinib, composição farmaceuticamente aceitável deste, imatinib e uso deste

Country Status (12)

Country Link
US (1) US7638627B2 (pt)
EP (1) EP1599462B1 (pt)
JP (1) JP5064024B2 (pt)
KR (1) KR101086845B1 (pt)
AU (1) AU2004213616B2 (pt)
BR (1) BRPI0407672A (pt)
CA (1) CA2516370C (pt)
GB (1) GB2398565A (pt)
NZ (1) NZ542040A (pt)
PL (1) PL378128A1 (pt)
RU (1) RU2415849C2 (pt)
WO (1) WO2004074502A2 (pt)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0202873D0 (en) * 2002-02-07 2002-03-27 Novartis Ag Organic compounds
ES2338557T3 (es) * 2003-06-13 2010-05-10 Novartis Ag Derivados de la 2-aminopirimidina utilizados como inhibidores de la raf cinasa.
AR047530A1 (es) 2004-02-04 2006-01-25 Novartis Ag Formas de sal de 4-(4-metilpiperazin-1-ilmetil)-n-(4-metil-3-(4-piridin-3-il)pirimidin-2-ilamino)fenil)-benzamida
PL1720853T3 (pl) 2004-02-11 2016-06-30 Natco Pharma Ltd Nowa odmiana polimorficzna metanosulfonianu imatynibu i sposób jej otrzymywania
WO2006024863A1 (en) * 2004-09-02 2006-03-09 Cipla Limited Stable crystal form of imatinib mesylate and process for the preparation thereof
US20080015205A1 (en) * 2004-09-27 2008-01-17 Wedge Stephen R Cancer Combination Therapy Comprising Azd2171 and Imatinib
WO2006054314A1 (en) * 2004-11-17 2006-05-26 Natco Pharma Limited Polymorphic forms of imatinib mesylate
US7507821B2 (en) 2004-12-30 2009-03-24 Chemagis Ltd. Process for preparing Imatinib
GT200600316A (es) * 2005-07-20 2007-04-02 Sales de 4-metilo-n-(3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo)-3-(4-piridina-3-ilo-pirimidina-2-iloamino)- benzamida.
US7439358B2 (en) * 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
CN102861338A (zh) * 2006-04-05 2013-01-09 诺瓦提斯公司 用于治疗癌症、包含bcr-abl/c-kit/pdgf-r tk抑制剂的组合
US8067421B2 (en) 2006-04-27 2011-11-29 Sicor Inc. Polymorphic forms of imatinib mesylate and processes for preparation of novel crystalline forms as well as amorphous and form α
EP2311821A1 (en) * 2006-04-27 2011-04-20 Sicor, Inc. Polymorphic form of Imatinib mesylate and processes for its preparation
US7977348B2 (en) 2006-04-27 2011-07-12 Sicor Inc. Polymorphic forms of imatinib mesylate and processes for preparation of novel crystalline forms as well as amorphous and form α
US20060223816A1 (en) * 2006-05-08 2006-10-05 Chemagis Ltd. Imatinib mesylate alpha form and production process therefor
WO2008024826A2 (en) * 2006-08-23 2008-02-28 Board Of Regents, The University Of Texas System Radiohalothymidines and methods of their synthesis and use in pet imaging of cancers
US20090324718A1 (en) * 2006-09-01 2009-12-31 Ilan Zalit Imatinib compositions
US20080103305A1 (en) * 2006-10-26 2008-05-01 Macdonald Peter Process for the preparation of imatinib
EP2009008A1 (en) 2006-10-26 2008-12-31 Sicor, Inc. Imatinib base, and imatinib mesylate and processes for preparation thereof
RU2329260C1 (ru) * 2007-02-20 2008-07-20 Юрий Иосифович Копырин Способ получения 2-анилинопиримидинов или их солей (варианты)
US7550591B2 (en) * 2007-05-02 2009-06-23 Chemagis Ltd. Imatinib production process
PL2305263T3 (pl) * 2007-06-07 2012-12-31 Novartis Ag Stabilizowane amorficzne formy mesylanu imatinibu
KR101041203B1 (ko) * 2007-09-25 2011-06-13 테바 파마슈티컬 인더스트리즈 리미티드 안정한 이매티닙 조성물
WO2009060463A1 (en) * 2007-11-05 2009-05-14 Natco Pharma Limited An environmentally friendly process for the preparation of imatinib base
EP2062885A1 (en) * 2007-11-21 2009-05-27 Eczacibasi-Zentiva Kimyasal Ürünler Sanayi ve Ticaret A.S. Acid addition salts of imatinib and formulations comprising the same
WO2009080366A1 (en) * 2007-12-22 2009-07-02 Synthon B.V. A process of making imatinib
WO2010009402A2 (en) * 2008-07-17 2010-01-21 Teva Pharmaceutical Industries Ltd. Nilotinib intermediates and preparation thereof
US20100330130A1 (en) 2009-05-22 2010-12-30 Actavis Group Ptc Ehf Substantially pure imatinib or a pharmaceutically acceptable salt thereof
WO2011070588A1 (en) 2009-12-10 2011-06-16 Arch Pharmalabs Limited Process for the preparation of imatinib and salts thereof
WO2011095835A1 (en) 2010-02-02 2011-08-11 Actavis Group Ptc Ehf Highly pure imatinib or a pharmaceutically acceptable salt thereof
CA2792472A1 (en) * 2010-03-15 2011-09-22 Natco Pharma Limited Process for the preparation of highly pure crystalline imatinib base
WO2011130918A1 (zh) * 2010-04-23 2011-10-27 上海百灵医药科技有限公司 一种伊马替尼的合成方法
CN102250063B (zh) * 2010-05-19 2014-10-22 江苏豪森药业股份有限公司 甲磺酸伊马替尼的晶型及其制备方法
EA024088B1 (ru) 2010-06-18 2016-08-31 КРКА, д.д., НОВО МЕСТО α-ФОРМА МЕЗИЛАТА ИМАТИНИБА, СПОСОБЫ ЕЕ ПОЛУЧЕНИЯ И СОДЕРЖАЩАЯ ЕЁ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ
TR201007005A2 (tr) * 2010-08-23 2011-09-21 Mustafa Nevzat İlaç Sanayi̇i̇ A.Ş. İmatinib baz üretim yöntemi
CN101899035B (zh) * 2010-09-03 2012-09-05 天津市炜杰科技有限公司 一种高纯度伊马替尼的制备方法
US8546566B2 (en) 2010-10-12 2013-10-01 Boehringer Ingelheim International Gmbh Process for manufacturing dihydropteridinones and intermediates thereof
IN2010CH03577A (pt) * 2010-11-26 2012-07-20 Hetero Research Foundation
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
TR201010618A2 (tr) 2010-12-20 2012-07-23 Bi̇lgi̇ç Mahmut İmatinib içeren bir oral dozaj formu ve bu oral dozaj formunun üretimi
CN102070605B (zh) * 2011-01-30 2013-03-13 南京卡文迪许生物工程技术有限公司 甲磺酸伊马替尼多晶型物和药用组合物
KR101286780B1 (ko) * 2011-02-01 2013-07-17 에스티팜 주식회사 비카보네이트 염 및 이를 이용한 이마티니브 또는 이의 염의 제조방법
CN102382100B (zh) * 2011-03-09 2014-04-16 上海昕盛医药科技有限公司 伊马替尼的制备方法
WO2012131711A1 (en) * 2011-03-31 2012-10-04 Ind-Swift Laboratories Limited Improved process for preparation of imatinib and its mesylate salt
US9370535B2 (en) 2011-05-17 2016-06-21 Boehringer Ingelheim International Gmbh Method for treatment of advanced solid tumors
CN102260242B (zh) * 2011-05-27 2014-08-06 南京卡文迪许生物工程技术有限公司 甲磺酸伊马替尼多晶型物及其药用组合物
CN102816145B (zh) * 2011-06-11 2014-09-03 南京卡文迪许生物工程技术有限公司 甲磺酸伊马替尼多晶型物及其药用组合物
WO2013035102A1 (en) 2011-09-05 2013-03-14 Natco Pharma Limited Processes for the preparation of imatinib base and intermediates thereof
WO2013067157A1 (en) * 2011-11-01 2013-05-10 Modgene, Llc Compositions and methods for reduction of amyloid-beta load
CN102659762A (zh) * 2012-05-24 2012-09-12 石药集团中奇制药技术（石家庄）有限公司 一种甲磺酸伊马替尼晶型及其制备方法
WO2014041551A1 (en) 2012-09-14 2014-03-20 Natco Pharma Limited Formulation comprising imatinib as oral solution
EP2749557A1 (en) 2012-12-31 2014-07-02 Deva Holding Anonim Sirketi Process for preparation of alpha polymorph of imatinib mesylate from IPA and THF solvate forms of imatinib mesylate
CN104163812A (zh) * 2013-05-17 2014-11-26 浙江九洲药业股份有限公司 一种无定型的伊马替尼甲磺酸盐及其制备方法
WO2015011236A1 (en) 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
CA3172586A1 (en) 2013-07-31 2015-02-05 Avalyn Pharma Inc. Aerosol imatininb compounds and uses thereof
CN103910711A (zh) * 2014-03-24 2014-07-09 福建天泉药业股份有限公司 一种伊马替尼游离碱晶型及其制备方法
CN104974133B (zh) * 2014-04-09 2018-04-27 石药集团中奇制药技术（石家庄）有限公司 一种甲磺酸伊马替尼晶型及其制备方法
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
WO2017129624A1 (en) 2016-01-25 2017-08-03 Krka, D.D., Novo Mesto Fast dispersible pharmaceutical composition comprising tyrosine-kinase inhibitor
US11229650B2 (en) 2019-05-16 2022-01-25 Aerovate Therapeutics, Inc. Inhalable imatinib formulations, manufacture, and uses thereof
US11464776B2 (en) 2019-05-16 2022-10-11 Aerovate Therapeutics, Inc. Inhalable imatinib formulations, manufacture, and uses thereof
SG10201909596RA (en) * 2019-10-14 2021-05-28 Esco Aster Pte Ltd Synthesis of Tyrosine Kinase Inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
TW225528B (pt) 1992-04-03 1994-06-21 Ciba Geigy Ag
CO4940418A1 (es) * 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso

Also Published As

Publication number Publication date
EP1599462B1 (en) 2013-03-27
PL378128A1 (pl) 2006-03-06
JP2006518360A (ja) 2006-08-10
GB2398565A (en) 2004-08-25
US7638627B2 (en) 2009-12-29
AU2004213616B2 (en) 2011-05-26
RU2415849C2 (ru) 2011-04-10
AU2004213616A2 (en) 2004-09-02
RU2005129100A (ru) 2006-06-10
KR20050108358A (ko) 2005-11-16
US20060173182A1 (en) 2006-08-03
JP5064024B2 (ja) 2012-10-31
CA2516370C (en) 2012-08-21
WO2004074502A3 (en) 2004-10-28
AU2004213616A1 (en) 2004-09-02
WO2004074502A2 (en) 2004-09-02
NZ542040A (en) 2009-02-28
KR101086845B1 (ko) 2011-11-24
GB0303730D0 (en) 2003-03-26
CA2516370A1 (en) 2004-09-02
EP1599462A2 (en) 2005-11-30

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B25G Requested change of headquarter approved

Owner name: CIPLA LIMITED (IN)

B08F Application fees: application dismissed [chapter 8.6 patent gazette]

Free format text: REFERENTE A 13A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]