BRPI0511318A - processo para a produção de 4-(benzimidazolilmetilamino)-benzamidinas - Google Patents

processo para a produção de 4-(benzimidazolilmetilamino)-benzamidinas

Info

Publication number
BRPI0511318A
BRPI0511318A BRPI0511318-0A BRPI0511318A BRPI0511318A BR PI0511318 A BRPI0511318 A BR PI0511318A BR PI0511318 A BRPI0511318 A BR PI0511318A BR PI0511318 A BRPI0511318 A BR PI0511318A
Authority
BR
Brazil
Prior art keywords
production
benzimidazolylmethylamino
benzamidines
optionally substituted
optionally
Prior art date
Application number
BRPI0511318-0A
Other languages
English (en)
Inventor
Georg Zerban
Arndt Hausherr
Kerstin Schlarb
Heinz-Peter Schmitt
Bjoern Weyell
Gunter Koch
Rainer Hamm
Original Assignee
Boehringer Ingelheim Int
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34925482&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0511318(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of BRPI0511318A publication Critical patent/BRPI0511318A/pt
Publication of BRPI0511318B1 publication Critical patent/BRPI0511318B1/pt
Publication of BRPI0511318B8 publication Critical patent/BRPI0511318B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

PROCESSO PARA A PRODUçãO DE 4-(BENZIMIDAZOLILMETILAMINO)-ENZAMIDINAS. A presente invenção refere-se a um processo para a produção de uma 4-benzimidazol-2-ilmetilamino)-benzamidina eventualmente substituída, caracterizado pelo fato de se (a) condensar um diaminobenzeno eventualmente correspondentemente substituído com ácido 2-¢4-( 1 ,2,4-oxadiazol-5-on-3-il)-fenilamino!-acético, (b) hidrogenar o produto obtido desse modo e (c) carbonilar eventualmente o grupo amidino.
BRPI0511318A 2004-06-25 2005-06-18 processo para a produção de 4-(benzimidazol-2-ilmetilamino)-benzamidinas, bem como produtos intermediários BRPI0511318B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP04014917A EP1609784A1 (de) 2004-06-25 2004-06-25 Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen
EP04014917.1 2004-06-25
PCT/EP2005/006586 WO2006000353A1 (de) 2004-06-25 2005-06-18 Verfahren zur herstellung von 4-(benzimidazolylmethylamino)- benzamidinen

Publications (3)

Publication Number Publication Date
BRPI0511318A true BRPI0511318A (pt) 2007-12-04
BRPI0511318B1 BRPI0511318B1 (pt) 2018-02-14
BRPI0511318B8 BRPI0511318B8 (pt) 2021-05-25

Family

ID=34925482

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0511318A BRPI0511318B8 (pt) 2004-06-25 2005-06-18 processo para a produção de 4-(benzimidazol-2-ilmetilamino)-benzamidinas, bem como produtos intermediários

Country Status (20)

Country Link
US (2) US7202368B2 (pt)
EP (2) EP1609784A1 (pt)
JP (1) JP5073486B2 (pt)
KR (1) KR101298507B1 (pt)
CN (1) CN1972919B (pt)
AR (1) AR049410A1 (pt)
AU (1) AU2005256424B2 (pt)
BR (1) BRPI0511318B8 (pt)
CA (1) CA2570499C (pt)
DK (1) DK1761510T3 (pt)
ES (1) ES2543982T3 (pt)
HU (1) HUE027198T2 (pt)
IL (2) IL180247A (pt)
MX (1) MXPA06015210A (pt)
NZ (1) NZ552809A (pt)
PL (1) PL1761510T3 (pt)
RU (1) RU2401264C2 (pt)
TW (1) TWI364417B (pt)
WO (1) WO2006000353A1 (pt)
ZA (1) ZA200609918B (pt)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030181488A1 (en) * 2002-03-07 2003-09-25 Boehringer Ingelheim Pharma Gmbh & Co. Kg Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and the salts thereof
DE10339862A1 (de) * 2003-08-29 2005-03-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 3-[(2-{[4-(Hexyloxycarbonylamino-imino-methyl)- phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsäure-ethylester-Methansulfonat und dessen Verwendung als Arzneimittel
DE102005020002A1 (de) * 2005-04-27 2006-11-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Physiologisch verträgliche Salze von 3-[(2-{[4-(Hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsäure-ethylester
DE102005061623A1 (de) 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verbessertes Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen und deren Salzen
DE102005061624A1 (de) * 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen
US20100087488A1 (en) * 2006-10-10 2010-04-08 Boehringer Ingelheim International Gmgh Physiologically Acceptable Salts of 3-[(2--1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester
DE102006054005A1 (de) * 2006-11-16 2008-05-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Polymorphe von 3-[(2-{[4-(Hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsäure-ethylester
EP1956018A1 (de) * 2007-02-06 2008-08-13 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung eines Benzimidazolderivats
CZ305085B6 (cs) * 2008-03-14 2015-04-29 Zentiva, K.S. Způsob přípravy dabigatranu
CN101980697A (zh) * 2008-03-28 2011-02-23 贝林格尔.英格海姆国际有限公司 制备口服给药的达比加群制剂的方法
AU2009259440B2 (en) * 2008-06-16 2014-05-29 Boehringer Ingelheim International Gmbh Method for producing an intermediate product of dabigatran etexilate
NZ589746A (en) 2008-07-14 2012-10-26 Boehringer Ingelheim Int Method for manufacturing medicinal compounds containing dabigatran
CZ2008669A3 (cs) * 2008-10-24 2010-05-05 Zentiva, A. S. Zpusob prípravy dabigatranu a jeho meziprodukty
CN102050814B (zh) * 2009-11-06 2014-05-28 北京美倍他药物研究有限公司 达比加群的酯衍生物
CN102050815B (zh) * 2009-11-06 2014-04-02 北京美倍他药物研究有限公司 作为前药的达比加群的酯衍生物
US8399678B2 (en) * 2009-11-18 2013-03-19 Boehringer Ingelheim International Gmbh Process for the manufacture of dabigatran etexilate
MX2013000295A (es) 2010-07-09 2013-05-28 Esteve Quimica Sa Procedimiento de preparacion de un inhibidor especifico de la trombina.
JP2013531004A (ja) 2010-07-09 2013-08-01 エステヴェ キミカ， エス．エー． トロンビン特異的インヒビターの調製のための中間体及び方法
ES2550771T3 (es) 2010-09-27 2015-11-12 Ratiopharm Gmbh Sal de bismesilato etexilato de dabigatrán, formas en estado sólido y proceso para la preparación de las mismas
EP2649060B1 (en) * 2010-12-06 2017-04-05 MSN Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts
HUP1100244A2 (hu) 2011-05-11 2012-11-28 Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag Gyógyszeripari intermedierek és eljárás elõállításukra
EP2522662A1 (en) 2011-05-11 2012-11-14 Medichem, S.A. Dabigatran etexilate and related substances, processes and compositions, and use of the substances as reference standards and markers
WO2013111163A2 (en) 2012-01-20 2013-08-01 Cadila Healthcare Limited Process for the preparation of dabigatran etexilate mesylate and polymorphs of intermediates thereof
US9273030B2 (en) 2012-04-02 2016-03-01 Msn Laboratories Private Limited Process for the preparation of benzimidazole derivatives and salts thereof
WO2014020555A2 (en) * 2012-08-01 2014-02-06 Alembic Pharmaceuticals Limited An improved process for the preparation of dabigatran etexilate mesylate
CA2885994A1 (en) * 2012-09-28 2014-04-03 Ranbaxy Laboratories Limited Process for the preparation of dabigatran etexilate or pharmaceutically acceptable salt thereof
US9399616B2 (en) 2012-10-22 2016-07-26 Boehringer Ingelheim International Gmbh Process for the manufacture of 4-aminobenzoamidine dihydrochloride
US9533971B2 (en) 2012-10-29 2017-01-03 Biophore India Pharmaceuticals Pvt. Ltd Process for the synthesis of dabigatran and its intermediates
US10077251B2 (en) 2012-10-29 2018-09-18 Biophore India Pharmaceuticals Pvt. Ltd. Process for the synthesis of Dabigatran Etexilate and its intermediates
WO2014178017A1 (en) * 2013-04-30 2014-11-06 Ranbaxy Laboratories Limited Dabigatran etexilate impurity, process of its preparation, and its use as a reference standard
EP2835370A1 (en) 2013-08-08 2015-02-11 Medichem, S.A. New crystals of dabigatran etexilate mesylate
CN103626740B (zh) * 2013-12-05 2015-02-04 南京欧信医药技术有限公司 一种化合物的合成方法
CN103772358A (zh) * 2014-01-07 2014-05-07 万特制药(海南)有限公司 一种制备达比加群酯的合成方法
WO2015128875A2 (en) 2014-02-26 2015-09-03 Megafine Pharma (P) Ltd. A process for preparation of dabigatran etexilate mesylate and intermediates thereof
CN105461686A (zh) * 2014-08-25 2016-04-06 江苏豪森药业股份有限公司 制备高纯度甲磺酸达比加群酯晶型的方法
CN104910047B (zh) * 2015-05-11 2017-06-06 常州市阳光药业有限公司 达比加群酯中间体的制备方法
WO2020091396A1 (ko) 2018-10-29 2020-05-07 주식회사 엘지화학 전기화학소자용 분리막 및 이를 제조하는 방법
EP3771465A1 (en) 2019-08-01 2021-02-03 Zaklady Farmaceutyczne Polpharma SA Pharmaceutical composition comprising dabigatran etexilate
CN116354952A (zh) * 2023-01-06 2023-06-30 宿迁盛基医药科技有限公司 一种达比加群酯关键中间体的合成工艺

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19516483A1 (de) * 1995-05-05 1996-11-07 Merck Patent Gmbh Adhäsionsrezeptor-Antagonisten
PE121699A1 (es) * 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
US6414008B1 (en) * 1997-04-29 2002-07-02 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions
TWI248435B (en) * 1998-07-04 2006-02-01 Boehringer Ingelheim Pharma Benzimidazoles, the preparation thereof and their use as pharmaceutical compositions
US6248770B1 (en) * 1998-07-09 2001-06-19 Boehringer Ingelheim Pharma Kg Benzimidazoles having antithrombotic activity
US6451832B2 (en) * 1999-12-23 2002-09-17 Boehringer Ingelheim Pharma Kg Benzimidazoles with antithrombotic activity
DE19962329A1 (de) * 1999-12-23 2001-06-28 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
EP1574516A1 (en) * 2004-03-05 2005-09-14 Sanofi-Aventis Antithrombotic compound

Also Published As

Publication number Publication date
IL180247A (en) 2011-11-30
EP1761510A1 (de) 2007-03-14
CN1972919A (zh) 2007-05-30
US7202368B2 (en) 2007-04-10
NZ552809A (en) 2009-06-26
AR049410A1 (es) 2006-07-26
MXPA06015210A (es) 2007-03-15
EP1609784A1 (de) 2005-12-28
JP5073486B2 (ja) 2012-11-14
ZA200609918B (en) 2008-10-29
KR20070029817A (ko) 2007-03-14
CA2570499C (en) 2013-08-06
HUE027198T2 (en) 2016-08-29
DK1761510T3 (en) 2015-08-17
BRPI0511318B8 (pt) 2021-05-25
IL211491A (en) 2012-05-31
AU2005256424A1 (en) 2006-01-05
CA2570499A1 (en) 2006-01-05
PL1761510T3 (pl) 2015-10-30
JP2008503519A (ja) 2008-02-07
ES2543982T3 (es) 2015-08-26
TWI364417B (en) 2012-05-21
US7459566B2 (en) 2008-12-02
US20070149589A1 (en) 2007-06-28
AU2005256424B2 (en) 2011-12-08
RU2007102631A (ru) 2008-07-27
IL211491A0 (en) 2011-05-31
WO2006000353A1 (de) 2006-01-05
BRPI0511318B1 (pt) 2018-02-14
RU2401264C2 (ru) 2010-10-10
KR101298507B1 (ko) 2013-08-22
EP1761510B1 (de) 2015-05-13
IL180247A0 (en) 2007-07-04
CN1972919B (zh) 2012-06-27
TW200613287A (en) 2006-05-01
US20060004064A1 (en) 2006-01-05

Similar Documents

Publication Publication Date Title
BRPI0511318A (pt) processo para a produção de 4-(benzimidazolilmetilamino)-benzamidinas
ATE453670T1 (de) Acrylierte hyaluronsäure
TW200641169A (en) Method for the production of a radiation-emitting optical component and radiation-emitting optical component
BRPI0510777A (pt) indazóis substituìdos, composições que os contêm, processo de produção e utilização
BRPI0720991A8 (pt) Preparação da romidepsina
BRPI0507184A (pt) processo para preparar adiposinitrila por hidrocianação de 1,3-butadieno em um catalisador
BR0314847A (pt) Procedimento e dispositivo para a produção de biodiesel
GT200600087A (es) Producción de ferroníquel
DK2102337T3 (da) Microorganisme af slægten Corynebacterium med forhøjet L-lysinproduktionsevne samt fremgangsmåde til fremstilling af L-lysin under anvendelse af denne
EA200801401A1 (ru) Продуцирование фруктоолигосахаридов и снижение содержания сахарозы in situ
DK1866414T3 (da) Inhibitorer af ribonukleotidreduktase-underenhed 2 og anvendelser deraf.
BR112013022359A2 (pt) método para dobrar chapa metálica e produto da chapa metálica
ATE554126T1 (de) Härtbare zusammensetzung, die eine thiolverbindung enthält
BRPI0807669A2 (pt) Processo para produzir um produto de cumento tendo uma pureza de pelo menos 99,50 por cento
AR063972A1 (es) Plantas con rasgos mejorados relacionados con el rendimiento y un metodo para producirlas
BRPI0517465A (pt) processo para a produção de maltodextrinas e maltodextrinas
BRPI0912164A2 (pt) processo para a degradação de lignina.
BR112018014160A2 (pt) processo para marcação de componentes elétricos
BRPI0518389A2 (pt) mÉtodo melhorado para a produÇço de anidrido metacrÍlico
BRPI0515186A (pt) derivados de alquilideno-tetrahidronaftaleno, processo para a sua produção e seu uso como antiinflamatório
BRPI0607862A2 (pt) artigos produzidos por um processo
BRPI0418746A (pt) produto e processo de indústria de laticìnios
EP2324864A4 (en) COMPOSITE MATERIAL WITH A MATRIX OF HIGH MOLECULAR WEIGHT AND A COMPOUND OF LOW MOLECULAR WEIGHT AND METHOD FOR THE PRODUCTION THEREOF
BRPI0605332A (pt) borracha de nitrila hidrogenada com distribuição de peso molecular limitada, seu uso e processo para sua preparação
BR112014013518A2 (pt) produto de confeitaria na base de um gel de gelatina e método para a sua produção

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]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]
B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 18/06/2005 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF