RU2401264C2 - Способ получения 4-(бензимидазолилметиламино)бензамидинов - Google Patents

Способ получения 4-(бензимидазолилметиламино)бензамидинов Download PDF

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Publication number
RU2401264C2
RU2401264C2 RU2007102631/04A RU2007102631A RU2401264C2 RU 2401264 C2 RU2401264 C2 RU 2401264C2 RU 2007102631/04 A RU2007102631/04 A RU 2007102631/04A RU 2007102631 A RU2007102631 A RU 2007102631A RU 2401264 C2 RU2401264 C2 RU 2401264C2
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RU
Russia
Prior art keywords
formula
group
oxadiazol
compound
acetic acid
Prior art date
Application number
RU2007102631/04A
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English (en)
Russian (ru)
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RU2007102631A (ru
Inventor
Георг ЦЕРБАН (DE)
Георг ЦЕРБАН
Арндт ХАУСХЕРР (DE)
Арндт ХАУСХЕРР
Керстин ШЛАРБ (DE)
Керстин ШЛАРБ
Хайнц-Петер ШМИТТ (DE)
Хайнц-Петер ШМИТТ
Бьёрн ВЕЙЕЛЛЬ (DE)
Бьёрн ВЕЙЕЛЛЬ
Гунтер КОХ (DE)
Гунтер КОХ
Райнер ХАММ (DE)
Райнер Хамм
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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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=RU2401264(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of RU2007102631A publication Critical patent/RU2007102631A/ru
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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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (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)
RU2007102631/04A 2004-06-25 2005-06-18 Способ получения 4-(бензимидазолилметиламино)бензамидинов RU2401264C2 (ru)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
RU2007102631A RU2007102631A (ru) 2008-07-27
RU2401264C2 true RU2401264C2 (ru) 2010-10-10

Family

ID=34925482

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2007102631/04A RU2401264C2 (ru) 2004-06-25 2005-06-18 Способ получения 4-(бензимидазолилметиламино)бензамидинов

Country Status (20)

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

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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
DE102005061624A1 (de) 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen
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
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
US20110129538A1 (en) * 2008-03-28 2011-06-02 Boehringer Ingelheim International Gmbh Process for preparing orally administered dabigatran formulations
NZ588488A (en) * 2008-06-16 2012-08-31 Boehringer Ingelheim Int Method for producing an intermediate product of dabigatran etexilate
TWI436994B (zh) 2008-07-14 2014-05-11 Boehringer Ingelheim Int 製備含有達比加群（ｄａｂｉｇａｔｒａｎ）之藥物組合物的新穎方法
CZ2008669A3 (cs) * 2008-10-24 2010-05-05 Zentiva, A. S. Zpusob prípravy dabigatranu a jeho meziprodukty
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
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
US8399678B2 (en) * 2009-11-18 2013-03-19 Boehringer Ingelheim International Gmbh Process for the manufacture of dabigatran etexilate
WO2012004397A1 (en) 2010-07-09 2012-01-12 Esteve Química, S.A. Intermediates and process for preparing a thrombin specific inhibitor
MX2013000295A (es) 2010-07-09 2013-05-28 Esteve Quimica Sa Procedimiento de preparacion de un inhibidor especifico de la trombina.
HUE026408T2 (en) 2010-09-27 2016-06-28 Ratiopharm Gmbh Dabigatran etexylate bis-mesylate salt, solid forms and process for their preparation
WO2012077136A2 (en) * 2010-12-06 2012-06-14 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts
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
HUP1100244A2 (hu) 2011-05-11 2012-11-28 Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag Gyógyszeripari intermedierek és eljárás elõállításukra
WO2013111163A2 (en) 2012-01-20 2013-08-01 Cadila Healthcare Limited Process for the preparation of dabigatran etexilate mesylate and polymorphs of intermediates thereof
EP2834224B1 (en) 2012-04-02 2018-06-06 MSN Laboratories 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
US20150246899A1 (en) * 2012-09-28 2015-09-03 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
US10077251B2 (en) 2012-10-29 2018-09-18 Biophore India Pharmaceuticals Pvt. Ltd. Process for the synthesis of Dabigatran Etexilate and its intermediates
US9533971B2 (en) 2012-10-29 2017-01-03 Biophore India Pharmaceuticals Pvt. Ltd Process for the synthesis of dabigatran 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
EP3848998A4 (en) 2018-10-29 2021-11-24 LG Chem, Ltd. SEPARATOR FOR ELECTROCHEMICAL DEVICE AND METHOD FOR MANUFACTURING IT
EP3771465A1 (en) 2019-08-01 2021-02-03 Zaklady Farmaceutyczne Polpharma SA Pharmaceutical composition comprising dabigatran etexilate
CN116178252A (zh) * 2022-07-26 2023-05-30 浙江海翔药业股份有限公司 一种甲磺酸达比加群酯的原料杂质及其制备方法和用途
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037075A1 (de) * 1997-02-18 1998-08-27 Boehringer Ingelheim Pharma Kg Disubstituierte bicyclische heterocyclen, ihre herstellung und ihre verwendung als arzneimittel
WO2000001704A2 (de) * 1998-07-04 2000-01-13 Boehringer Ingelheim Pharma Kg Benzimidazole, deren herstellung und deren verwendung als arzneimittel
DE19962329A1 (de) * 1999-12-23 2001-06-28 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
RU2001135715A (ru) * 1999-05-29 2003-08-20 Байер Акциенгезельшафт Замещенные амиды фенилциклогексанкарбоновой кислоты

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US6414008B1 (en) * 1997-04-29 2002-07-02 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, 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
DE19924818A1 (de) * 1999-05-29 2000-11-30 Bayer Ag Substituierte Phenylcyclohexancarbonsäureamide
US6451832B2 (en) * 1999-12-23 2002-09-17 Boehringer Ingelheim Pharma Kg Benzimidazoles with antithrombotic activity
EP1574516A1 (en) * 2004-03-05 2005-09-14 Sanofi-Aventis Antithrombotic compound

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
WO1998037075A1 (de) * 1997-02-18 1998-08-27 Boehringer Ingelheim Pharma Kg Disubstituierte bicyclische heterocyclen, ihre herstellung und ihre verwendung als arzneimittel
WO2000001704A2 (de) * 1998-07-04 2000-01-13 Boehringer Ingelheim Pharma Kg Benzimidazole, deren herstellung und deren verwendung als arzneimittel
RU2001135715A (ru) * 1999-05-29 2003-08-20 Байер Акциенгезельшафт Замещенные амиды фенилциклогексанкарбоновой кислоты
DE19962329A1 (de) * 1999-12-23 2001-06-28 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel

Also Published As

Publication number Publication date
TW200613287A (en) 2006-05-01
US20070149589A1 (en) 2007-06-28
JP2008503519A (ja) 2008-02-07
NZ552809A (en) 2009-06-26
HUE027198T2 (en) 2016-08-29
CN1972919A (zh) 2007-05-30
BRPI0511318A (pt) 2007-12-04
US7459566B2 (en) 2008-12-02
KR101298507B1 (ko) 2013-08-22
EP1609784A1 (de) 2005-12-28
EP1761510A1 (de) 2007-03-14
US20060004064A1 (en) 2006-01-05
EP1761510B1 (de) 2015-05-13
CN1972919B (zh) 2012-06-27
RU2007102631A (ru) 2008-07-27
IL180247A0 (en) 2007-07-04
AU2005256424A1 (en) 2006-01-05
MXPA06015210A (es) 2007-03-15
BRPI0511318B8 (pt) 2021-05-25
IL180247A (en) 2011-11-30
AU2005256424B2 (en) 2011-12-08
IL211491A0 (en) 2011-05-31
BRPI0511318B1 (pt) 2018-02-14
AR049410A1 (es) 2006-07-26
KR20070029817A (ko) 2007-03-14
PL1761510T3 (pl) 2015-10-30
JP5073486B2 (ja) 2012-11-14
US7202368B2 (en) 2007-04-10
ZA200609918B (en) 2008-10-29
WO2006000353A1 (de) 2006-01-05
DK1761510T3 (en) 2015-08-17
CA2570499C (en) 2013-08-06
IL211491A (en) 2012-05-31
TWI364417B (en) 2012-05-21
CA2570499A1 (en) 2006-01-05
ES2543982T3 (es) 2015-08-26

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