DE102005061624A1 - Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen - Google Patents

Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen Download PDF

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Publication number
DE102005061624A1
DE102005061624A1 DE102005061624A DE102005061624A DE102005061624A1 DE 102005061624 A1 DE102005061624 A1 DE 102005061624A1 DE 102005061624 A DE102005061624 A DE 102005061624A DE 102005061624 A DE102005061624 A DE 102005061624A DE 102005061624 A1 DE102005061624 A1 DE 102005061624A1
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DE
Germany
Prior art keywords
group
substituted
alkyl
formula
alkoxycarbonyl
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
DE102005061624A
Other languages
German (de)
English (en)
Inventor
Georg Dr. Zerban
Arndt Dr. Hausherr
Rainer Hamm
Gunter Koch
Kerstin Schlarb
Heinz-Peter Schmitt
Björn WEYELL
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
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 Boehringer Ingelheim Pharma GmbH and Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH and Co KG
Priority to DE102005061624A priority Critical patent/DE102005061624A1/de
Priority to ES06830756T priority patent/ES2355045T3/es
Priority to AU2006326980A priority patent/AU2006326980B2/en
Priority to NZ569636A priority patent/NZ569636A/en
Priority to KR1020087017836A priority patent/KR101411961B1/ko
Priority to PT06830756T priority patent/PT1968949E/pt
Priority to TW095148016A priority patent/TWI411608B/zh
Priority to DK06830756.0T priority patent/DK1968949T3/da
Priority to PCT/EP2006/070034 priority patent/WO2007071743A1/en
Priority to ARP060105633A priority patent/AR058571A1/es
Priority to BRPI0620150-4A priority patent/BRPI0620150A2/pt
Priority to SI200630879T priority patent/SI1968949T1/sl
Priority to AT06830756T priority patent/ATE485279T1/de
Priority to PL06830756T priority patent/PL1968949T3/pl
Priority to JP2008546456A priority patent/JP5317702B2/ja
Priority to DE602006017743T priority patent/DE602006017743D1/de
Priority to CN2006800488945A priority patent/CN101346355B/zh
Priority to CA2632310A priority patent/CA2632310C/en
Priority to RU2008129637/04A priority patent/RU2425827C2/ru
Priority to EP06830756A priority patent/EP1968949B1/en
Priority to US11/614,299 priority patent/US7880016B2/en
Publication of DE102005061624A1 publication Critical patent/DE102005061624A1/de
Priority to ZA200804198A priority patent/ZA200804198B/xx
Priority to IL192242A priority patent/IL192242A/en
Priority to CY20111100047T priority patent/CY1111113T1/el
Withdrawn legal-status Critical Current

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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
DE102005061624A 2005-12-21 2005-12-21 Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen Withdrawn DE102005061624A1 (de)

Priority Applications (24)

Application Number Priority Date Filing Date Title
DE102005061624A DE102005061624A1 (de) 2005-12-21 2005-12-21 Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen
SI200630879T SI1968949T1 (sl) 2005-12-21 2006-12-20 Izboljšani postopek za pripravo soli 4-(benzimidazolilmetilamino)-benzamidov
PL06830756T PL1968949T3 (pl) 2005-12-21 2006-12-20 Ulepszony sposób otrzymywania soli 4-(benzimidazolilometyloamino)-benzamidów
NZ569636A NZ569636A (en) 2005-12-21 2006-12-20 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
KR1020087017836A KR101411961B1 (ko) 2005-12-21 2006-12-20 4-(벤즈이미다졸릴메틸아미노)-벤즈아미드의 염을 제조하기위한 개선된 방법
PT06830756T PT1968949E (pt) 2005-12-21 2006-12-20 4-(benzimidazolilmetilamino)-benzamidinas
TW095148016A TWI411608B (zh) 2005-12-21 2006-12-20 製備４-（苯并咪唑基甲基胺基）-苯甲醯胺之塩類的改良方法
DK06830756.0T DK1968949T3 (da) 2005-12-21 2006-12-20 Forbedret fremgangsmåde til fremstilling af salte af 4-(benzimidazolylmethylamino)-benzamider
PCT/EP2006/070034 WO2007071743A1 (en) 2005-12-21 2006-12-20 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
ARP060105633A AR058571A1 (es) 2005-12-21 2006-12-20 Procedimiento mejorado para la preparacion de sales de 4-(bencimidazolilmetilamino)-benzamidinas
AU2006326980A AU2006326980B2 (en) 2005-12-21 2006-12-20 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
ES06830756T ES2355045T3 (es) 2005-12-21 2006-12-20 Procedimiento mejorado para la preparación de las sales de 4-(bencimidazolilmetilamino)-benzamidas.
AT06830756T ATE485279T1 (de) 2005-12-21 2006-12-20 Verbessertes verfahren zur herstellung der salze von 4-(benzimidazolylmethylamin)-benzamiden
DE602006017743T DE602006017743D1 (de) 2005-12-21 2006-12-20 Verbessertes verfahren zur herstellung der salze von 4-(benzimidazolylmethylamin)-benzamiden
JP2008546456A JP5317702B2 (ja) 2005-12-21 2006-12-20 ４−（ベンゾイミダゾリルメチルアミノ）−ベンゾアミドの塩の改良された製造方法
BRPI0620150-4A BRPI0620150A2 (pt) 2005-12-21 2006-12-20 processo melhorado da preparação dos sais de 4-(benzimidazolil metilamina)-benzamidas
CN2006800488945A CN101346355B (zh) 2005-12-21 2006-12-20 制备4-（苯并咪唑基甲基氨基）-苯甲脒的盐的改良方法
CA2632310A CA2632310C (en) 2005-12-21 2006-12-20 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
RU2008129637/04A RU2425827C2 (ru) 2005-12-21 2006-12-20 Улучшенный способ получения солей 4-(бензимидазолилметиламино)-бензамидов
EP06830756A EP1968949B1 (en) 2005-12-21 2006-12-20 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
US11/614,299 US7880016B2 (en) 2005-12-21 2006-12-21 Process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
ZA200804198A ZA200804198B (en) 2005-12-21 2008-05-15 Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
IL192242A IL192242A (en) 2005-12-21 2008-06-17 Improved process for the preparation of salts of 4- (benzimidazolylmethylamino) -benzamides
CY20111100047T CY1111113T1 (el) 2005-12-21 2011-01-14 Βελτιωμενη διεργασια για την παρασκευη των αλατων των 4-(βενζιμιδαζολυλομεθυλαμινο)-βενζαμιδων

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005061624A DE102005061624A1 (de) 2005-12-21 2005-12-21 Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen

Publications (1)

Publication Number Publication Date
DE102005061624A1 true DE102005061624A1 (de) 2007-06-28

Family

ID=37950582

Family Applications (2)

Application Number Title Priority Date Filing Date
DE102005061624A Withdrawn DE102005061624A1 (de) 2005-12-21 2005-12-21 Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen
DE602006017743T Active DE602006017743D1 (de) 2005-12-21 2006-12-20 Verbessertes verfahren zur herstellung der salze von 4-(benzimidazolylmethylamin)-benzamiden

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE602006017743T Active DE602006017743D1 (de) 2005-12-21 2006-12-20 Verbessertes verfahren zur herstellung der salze von 4-(benzimidazolylmethylamin)-benzamiden

Country Status (23)

Country Link
US (1) US7880016B2 (https=)
EP (1) EP1968949B1 (https=)
JP (1) JP5317702B2 (https=)
KR (1) KR101411961B1 (https=)
CN (1) CN101346355B (https=)
AR (1) AR058571A1 (https=)
AT (1) ATE485279T1 (https=)
AU (1) AU2006326980B2 (https=)
BR (1) BRPI0620150A2 (https=)
CA (1) CA2632310C (https=)
CY (1) CY1111113T1 (https=)
DE (2) DE102005061624A1 (https=)
DK (1) DK1968949T3 (https=)
ES (1) ES2355045T3 (https=)
IL (1) IL192242A (https=)
NZ (1) NZ569636A (https=)
PL (1) PL1968949T3 (https=)
PT (1) PT1968949E (https=)
RU (1) RU2425827C2 (https=)
SI (1) SI1968949T1 (https=)
TW (1) TWI411608B (https=)
WO (1) WO2007071743A1 (https=)
ZA (1) ZA200804198B (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011110478A1 (en) * 2010-03-08 2011-09-15 Ratiopharm Gmbh Dabigatran etexilate-containing pharmaceutical composition

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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
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
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
US8173906B2 (en) * 2007-02-07 2012-05-08 Raytheon Company Environmental protection coating system and method
US7767589B2 (en) * 2007-02-07 2010-08-03 Raytheon Company Passivation layer for a circuit device and method of manufacture
RU2010143901A (ru) * 2008-03-28 2012-05-10 Бёрингер Ингельхайм Интернациональ Гмбх (De) Способ получения композиций дабигатрана для перорального введения
WO2009153214A1 (en) * 2008-06-16 2009-12-23 Boehringer Ingelheim International Gmbh Process for the manufacture of an intermediate in the synthesis of dabigatran
NZ588488A (en) * 2008-06-16 2012-08-31 Boehringer Ingelheim Int Method for producing an intermediate product of dabigatran etexilate
BRPI0915942A2 (pt) * 2008-07-14 2019-04-09 Boehringer Ingelheim International Gmbh método para produção de compostos medicinais contendo dabigatrana
JP2013510072A (ja) 2008-11-11 2013-03-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 従来のワルファリン治療に対して安全性プロフィールが改善されたダビガトランエテキシレートまたはその塩を使用して血栓症を治療または予防するための方法
US8399678B2 (en) 2009-11-18 2013-03-19 Boehringer Ingelheim International Gmbh Process for the manufacture of dabigatran etexilate
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
EP2834224B1 (en) 2012-04-02 2018-06-06 MSN Laboratories Limited Process for the preparation of benzimidazole derivatives and salts thereof
EP2890692A1 (en) 2012-08-31 2015-07-08 Ranbaxy Laboratories Limited Process for the preparation of crystalline form i of methanesulfonate salt of dabigatran etexilate
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
CN103275065A (zh) * 2013-05-30 2013-09-04 上海同昌生物医药科技有限公司 一种新的生产达比加群酯的方法
EP2835370A1 (en) 2013-08-08 2015-02-11 Medichem, S.A. New crystals of dabigatran etexilate mesylate
JP6403865B2 (ja) 2014-07-03 2018-10-10 シャンハイ インスティテュート オブ ファーマシューティカル インダストリー ダビガトランエテキシラート中間体の製造方法及び中間体化合物
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
CN104987323B (zh) * 2015-07-10 2017-08-22 浙江美诺华药物化学有限公司 一种达比加群酯的制备方法

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Publication number Priority date Publication date Assignee Title
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Also Published As

Publication number Publication date
ES2355045T3 (es) 2011-03-22
AU2006326980A1 (en) 2007-06-28
TWI411608B (zh) 2013-10-11
DK1968949T3 (da) 2011-01-24
BRPI0620150A2 (pt) 2011-11-01
IL192242A (en) 2012-02-29
ZA200804198B (en) 2009-04-29
SI1968949T1 (sl) 2011-02-28
AR058571A1 (es) 2008-02-13
IL192242A0 (en) 2008-12-29
EP1968949B1 (en) 2010-10-20
CY1111113T1 (el) 2015-06-11
CA2632310A1 (en) 2007-06-28
CN101346355A (zh) 2009-01-14
WO2007071743A1 (en) 2007-06-28
AU2006326980B2 (en) 2012-07-05
PL1968949T3 (pl) 2011-04-29
US20070185173A1 (en) 2007-08-09
ATE485279T1 (de) 2010-11-15
CN101346355B (zh) 2012-09-05
CA2632310C (en) 2014-02-11
KR101411961B1 (ko) 2014-06-27
US7880016B2 (en) 2011-02-01
RU2008129637A (ru) 2010-01-27
PT1968949E (pt) 2010-12-22
JP2009520766A (ja) 2009-05-28
NZ569636A (en) 2010-04-30
RU2425827C2 (ru) 2011-08-10
DE602006017743D1 (de) 2010-12-02
JP5317702B2 (ja) 2013-10-16
TW200740791A (en) 2007-11-01
KR20080081179A (ko) 2008-09-08
EP1968949A1 (en) 2008-09-17

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R119 Application deemed withdrawn, or ip right lapsed, due to non-payment of renewal fee

Effective date: 20120703