CN101346355B - 制备4-（苯并咪唑基甲基氨基）-苯甲脒的盐的改良方法 - Google Patents
制备4-（苯并咪唑基甲基氨基）-苯甲脒的盐的改良方法 Download PDFInfo
- Publication number
- CN101346355B CN101346355B CN2006800488945A CN200680048894A CN101346355B CN 101346355 B CN101346355 B CN 101346355B CN 2006800488945 A CN2006800488945 A CN 2006800488945A CN 200680048894 A CN200680048894 A CN 200680048894A CN 101346355 B CN101346355 B CN 101346355B
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- CN
- China
- Prior art keywords
- hydrogenation
- water
- acid
- reaction
- formula
- 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.)
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Links
- 0 *C(c(cc1)cc2c1[n](*)c(CNc(cc1)ccc1C(N)=*)n2)=O Chemical compound *C(c(cc1)cc2c1[n](*)c(CNc(cc1)ccc1C(N)=*)n2)=O 0.000 description 1
- QQIIBPABBFMLAK-UHFFFAOYSA-N CCOC(CCN(C(c(cc1N)ccc1NC)O)c1ncccc1)=O Chemical compound CCOC(CCN(C(c(cc1N)ccc1NC)O)c1ncccc1)=O QQIIBPABBFMLAK-UHFFFAOYSA-N 0.000 description 1
- FYSFQBXGCDIVMA-UHFFFAOYSA-N CCOC(CCN(C(c(cc1[N+]([O-])=O)ccc1NC)=O)c1ncccc1)=O Chemical compound CCOC(CCN(C(c(cc1[N+]([O-])=O)ccc1NC)=O)c1ncccc1)=O FYSFQBXGCDIVMA-UHFFFAOYSA-N 0.000 description 1
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
Landscapes
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005061624.0 | 2005-12-21 | ||
| DE102005061624A DE102005061624A1 (de) | 2005-12-21 | 2005-12-21 | Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen |
| PCT/EP2006/070034 WO2007071743A1 (en) | 2005-12-21 | 2006-12-20 | Improved process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101346355A CN101346355A (zh) | 2009-01-14 |
| CN101346355B true CN101346355B (zh) | 2012-09-05 |
Family
ID=37950582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2006800488945A Active 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 |
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=) |
Families Citing this family (25)
| 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 |
| 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 |
| JP2013521318A (ja) * | 2010-03-08 | 2013-06-10 | ラティオファルム ゲー・エム・ベー・ハー | ダビガトランエテキシラートを含有する医薬組成物 |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1248251A (zh) * | 1997-02-18 | 2000-03-22 | 贝林格尔英格海姆法玛公司 | 二取代双环杂环,其制备法及作为药物的用途 |
| CN1308614A (zh) * | 1998-07-04 | 2001-08-15 | 贝林格尔英格海姆法玛公司 | 苯并咪唑,其制法及其作为药物组合物的用途 |
| WO2006000353A1 (de) * | 2004-06-25 | 2006-01-05 | Boehringer Ingelheim International Gmbh | Verfahren zur herstellung von 4-(benzimidazolylmethylamino)- benzamidinen |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6087380A (en) * | 1949-11-24 | 2000-07-11 | Boehringer Ingelheim Pharma Kg | Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions |
| DE19743435A1 (de) * | 1997-10-01 | 1999-04-08 | Merck Patent Gmbh | Benzamidinderivate |
| US6248770B1 (en) * | 1998-07-09 | 2001-06-19 | Boehringer Ingelheim Pharma Kg | Benzimidazoles having antithrombotic activity |
| DE19962329A1 (de) * | 1999-12-23 | 2001-06-28 | Boehringer Ingelheim Pharma | Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel |
| US6451832B2 (en) * | 1999-12-23 | 2002-09-17 | Boehringer Ingelheim Pharma Kg | Benzimidazoles with antithrombotic activity |
| KR101005716B1 (ko) * | 2002-03-07 | 2011-01-05 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | ３－［（２－｛［４－（헥실옥시카보닐아미노－이미노-메틸）－페닐아미노］－메틸｝－１－메틸－１ｈ－벤즈이미다졸－５－카보닐）－피리딘－２－일－아미노］ 프로피온산 에틸에스테르의 경구 투여 형태 |
| NL1026498C2 (nl) * | 2004-06-24 | 2005-12-28 | Free Lift B V | Hellinglifteenheid met blokkeerinrichting en blokkeerinrichting bestemd voor hellinglifteenheid. |
| 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 |
-
2005
- 2005-12-21 DE DE102005061624A patent/DE102005061624A1/de not_active Withdrawn
-
2006
- 2006-12-20 AU AU2006326980A patent/AU2006326980B2/en active Active
- 2006-12-20 RU RU2008129637/04A patent/RU2425827C2/ru active
- 2006-12-20 AT AT06830756T patent/ATE485279T1/de active
- 2006-12-20 BR BRPI0620150-4A patent/BRPI0620150A2/pt not_active Application Discontinuation
- 2006-12-20 DK DK06830756.0T patent/DK1968949T3/da active
- 2006-12-20 PL PL06830756T patent/PL1968949T3/pl unknown
- 2006-12-20 EP EP06830756A patent/EP1968949B1/en active Active
- 2006-12-20 TW TW095148016A patent/TWI411608B/zh not_active IP Right Cessation
- 2006-12-20 CN CN2006800488945A patent/CN101346355B/zh active Active
- 2006-12-20 KR KR1020087017836A patent/KR101411961B1/ko active Active
- 2006-12-20 NZ NZ569636A patent/NZ569636A/en unknown
- 2006-12-20 DE DE602006017743T patent/DE602006017743D1/de active Active
- 2006-12-20 ES ES06830756T patent/ES2355045T3/es active Active
- 2006-12-20 PT PT06830756T patent/PT1968949E/pt unknown
- 2006-12-20 JP JP2008546456A patent/JP5317702B2/ja active Active
- 2006-12-20 SI SI200630879T patent/SI1968949T1/sl unknown
- 2006-12-20 CA CA2632310A patent/CA2632310C/en active Active
- 2006-12-20 WO PCT/EP2006/070034 patent/WO2007071743A1/en not_active Ceased
- 2006-12-20 AR ARP060105633A patent/AR058571A1/es not_active Application Discontinuation
- 2006-12-21 US US11/614,299 patent/US7880016B2/en active Active
-
2008
- 2008-05-15 ZA ZA200804198A patent/ZA200804198B/xx unknown
- 2008-06-17 IL IL192242A patent/IL192242A/en active IP Right Grant
-
2011
- 2011-01-14 CY CY20111100047T patent/CY1111113T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1248251A (zh) * | 1997-02-18 | 2000-03-22 | 贝林格尔英格海姆法玛公司 | 二取代双环杂环,其制备法及作为药物的用途 |
| CN1308614A (zh) * | 1998-07-04 | 2001-08-15 | 贝林格尔英格海姆法玛公司 | 苯并咪唑,其制法及其作为药物组合物的用途 |
| WO2006000353A1 (de) * | 2004-06-25 | 2006-01-05 | Boehringer Ingelheim International Gmbh | Verfahren zur herstellung von 4-(benzimidazolylmethylamino)- benzamidinen |
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 |
| DE102005061624A1 (de) | 2007-06-28 |
| 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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C56 | Change in the name or address of the patentee | ||
| CP03 | Change of name, title or address |
Address after: In Germany Patentee after: Boehringer Ingelheim Int Address before: In Germany Patentee before: Boehringer Ingelheim International GmbH |