EP2872500A4 - Verbessertes verfahren zur herstellung von dabigatranetexilatmesylat und zwischenprodukten davon - Google Patents
Verbessertes verfahren zur herstellung von dabigatranetexilatmesylat und zwischenprodukten davonInfo
- Publication number
- EP2872500A4 EP2872500A4 EP13816563.4A EP13816563A EP2872500A4 EP 2872500 A4 EP2872500 A4 EP 2872500A4 EP 13816563 A EP13816563 A EP 13816563A EP 2872500 A4 EP2872500 A4 EP 2872500A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- etexilate
- dabigatran
- mesylate
- intermediates
- preparation
- 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.)
- Ceased
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
- C07D401/02—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
-
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2838CH2012 | 2012-07-12 | ||
| IN4298CH2012 | 2012-10-15 | ||
| PCT/IN2013/000413 WO2014009966A2 (en) | 2012-07-12 | 2013-07-05 | An improved process for the preparation of dabigatran etexilate mesylate and its intermediates thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EP2872500A2 EP2872500A2 (de) | 2015-05-20 |
| EP2872500A4 true EP2872500A4 (de) | 2016-03-30 |
Family
ID=49916616
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP13816563.4A Ceased EP2872500A4 (de) | 2012-07-12 | 2013-07-05 | Verbessertes verfahren zur herstellung von dabigatranetexilatmesylat und zwischenprodukten davon |
Country Status (2)
| Country | Link |
|---|---|
| EP (1) | EP2872500A4 (de) |
| WO (1) | WO2014009966A2 (de) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104892574A (zh) * | 2014-03-04 | 2015-09-09 | 浙江海正药业股份有限公司 | 达比加群酯甲磺酸盐的晶型及其制备方法和用途 |
| WO2015137680A1 (ko) * | 2014-03-10 | 2015-09-17 | 동아에스티 주식회사 | 뇌졸중 및 전신색전증 치료 또는 예방용 약학적 조성물 |
| CN104974137A (zh) * | 2014-04-04 | 2015-10-14 | 江苏天士力帝益药业有限公司 | 达比加群酯甲磺酸盐新晶型及其制备方法 |
| CN103951654B (zh) * | 2014-05-13 | 2016-08-24 | 南京生命能科技开发有限公司 | 甲磺酸达比加群酯的晶体v及其制备方法 |
| CN103965164A (zh) * | 2014-05-13 | 2014-08-06 | 南京生命能科技开发有限公司 | 甲磺酸达比加群酯的晶体ⅵ及其制备方法 |
| CN105348263B (zh) * | 2015-12-15 | 2018-03-23 | 乐普药业股份有限公司 | 一种达比加群酯中间体的制备方法 |
| CN108727334B (zh) * | 2018-07-12 | 2020-10-30 | 江西国药有限责任公司 | 一种甲磺酸达比加群酯的生产工艺 |
| WO2022006007A1 (en) * | 2020-06-29 | 2022-01-06 | The General Hospital Corporation | Methods for imaging bacterial infections |
| CN116041724B (zh) * | 2023-02-23 | 2024-03-01 | 天津工业大学 | 一种多孔手性金属-有机框架材料及其制备方法和应用 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1861596A (zh) * | 2005-12-16 | 2006-11-15 | 复旦大学 | 一种合成非手性,非肽类的抗凝血酶抑制剂的方法 |
| WO2007071742A1 (en) * | 2005-12-21 | 2007-06-28 | Boehringer Ingelheim International Gmbh | Improved process for the preparation of 4-(benzimidazolylmethylamino)-benzamides and the salts thereof |
| WO2012004396A2 (en) * | 2010-07-09 | 2012-01-12 | Esteve Química, S.A. | Process of preparing a thrombin specific inhibitor |
| WO2012027543A1 (en) * | 2010-08-25 | 2012-03-01 | Teva Pharmaceuticals Usa, Inc. | Solid state forms of dabigatran etexilate, dabigatran etexilate mesylate and processes for preparation thereof |
| EP2522662A1 (de) * | 2011-05-11 | 2012-11-14 | Medichem, S.A. | Dabigatranetexilat und zugehörige Substanzen, Verfahren und Zusammensetzungen sowie Verwendung der Substanzen als Referenzstandards und Marker |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2013
- 2013-07-05 EP EP13816563.4A patent/EP2872500A4/de not_active Ceased
- 2013-07-05 WO PCT/IN2013/000413 patent/WO2014009966A2/en not_active Ceased
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1861596A (zh) * | 2005-12-16 | 2006-11-15 | 复旦大学 | 一种合成非手性,非肽类的抗凝血酶抑制剂的方法 |
| WO2007071742A1 (en) * | 2005-12-21 | 2007-06-28 | Boehringer Ingelheim International Gmbh | Improved process for the preparation of 4-(benzimidazolylmethylamino)-benzamides and the salts thereof |
| WO2012004396A2 (en) * | 2010-07-09 | 2012-01-12 | Esteve Química, S.A. | Process of preparing a thrombin specific inhibitor |
| WO2012027543A1 (en) * | 2010-08-25 | 2012-03-01 | Teva Pharmaceuticals Usa, Inc. | Solid state forms of dabigatran etexilate, dabigatran etexilate mesylate and processes for preparation thereof |
| EP2522662A1 (de) * | 2011-05-11 | 2012-11-14 | Medichem, S.A. | Dabigatranetexilat und zugehörige Substanzen, Verfahren und Zusammensetzungen sowie Verwendung der Substanzen als Referenzstandards und Marker |
Non-Patent Citations (3)
| Title |
|---|
| CHENG ET AL: "Synthesis of dabigatran etexilate mesylate", ZHONGGUO XIN YAO ZAZHI - CHINESE NEW DRUGS JOU, GAI-KAN BIANJIBU, BEIJING, CN, vol. 21, no. 1, 1 January 2012 (2012-01-01), pages 88 - 91, XP008175968, ISSN: 1003-3734 * |
| HAUEL N H ET AL: "STRUCTURE-BASED DESIGN OF NOVEL POTENT NONPEPTIDE THROMBIN INHIBITORS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 45, no. 9, 1 January 2002 (2002-01-01), pages 1757 - 1766, XP001098844, ISSN: 0022-2623, DOI: 10.1021/JM0109513 * |
| ZHU ET AL: "Improved synthesis of dabigatran etexilate", ZHONGGUO YAOWU HUAXUE ZAZHI - CHINESE JOURNAL OF MEDICINAL CHEMIS, GAI-KAI BIANJIBU, SHENYANG, CN, vol. 22, no. 3, 1 June 2012 (2012-06-01), pages 204 - 208, XP008175937, ISSN: 1005-0108 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2014009966A3 (en) | 2014-03-06 |
| WO2014009966A2 (en) | 2014-01-16 |
| EP2872500A2 (de) | 2015-05-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
| 17P | Request for examination filed |
Effective date: 20150116 |
|
| AK | Designated contracting states |
Kind code of ref document: A2 Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR |
|
| AX | Request for extension of the european patent |
Extension state: BA ME |
|
| DAX | Request for extension of the european patent (deleted) | ||
| A4 | Supplementary search report drawn up and despatched |
Effective date: 20160225 |
|
| RIC1 | Information provided on ipc code assigned before grant |
Ipc: C07D 401/12 20060101AFI20160219BHEP Ipc: A61K 31/4439 20060101ALI20160219BHEP Ipc: A61P 7/02 20060101ALI20160219BHEP |
|
| 17Q | First examination report despatched |
Effective date: 20161209 |
|
| REG | Reference to a national code |
Ref country code: DE Ref legal event code: R003 |
|
| 18R | Application refused |
Effective date: 20180702 |