JP2010505906A5 - - Google Patents
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- Publication number
- JP2010505906A5 JP2010505906A5 JP2009531826A JP2009531826A JP2010505906A5 JP 2010505906 A5 JP2010505906 A5 JP 2010505906A5 JP 2009531826 A JP2009531826 A JP 2009531826A JP 2009531826 A JP2009531826 A JP 2009531826A JP 2010505906 A5 JP2010505906 A5 JP 2010505906A5
- Authority
- JP
- Japan
- Prior art keywords
- forms
- methyl
- malate
- naphthalene
- propionate
- 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.)
- Pending
Links
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 4
- BJEPYKJPYRNKOW-UWTATZPHSA-N (R)-malic acid Chemical compound OC(=O)[C@H](O)CC(O)=O BJEPYKJPYRNKOW-UWTATZPHSA-N 0.000 claims 3
- CVHZOJJKTDOEJC-UHFFFAOYSA-M 1,1-dioxo-1,2-benzothiazol-3-olate Chemical compound C1=CC=C2C([O-])=NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-M 0.000 claims 3
- -1 2-{[4- (hexyloxycarbonylamino-imino-methyl) -phenylamino] -methyl} -1-methyl-1H-benzimidazol-5-carbonyl Chemical group 0.000 claims 3
- AEMOLEFTQBMNLQ-AQKNRBDQSA-M D-glucopyranuronate Chemical compound OC1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-M 0.000 claims 3
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 3
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical group OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 3
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 229940109275 cyclamate Drugs 0.000 claims 2
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 claims 2
- KVBGVZZKJNLNJU-UHFFFAOYSA-N naphthalene-2-sulfonic acid Chemical compound C1=CC=CC2=CC(S(=O)(=O)O)=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000005490 tosylate group Chemical group 0.000 claims 2
- FEWJPZIEWOKRBE-LWMBPPNESA-L D-tartrate(2-) Chemical compound [O-]C(=O)[C@@H](O)[C@H](O)C([O-])=O FEWJPZIEWOKRBE-LWMBPPNESA-L 0.000 claims 1
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 claims 1
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical group OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- FEWJPZIEWOKRBE-LWMBPPNESA-N levotartaric acid Chemical group OC(=O)[C@@H](O)[C@H](O)C(O)=O FEWJPZIEWOKRBE-LWMBPPNESA-N 0.000 claims 1
- XTEGVFVZDVNBPF-UHFFFAOYSA-L naphthalene-1,5-disulfonate(2-) Chemical compound C1=CC=C2C(S(=O)(=O)[O-])=CC=CC2=C1S([O-])(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-L 0.000 claims 1
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical group C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06122047 | 2006-10-10 | ||
| PCT/EP2007/060711 WO2008043759A1 (en) | 2006-10-10 | 2007-10-09 | Physiologically acceptable salts of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1h-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010505906A JP2010505906A (ja) | 2010-02-25 |
| JP2010505906A5 true JP2010505906A5 (enExample) | 2010-12-02 |
Family
ID=38935428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009531826A Pending JP2010505906A (ja) | 2006-10-10 | 2007-10-09 | ３−［（２−｛［４−（ヘキシルオキシカルボニルアミノ−イミノ−メチル）−フェニルアミノ］−メチル｝−１−メチル−１ｈ−ベンゾイミダゾール−５−カルボニル）−ピリジン−２−イル−アミノ］−プロピオン酸エチルエステルの生理学的に許容される塩 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20100087488A1 (enExample) |
| EP (1) | EP2074112A1 (enExample) |
| JP (1) | JP2010505906A (enExample) |
| CA (1) | CA2666396A1 (enExample) |
| WO (1) | WO2008043759A1 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20100129281A (ko) * | 2008-03-28 | 2010-12-08 | 베링거 인겔하임 인터내셔날 게엠베하 | 경구 투여되는 다비가트란 제형의 제조 방법 |
| US7935817B2 (en) * | 2008-03-31 | 2011-05-03 | Apotex Pharmachem Inc. | Salt form and cocrystals of adefovir dipivoxil and processes for preparation thereof |
| US20110123635A1 (en) | 2008-07-14 | 2011-05-26 | Boehringer Ingelheim International Gmbh | Method for manufacturing medicinal compounds containing dabigatran |
| EA201100358A1 (ru) * | 2008-08-19 | 2011-10-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Дабигатран для чрескожной хирургической катетеризации сердца |
| CN102209544A (zh) | 2008-11-11 | 2011-10-05 | 贝林格尔.英格海姆国际有限公司 | 使用达比加群酯或其盐治疗或预防血栓形成且与常规的华法林疗法相比具有改良安全性的方法 |
| HUP1000069A2 (en) | 2010-02-02 | 2012-05-02 | Egis Gyogyszergyar Nyilvanosan M Kod Ruszvunytarsasag | New salts for the preparation of pharmaceutical composition |
| CA2791561A1 (en) * | 2010-03-01 | 2011-09-09 | Ratiopharm Gmbh | Dabigatran etexilate-containing oral pharmaceutical composition |
| US8981105B2 (en) | 2010-07-09 | 2015-03-17 | Esteve Quimica, S.A. | Process of preparing a thrombin specific inhibitor |
| WO2012004397A1 (en) | 2010-07-09 | 2012-01-12 | Esteve Química, S.A. | Intermediates and process for preparing a thrombin specific inhibitor |
| HUE026408T2 (en) | 2010-09-27 | 2016-06-28 | Ratiopharm Gmbh | Dabigatran etexylate bis-mesylate salt, solid forms and process for their preparation |
| US9006448B2 (en) | 2010-12-06 | 2015-04-14 | Msn Laboratories Private Limited | Process for the preparation of benzimidazole derivatives and its salts |
| WO2012162492A1 (en) | 2011-05-24 | 2012-11-29 | Teva Pharmaceutical Industries Ltd. | Compressed core comprising organic acids for a pharmaceutical composition |
| CN102558153A (zh) * | 2012-02-08 | 2012-07-11 | 北京阜康仁生物制药科技有限公司 | 达比加群酯的新药用盐及其制备方法 |
| CN103304539A (zh) * | 2012-03-07 | 2013-09-18 | 天津药物研究院 | 达比加群酯苹果酸盐及其制备方法和应用 |
| CN103304602B (zh) * | 2012-03-07 | 2016-08-17 | 天津药物研究院 | 达比加群酯葡萄糖醛酸盐及其制备方法和应用 |
| WO2013144971A1 (en) | 2012-03-27 | 2013-10-03 | Cadila Healthcare Limited | New solid forms of dabigatran etexilate bisulfate and mesylate and processes to prepare them |
| EP2834224B1 (en) | 2012-04-02 | 2018-06-06 | MSN Laboratories Limited | Process for the preparation of benzimidazole derivatives and salts thereof |
| US20150225370A1 (en) | 2012-09-28 | 2015-08-13 | Ranbaxy Laboratories Limited | Process for the preparation of dabigatran etexilate or pharmaceutically acceptable salt thereof |
| CA2885994A1 (en) | 2012-09-28 | 2014-04-03 | Ranbaxy Laboratories Limited | Process for the preparation of dabigatran etexilate or pharmaceutically acceptable salt thereof |
| CN103864756B (zh) * | 2012-12-11 | 2018-06-15 | 四川海思科制药有限公司 | 丁二磺酸达比加群酯及其制备方法和用途 |
| 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 |
| WO2015124764A1 (en) | 2014-02-24 | 2015-08-27 | Erregierre S.P.A. | Synthesis process of dabigatran etexilate mesylate, intermediates of the process and novel polymorph of dabigatran etexilate |
| 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 |
| CN108864049A (zh) * | 2014-04-04 | 2018-11-23 | 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 |
| WO2016009405A1 (en) * | 2014-07-18 | 2016-01-21 | Sifavitor S.R.L. | Crystalline compounds of dabigatran etexilate |
| CN105440017B (zh) * | 2014-08-19 | 2018-03-02 | 天津药物研究院 | 达比加群酯香草酸盐及其制备方法和应用 |
| CN105348261A (zh) * | 2014-08-19 | 2016-02-24 | 天津药物研究院 | 达比加群酯丙酮酸盐及其制备方法和应用 |
| CN105348259A (zh) * | 2014-08-19 | 2016-02-24 | 天津药物研究院 | 达比加群酯草酰乙酸盐及其制备方法和应用 |
| CN105367551A (zh) * | 2014-08-19 | 2016-03-02 | 天津药物研究院 | 达比加群酯乙醇酸盐及其制备方法和应用 |
| CN105732584A (zh) * | 2014-12-12 | 2016-07-06 | 天津药物研究院有限公司 | 一种达比加群酯2-酮戊二酸盐晶型i及其制备方法和用途 |
| KR102147600B1 (ko) * | 2019-04-15 | 2020-08-25 | 유니셀랩 주식회사 | 신규한 다비가트란 에텍실레이트 헤미에데실레이트의 다형체 및, 이의 제조방법 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE121699A1 (es) * | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| SI1870100T1 (sl) * | 2002-03-07 | 2012-05-31 | Boehringer Ingelheim Int | Metansulfonat etil estra heksiloksikarbonilamino imino metil fenilamino metil metil H benzimidazol karbonil piridin il amino propionske kisline |
| EP1609784A1 (de) * | 2004-06-25 | 2005-12-28 | Boehringer Ingelheim Pharma GmbH & Co.KG | Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen |
| US20060222640A1 (en) * | 2005-03-29 | 2006-10-05 | Boehringer Ingelheim International Gmbh | New pharmaceutical compositions for treatment of thrombosis |
| 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 |
-
2007
- 2007-10-09 EP EP07821080A patent/EP2074112A1/en not_active Withdrawn
- 2007-10-09 CA CA002666396A patent/CA2666396A1/en not_active Abandoned
- 2007-10-09 JP JP2009531826A patent/JP2010505906A/ja active Pending
- 2007-10-09 WO PCT/EP2007/060711 patent/WO2008043759A1/en not_active Ceased
- 2007-10-09 US US12/444,762 patent/US20100087488A1/en not_active Abandoned
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