AR079491A1 - Metodos de sintesis de inhibidores del factor xa tal como el betrixaban y composiciones farmaceuticas que contienen la base libre de betrixaban o su sal sustancialmente pura. - Google Patents
Metodos de sintesis de inhibidores del factor xa tal como el betrixaban y composiciones farmaceuticas que contienen la base libre de betrixaban o su sal sustancialmente pura.Info
- Publication number
- AR079491A1 AR079491A1 ARP100104654A ARP100104654A AR079491A1 AR 079491 A1 AR079491 A1 AR 079491A1 AR P100104654 A ARP100104654 A AR P100104654A AR P100104654 A ARP100104654 A AR P100104654A AR 079491 A1 AR079491 A1 AR 079491A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compound
- betrixaban
- salt
- inhibitors
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
Abstract
Reivindicacion 1: Un método de preparacion de un compuesto de la Formula II, o una sus sales, que comprende: el contacto de un compuesto de la Formula II-A: con un compuesto de la formula II-B: en condiciones de reaccion para formar el compuesto de la Formula II o su sal; donde: R1 y R2 son, de modo independiente, alquilo C1-6; R3 y R4 se seleccionan de manera independiente del grupo que consiste en hidrogeno, fluor, cloro, bromo y metoxi; y R5 se selecciona del grupo que consiste en fluor, cloro, bromo y metoxi. Reivindicacion 9: un método para la preparacion de betrixabán, que tiene la formula I, o una de sus sales, que comprende: el contacto de un compuesto de la Formula A: con un compuesto de la Formula B: en condiciones de reaccion para formar betrixabán o su sal. Reivindicacion 36: Un método para la preparacion de betrixabán, que tiene la Formula I, o una de sus sales: que comprende: a) el contacto de un compuesto de la Formula D: con un compuesto de la Formula E: en condiciones de reaccion que comprenden acetonitrilo como solvente, para formar un compuesto de la Formula C: b) la exposicion del compuesto de la Formula C a condiciones de reduccion que comprenden gas hidrogeno, en presencia de un catalizador, para formar un compuesto de la Formula B: c) el contacto del compuesto de la Formula B con un compuesto de la Formula A: en condiciones de reaccion que comprenden un reactivo de acoplamiento de amida para formar betrixabán o su sal.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28768009P | 2009-12-17 | 2009-12-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079491A1 true AR079491A1 (es) | 2012-02-01 |
Family
ID=43532100
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104654A AR079491A1 (es) | 2009-12-17 | 2010-12-15 | Metodos de sintesis de inhibidores del factor xa tal como el betrixaban y composiciones farmaceuticas que contienen la base libre de betrixaban o su sal sustancialmente pura. |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8394964B2 (es) |
| EP (1) | EP2513058B1 (es) |
| JP (2) | JP5766204B2 (es) |
| CN (2) | CN102762538B (es) |
| AR (1) | AR079491A1 (es) |
| CA (1) | CA2784904C (es) |
| ES (1) | ES2610145T3 (es) |
| PT (1) | PT2513058T (es) |
| TW (1) | TW201144283A (es) |
| WO (1) | WO2011084519A1 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2667488C (en) * | 2006-11-02 | 2015-07-07 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing pharmaceutical salts of a factor xa inhibitor |
| EP2513058B1 (en) * | 2009-12-17 | 2016-11-09 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing factor xa inhibitors |
| AR082804A1 (es) * | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Formas cristalinas de un inhibidor del factor xa |
| US20150224091A1 (en) * | 2011-08-31 | 2015-08-13 | Portola Pharmaceuticals, Inc. | Prevention and treatment of thrombosis in medically ill patients |
| US9200268B2 (en) | 2012-12-27 | 2015-12-01 | Portola Pharmaceuticals, Inc. | Compounds and methods for purification of serine proteases |
| US20140346397A1 (en) | 2012-12-27 | 2014-11-27 | Portola Pharmaceuticals, Inc. | Compounds and methods for purification of serine proteases |
| CN104341343B (zh) * | 2013-07-24 | 2018-09-28 | 四川海思科制药有限公司 | 贝曲西班的晶型及其制备方法和用途 |
| CN105017078B (zh) * | 2014-04-23 | 2017-02-15 | 中国科学院大连化学物理研究所 | 一种芳香醛催化转化制备亚胺酸酯的方法 |
| CN105085387A (zh) * | 2014-05-20 | 2015-11-25 | 四川海思科制药有限公司 | 贝曲西班盐及其制备方法和用途 |
| US20180180994A1 (en) * | 2015-06-23 | 2018-06-28 | Covestro Deutschland Ag | Substituted triazines |
| WO2017091757A1 (en) | 2015-11-24 | 2017-06-01 | Portola Pharmaceuticals, Inc. | Isotopically enriched betrixaban |
| CN106995405A (zh) * | 2016-01-25 | 2017-08-01 | 重庆医药工业研究院有限责任公司 | 一种贝曲西班马来酸盐无定型物及其制备方法 |
| CN107098853A (zh) * | 2016-02-20 | 2017-08-29 | 天津科伦药物研究有限公司 | 贝曲西班马来酸盐的制备方法 |
| CN105732490A (zh) * | 2016-03-25 | 2016-07-06 | 重庆医科大学 | 一种贝曲西班的制备方法 |
| EP3463352A4 (en) * | 2016-06-02 | 2019-10-30 | Dr. Reddy S Laboratories Limited | POLYMORPH OF BETRIXABAN AND ITS MALEATE SALT |
| EP3254674A1 (en) | 2016-06-08 | 2017-12-13 | Sandoz Ag | Pharmaceutical compositions of betrixaban maleate |
| WO2018042320A1 (en) * | 2016-08-30 | 2018-03-08 | Dr. Reddy’S Laboratories Limited | Salts of betrixaban and processes for preparation thereof |
| CN107778223B (zh) * | 2016-08-31 | 2020-05-15 | 鲁南制药集团股份有限公司 | 一种马来酸贝曲西班的制备方法 |
| KR102031186B1 (ko) * | 2017-01-11 | 2019-11-08 | 주식회사 엘지생활건강 | 단백질 강도 강화용 조성물 |
| CN107868039A (zh) * | 2017-11-27 | 2018-04-03 | 中国药科大学 | 一种贝曲沙班中间体n－（5－氯－2－吡啶基）－2－［（4－氰基苯甲酰基）氨基］－5－甲氧基苯甲酰胺的制备方法 |
| WO2020021083A1 (en) * | 2018-07-27 | 2020-01-30 | Umicore Ag & Co. Kg | Organometallic compounds for the manufacture of a semiconductor element or electronic memory |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1302292A (zh) | 1998-03-19 | 2001-07-04 | 味之素株式会社 | 氨基异喹啉衍生物 |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| DE60115394T2 (de) | 2000-02-29 | 2006-10-19 | Millennium Pharmaceuticals, Inc., Cambridge | Benzamide und ähnliche inhibitoren vom faktor xa |
| US7312235B2 (en) | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| US7122557B2 (en) * | 2003-03-18 | 2006-10-17 | Bristol-Myers Squibb Company | Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors |
| WO2005034867A2 (en) * | 2003-10-09 | 2005-04-21 | Millennium Pharmaceuticals, Inc. | Thioether-substituted benzamides as inhibitors of factor xa |
| AU2005257999B2 (en) | 2004-06-18 | 2011-12-08 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| US7696352B2 (en) | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| CN102336702B (zh) | 2005-11-08 | 2015-02-11 | 米伦纽姆医药公司 | Xa因子抑制剂n-(5-氯-2-吡啶基)-2-[[4-[(二甲氨基)亚氨基甲基]苯甲酰基]氨基]-5-甲氧基-苯甲酰胺的医药盐和多晶型 |
| AU2007247928B2 (en) | 2006-05-05 | 2013-06-13 | Millennium Pharmaceuticals, Inc. | Factor XA inhibitors |
| CA2667488C (en) * | 2006-11-02 | 2015-07-07 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing pharmaceutical salts of a factor xa inhibitor |
| NZ578180A (en) | 2006-12-08 | 2012-02-24 | Millennium Pharm Inc | Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor |
| JP2010515691A (ja) | 2007-01-05 | 2010-05-13 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | 第Ｘａ因子阻害剤 |
| CN101743001B (zh) | 2007-04-13 | 2013-02-06 | 千年药品公司 | 用起因子xa抑制剂作用的化合物的组合抗凝治疗 |
| EP2513058B1 (en) * | 2009-12-17 | 2016-11-09 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing factor xa inhibitors |
| US8530501B2 (en) | 2009-12-17 | 2013-09-10 | Millennium Pharmaceuticals, Inc. | Salts and crystalline forms of a factor Xa inhibitor |
| US20110160250A1 (en) | 2009-12-17 | 2011-06-30 | Millennium Pharmaceuticals, Inc. | Crystalline forms of a factor xa inhibitor |
| WO2011075602A1 (en) | 2009-12-17 | 2011-06-23 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
-
2010
- 2010-12-15 EP EP10801495.2A patent/EP2513058B1/en not_active Not-in-force
- 2010-12-15 JP JP2012544794A patent/JP5766204B2/ja active Active
- 2010-12-15 TW TW099144090A patent/TW201144283A/zh unknown
- 2010-12-15 PT PT108014952T patent/PT2513058T/pt unknown
- 2010-12-15 CN CN201080064124.6A patent/CN102762538B/zh not_active Expired - Fee Related
- 2010-12-15 US US12/969,371 patent/US8394964B2/en not_active Expired - Fee Related
- 2010-12-15 CN CN201510052519.9A patent/CN104774176A/zh active Pending
- 2010-12-15 WO PCT/US2010/060572 patent/WO2011084519A1/en active Application Filing
- 2010-12-15 ES ES10801495.2T patent/ES2610145T3/es active Active
- 2010-12-15 AR ARP100104654A patent/AR079491A1/es unknown
- 2010-12-15 CA CA2784904A patent/CA2784904C/en not_active Expired - Fee Related
-
2013
- 2013-02-01 US US13/757,483 patent/US8987463B2/en active Active
-
2014
- 2014-12-24 JP JP2014260157A patent/JP2015091840A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| EP2513058A1 (en) | 2012-10-24 |
| JP5766204B2 (ja) | 2015-08-19 |
| CN104774176A (zh) | 2015-07-15 |
| US20130211094A1 (en) | 2013-08-15 |
| WO2011084519A1 (en) | 2011-07-14 |
| US8394964B2 (en) | 2013-03-12 |
| PT2513058T (pt) | 2017-01-26 |
| JP2015091840A (ja) | 2015-05-14 |
| EP2513058B1 (en) | 2016-11-09 |
| CN102762538A (zh) | 2012-10-31 |
| TW201144283A (en) | 2011-12-16 |
| CA2784904A1 (en) | 2011-07-14 |
| ES2610145T3 (es) | 2017-04-26 |
| CN102762538B (zh) | 2015-11-25 |
| US8987463B2 (en) | 2015-03-24 |
| CA2784904C (en) | 2017-10-10 |
| JP2013514380A (ja) | 2013-04-25 |
| US20110319627A1 (en) | 2011-12-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR079491A1 (es) | Metodos de sintesis de inhibidores del factor xa tal como el betrixaban y composiciones farmaceuticas que contienen la base libre de betrixaban o su sal sustancialmente pura. | |
| BR112012028630A2 (pt) | dispositivo para comprimir e secar gás | |
| CO6140053A2 (es) | Proceso para fabricar 2-amino-5-halobenzamidas 3-sustituidas | |
| AR074845A1 (es) | Procedimiento de sintesis de la ivabradina y de sus sales de adicion a un acido farmaceuticamente aceptable | |
| PE20140727A1 (es) | Medio de absorcion con contenido de amina, procedimiento y dispositivo para la absorcion de gases acidos a partir de mezclas gaseosas | |
| AR076897A1 (es) | Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos | |
| BR112012028637A2 (pt) | composição de gasolina, pacote de aditivo, uso de aditivo e método | |
| AR077526A1 (es) | Metodo para la sintesis de (1s,2r)- milnacipran | |
| AR049401A1 (es) | Aza-biciclononanos | |
| EA201390916A1 (ru) | Новые ферроценовые метки для электрохимического анализа и их применение в аналитических способах | |
| AR123584A2 (es) | Procesos y compuestos intermediarios para la preparación de derivados de 2-carboxamida-cicloamino-urea | |
| CO5700747A2 (es) | Piperidinas novedosas como moduladores de quimoquina (ccr) | |
| PE20100051A1 (es) | Nuevo procedimiento de sintesis de 7,8-dimetoxi-1,3-dihidro-2h-3-benzazepin-2-oa y aplicacion en la sintesis de ivabradina y de sus sales de adicion a un acido farmaceuticamente aceptable | |
| AR076969A1 (es) | Un procedimiento para la preparacion de febuxostat | |
| AR107494A1 (es) | Proceso para la preparación de osimertinib (azd9291) o una sal del mismo, y azd9291 anilina o una sal de la misma | |
| CO6231030A2 (es) | Metodos para preparar compuestos basados en imidazol como potentes inhibidores de respuesta inmune | |
| AR049668A1 (es) | Proceso quimico para preparar esteres de 4,4 - difluorometil - 3 - oxo - butanoico por reaccion entre una amida y un ester. | |
| AR047686A1 (es) | Un procedimiento de sintesis de compuestos de 1,3-dihidro-2h-3-benzazepin-2-ona, y su aplicacion a la sintesis de la ivabradina y sus sales de adicion con un acido farmaceuticamente aceptable | |
| NO20092259L (no) | Prosess | |
| AR074630A1 (es) | Proceso para preparar acidos 1-hidroxialquiliden-1,1-bifosfonicos | |
| AR073773A1 (es) | Metodo para producir decitabina protegida beta-enriquecida. | |
| AR071005A1 (es) | Preparacion selectiva de pirimidinas sustituidas | |
| AR087072A1 (es) | Procesos para la preparacion de tietanamina | |
| RU2012142223A (ru) | Пространственно-затрудненные амины | |
| AR057778A1 (es) | Proceso para la produccion de anilinas |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |