AR082804A1 - Formas cristalinas de un inhibidor del factor xa - Google Patents
Formas cristalinas de un inhibidor del factor xaInfo
- Publication number
- AR082804A1 AR082804A1 ARP110103159A ARP110103159A AR082804A1 AR 082804 A1 AR082804 A1 AR 082804A1 AR P110103159 A ARP110103159 A AR P110103159A AR P110103159 A ARP110103159 A AR P110103159A AR 082804 A1 AR082804 A1 AR 082804A1
- Authority
- AR
- Argentina
- Prior art keywords
- degrees
- crystalline form
- crystal forms
- factor inhibitor
- betrixaban maleate
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- DTSJEZCXVWQKCL-BTJKTKAUSA-N (z)-but-2-enedioic acid;n-(5-chloropyridin-2-yl)-2-[[4-(n,n-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide Chemical class OC(=O)\C=C/C(O)=O.C=1C=C(Cl)C=NC=1NC(=O)C1=CC(OC)=CC=C1NC(=O)C1=CC=C(C(=N)N(C)C)C=C1 DTSJEZCXVWQKCL-BTJKTKAUSA-N 0.000 abstract 3
- 229950011103 betrixaban Drugs 0.000 abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37933910P | 2010-09-01 | 2010-09-01 | |
| US201161454396P | 2011-03-18 | 2011-03-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR082804A1 true AR082804A1 (es) | 2013-01-09 |
Family
ID=45773260
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103159A AR082804A1 (es) | 2010-09-01 | 2011-08-30 | Formas cristalinas de un inhibidor del factor xa |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8946269B2 (https=) |
| EP (1) | EP2611779B1 (https=) |
| JP (4) | JP2013536864A (https=) |
| CN (1) | CN103261161B (https=) |
| AR (1) | AR082804A1 (https=) |
| AU (1) | AU2011295909B2 (https=) |
| CA (1) | CA2810004C (https=) |
| ES (1) | ES2603084T3 (https=) |
| IL (1) | IL224698A (https=) |
| NZ (1) | NZ608442A (https=) |
| PT (1) | PT2611779T (https=) |
| TW (1) | TW201221128A (https=) |
| WO (1) | WO2012031017A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8980876B2 (en) | 2010-10-28 | 2015-03-17 | The Procter & Gamble Company | Inhibition of microbial growth by aconitase inhibition |
| WO2013033370A1 (en) * | 2011-08-31 | 2013-03-07 | Portola Pharmaceuticals, Inc. | Prevention and treatment of thrombosis in medically ill patients |
| TWI686904B (zh) * | 2012-03-16 | 2020-03-01 | 美商樂仕特拉公司 | 光子材料中介層的方法及系統 |
| 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 |
| CN104693114B (zh) * | 2013-12-10 | 2019-08-16 | 四川海思科制药有限公司 | 一种贝曲西班的改进的制备方法 |
| 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 |
| 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 |
| WO2017208169A1 (en) * | 2016-06-02 | 2017-12-07 | Dr. Reddy’S Laboratories Limited | Polymorphs of betrixaban & its maleate salt |
| EP3254674A1 (en) | 2016-06-08 | 2017-12-13 | Sandoz Ag | Pharmaceutical compositions of betrixaban maleate |
| EP3293174A1 (en) | 2016-09-09 | 2018-03-14 | Sandoz Ag | Crystalline salts of betrixaban |
| WO2018069936A1 (en) * | 2016-10-13 | 2018-04-19 | Mylan Laboratories Limited | Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof |
| CN107382897B (zh) * | 2017-07-10 | 2021-05-04 | 浙江宏元药业股份有限公司 | 一种贝曲西班的中间体及其制备方法和应用 |
| EP3510996A1 (en) * | 2018-01-11 | 2019-07-17 | Sandoz AG | Pharmaceutical compositions of betrixaban |
| CN108570003A (zh) * | 2018-06-01 | 2018-09-25 | 浙江宏元药业股份有限公司 | 一种贝曲西班马来酸盐的一水无定形及其制备方法 |
| CN113905715B (zh) | 2019-06-28 | 2025-04-15 | 宝洁公司 | 光增强处理方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9226238D0 (en) | 1992-12-16 | 1993-02-10 | Scherer Ltd R P | Encapsulation apparatus and process |
| US6140351A (en) | 1997-12-19 | 2000-10-31 | Berlex Laboratories, Inc. | Ortho-anthranilamide derivatives as anti-coagulants |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| WO2001051919A2 (en) * | 2000-01-07 | 2001-07-19 | Transform Pharmaceuticals, Inc. | High-throughput formation, identification, and analysis of diverse solid-forms |
| AU2001250783A1 (en) | 2000-02-29 | 2001-09-12 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| US6627646B2 (en) | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
| DE10322469A1 (de) | 2003-05-19 | 2004-12-16 | Bayer Healthcare Ag | Heterocyclische Verbindungen |
| US7696352B2 (en) | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｘａ 인자 억제제 |
| NZ592533A (en) * | 2005-11-08 | 2012-08-31 | Millennium Pharm Inc | METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR |
| MX2008014193A (es) | 2006-05-05 | 2009-03-31 | Millennium Pharm Inc | Inhibidores del factor xa. |
| US20080051578A1 (en) | 2006-08-24 | 2008-02-28 | Georg Dahmann | Substituted biaryls, process for their manufacture and use thereof as medicaments |
| ES2550057T3 (es) | 2006-11-02 | 2015-11-04 | Millennium Pharmaceuticals, Inc. | Métodos para sintetizar sales farmacéuticas de un inhibidor del Factor Xa |
| CN105193799A (zh) | 2006-12-08 | 2015-12-30 | 米伦纽姆医药公司 | 使用经口因子xa抑制剂治疗血栓形成的单位剂量调配物和方法 |
| 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 |
| EP2155195B1 (en) | 2007-04-13 | 2014-07-16 | Millennium Pharmaceuticals, Inc. | Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor |
| MX2009011755A (es) * | 2007-05-02 | 2010-02-12 | Portola Pharm Inc | Terapia de combinacion con un compuesto que actua como un inhibidor del receptor adp de plaquetas. |
| KR102069498B1 (ko) | 2007-09-28 | 2020-01-23 | 포톨라 파마슈티컬스, 인코포레이티드 | 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법 |
| EP2364165B1 (en) | 2008-11-14 | 2018-01-03 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents |
| CA2784904C (en) * | 2009-12-17 | 2017-10-10 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing factor xa inhibitors |
| TW201240664A (en) | 2010-09-01 | 2012-10-16 | Portola Pharm Inc | Methods and formulations of treating thrombosis with betrixaban and a P-glycoprotein inhibitor |
-
2011
- 2011-08-30 TW TW100131157A patent/TW201221128A/zh unknown
- 2011-08-30 AR ARP110103159A patent/AR082804A1/es unknown
- 2011-08-31 WO PCT/US2011/050057 patent/WO2012031017A1/en not_active Ceased
- 2011-08-31 AU AU2011295909A patent/AU2011295909B2/en not_active Ceased
- 2011-08-31 EP EP11757467.3A patent/EP2611779B1/en not_active Not-in-force
- 2011-08-31 PT PT117574673T patent/PT2611779T/pt unknown
- 2011-08-31 NZ NZ60844211A patent/NZ608442A/en not_active IP Right Cessation
- 2011-08-31 US US13/223,023 patent/US8946269B2/en active Active
- 2011-08-31 CN CN201180052042.4A patent/CN103261161B/zh not_active Expired - Fee Related
- 2011-08-31 JP JP2013527286A patent/JP2013536864A/ja active Pending
- 2011-08-31 ES ES11757467.3T patent/ES2603084T3/es active Active
- 2011-08-31 CA CA2810004A patent/CA2810004C/en not_active Expired - Fee Related
-
2013
- 2013-02-13 IL IL224698A patent/IL224698A/en active IP Right Grant
-
2015
- 2015-09-24 JP JP2015187427A patent/JP2015232046A/ja active Pending
-
2017
- 2017-11-16 JP JP2017221050A patent/JP2018024709A/ja active Pending
-
2019
- 2019-04-23 JP JP2019081907A patent/JP2019135258A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013536864A (ja) | 2013-09-26 |
| US20120071519A1 (en) | 2012-03-22 |
| CN103261161B (zh) | 2016-04-27 |
| JP2018024709A (ja) | 2018-02-15 |
| IL224698A (en) | 2017-01-31 |
| JP2019135258A (ja) | 2019-08-15 |
| WO2012031017A1 (en) | 2012-03-08 |
| JP2015232046A (ja) | 2015-12-24 |
| PT2611779T (pt) | 2016-11-21 |
| AU2011295909B2 (en) | 2015-05-21 |
| CA2810004A1 (en) | 2012-03-08 |
| AU2011295909A1 (en) | 2013-04-04 |
| EP2611779B1 (en) | 2016-08-10 |
| ES2603084T3 (es) | 2017-02-23 |
| EP2611779A1 (en) | 2013-07-10 |
| US8946269B2 (en) | 2015-02-03 |
| NZ608442A (en) | 2015-04-24 |
| CN103261161A (zh) | 2013-08-21 |
| TW201221128A (en) | 2012-06-01 |
| CA2810004C (en) | 2019-09-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |