TW201221128A - Crystalline forms of a factor Xa inhibitor - Google Patents
Crystalline forms of a factor Xa inhibitor Download PDFInfo
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- TW201221128A TW201221128A TW100131157A TW100131157A TW201221128A TW 201221128 A TW201221128 A TW 201221128A TW 100131157 A TW100131157 A TW 100131157A TW 100131157 A TW100131157 A TW 100131157A TW 201221128 A TW201221128 A TW 201221128A
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Diabetes (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 |
|---|---|
| TW201221128A true TW201221128A (en) | 2012-06-01 |
Family
ID=45773260
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW100131157A TW201221128A (en) | 2010-09-01 | 2011-08-30 | Crystalline forms of a factor Xa inhibitor |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8946269B2 (enExample) |
| EP (1) | EP2611779B1 (enExample) |
| JP (4) | JP2013536864A (enExample) |
| CN (1) | CN103261161B (enExample) |
| AR (1) | AR082804A1 (enExample) |
| AU (1) | AU2011295909B2 (enExample) |
| CA (1) | CA2810004C (enExample) |
| ES (1) | ES2603084T3 (enExample) |
| IL (1) | IL224698A (enExample) |
| NZ (1) | NZ608442A (enExample) |
| PT (1) | PT2611779T (enExample) |
| TW (1) | TW201221128A (enExample) |
| WO (1) | WO2012031017A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Families Citing this family (16)
| 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 |
| 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 |
| US20190300483A1 (en) * | 2016-06-02 | 2019-10-03 | Dr. Reddy's Laboratories Limited | POLYMORPHS OF BETRlXABAN & 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 |
| WO2020264076A1 (en) | 2019-06-28 | 2020-12-30 | The Procter & Gamble Company | Light augmented treatment method |
Family Cites Families (21)
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| 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 |
| IL150524A0 (en) * | 2000-01-07 | 2003-02-12 | Transform Pharmaceuticals Inc | High-throughput formation, identification, and analysis of diverse solid-forms |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | 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 |
| KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｘａ 인자 억제제 |
| US7696352B2 (en) | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| CN101304971B (zh) | 2005-11-08 | 2011-09-07 | 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 |
| EP2016072B1 (en) | 2006-05-05 | 2014-07-16 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| US20080051578A1 (en) | 2006-08-24 | 2008-02-28 | Georg Dahmann | Substituted biaryls, process for their manufacture and use thereof as medicaments |
| EP2077995B1 (en) | 2006-11-02 | 2012-02-08 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing pharmaceutical salts of a factor xa inhibitor |
| PT2101760E (pt) | 2006-12-08 | 2013-05-07 | Millennium Pharm Inc | Formulações de dose unitária e métodos de tratamento da trombose com um inibidor oral do fator xa |
| CA2674924A1 (en) | 2007-01-05 | 2008-07-17 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| EP2155195B1 (en) | 2007-04-13 | 2014-07-16 | Millennium Pharmaceuticals, Inc. | Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor |
| KR101509829B1 (ko) * | 2007-05-02 | 2015-04-06 | 포톨라 파마슈티컬스, 인코포레이티드 | 혈소판 ａｄｐ 수용체 억제제로 작용하는 화합물을 이용한 병용요법 |
| KR102069498B1 (ko) | 2007-09-28 | 2020-01-23 | 포톨라 파마슈티컬스, 인코포레이티드 | 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법 |
| CA2743496C (en) * | 2008-11-14 | 2018-03-27 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents |
| JP5766204B2 (ja) * | 2009-12-17 | 2015-08-19 | 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Ｍｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | 第Ｘａ因子阻害剤の合成方法 |
| AR082803A1 (es) | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Metodos y formulaciones para el tratamiento de la trombosis con betrixaban y un inhibidor de la glicoproteina p |
-
2011
- 2011-08-30 TW TW100131157A patent/TW201221128A/zh unknown
- 2011-08-30 AR ARP110103159A patent/AR082804A1/es unknown
- 2011-08-31 CA CA2810004A patent/CA2810004C/en not_active Expired - Fee Related
- 2011-08-31 ES ES11757467.3T patent/ES2603084T3/es active Active
- 2011-08-31 EP EP11757467.3A patent/EP2611779B1/en not_active Not-in-force
- 2011-08-31 WO PCT/US2011/050057 patent/WO2012031017A1/en not_active Ceased
- 2011-08-31 NZ NZ60844211A patent/NZ608442A/en not_active IP Right Cessation
- 2011-08-31 AU AU2011295909A patent/AU2011295909B2/en not_active Ceased
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2019
- 2019-04-23 JP JP2019081907A patent/JP2019135258A/ja active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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| NZ608442A (en) | 2015-04-24 |
| US20120071519A1 (en) | 2012-03-22 |
| IL224698A (en) | 2017-01-31 |
| JP2013536864A (ja) | 2013-09-26 |
| CN103261161B (zh) | 2016-04-27 |
| WO2012031017A1 (en) | 2012-03-08 |
| JP2019135258A (ja) | 2019-08-15 |
| CA2810004C (en) | 2019-09-10 |
| JP2015232046A (ja) | 2015-12-24 |
| AU2011295909B2 (en) | 2015-05-21 |
| CN103261161A (zh) | 2013-08-21 |
| EP2611779A1 (en) | 2013-07-10 |
| JP2018024709A (ja) | 2018-02-15 |
| PT2611779T (pt) | 2016-11-21 |
| CA2810004A1 (en) | 2012-03-08 |
| US8946269B2 (en) | 2015-02-03 |
| EP2611779B1 (en) | 2016-08-10 |
| ES2603084T3 (es) | 2017-02-23 |
| AR082804A1 (es) | 2013-01-09 |
| AU2011295909A1 (en) | 2013-04-04 |
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