CN102762550B - Xa因子抑制剂的盐和结晶形式 - Google Patents
Xa因子抑制剂的盐和结晶形式 Download PDFInfo
- Publication number
- CN102762550B CN102762550B CN201080064120.8A CN201080064120A CN102762550B CN 102762550 B CN102762550 B CN 102762550B CN 201080064120 A CN201080064120 A CN 201080064120A CN 102762550 B CN102762550 B CN 102762550B
- Authority
- CN
- China
- Prior art keywords
- compound
- salt
- crystalline form
- crystalline
- weight
- 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.)
- Expired - Fee Related
Links
- QZWFIJCOFXOLBT-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCc(nc1)c[n]1-c(cc1)ccc1N(C=CC=C1)C1=O Chemical compound O=C(c([s]1)ccc1Cl)NCc(nc1)c[n]1-c(cc1)ccc1N(C=CC=C1)C1=O QZWFIJCOFXOLBT-UHFFFAOYSA-N 0.000 description 2
- 0 CCC(CC=C(C=C1)N2C=C*=CC2C)C1N1*=NC(CN*)=C2C1C2 Chemical compound CCC(CC=C(C=C1)N2C=C*=CC2C)C1N1*=NC(CN*)=C2C1C2 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28768309P | 2009-12-17 | 2009-12-17 | |
| US61/287,683 | 2009-12-17 | ||
| PCT/US2010/060885 WO2011084652A2 (en) | 2009-12-17 | 2010-12-16 | Salts and crystalline forms of a factor xa inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102762550A CN102762550A (zh) | 2012-10-31 |
| CN102762550B true CN102762550B (zh) | 2015-04-01 |
Family
ID=43618959
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080064120.8A Expired - Fee Related CN102762550B (zh) | 2009-12-17 | 2010-12-16 | Xa因子抑制剂的盐和结晶形式 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8530501B2 (https=) |
| EP (1) | EP2513094B1 (https=) |
| JP (1) | JP5796872B2 (https=) |
| CN (1) | CN102762550B (https=) |
| CA (1) | CA2784921A1 (https=) |
| WO (1) | WO2011084652A2 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8742120B2 (en) * | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| AR079491A1 (es) | 2009-12-17 | 2012-02-01 | Millennium Pharm Inc | 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. |
| CN120633248B (zh) * | 2025-08-08 | 2025-10-17 | 成都理工大学 | 超临界地热流体体系KCl-H2O的电导率计算方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1523986A (zh) * | 2001-06-20 | 2004-08-25 | �����ɷ� | 用于联合治疗的取代的噁唑烷酮类化合物 |
| WO2007025940A1 (de) * | 2005-08-29 | 2007-03-08 | Boehringer Ingelheim International Gmbh | Substituierte biaryle und deren verwendung als faktor xa-inhibitoren |
| CN1968922A (zh) * | 2004-06-18 | 2007-05-23 | 米伦纽姆医药公司 | 因子xa抑制剂 |
| WO2007131179A1 (en) * | 2006-05-05 | 2007-11-15 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
Family Cites Families (44)
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| GB9226238D0 (en) | 1992-12-16 | 1993-02-10 | Scherer Ltd R P | Encapsulation apparatus and process |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| CA2295620A1 (en) | 1997-08-11 | 1999-02-18 | Boehringer Ingelheim Pharmaceuticals, Inc. | 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection |
| GB9725244D0 (en) | 1997-11-29 | 1998-01-28 | Zeneca Ltd | Chemical compounds |
| JP2000178243A (ja) | 1998-12-14 | 2000-06-27 | Teijin Ltd | ビフェニルアミジン誘導体 |
| ES2316383T3 (es) | 1999-09-17 | 2009-04-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| WO2001021160A2 (en) | 1999-09-23 | 2001-03-29 | Axxima Pharmaceuticals Aktiengesellschaft | Carboxymide and aniline derivatives as selective inhibitors of pathogens |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| US6906063B2 (en) | 2000-02-04 | 2005-06-14 | Portola Pharmaceuticals, Inc. | Platelet ADP receptor inhibitors |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| DE10027151A1 (de) | 2000-05-31 | 2001-12-06 | Bayer Ag | Herbizide Mittel auf Basis von substituierten Carbonsäureamiden |
| AU2001273040A1 (en) | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| ATE368643T1 (de) | 2001-03-30 | 2007-08-15 | Millennium Pharm Inc | Faktor xa benzamidin inhibitoren |
| US7312235B2 (en) | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| US6627646B2 (en) * | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
| ES2180456B1 (es) | 2001-07-20 | 2004-05-01 | Laboratorios S.A.L.V.A.T., S.A. | Isoxazoles sustituidos y su utilizacion como antibioticos. |
| US6914058B2 (en) | 2002-01-18 | 2005-07-05 | Dr. Reddy's Laboratories, Limited | Antibacterial compounds: process for their preparation and pharmaceutical compositions containing them |
| JP4471262B2 (ja) | 2002-03-07 | 2010-06-02 | 株式会社エス・ディー・エス バイオテック | 置換イソキサゾールアルキルアミン誘導体及び農園芸用殺菌剤 |
| US20070043079A1 (en) | 2003-04-18 | 2007-02-22 | Hiromu Habashita | Heterocyclic compound containing nitrogen atom and use thereof |
| WO2004101531A1 (en) | 2003-04-29 | 2004-11-25 | Dr. Reddy's Laboratories Ltd. | Antiinfective 1,2,3-triazole derivatives, process for their preparation and pharmaceutical compositions containing them |
| DE10322469A1 (de) | 2003-05-19 | 2004-12-16 | Bayer Healthcare Ag | Heterocyclische Verbindungen |
| WO2004106329A2 (en) | 2003-06-03 | 2004-12-09 | Dr. Reddy's Laboratories Ltd. | Novel antiinfective compounds and their pharmaceutical compositions |
| US7199149B2 (en) | 2003-10-01 | 2007-04-03 | Bristol Myers Squibb Company | Monocyclic and bicyclic lactams as factor Xa inhibitors |
| US7022695B2 (en) | 2003-10-09 | 2006-04-04 | Millennium Pharmaceuticals, Inc. | Thioether-substituted benzamides as inhibitors of Factor Xa |
| WO2005035528A2 (en) | 2003-10-14 | 2005-04-21 | Dr. Reddy's Laboratories Ltd. | Triazole derivatives as antibacterial agents |
| WO2005082892A2 (en) | 2004-02-17 | 2005-09-09 | Dr. Reddy's Laboratories Ltd. | Triazole compounds as antibacterial agents and pharmaceutical compositions containing them |
| US7696352B2 (en) | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| WO2007007588A1 (ja) | 2005-07-08 | 2007-01-18 | Ono Pharmaceutical Co., Ltd. | 平面性を有する環状基を母核とする化合物 |
| PT1951254E (pt) | 2005-11-03 | 2012-04-12 | Portola Pharm Inc | [4-(6-halo-7-substituído-2,4-dioxo-1,4-di-hidro-2hquinazolin- 3-il)-fenil]-5-cloro-tiofen-2-il-sulfonilureias e formas e métodos relacionados com as mesmas |
| PE20070717A1 (es) | 2005-11-08 | 2007-08-17 | Millennium Pharm Inc | Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida |
| US20090186810A1 (en) | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| DE102006025314A1 (de) | 2006-05-31 | 2007-12-06 | Bayer Healthcare Ag | Arylsubstituierte Heterozyklen und ihre Verwendung |
| US20080051578A1 (en) | 2006-08-24 | 2008-02-28 | Georg Dahmann | Substituted biaryls, process for their manufacture and use thereof as medicaments |
| CN101595092B (zh) | 2006-11-02 | 2012-02-01 | 米伦纽姆医药公司 | 合成因子xa抑制剂的医药盐的方法 |
| KR101472765B1 (ko) | 2006-12-08 | 2014-12-15 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 경구용 Xa 인자 억제제를 포함하는 단위 용량 제형 및 경구용 Xa 인자 억제제를 사용하는 혈전증의 치료 방법 |
| WO2008086226A2 (en) | 2007-01-05 | 2008-07-17 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| WO2008121721A2 (en) | 2007-03-28 | 2008-10-09 | Portola Pharmaceuticals, Inc. | Targeted delivery and expression of procoagulant hemostatic activity |
| EA020531B1 (ru) | 2007-04-13 | 2014-11-28 | Милленниум Фармасьютикалз, Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ АНТИКОАГУЛИРУЮЩЕГО СРЕДСТВА С СОЕДИНЕНИЕМ, КОТОРОЕ ДЕЙСТВУЕТ КАК ИНГИБИТОР ФАКТОРА Ха |
| KR101509829B1 (ko) | 2007-05-02 | 2015-04-06 | 포톨라 파마슈티컬스, 인코포레이티드 | 혈소판 adp 수용체 억제제로 작용하는 화합물을 이용한 병용요법 |
| EP2915564B1 (en) | 2007-09-28 | 2020-11-04 | Portola Pharmaceuticals, Inc. | Antidotes for factor XA inhibitors and methods of using the same |
| MX2011004907A (es) | 2008-11-14 | 2011-07-29 | Portola Pharm Inc | Antidotos para inhibidores del factor xa y metodos para el uso de los mismos en combinacion con agentes de coagulacion de sangre. |
| EP3121271B1 (en) | 2009-03-30 | 2019-07-24 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same |
| ES2605801T3 (es) | 2009-07-15 | 2017-03-16 | Portola Pharmaceuticals, Inc. | Formulación de dosis unitaria de antídoto para inhibidores del factor Xa para su uso en la prevención de la hemorragia |
-
2010
- 2010-12-16 CN CN201080064120.8A patent/CN102762550B/zh not_active Expired - Fee Related
- 2010-12-16 EP EP10801041.4A patent/EP2513094B1/en not_active Not-in-force
- 2010-12-16 JP JP2012544856A patent/JP5796872B2/ja not_active Expired - Fee Related
- 2010-12-16 US US12/970,785 patent/US8530501B2/en not_active Expired - Fee Related
- 2010-12-16 CA CA2784921A patent/CA2784921A1/en not_active Abandoned
- 2010-12-16 WO PCT/US2010/060885 patent/WO2011084652A2/en not_active Ceased
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1523986A (zh) * | 2001-06-20 | 2004-08-25 | �����ɷ� | 用于联合治疗的取代的噁唑烷酮类化合物 |
| CN1968922A (zh) * | 2004-06-18 | 2007-05-23 | 米伦纽姆医药公司 | 因子xa抑制剂 |
| WO2007025940A1 (de) * | 2005-08-29 | 2007-03-08 | Boehringer Ingelheim International Gmbh | Substituierte biaryle und deren verwendung als faktor xa-inhibitoren |
| WO2007131179A1 (en) * | 2006-05-05 | 2007-11-15 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
Non-Patent Citations (2)
| Title |
|---|
| "Xa 因子抑制剂的药效团模型初探";王坚毅,等;《药学进展》;20031231;第27卷(第1期);第5-9页 * |
| "新型抗凝药物直接Xa因子抑制剂利伐沙班";柯永胜;《中国临床药理学与治疗学》;20090430;第14卷(第4期);第361-367页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011084652A3 (en) | 2011-09-09 |
| CA2784921A1 (en) | 2011-07-14 |
| JP5796872B2 (ja) | 2015-10-21 |
| US20110178135A1 (en) | 2011-07-21 |
| EP2513094A2 (en) | 2012-10-24 |
| JP2013514981A (ja) | 2013-05-02 |
| WO2011084652A2 (en) | 2011-07-14 |
| HK1177459A1 (zh) | 2013-08-23 |
| CN102762550A (zh) | 2012-10-31 |
| US8530501B2 (en) | 2013-09-10 |
| EP2513094B1 (en) | 2015-12-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150401 Termination date: 20191216 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |