JP2006504745A - エポｄ及び５−ｆｕ／ゲムシタビン - Google Patents
エポｄ及び５−ｆｕ／ゲムシタビン Download PDFInfo
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- JP2006504745A JP2006504745A JP2004543655A JP2004543655A JP2006504745A JP 2006504745 A JP2006504745 A JP 2006504745A JP 2004543655 A JP2004543655 A JP 2004543655A JP 2004543655 A JP2004543655 A JP 2004543655A JP 2006504745 A JP2006504745 A JP 2006504745A
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- epothilone
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- dehydroepothilone
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| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| ATE350383T1 (de) | 2002-08-23 | 2007-01-15 | Sloan Kettering Inst Cancer | Synthese von epothilonen, zwischenprodukte dafür, analoga und deren verwendungen |
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| JP4303726B2 (ja) | 2003-11-11 | 2009-07-29 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ウレア誘導体およびその製造方法 |
| US20050215604A1 (en) * | 2004-03-26 | 2005-09-29 | Kosan Biosciences, Inc. | Combination therapies with epothilones and carboplatin |
| US8969379B2 (en) | 2004-09-17 | 2015-03-03 | Eisai R&D Management Co., Ltd. | Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7=methoxy-6-quinolinecarboxide |
| JP4989476B2 (ja) | 2005-08-02 | 2012-08-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管新生阻害物質の効果を検定する方法 |
| CN104706637A (zh) | 2006-05-18 | 2015-06-17 | 卫材R&D管理有限公司 | 针对甲状腺癌的抗肿瘤剂 |
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| CA2704000C (en) | 2007-11-09 | 2016-12-13 | Eisai R&D Management Co., Ltd. | Combination of anti-angiogenic substance and anti-tumor platinum complex |
| CA2771403C (en) | 2009-08-19 | 2015-02-24 | Eisai R&D Management Co. Ltd. | Quinoline derivative-containing pharmaceutical composition |
| CA2927832C (en) | 2010-05-18 | 2021-03-23 | Cerulean Pharma Inc. | Cyclodextrin-containing polymer-therapeutic agent conjugates and their use |
| CN102958523B (zh) | 2010-06-25 | 2014-11-19 | 卫材R&D管理有限公司 | 使用具有激酶抑制作用的组合的抗肿瘤剂 |
| AU2012246490B2 (en) | 2011-04-18 | 2016-08-04 | Eisai R&D Management Co., Ltd. | Therapeutic agent for tumor |
| JP6038128B2 (ja) | 2011-06-03 | 2016-12-07 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー |
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| US20180028662A1 (en) | 2015-02-25 | 2018-02-01 | Eisai R&D Management Co., Ltd. | Method for Suppressing Bitterness of Quinoline Derivative |
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| WO2018212202A1 (en) | 2017-05-16 | 2018-11-22 | Eisai R&D Management Co., Ltd. | Treatment of hepatocellular carcinoma |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000061142A1 (en) * | 1999-04-14 | 2000-10-19 | Dana-Farber Cancer Institute, Inc. | Method and composition for the treatment of cancer |
| JP2005513167A (ja) * | 2002-01-14 | 2005-05-12 | ノバルティス アクチエンゲゼルシャフト | エポシロン誘導体と代謝拮抗剤からなる組合せ |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1386922B1 (en) * | 1996-12-03 | 2012-04-11 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereof, analogues and uses thereof |
| US6204388B1 (en) * | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6596875B2 (en) * | 2000-02-07 | 2003-07-22 | James David White | Method for synthesizing epothilones and epothilone analogs |
| EE04852B1 (et) * | 1999-02-22 | 2007-06-15 | Gesellschaft Fuer Biotechnologische Forschung Mbh | C-21 modifitseeritud epotioloonid, nende valmistamise meetod ning kasutamine ja ravimkoostise kasutamine vähkkasvajate või teiste proliferatiivsete haiguste ravimisel |
| US6291684B1 (en) * | 1999-03-29 | 2001-09-18 | Bristol-Myers Squibb Company | Process for the preparation of aziridinyl epothilones from oxiranyl epothilones |
| US6489314B1 (en) * | 2001-04-03 | 2002-12-03 | Kosan Biosciences, Inc. | Epothilone derivatives and methods for making and using the same |
| ATE554756T1 (de) * | 2001-03-14 | 2012-05-15 | Bristol Myers Squibb Co | Kombination aus epothilon-analog und chemotherapeutika zur behandlung von proliferativen erkrankungen |
| TWI287986B (en) * | 2001-12-13 | 2007-10-11 | Novartis Ag | Use of Epothilones for the treatment of the carcinoid syndrome |
-
2003
- 2003-10-09 BR BR0315169-7A patent/BR0315169A/pt not_active IP Right Cessation
- 2003-10-09 RU RU2005114018/14A patent/RU2005114018A/ru not_active Application Discontinuation
- 2003-10-09 WO PCT/US2003/032148 patent/WO2004032872A2/en not_active Ceased
- 2003-10-09 EP EP03773239A patent/EP1551378A4/en not_active Withdrawn
- 2003-10-09 CA CA002499682A patent/CA2499682A1/en not_active Abandoned
- 2003-10-09 MX MXPA05003706A patent/MXPA05003706A/es not_active Application Discontinuation
- 2003-10-09 AU AU2003279923A patent/AU2003279923A1/en not_active Abandoned
- 2003-10-09 JP JP2004543655A patent/JP2006504745A/ja active Pending
- 2003-10-09 CN CNB2003801009323A patent/CN1297258C/zh not_active Expired - Fee Related
- 2003-10-09 KR KR1020057006143A patent/KR20050051688A/ko not_active Withdrawn
-
2004
- 2004-05-03 US US10/683,203 patent/US20040167097A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000061142A1 (en) * | 1999-04-14 | 2000-10-19 | Dana-Farber Cancer Institute, Inc. | Method and composition for the treatment of cancer |
| JP2005513167A (ja) * | 2002-01-14 | 2005-05-12 | ノバルティス アクチエンゲゼルシャフト | エポシロン誘導体と代謝拮抗剤からなる組合せ |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019504893A (ja) * | 2016-02-06 | 2019-02-21 | ベイジン バイオスター テクノロジーズ， リミテッド | 脱エポキシ化エポチロン誘導体の製剤、その調製及び腫瘍の治療におけるその使用 |
| US10980782B2 (en) | 2016-02-06 | 2021-04-20 | Beijing Biostar Technologies, Ltd. | De-epoxidized epothilone derivative preparation, preparation of same and use thereof in the treatment of tumor |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2005114018A (ru) | 2006-01-20 |
| WO2004032872A2 (en) | 2004-04-22 |
| EP1551378A2 (en) | 2005-07-13 |
| AU2003279923A1 (en) | 2004-05-04 |
| WO2004032872A3 (en) | 2004-11-11 |
| EP1551378A4 (en) | 2006-09-06 |
| MXPA05003706A (es) | 2005-07-01 |
| KR20050051688A (ko) | 2005-06-01 |
| US20040167097A1 (en) | 2004-08-26 |
| CN1703208A (zh) | 2005-11-30 |
| CN1297258C (zh) | 2007-01-31 |
| BR0315169A (pt) | 2005-08-23 |
| CA2499682A1 (en) | 2004-04-22 |
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