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61.发明公开
公开(公告)号：EP3231798A1
公开(公告)日：2017-10-18
申请号：EP17168722.1
申请日：2008-06-30
发明人： CHEN, Weirong , COSSROW, Jennifer , FRANKLIN, Lioyd , GUAN, Bing , JONES, John, Howard , KUMARAVEL, Gnanasambandam , LANE, Benjamin , LITTKE, Adam , LUGOVSKOY, Alexey , PENG, Hairuo , POWELL, Noel , RAIMUNDO, Brian , TANAKA, Hiroko , VESSELS, Jeffrey , WYNN, Thomas , XIN, Zhili
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , A61K31/506 , A61P29/00 , A61P35/00
摘要： The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
摘要翻译： 本发明提供可用作Raf蛋白激酶抑制剂的化合物。 本发明还提供了其组合物和治疗Raf介导的疾病的方法。
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62.发明公开METHODS OF USING (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID IN COMBINATION THERAPY 审中-公开使用方法（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基） - -1,8-二氮杂萘-3-羧酸在组合疗法
公开(公告)号：EP3141250A1
公开(公告)日：2017-03-15
申请号：EP16177763.6
申请日：2008-10-21
IPC分类号： A61K31/282 , A61K31/4178 , A61K31/4375 , A61K31/555 , A61P35/00 , A61K31/7068 , A61K33/24
CPC分类号： A61K31/4375 , A61K9/0019 , A61K31/282 , A61K31/555 , A61K31/7068 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： Methods of treating cancers are disclosed. The methods encompass the administration of SNS-595 in combination with cisplatin and carboplatin.
摘要翻译： 治疗癌症的方法是游离缺失盘。 该方法包括在用顺铂和卡铂组合SNS-595的给药。
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63.发明公开BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY 有权用于治疗肿瘤，神经学和免疫学中的人类疾病的双芳基化合物
公开(公告)号：EP3080103A1
公开(公告)日：2016-10-19
申请号：EP14825001.2
申请日：2014-12-11
发明人： HOPKINS, Brian, T. , MA, Bin , CHAN, Timothy, Raymond , SUN, Lihong , ZHANG, Lei , KUMARAVEL, Gnanasambandam , LYSSIKATOS, Joseph, P. , KOCH, Kevin , MIAO, Hua
IPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07D513/04 , A61K31/44 , A61K31/505 , A61K31/506 , A61P25/02 , A61P35/00 , A61P37/00
CPC分类号： C07D403/12 , A61K31/506 , C07D239/30 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D495/04 , C07D513/04 , C07F5/027
摘要： The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
摘要翻译： 本发明提供了可用作布鲁顿酪氨酸激酶抑制剂并表现出其所需特性的化合物及其组合物。
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64.发明授权(+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID IN COMBINATION WITH GEMCITABINE FOR USE IN TREATING CANCER 有权（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基）-1,8- 萘啶-3-羧酸在组合疗法中用于癌症吉西他滨的治疗
公开(公告)号：EP2214662B1
公开(公告)日：2016-07-13
申请号：EP08843165.5
申请日：2008-10-21
IPC分类号： A61K31/282 , A61K31/4178 , A61K31/4375 , A61K31/555 , A61P35/00
CPC分类号： A61K31/4375 , A61K9/0019 , A61K31/282 , A61K31/555 , A61K31/7068 , A61K33/24 , A61K45/06 , A61K2300/00
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65.发明授权COMBINED USE OF (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID AND CYTARABINE (ARA-C) FOR THE TREATMENT OF LEUKEMIA 有权组合使用的（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基）-1- ，8-萘啶-3-羧酸和阿糖胞苷（ARA-C）以治疗白血病
公开(公告)号：EP2049109B1
公开(公告)日：2015-11-18
申请号：EP07811049.1
申请日：2007-08-02
IPC分类号： A61K31/4375 , A61K31/513 , A61P35/02
CPC分类号： A61K31/4375 , A61K31/513 , A61K31/7068 , C07D417/14 , A61K2300/00
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公开(公告)号：EP2473507B1
公开(公告)日：2014-03-19
申请号：EP10759761.9
申请日：2010-09-03
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D471/04 , A61K31/4375 , C07D417/04 , C07D417/14
摘要： Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.
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67.发明公开Stable SNS-595 compositions and methods of preparation 审中-公开Stabile SNS-595-Zusammensetzungen und Herstellungsverfahrendafür
公开(公告)号：EP2674431A1
公开(公告)日：2013-12-18
申请号：EP13184180.1
申请日：2010-09-03
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D471/04 , A61K31/4375 , C07D417/04 , C07D417/14
摘要： Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.
摘要翻译： 公开了制备基本上纯的SNS-595物质的方法。 还提供了包含基本上纯的且基本上不含可见颗粒的SNS-595物质的组合物。
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68.发明公开(+)-1,4-dihydro-7-[(3s,4s)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid for use in the treatment of antecedent hematologic disorders 审中-公开（+）-1,4-二氢-7- [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基）-1,8- 萘-3-羧酸用于遗传性疾病的治疗中，血液学
公开(公告)号：EP2649997A1
公开(公告)日：2013-10-16
申请号：EP13166632.3
申请日：2008-12-10
发明人： Michelson, Glenn
IPC分类号： A61K31/4375 , A61K31/513 , A61P35/02 , A61K45/06
CPC分类号： A61K31/4375 , A61K31/513 , A61K31/706 , A61K31/7068 , A61K38/18 , A61K38/19 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2039/54 , C07D471/04 , A61K2300/00
摘要： The invention provides SNS-595 for use in a method of treating myelodysplastic syndrome, including chronic myelomonocytic leukemia. The treatment with SNS-595 may be combined with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the treatment comprises administering SNS-595 in combination with cytarabine. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.
摘要翻译： 本发明提供了SNS-595用于治疗骨髓增生异常综合征，慢性骨髓性白血病的方法，包括使用。 用SNS-595治疗可以与化学疗法，放射疗法，激素疗法，生物疗法或免疫疗法进行组合。 在某些实施方案中，治疗包括给予SNS-595与阿糖胞苷组合。 药物组合物和适用于本方法中使用的单一单位剂型是如此游离缺失盘。
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公开(公告)号：EP2038272A4
公开(公告)日：2011-01-05
申请号：EP07810166
申请日：2007-07-02
发明人： LIND KENNETH EGNARD , CAO KATHY , LIN EDWARD YIN-SHIANG , NGUYEN THINH BA , TANGONAN BRADLEY T , ERLANSON DANIEL A , GUCKIAN KEVIN , SIMMONS ROBERT LOWELL , LEE WEN-CHERNG , SUN LIHONG , HANSEN STIG , PATHAN NUZHAT , ZHANG LEI
IPC分类号： C07D401/12
CPC分类号： C07D471/04 , A61K31/4412 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D211/86 , C07D213/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
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公开(公告)号：EP2257637A1
公开(公告)日：2010-12-08
申请号：EP09724229.1
申请日：2009-03-25
发明人： HANSEN, Stig , ERLANSON, Dan , CANCILLA, Mark
IPC分类号： C12Q1/48 , G01N33/531 , C40B50/04 , C40B30/04
CPC分类号： G01N33/531 , C12Q1/485
摘要： Herein is described a method to rapidly screen a large chemical space for a compound that binds to a target protein through an iterative fragment assembly approach that can be performed at low reagent cost and without requiring purification of the assembled product. The method employs a library of test ligands each of which comprise a 'bait' molecule, which is known from prior art or prior screening to have some intrinsic affinity for the target protein, and a test moiety.
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