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公开(公告)号：US08927597B2
公开(公告)日：2015-01-06
申请号：US13735516
申请日：2013-01-07
申请人： Atsushi Endo , Charles E. Chase , Francis G. Fang
发明人： Atsushi Endo , Charles E. Chase , Francis G. Fang
IPC分类号： A61K31/351 , C07D407/00 , C07D405/06 , C07D407/06 , C07D493/04 , C07D405/12
CPC分类号： C07F7/1804 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55
摘要： In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
摘要翻译： 通常，本发明的特征在于可用于合成软骨素B的类似物的化合物，例如胡椒素或其药学上可接受的盐，例如甲磺酸埃布林。 示例性化合物具有式（I），（II）或（III）：
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![Crystalline 1H-imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate and its pharmaceutical uses](/abs-image/US/2010/02/02/US07655800B2/abs.jpg.150x150.jpg)
2.发明授权Crystalline 1H-imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate and its pharmaceutical uses 失效结晶的1H-咪唑并[4,5-b]吡啶-5-胺，7- [5 - [（环己基甲基氨基） - 甲基] -1H-吲哚-2-基] -2-甲基硫酸盐（1:1） 三水合物及其制药用途公开(公告)号：US07655800B2
公开(公告)日：2010-02-02
申请号：US11344534
申请日：2006-02-01
申请人： Charles E. Chase , Ikuo Kushida
发明人： Charles E. Chase , Ikuo Kushida
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to crystalline 1H-Imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate, E6070, its method of preparation, and its therapeutic uses. Pharmaceutical compositions containing crystalline E6070 and a pharmaceutically acceptable carrier represent one embodiment of the invention. The invention also relates to methods for treating an inflammatory disorder, an autoimmune disorder, or a proliferative disorder comprising the step of administering to a patient in need thereof a therapeutically effective amount of crystalline E6070.
摘要翻译： 本发明涉及结晶1H-咪唑并[4,5-b]吡啶-5-胺，7- [5 - [（环己基甲基氨基）甲基] -1H-吲哚-2-基] -2-甲基硫酸盐（1 ：1），三水合物，E6070，其制备方法及其治疗用途。 含有结晶E6070和药学上可接受的载体的药物组合物代表本发明的一个实施方案。 本发明还涉及用于治疗炎症性疾病，自身免疫性疾病或增殖性疾病的方法，包括向有需要的患者施用治疗有效量的结晶E6070的步骤。
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公开(公告)号：US08445701B2
公开(公告)日：2013-05-21
申请号：US13476276
申请日：2012-05-21
申请人： Brian Austad , Charles E. Chase , Francis G. Fang , Marc Pesant
发明人： Brian Austad , Charles E. Chase , Francis G. Fang , Marc Pesant
IPC分类号： C07F7/02
CPC分类号： C07F7/1804 , A61K31/341 , C07C33/423 , C07D307/12 , C07D307/28 , C07D307/33 , C07D317/72 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/18 , C07D493/20 , C07D493/22 , C07F7/188 , C07H15/26 , Y02P20/55
摘要： Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
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公开(公告)号：US08350067B2
公开(公告)日：2013-01-08
申请号：US13477483
申请日：2012-05-22
申请人： Atsushi Endo , Charles E. Chase , Francis G. Fang
发明人： Atsushi Endo , Charles E. Chase , Francis G. Fang
IPC分类号： C07D307/20
CPC分类号： C07F7/1804 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55
摘要： In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
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公开(公告)号：US20120309988A1
公开(公告)日：2012-12-06
申请号：US13476276
申请日：2012-05-21
申请人： Brian Austad , Charles E. Chase , Francis G. Fang , Marc Pesant
发明人： Brian Austad , Charles E. Chase , Francis G. Fang , Marc Pesant
IPC分类号： C07F7/08 , C07D307/20
CPC分类号： C07F7/1804 , A61K31/341 , C07C33/423 , C07D307/12 , C07D307/28 , C07D307/33 , C07D317/72 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/18 , C07D493/20 , C07D493/22 , C07F7/188 , C07H15/26 , Y02P20/55
摘要： Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided.
摘要翻译： 提供了中间体及其在软骨素B的合成中的应用。
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公开(公告)号：US20120289718A1
公开(公告)日：2012-11-15
申请号：US13477483
申请日：2012-05-22
申请人： Atsushi ENDO , Charles E. CHASE , Francis G. FANG
发明人： Atsushi ENDO , Charles E. CHASE , Francis G. FANG
IPC分类号： C07D407/06
CPC分类号： C07F7/1804 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55
摘要： In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
摘要翻译： 通常，本发明的特征在于可用于合成软骨素B的类似物的化合物，例如胡椒素或其药学上可接受的盐，例如甲磺酸埃布林。 示例性化合物具有式（I），（II）或（III）：
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公开(公告)号：US08203010B2
公开(公告)日：2012-06-19
申请号：US13014517
申请日：2011-01-26
申请人： Atsushi Endo , Charles E. Chase , Francis G. Fang
发明人： Atsushi Endo , Charles E. Chase , Francis G. Fang
IPC分类号： C07D311/94
CPC分类号： C07F7/1804 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55
摘要： In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
摘要翻译： 通常，本发明的特征在于可用于合成软骨素B的类似物的化合物，例如胡椒素或其药学上可接受的盐，例如甲磺酸埃布林。 示例性化合物具有式（I），（II）或（III）：
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公开(公告)号：US4639697A
公开(公告)日：1987-01-27
申请号：US650019
申请日：1984-09-13
CPC分类号： H03H9/02834 , H03H9/68
摘要： A surface acoustic wave (SAW) device provides a phase shift and a first predetermined phase shift variation as a function of temperature. A passive network including a passive, reactive component is thermally and electrically coupled to the SAW device. An electrical characteristic of the component has a predetermined variation as a function of the temperature of the reactive component which provides the network with a second, predetermined phase variation as a function of temperature to compensate for the first predetermined phase variation as a function of temperature provided from the surface acoustic wave device. With this arrangement, the phase shift provided from the surface acoustic wave device is substantially invariant with temperature.
摘要翻译： 表面声波（SAW）装置提供相移和作为温度的函数的第一预定相移变化。 包括无源的无源分量的无源网络热和电耦合到SAW器件。 组件的电特性具有作为无功部件的温度的函数的预定变化，其提供作为温度的函数的第二预定相位变化的网络，以补偿作为提供的温度的函数的第一预定相位变化 从声表面波装置。 通过这种布置，从表面声波装置提供的相移基本上与温度不变。
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9.发明申请公开(公告)号：US20190161495A1
公开(公告)日：2019-05-30
申请号：US16313196
申请日：2017-06-30
申请人： Charles E. Chase , Hyeong-Wook CHOI , Atsushi ENDO , Francis G. FANG , Dae-Shik KIM , EISAI R&D MANAGEMENT CO., LTD.
IPC分类号： C07D493/22
摘要： The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
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10.发明申请公开(公告)号：US20180118755A1
公开(公告)日：2018-05-03
申请号：US15571921
申请日：2016-05-09
IPC分类号： C07D493/22 , C07F9/655
CPC分类号： C07D493/22 , C07F9/6552
摘要： The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
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