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公开(公告)号:US07563787B2
公开(公告)日:2009-07-21
申请号:US11541484
申请日:2006-09-29
申请人: Xiao-Yi Xiao , Dinish V. Patel , John S. Ward , Mark R. Bray , Gregory E. Agoston , Anthony M. Treston
发明人: Xiao-Yi Xiao , Dinish V. Patel , John S. Ward , Mark R. Bray , Gregory E. Agoston , Anthony M. Treston
IPC分类号: A61K31/535 , C07D413/00
CPC分类号: C07D401/14 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D487/04
摘要: Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.
摘要翻译: 公开了蛋白激酶抑制剂,包含这种抑制剂的组合物及其使用方法。 更具体地,公开了Aurora A(Aurora-2)蛋白激酶的抑制剂。 还公开了治疗与蛋白激酶相关疾病,特别是与Aurora-2相关的疾病如癌症的方法。
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2.
公开(公告)号:US08114870B2
公开(公告)日:2012-02-14
申请号:US12494677
申请日:2009-06-30
申请人: Xiao-Yi Xiao , Dinish V. Patel , John S. Ward , Mark R. Bray , Gregory E. Agoston , Anthony M. Treston
发明人: Xiao-Yi Xiao , Dinish V. Patel , John S. Ward , Mark R. Bray , Gregory E. Agoston , Anthony M. Treston
IPC分类号: A61K31/535
CPC分类号: C07D401/14 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D487/04
摘要: Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.
摘要翻译: 公开了蛋白激酶抑制剂,包含这种抑制剂的组合物及其使用方法。 更具体地,公开了Aurora A(Aurora-2)蛋白激酶的抑制剂。 还公开了治疗与蛋白激酶相关疾病,特别是与Aurora-2相关的疾病如癌症的方法。
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3.
公开(公告)号:US20090264422A1
公开(公告)日:2009-10-22
申请号:US12494677
申请日:2009-06-30
申请人: Xiao-Yi Xiao , Dinish V. Patel , John S. Ward , Mark R. Bray , Gregory E. Agoston , Anthony M. Treston
发明人: Xiao-Yi Xiao , Dinish V. Patel , John S. Ward , Mark R. Bray , Gregory E. Agoston , Anthony M. Treston
IPC分类号: A61K31/541 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P3/10 , A61P25/00
CPC分类号: C07D401/14 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D487/04
摘要: Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.
摘要翻译: 公开了蛋白激酶抑制剂,包含这种抑制剂的组合物及其使用方法。 更具体地,公开了Aurora A(Aurora-2)蛋白激酶的抑制剂。 还公开了治疗与蛋白激酶相关疾病,特别是与Aurora-2相关的疾病如癌症的方法。
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公开(公告)号:US20080139535A1
公开(公告)日:2008-06-12
申请号:US12019356
申请日:2008-01-24
IPC分类号: A61K31/5513 , C07D417/02 , C07D243/14 , A61K31/445 , A61P35/00 , C07D401/02 , A61K31/497
CPC分类号: C07D277/56 , C07D277/42 , C07D417/04
摘要: Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.
摘要翻译: 公开了抑制组蛋白脱乙酰酶(HDAC)酶活性的化合物。 还公开了包含这些化合物的药物组合物以及至少部分由HDAC介导的治疗条件,特别是增殖病症的方法。
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公开(公告)号:US07772245B2
公开(公告)日:2010-08-10
申请号:US11354594
申请日:2006-02-14
IPC分类号: A61K31/506 , C07D471/02
CPC分类号: C07D471/04 , C07D401/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要: Disclosed are compounds of formula I that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein.
摘要翻译: 公开了抑制组蛋白脱乙酰酶(HDAC)酶活性的式I化合物,包含这些化合物的药物组合物以及至少部分由HDAC介导的条件,特别是增殖性病症的方法,其中A,W,W1,W2 ,Ar2和G。
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公开(公告)号:US20100090887A1
公开(公告)日:2010-04-15
申请号:US12580210
申请日:2009-10-15
申请人: Ken B. Cooper , Robert J. Dengler , Peter H. Siegel , Goutam Chattopadhyay , John S. Ward , Nuria Llombart Juan , Tomas E. Bryllert , Imran Mehdi , Jan A. Tarsala
发明人: Ken B. Cooper , Robert J. Dengler , Peter H. Siegel , Goutam Chattopadhyay , John S. Ward , Nuria Llombart Juan , Tomas E. Bryllert , Imran Mehdi , Jan A. Tarsala
IPC分类号: G01S13/90
CPC分类号: G01S13/89 , G01S7/024 , G01S7/03 , G01S7/35 , G01S13/34 , G01S13/87 , H01Q19/191 , H01Q19/195
摘要: A three-dimensional imaging radar operating at high frequency e.g., 670 GHz radar using low phase-noise synthesizers and a fast chirper to generate a frequency-modulated continuous-wave (FMCW) waveform, is disclosed that operates with a multiplexed beam to obtain range information simultaneously on multiple pixels of a target. A source transmit beam may be divided by a hybrid coupler into multiple transmit beams multiplexed together and directed to be reflected off a target and return as a single receive beam which is demultiplexed and processed to reveal range information of separate pixels of the target associated with each transmit beam simultaneously. The multiple transmit beams may be developed with appropriate optics to be temporally and spatially differentiated before being directed to the target. Temporal differentiation corresponds to a different intermediate frequencies separating the range information of the multiple pixels. Collinear transmit beams having differentiated polarizations may also be implemented.
摘要翻译: 公开了以高频率操作的三维成像雷达,例如使用低相位噪声合成器的670GHz雷达和用于产生调频连续波(FMCW)波形的快速啁啾声),其以多路波束操作以获得范围 信息同时在目标的多个像素上。 源发射波束可以被混合耦合器划分成多个复用在一起的多个发射波束并被引导为从目标反射并作为单个接收波束返回,该单个接收波束被解复用并被处理以显示与每个相关联的目标的单独像素的范围信息 同时发射波束。 多个发射光束可以用合适的光学器件显影,以在被引导到目标之前在时间和空间上被区分。 时间微分对应于分离多个像素的范围信息的不同中间频率。 也可以实现具有差分极化的共线发射波束。
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公开(公告)号:US07683097B2
公开(公告)日:2010-03-23
申请号:US11138636
申请日:2005-05-25
IPC分类号: C07C233/64 , C07D251/12 , C07D241/10 , C07D239/24 , C07D207/04 , C07D213/02 , C07D277/08 , C07D307/04 , A61K31/53 , A61K31/505 , A61K31/166 , A61K31/34 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/4965 , A61P35/00
CPC分类号: C07D213/40 , C07C63/72 , C07C63/74 , C07C233/78 , C07C233/81 , C07C233/83 , C07C233/84 , C07C239/22 , C07C243/38 , C07C271/20 , C07C291/04 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07D207/14 , C07D211/26 , C07D213/75 , C07D213/77 , C07D217/26 , C07D239/42 , C07D239/47 , C07D241/20 , C07D277/18 , C07D285/135 , C07D295/13 , C07D317/66 , C07D401/04
摘要: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.
摘要翻译: 本发明提供了有效抵抗拓扑异构酶(即拓扑异构酶I和/或拓扑异构酶II)的化合物。 这些化合物用于治疗细胞增殖性疾病。 在一些情况下,这些化合物具有抗癌活性,例如抗多药耐药性癌症。
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公开(公告)号:US5929247A
公开(公告)日:1999-07-27
申请号:US470790
申请日:1995-06-06
申请人: Charles A. Alt , Leander Merritt , Gary A. Rhodes , Roger L. Robey , Eldon E. Van Meter , John S. Ward , Charles H. Mitch
发明人: Charles A. Alt , Leander Merritt , Gary A. Rhodes , Roger L. Robey , Eldon E. Van Meter , John S. Ward , Charles H. Mitch
IPC分类号: C07D285/06 , A61K31/41 , A61K31/425 , A61K31/433 , A61K31/435 , A61K31/445 , A61K31/46 , A61P1/00 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P43/00 , C07D285/10 , C07D417/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D453/02 , C07D453/06 , C07D471/04 , C07D471/08 , C07D487/08
CPC分类号: C07D285/10 , C07D417/12 , C07D451/06 , C07D453/02 , C07D453/06 , C07D471/04 , C07D471/08 , C07D487/08
摘要: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
摘要翻译: 本发明涉及治疗活性的氮杂环或氮杂双环化合物,其制备方法和包含该化合物的药物组合物。 新型化合物可用于治疗由毒蕈碱胆碱能系统功能障碍引起的中枢神经系统疾病。
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公开(公告)号:US5821370A
公开(公告)日:1998-10-13
申请号:US470787
申请日:1995-06-06
申请人: Charles A. Alt , Leander Merritt , Gary A. Rhodes , Roger L. Robey , Eldon E. Van Meter , John S. Ward
发明人: Charles A. Alt , Leander Merritt , Gary A. Rhodes , Roger L. Robey , Eldon E. Van Meter , John S. Ward
IPC分类号: C07D285/06 , A61K31/41 , A61K31/425 , A61K31/433 , A61K31/435 , A61K31/445 , A61K31/46 , A61P1/00 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P43/00 , C07D285/10 , C07D417/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D453/02 , C07D453/06 , C07D471/04 , C07D471/08 , C07D487/08
CPC分类号: C07D285/10 , C07D417/12 , C07D451/06 , C07D453/02 , C07D453/06 , C07D471/04 , C07D471/08 , C07D487/08
摘要: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
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公开(公告)号:US06194416B1
公开(公告)日:2001-02-27
申请号:US08844307
申请日:1997-04-10
申请人: Leander Merritt , Jon K. Reel , John S. Ward , Celia A. Whitesitt
发明人: Leander Merritt , Jon K. Reel , John S. Ward , Celia A. Whitesitt
IPC分类号: A61K31496
CPC分类号: C07D451/06 , C07D209/52 , C07D241/18 , C07D271/08 , C07D403/12 , C07D413/12 , C07D453/02 , C07D471/08 , C07D487/08
摘要: The present invention relates to therapeutically active compounds of the formula: wherein G is an azacyclic or azabicyclic ring system, W is oxygen or sulfur, r is 0, 1, or 2, and R is defined in the specification; and to methods of treatment using, and pharmaceutical compositions comprising, these compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
摘要翻译: 本发明涉及下式的治疗活性化合物:其中G是氮杂环或氮杂双环系,W是氧或硫,r是0,1或2,R在说明书中定义; 以及使用这些化合物的治疗方法和药物组合物。 新型化合物可用于治疗由毒蕈碱胆碱能系统功能障碍引起的中枢神经系统疾病。
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