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公开(公告)号：US08518942B2
公开(公告)日：2013-08-27
申请号：US13056283
申请日：2009-08-06
IPC分类号： A61K31/41 , A61K31/53 , C07D249/00
CPC分类号： G06Q30/0627 , C07D249/04 , C07D405/12
摘要： This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6.
摘要翻译： 本发明提供了可用于预防或治疗许多病症的新型胱天蛋白酶抑制剂，包括例如亨廷顿氏病。 在某些实施方案中，抑制剂包括casepase-3和/或casepase-6的抑制剂。
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公开(公告)号：US08476451B2
公开(公告)日：2013-07-02
申请号：US12669364
申请日：2008-07-21
IPC分类号： A61K31/426 , A61K31/427 , C07D277/30 , A01N43/78
CPC分类号： A61K38/07 , C07D277/28 , C07D277/30 , C07D277/56 , C07D417/12
摘要： The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
摘要翻译： 本发明提供新型的微管蛋白酶类似物，制备方法以及使用其类似物和缀合物的方法。 本发明的化合物是高度有效的细胞生长抑制剂，其已被开发出比管状蛋白D更小和更稳定。
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3.发明授权Detection of protease and protease activity using a single nanoscrescent SERS probe 有权使用单个纳米SERS探针检测蛋白酶和蛋白酶活性公开(公告)号：US08361932B2
公开(公告)日：2013-01-29
申请号：US12299284
申请日：2007-05-02
IPC分类号： C40B30/04 , C40B40/10 , G01N33/573
CPC分类号： C12Q1/37 , G01N33/57434 , G01N33/587 , G01N2333/96433 , G01N2333/96466 , G01N2333/974
摘要： This invention pertains to the in vitro detection of proteases using a single peptide-conjugate nanocrescent surface enhanced Raman scattering (SERS) probes with at least nanomolar sensitivity. The probe enables detection of proteolytic activity in extremely small volume and at low concentration. In certain embodiments the probes comprise an indicator for the detection of an active protease, where the indicator comprises a nanocrescent attached to a peptide, where said peptide comprises a recognition site for the protease and a Raman tag attached to the peptide.
摘要翻译： 本发明涉及使用具有至少纳摩尔灵敏度的单个肽 - 缀合的纳米新月面增强拉曼散射（SERS）探针的体外检测蛋白酶。 该探针能够以非常小的体积和低浓度检测蛋白水解活性。 在某些实施方案中，探针包含用于检测活性蛋白酶的指示剂，其中指示剂包含连接到肽的纳米新月形，其中所述肽包含蛋白酶的识别位点和与肽连接的拉曼标签。
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公开(公告)号：US20090287004A1
公开(公告)日：2009-11-19
申请号：US12509985
申请日：2009-07-27
IPC分类号： C07D307/06 , C07C29/00 , C07C1/207 , C07C51/00
摘要： A method of preparing an olefin comprising: reacting a polyol in the presence of a carboxylic acid, such that an olefin is produced by the deoxygenation of the polyol. The reacting step can comprise (a) providing a composition comprising the polyol, (b) heating the composition, and (c) introducing the carboxylic acid to the composition wherein the introducing step occurs prior to, at the same time as, or subsequent to the heating step. In one embodiment, the polyol is glycerol, the carboxylic acid is formic acid, and the olefin is allyl alcohol, which is produced at a yield of about 80% or greater.
摘要翻译： 一种制备烯烃的方法，包括：在羧酸存在下使多元醇反应，使得通过多元醇的脱氧生成烯烃。 反应步骤可以包括（a）提供包含多元醇的组合物，（b）加热组合物，和（c）将羧酸引入到组合物中，其中引入步骤在同时或之后 加热步骤。 在一个实施方案中，多元醇是甘油，羧酸是甲酸，烯烃是以约80％或更高的产率生产的烯丙醇。
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5.发明授权
公开(公告)号：US5545568A
公开(公告)日：1996-08-13
申请号：US161677
申请日：1993-12-02
申请人： Jonathan A. Ellman
发明人： Jonathan A. Ellman
IPC分类号： A61K49/00 , B01J19/00 , C07C405/00 , C07D243/24 , C07K5/078 , C40B50/14 , C40B60/14 , G01N33/543
CPC分类号： B82Y30/00 , A61K49/0004 , B01J19/0046 , C07C405/00 , C07D243/24 , C07K5/06139 , C40B80/00 , B01J2219/00315 , B01J2219/00432 , B01J2219/00454 , B01J2219/005 , B01J2219/00504 , B01J2219/00527 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00626 , B01J2219/00659 , B01J2219/00711 , B01J2219/0072 , C40B50/14 , C40B60/14
摘要： Methods, compositions, and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, .beta.-turn mimetics and glycerol-derived drugs is described. In order to expediently synthesize such combinatorial libraries of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.
摘要翻译： 描述了用于合成各种有用化合物的组合文库的方法，组合物和装置，例如苯并二氮杂，前列腺素，β-转角模拟物和甘油衍生药物。 为了方便合成基于这些核心结构的衍生物组合文库，还提供了这些衍生物的固相合成的一般方法。 因此，本公开内容还描述了固相合成方法对非聚合有机化合物的重要延伸。
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公开(公告)号：US08273926B2
公开(公告)日：2012-09-25
申请号：US12509985
申请日：2009-07-27
摘要： A method of preparing an olefin comprising: reacting a polyol in the presence of a carboxylic acid, such that an olefin is produced by the deoxygenation of the polyol. The reacting step can comprise (a) providing a composition comprising the polyol, (b) heating the composition, and (c) introducing the carboxylic acid to the composition wherein the introducing step occurs prior to, at the same time as, or subsequent to the heating step. In one embodiment, the polyol is glycerol, the carboxylic acid is formic acid, and the olefin is allyl alcohol, which is produced at a yield of about 80% or greater.
摘要翻译： 一种制备烯烃的方法，包括：在羧酸存在下使多元醇反应，使得通过多元醇的脱氧生成烯烃。 反应步骤可以包括（a）提供包含多元醇的组合物，（b）加热组合物，和（c）将羧酸引入到组合物中，其中引入步骤在同时或之后 加热步骤。 在一个实施方案中，多元醇是甘油，羧酸是甲酸，烯烃是以约80％或更高的产率生产的烯丙醇。
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公开(公告)号：US20110230527A1
公开(公告)日：2011-09-22
申请号：US13056283
申请日：2009-08-06
IPC分类号： A61K31/4192 , C07D249/04 , C07D405/12 , C12Q1/37 , A61P25/28
CPC分类号： G06Q30/0627 , C07D249/04 , C07D405/12
摘要： This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6.
摘要翻译： 本发明提供了可用于预防或治疗许多病症的新型胱天蛋白酶抑制剂，包括例如亨廷顿氏病。 在某些实施方案中，抑制剂包括casepase-3和/或casepase-6的抑制剂。
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公开(公告)号：US20110021568A1
公开(公告)日：2011-01-27
申请号：US12669364
申请日：2008-07-21
IPC分类号： A61K31/426 , C07D401/12 , A61K31/454 , A61P35/00
CPC分类号： A61K38/07 , C07D277/28 , C07D277/30 , C07D277/56 , C07D417/12
摘要： The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
摘要翻译： 本发明提供新型的微管蛋白酶类似物，制备方法以及使用其类似物和缀合物的方法。 本发明的化合物是高度有效的细胞生长抑制剂，其已被开发出比管状蛋白D更小和更稳定。
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9.发明申请DETECTION OF PROTEASE AND PROTEASE ACTIVITY USING A SINGLE NANOSCRESCENT SERS PROBE 有权使用单个纳米粒子探针检测蛋白质和蛋白酶活性公开(公告)号：US20100048412A1
公开(公告)日：2010-02-25
申请号：US12299284
申请日：2007-05-02
IPC分类号： C40B30/04 , G01N33/573 , C40B40/10
CPC分类号： C12Q1/37 , G01N33/57434 , G01N33/587 , G01N2333/96433 , G01N2333/96466 , G01N2333/974
摘要： This invention pertains to the in vitro detection of proteases using a single peptide-conjugate nanocrescent surface enhanced Raman scattering (SERS) probes with at least nanomolar sensitivity. The probe enables detection of proteolytic activity in extremely small volume and at low concentration. In certain embodiments the probes comprise an indicator for the detection of an active protease, where the indicator comprises a nanocrescent attached to a peptide, where said peptide comprises a recognition site for the protease and a Raman tag attached to the peptide.
摘要翻译： 本发明涉及使用具有至少纳摩尔灵敏度的单个肽 - 缀合的纳米新月面增强拉曼散射（SERS）探针的体外检测蛋白酶。 该探针能够以非常小的体积和低浓度检测蛋白水解活性。 在某些实施方案中，探针包含用于检测活性蛋白酶的指示剂，其中指示剂包含连接到肽的纳米新月形，其中所述肽包含蛋白酶的识别位点和与肽连接的拉曼标签。
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公开(公告)号：US07629437B2
公开(公告)日：2009-12-08
申请号：US10686884
申请日：2003-10-15
CPC分类号： C12Q1/37 , C07K1/047 , C07K5/101 , C07K5/1024
摘要： A method is presented for the preparation and use of fluorogenic peptide substrates that allows for the configuration of general substrate libraries to rapidly identify the primary and extended specificity of enzymes, such as proteases. The substrates contain a fluorogenic-leaving group, such as 7-amino-4-carbamoylmethyl-coumarin (ACC). Substrates incorporating the ACC leaving group show comparable kinetic profiles as those with the traditionally used 7-amino-4-methyl-coumarin (AMC) leaving group. The bifunctional nature of ACC allows for the efficient production of single substrates and substrate libraries using solid-phase synthesis techniques.
摘要翻译： 提出了一种用于制备和使用荧光肽底物的方法，其允许构建一般底物文库以快速鉴定酶（例如蛋白酶）的主要和延伸的特异性。 底物含有荧光离去基团，如7-氨基-4-氨基甲酰甲基香豆素（ACC）。 结合ACC离去基团的底物显示与传统使用的7-氨基-4-甲基香豆素（AMC）离去基团相似的动力学曲线。 ACC的双功能特性允许使用固相合成技术有效地生产单个底物和底物文库。
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