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1. 发明申请

WO2007027742A2 SMALL MOLECULE INTEGRIN α2βl/GPIa-IIa ANTAGONISTS 审中-公开
标题翻译：小分子整合素α2β1/ GPIa-IIa拮抗剂
公开(公告)号：WO2007027742A2
公开(公告)日：2007-03-08
申请号：PCT/US2006/033819
申请日：2006-08-29
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , CHOI, Sungwook , SNYDER, Seth, E. , DEGRADO, William, F. , BENNETT, Joel, S.
发明人： CHOI, Sungwook , SNYDER, Seth, E. , DEGRADO, William, F. , BENNETT, Joel, S.
IPC分类号： A61K38/04
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/06113 , C07K5/06191
摘要： Novel compounds inhibiting the integrin α2βl /GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic uses. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2βl/GPIa-IIa-mediated activity.
摘要翻译：公开了抑制整联蛋白a2β1/ GPIa-IIa受体的新型化合物。还公开了含有这些化合物的药物组合物及其治疗用途的方法。所公开的化合物尤其可用作整联蛋白a2β1/ GPIa-IIa介导活性的抑制剂。

2. 发明申请

WO2006133338A1 INHIBITORS OF THE α2β1/GPIa-IIa INTEGRIN 审中-公开
标题翻译： a2β1/ GPIa-IIa INTEGRIN的抑制剂
公开(公告)号：WO2006133338A1
公开(公告)日：2006-12-14
申请号：PCT/US2006/022225
申请日：2006-06-07
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNESYLVANIA , DEGRADO, William, F. , BENNETT, Joel, S. , SNYDER, Seth, Elliot , CHOI, Sungwook
发明人： DEGRADO, William, F. , BENNETT, Joel, S. , SNYDER, Seth, Elliot , CHOI, Sungwook
IPC分类号： A61K38/00
CPC分类号： C07D207/48 , C07D211/96 , C07D277/06 , C07K5/06165
摘要： Novel compounds inhibiting the integrin α2βl/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2βl/GPIa-IIa-mediated activity.
摘要翻译：公开了抑制整联蛋白a2β1/ GPIa-IIa受体的新型化合物。还公开了含有这些化合物的药物组合物及其治疗用途的方法。所公开的化合物尤其可用作整联蛋白a2β1/ GPIa-IIa介导活性的抑制剂。

3. 发明公开

EP1535235A1 METHODS, SYSTEMS, AND COMPUTER PROGRAM PRODUCTS FOR COMPUTATIONAL ANALYSIS AND DESIGN OF AMPHIPHILIC POLYMERS 审中-公开
标题翻译：方法，系统和计算机程序产品进行分析和概念上的两亲聚合物的设计
公开(公告)号：EP1535235A1
公开(公告)日：2005-06-01
申请号：EP03755525.7
申请日：2003-05-28
申请人： The Trustees of The University of Pennsylvania , Chen, Bin , Klein, Michael L. , Degrado, William F.
发明人： DOERKSEN, Robert,J. , CHEN, Bin , KLEIN, Michael, L. , DEGRADO, William, F.
IPC分类号： G06G7/48
CPC分类号： G06F19/701
摘要： Methods, systems, and computer program products for computational polymer processing including, without limitation, computational amphiphilic polymer design, conformational energy minimization, generation and refinement of torsional parameters for sub-units of potential polymers, generation of modified force field parameters, and prediction of conformational information for potential polymers. The predicted conformational information is then used to select one or more of the target polymer backbones as candidate amphiphilic polymer backbones for synthesis.

4. 发明申请

WO2008005470A3 POLYPEPTIDES THAT BIND MEMBRANE PROTEINS 审中-公开
公开(公告)号：WO2008005470A3
公开(公告)日：2008-01-10
申请号：PCT/US2007/015425
申请日：2007-06-29
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , SLUSKY, Joanna, S. , YIN, Hang , DEGRADO, William, F.
发明人： SLUSKY, Joanna, S. , YIN, Hang , DEGRADO, William, F.
IPC分类号： A01N37/18 , A61K38/00
摘要： Polypeptides which bind to the helical transmembrane region of membrane proteins are disclosed, as are methods for the design of polypeptides that bind to the transmembrane region of membrane proteins. Also provided are methods for the use of the disclosed polypeptides in various applications, as well as products made through the practice of the instant methods.

5. 发明申请

WO2010033339A1 INHIBITION OF INFLUENZA M2 PROTON CHANNEL 审中-公开
标题翻译：抑制流感M2原子通道
公开(公告)号：WO2010033339A1
公开(公告)日：2010-03-25
申请号：PCT/US2009/054603
申请日：2009-08-21
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , DEGRADO, William, F. , WANG, Jun
发明人： DEGRADO, William, F. , WANG, Jun
IPC分类号： A61K31/58
CPC分类号： C07D409/06 , A61K31/438 , A61K31/4465 , C07D211/08 , C07D401/04 , C07D401/06 , C07D413/06
摘要： Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
摘要翻译：提供能够通过与M2跨膜蛋白相互作用来调节甲型流感病毒的活性的化合物。还提供了用于治疗受甲型流感感染的疾病状态或感染的方法，其包括施用包含一种或多种已被鉴定为能够与M2蛋白相互作用的化合物的组合物。

6. 发明申请

WO2010033340A1 INFLUENZA A VIRUS INHIBITION 审中-公开
标题翻译：流感病毒感染
公开(公告)号：WO2010033340A1
公开(公告)日：2010-03-25
申请号：PCT/US2009/054608
申请日：2009-08-21
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , DEGRADO, William, F. , WANG, Jun
发明人： DEGRADO, William, F. , WANG, Jun
IPC分类号： A61K31/58
CPC分类号： C07D409/06 , A61K31/438 , A61K31/4465 , C07D211/08 , C07D401/04 , C07D401/06 , C07D413/06
摘要： Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
摘要翻译：提供的是能够通过与M2跨膜蛋白的相互作用来调节甲型流感病毒的活性的化合物。还提供了用于治疗感染A型流感的疾病状态或感染的方法，其包括施用包含已被鉴定为能够与M2蛋白相互作用的一种或多种化合物的组合物。

7. 发明申请

WO2010019712A1 MODULATION OF INFLUENZA VIRUS 审中-公开
标题翻译：流感病毒调控
公开(公告)号：WO2010019712A1
公开(公告)日：2010-02-18
申请号：PCT/US2009/053612
申请日：2009-08-12
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , DEGRADO, William, F. , STOUFFER, Amanda, L. , ACHARYA, Rudresh , SALOM-ARBONA, David , POLISHCHUK, Alexei
发明人： DEGRADO, William, F. , STOUFFER, Amanda, L. , ACHARYA, Rudresh , SALOM-ARBONA, David , POLISHCHUK, Alexei
IPC分类号： C40B30/02
CPC分类号： G06F19/706 , G06F19/16
摘要： The present invention provides, among other things, methods for the identification of compounds that are capable of modulating the activity of the influenza A virus. For example, the present methods provide platforms for identifying small molecule inhibitors that target the proton transport pathway defined at least in part by two or more of the highly conserved channel residues 27, 30, 31, 34, 37, 41, 44, and 45 of the influenza A M2 protein. In one aspect, the present invention is directed to methods comprising comparing spatial models of a plurality of test compounds with the spatial model of the pathway defined by at least two residues from among residues 27, 30, 31, 34, 37 or 41, 44, and 45 on one or more subunits of the M2 transmembrane protein of the influenza A virus to determine the spatial complementarity of each of the test compounds with the pathway; assessing the ability of the test compounds to bind to the pathway; and, based on the assessed ability of the test compounds to bind the pathway, determining the compound that modulates the activity of influenza A.
摘要翻译：本发明尤其提供了用于鉴定能够调节甲型流感病毒活性的化合物的方法。例如，本方法提供用于鉴定靶向至少部分由两个或更多个高度保守通道残基27,30,31,34,37,41,44和45定义的质子转运途径的小分子抑制剂的平台的流感A M2蛋白。在一个方面，本发明涉及包括将多个测试化合物的空间模型与由残基27,30,31,34,37或41,44中的至少两个残基限定的途径的空间模型进行比较的方法和45个在甲型流感病毒的M2跨膜蛋白的一个或多个亚基上，以确定每种测试化合物与途径的空间互补性; 评估测试化合物结合途径的能力; 并且基于测试化合物结合途径的评估能力，确定调节流感A的活性的化合物。

8. 发明申请

WO2004065363A2 COMPUTATIONAL DESIGN OF A WATER-SOLUBLE ANALOG OF A PROTEIN, SUCH AS PHOSPHOLAMBAN AND POTASSIUM CHANNEL KCSA 审中-公开
标题翻译：蛋白质水溶性模拟物的计算设计，如磷酰胺和钾通道KCSA
公开(公告)号：WO2004065363A2
公开(公告)日：2004-08-05
申请号：PCT/US2004/001317
申请日：2004-01-21
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , SAVEN, Jeffrery, G. , DEGRADO, William, F. , SLOVIC, Avram, M. , SUMMA, Christopher, M. , KONO, Hidetoshi
发明人： SAVEN, Jeffrery, G. , DEGRADO, William, F. , SLOVIC, Avram, M. , SUMMA, Christopher, M. , KONO, Hidetoshi
IPC分类号： C07D
CPC分类号： G06F19/16 , G06F19/18
摘要： Membrane proteins and water-soluble proteins share a similar core. This similarity suggests that it should be possible to water-solubilize membrane proteins by mutating only their lipid-exposed residues. Computational tools and methods are disclosed herein that can be used to design water-soluble variants of helical membrane proteins, using the pentameric phospholamban (PLB) and potassium channel KcsA as models. To water-solublize PLB, the membrane-exposed positions were changed to polar or charged amino acids, while the putative core was left unaltered. We generated water-soluble phospholamban (WSPLB), and compared its properties to its predecessor PLB. As a probe of the correctness of the fold of the water soluble KcsA, the computationally designed proteins contain an agitoxin-2 binding site from a mammalian homologue of the channel. The resulting proteins express in high yield in E. coli and share the intended functional and structural properties with KcsA, including secondary structure, tetrameric quaternary structure, and tight, specific binding to both agitoxin2 and a small molecule channel blocker.
摘要翻译：膜蛋白和水溶性蛋白质共享相似的核心。这种相似性表明，应该可以通过仅突变其暴露于脂质的残留物来水溶性膜蛋白。本文公开了可用于设计螺旋膜蛋白质的水溶性变体的计算工具和方法，其使用五聚磷酸甘油（PLB）和钾通道KcsA作为模型。为了水解PLB，将膜暴露的位置改为极性或带电荷的氨基酸，而假定的核心保持不变。我们产生了水溶性磷脂蛋白（WSPLB），并将其性能与其前身PLB进行了比较。作为水溶性KcsA的倍数的正确性的探针，计算设计的蛋白质含有来自哺乳动物同源物的通道的搅拌毒素-2结合位点。所得蛋白质在大肠杆菌中以高产率表达，并且与KcsA共享预期的功能和结构性质，包括二级结构，四聚体四级结构，以及紧密的，特异性结合于vibroxin2和小分子通道阻断剂。

9. 发明申请

WO2006132647A3 ANTIMICROBIAL COPOLYMERS AND USES THEREOF 审中-公开
公开(公告)号：WO2006132647A3
公开(公告)日：2006-12-14
申请号：PCT/US2005/026188
申请日：2005-07-22
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , KURODA, Kenichi , DEGRADO, William, F.
发明人： KURODA, Kenichi , DEGRADO, William, F.
IPC分类号： C08F226/06 , A61K31/765
摘要： The present invention discloses random copolymers and methods of their use, including use of the copolymers as antimicrobial agents in pharmaceutical and non-pharmaceutical applications. The present invention also discloses compositions of the copolymers, and methods of preparing the copolymers.

10. 发明申请

WO2004082634A2 FACIALLY AMPHIPHILIC POLYMERS AND OLIGOMERS AND USES THEREOF 审中-公开
标题翻译：全氟聚合物和低聚物及其用途
公开(公告)号：WO2004082634A2
公开(公告)日：2004-09-30
申请号：PCT/US2004/008155
申请日：2004-03-17
申请人： DEGRADO, William, F. , LIU, Dahui , TEW, Gregory, N. , KLEIN, Michael, L. , YUAN, Jing , CHOI, Sungwook
发明人： DEGRADO, William, F. , LIU, Dahui , TEW, Gregory, N. , KLEIN, Michael, L. , YUAN, Jing , CHOI, Sungwook
IPC分类号： A61K
CPC分类号： A61K31/17 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/3225 , C08G73/028 , C08L75/02
摘要： The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
摘要翻译：本发明公开了使用表面两亲性聚合物和低聚物的方法，包括聚合物和低聚物作为抗微生物剂的药物用途和与肝素治疗相关的出血并发症的解毒剂。本发明还公开了新颖的表面两亲聚合物和低聚物及其组合物，包括药物组合物。本发明还公开了表面两亲聚合物和低聚物的设计和合成。

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