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1. 发明授权

US08476037B2 Method for screening of antiviral agents 有权
标题翻译：筛选抗病毒剂的方法
公开(公告)号：US08476037B2
公开(公告)日：2013-07-02
申请号：US13213230
申请日：2011-08-19
申请人： Masayori Inouye , Lili Mao , William F. Degrado , Nathan H. Joh
发明人： Masayori Inouye , Lili Mao , William F. Degrado , Nathan H. Joh
IPC分类号： C12Q1/02
CPC分类号： C12Q1/18
摘要： A method for screening for an antiviral agent capable of blocking a viral viroporin by determining whether a test agent can rescue expression of a fragment of a viral viroporin in a Single Protein Production system of Escherichia coli is provided.
摘要翻译：提供了通过确定测试试剂是否可以在大肠杆菌的单一蛋白质生产系统中拯救病毒性异丙肾上腺素的片段的表达来筛选能够阻断病毒性丙泊酚的抗病毒剂的方法。

2. 发明申请

US20120045789A1 Method for Screening of Antiviral Agents 有权
标题翻译：抗病毒药物筛选方法
公开(公告)号：US20120045789A1
公开(公告)日：2012-02-23
申请号：US13213230
申请日：2011-08-19
申请人： Masayori Inouye , Lili Mao , William F. Degrado , Nathan H. Joh
发明人： Masayori Inouye , Lili Mao , William F. Degrado , Nathan H. Joh
IPC分类号： C12Q1/02
CPC分类号： C12Q1/18
摘要： A method for screening for an antiviral agent capable of blocking a viral viroporin by determining whether a test agent can rescue expression of a fragment of a viral viroporin in a Single Protein Production system of Escherichia coli is provided.
摘要翻译：提供了通过确定测试试剂是否可以在大肠杆菌的单一蛋白质生产系统中拯救病毒性异丙肾上腺素的片段的表达来筛选能够阻断病毒性丙泊酚的抗病毒剂的方法。

3. 发明授权

US5635477A Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA 失效
标题翻译：可用作血小板糖蛋白IIB / IIIA抑制剂的循环化合物
公开(公告)号：US5635477A
公开(公告)日：1997-06-03
申请号：US461611
申请日：1995-06-05
申请人： William F. Degrado , Sharon A. Jackson , Shaker A. Mousa , Anju Parthasarathy , Michael Sworin , Maria Rafalski
发明人： William F. Degrado , Sharon A. Jackson , Shaker A. Mousa , Anju Parthasarathy , Michael Sworin , Maria Rafalski
IPC分类号： A61K38/00 , C07K7/56 , C07K14/75 , A61K38/12
CPC分类号： C07K14/75 , C07K7/56 , A61K38/00
摘要： This invention relates to novel cyclic compounds containing carbocyclic ring systems useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, with or without other therapeutic agents, and to methods of using these compounds, with or without other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. This invention also relates to methods of using the cyclic compounds of the invention in combination with anti-coagulants such as warfarin or heparin, or additional anti-platelet agents such as aspirin, piroxicam or ticlopidine, or thrombin inhibitors such as boropeptides, hirudin or argatroban, or thrombolytic agents such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, for the treatment of thromboembolic disorders. A representative compound of the invention is cyclo(D-Val-(.sup..alpha. N-methyl Arg)-Gly-Asp-(3-aminomethylbenzoic acid).
摘要翻译：本发明涉及含有可用作血小板糖蛋白IIb / IIIa复合物的拮抗剂的碳环系的新型环状化合物，含有或不含其它治疗剂的含有环状化合物的药物组合物，以及使用或不使用其它治疗剂的方法治疗剂，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗其他血栓栓塞障碍。本发明还涉及使用本发明的环状化合物与抗凝血剂如华法林或肝素或另外的抗血小板药如阿司匹林，吡罗昔康或噻氯匹定或凝血酶抑制剂如硼多肽，水蛭素或阿加曲班联合使用的方法，或血栓溶解剂如组织纤溶酶原激活剂，anistreplase，尿激酶或链激酶或其组合，用于治疗血栓栓塞性疾病。本发明的代表性化合物是环（D-Val-（αN-甲基Arg）-Gly-Asp-（3-氨基甲基苯甲酸）。

4. 发明申请

US20110236881A1 MODULATION OF INFLUENZA VIRUS 审中-公开
标题翻译：流感病毒调控
公开(公告)号：US20110236881A1
公开(公告)日：2011-09-29
申请号：US13058930
申请日：2009-08-12
申请人： William F. Degrado , Amanda L. Stouffer , Rudresh Acharya , David Salom-Arbona , Alexei Polishchuk
发明人： William F. Degrado , Amanda L. Stouffer , Rudresh Acharya , David Salom-Arbona , Alexei Polishchuk
IPC分类号： C12Q1/70 , G06F19/00
CPC分类号： G16C20/50 , G16B15/00
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。

5. 发明申请

US20090233968A1 INHIBITORS OF THE ALPHA2BETA1/GPIa-IIA INTEGRIN 有权
标题翻译： ALPHA2BETA1 / GPIa-IIA INTEGRIN的抑制剂
公开(公告)号：US20090233968A1
公开(公告)日：2009-09-17
申请号：US11916746
申请日：2006-06-07
申请人： William F. Degrado , Joel S. Bennett , Seth Elliott Snyder , Sungwook Choi
发明人： William F. Degrado , Joel S. Bennett , Seth Elliott Snyder , Sungwook Choi
IPC分类号： A61K31/445 , A61K31/425 , A61K31/40 , C07D211/22 , C07D277/00 , C07D207/00
CPC分类号： C07D207/48 , C07D211/96 , C07D277/06 , C07K5/06165
摘要： Novel compounds inhibiting the integrin α2β1/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 α2β1/GPIa-IIa-mediated activity.
摘要翻译：公开了抑制整联蛋白α2beta1/ 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α2beta1/ GPIa-IIa介导活性的抑制剂。

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