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1. 发明申请

US20060024844A1 Method for the idenification of ligands 审中-公开
标题翻译：配体鉴定方法
公开(公告)号：US20060024844A1
公开(公告)日：2006-02-02
申请号：US10522660
申请日：2002-09-20
申请人： Dionisios Rentzeperis , Hossein Askari , Barry Springer , Roger Bone , Francis Salemme
发明人： Dionisios Rentzeperis , Hossein Askari , Barry Springer , Roger Bone , Francis Salemme
IPC分类号： G01N33/543 , G06F19/00 , G01N33/48 , G01N33/50
CPC分类号： C40B30/04 , G01N33/566 , G01N33/68 , G01N33/6803 , G01N33/6845 , G01N2333/4703 , G01N2333/70567 , G01N2333/723 , G01N2333/726 , G01N2333/9121 , G01N2500/00
摘要： The present invention relates generally to a method of identifying ligands that modulate protein-protein interactions. More particularly, the present invention relates to methods of determining agonists or antagonists of a co-regulator dependent target molecule based on the ability to modify the stability of the target molecule.
摘要翻译：本发明一般涉及鉴定调节蛋白质 - 蛋白质相互作用的配体的方法。更具体地，本发明涉及基于调节靶分子的稳定性的能力来确定共调节因子依赖性靶分子的激动剂或拮抗剂的方法。

2. 发明申请

US20060110732A1 Method for the identification of ligands 审中-公开
标题翻译：鉴定配体的方法
公开(公告)号：US20060110732A1
公开(公告)日：2006-05-25
申请号：US10519757
申请日：2003-07-23
申请人： Roger Bone , Dionisios Rentzeperis , Hossein Askari , Barry Springer
发明人： Roger Bone , Dionisios Rentzeperis , Hossein Askari , Barry Springer
IPC分类号： C12Q1/68 , G01N33/53
CPC分类号： C40B30/04 , G01N33/6845
摘要： The present invention relates generally to a method of identifying ligands that modulate protein-protein interactions. More particularly, the present invention relates to methods of determining agonists or antagonists of a co-regulator dependent target molecule based on the ability to modify the stability of the target molecule in a tissue-selective manner.
摘要翻译：本发明一般涉及鉴定调节蛋白质 - 蛋白质相互作用的配体的方法。更具体地，本发明涉及基于以组织选择性方式改变靶分子的稳定性的能力来确定共调节因子依赖性靶分子的激动剂或拮抗剂的方法。

3. 发明申请

US20060099643A1 Method for determining the regulation of xenobiotic removal 审中-公开
标题翻译：确定异种移植调节的方法
公开(公告)号：US20060099643A1
公开(公告)日：2006-05-11
申请号：US10522396
申请日：2003-07-23
申请人： Roger Bone , Dionisios Rentzeperis
发明人： Roger Bone , Dionisios Rentzeperis
IPC分类号： G01N33/53 , G06F19/00
CPC分类号： G01N33/5023 , C12Q1/26 , G01N33/5735 , G01N33/743 , G01N2333/723 , G01N2333/80 , G01N2333/90245 , G01N2500/04
摘要： The present invention relates generally to a method for identifying ligands that affect xenobiotic removal based upon their ability to modify the stability of receptors that regulate cytochrome P450 expression and/or drug transport proteins.
摘要翻译：本发明一般涉及一种基于其修饰调节细胞色素P450表达和/或药物转运蛋白的受体的稳定性的能力鉴定影响异生物去除的配体的方法。

4. 发明授权

US06326492B1 Heterocyclic protease inhibitors 有权
标题翻译：杂环蛋白酶抑制剂
公开(公告)号：US06326492B1
公开(公告)日：2001-12-04
申请号：US09578487
申请日：2000-05-26
申请人： Aihua Wang , Tianbao Lu , Bruce E. Tomczuk , Richard M. Soll , John Spurlino , Roger Bone
发明人： Aihua Wang , Tianbao Lu , Bruce E. Tomczuk , Richard M. Soll , John Spurlino , Roger Bone
IPC分类号： C07D26502
CPC分类号： C07D413/12 , C07D413/14
摘要： Described are compounds of the Formula VII: wherein Het, R1, R7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
摘要翻译：描述了式VII的化合物：其中Het，R 1，R 7和A在本说明书中列出，以及其抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。还描述了制备这些化合物的方法。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理连接于制造用于血液收集，血液循环和血液储存中的装置的材料的抗凝剂，例如导管，血液透析机，采血注射器和管，血线和支架。另外，化合物可以被可检测地标记并用于血栓的体内成像。

5. 发明申请

US20060058291A1 Cyclic oxyguanidine pyrazinones as protease inhibitors 审中-公开
标题翻译：环氧乙酰吡嗪酮作为蛋白酶抑制剂
公开(公告)号：US20060058291A1
公开(公告)日：2006-03-16
申请号：US11253447
申请日：2005-10-19
申请人： Aihua Wang , Bruce Tomczuk , Tianbao Lu , Richard Soll , John Spurlino , Roger Bone
发明人： Aihua Wang , Bruce Tomczuk , Tianbao Lu , Richard Soll , John Spurlino , Roger Bone
IPC分类号： A61K31/553 , A61K31/535 , A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
摘要翻译：描述了环状氧基胍吡嗪酮化合物，包括式I的化合物：

6. 发明申请

US20050004031A1 Conjugated complement cascade inhibitors 失效
标题翻译：共轭补体级联抑制剂
公开(公告)号：US20050004031A1
公开(公告)日：2005-01-06
申请号：US10869430
申请日：2004-06-16
申请人： Nalin Subasinghe , Ehab Khalil , Farah Ali , Heather Hufnagel , Shelley Ballentine , Jeremy Travins , Kristi Leonard , Roger Bone
发明人： Nalin Subasinghe , Ehab Khalil , Farah Ali , Heather Hufnagel , Shelley Ballentine , Jeremy Travins , Kristi Leonard , Roger Bone
IPC分类号： A61K47/48 , A61K38/17
CPC分类号： A61K47/60
摘要： The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.
摘要翻译：本发明涉及缀合的补体级联抑制剂，以及使用缀合的补体级联抑制剂治疗患者的方法。

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