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1.发明授权公开(公告)号：US06846838B2
公开(公告)日：2005-01-25
申请号：US10464035
申请日：2003-06-17
申请人： William A. Slusarchyk , Scott A. Bolton , Timothy Herpin , Gregory S. Bisacchi , Zulan Pi , E. Scott Priestley
发明人： William A. Slusarchyk , Scott A. Bolton , Timothy Herpin , Gregory S. Bisacchi , Zulan Pi , E. Scott Priestley
IPC分类号： A61K31/136 , A61K31/4155 , A61K31/422 , A61K45/06 , A61P9/08 , C07D263/48 , A61K31/44 , A61K31/41 , A61K31/415 , A61K31/42
CPC分类号： C07D263/48 , A61K31/136 , A61K31/4155 , A61K31/422 , A61K45/06 , A61K2300/00
摘要： Compounds having the formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.
摘要翻译： 具有式（I）化合物或其药学上可接受的盐，水合物或前体药物作为因子VIIa的抑制剂是有效的。
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2.发明授权Methods of treating factor VIIa-associated conditions with compounds having an amine nucleus 失效用具有胺核的化合物治疗因子VIIa相关病症的方法公开(公告)号：US07041692B2
公开(公告)日：2006-05-09
申请号：US10464366
申请日：2003-06-17
IPC分类号： A61K31/42 , A61K31/41 , A61K31/415
CPC分类号： C07D231/12 , A61K31/415 , A61K31/4172 , A61K31/4196 , A61K31/421 , A61K31/422 , C07D233/56 , C07D249/08 , C07D263/48 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Methods of treating Factor VIIa-associated conditions in a mammal are described, comprising administering to the mammal in need of treatment thereof an effective amount of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof.
摘要翻译： 描述了治疗哺乳动物中因子VIIa相关病症的方法，包括向需要治疗的哺乳动物施用有效量的至少一种具有式（I）的化合物或其药学上可接受的盐，水合物或前体药物 。
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公开(公告)号：US07122559B2
公开(公告)日：2006-10-17
申请号：US10775923
申请日：2004-02-10
申请人： Peter W. Glunz , Gregory S. Bisacchi , George C. Morton , Alexandra A. Holubec , E. Scott Priestley , Xiaojun Zhang , Uwe D. Treuner
发明人： Peter W. Glunz , Gregory S. Bisacchi , George C. Morton , Alexandra A. Holubec , E. Scott Priestley , Xiaojun Zhang , Uwe D. Treuner
IPC分类号： A61K31/472 , C07D217/22
CPC分类号： C07D231/56 , C07C311/51 , C07D217/02 , C07D217/06 , C07D217/22 , C07D233/36 , C07D235/30 , C07D239/94 , C07D261/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is —NR6S(O)pR16; W is hydrogen or —(CR7R8)q—W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3, R6, R7, and R16 are as defined in the specification.
摘要翻译： 具有式（I）的化合物或其立体异构体或药学上可接受的盐或其水合物可用作因子VIIa抑制剂，其中X为-NR 6 S（O） 16＆lt; 16＆gt; W是氢或 - （CR 7 R 8）。 W 1是氢或与R 6的键; Z是5元杂芳基，5至6元杂环基或环烷基，9至10元双环芳基或杂芳基，或6元芳基或杂芳基，R 1，R 2， R 2，R 3，R 6，R 7和R 16均为 在规范中定义。
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公开(公告)号：US06846806B2
公开(公告)日：2005-01-25
申请号：US10039317
申请日：2001-10-23
申请人： E. Scott Priestley
发明人： E. Scott Priestley
CPC分类号： C07K7/06 , A61K38/00 , C07F5/025 , C07K5/06191
摘要： This invention relates to a novel class of peptides having the Formula (I): which are useful as serine protease inhibitors, and more particularly as Hepatitis C virus(HCV) NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same in the treatment of HCV infection.
摘要翻译： 本发明涉及一类具有式（I）的肽，它们可用作丝氨酸蛋白酶抑制剂，更具体地说，涉及丙型肝炎病毒（HCV）NS3蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物及其用于治疗HCV感染的方法。
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5.发明授权3,4-disubstituted benzamidines and benzylamines, and analogues thereof, useful as serine protease inhibitors 有权3,4-二取代的苯甲脒和苄胺及其类似物，可用作丝氨酸蛋白酶抑制剂公开(公告)号：US07247654B2
公开(公告)日：2007-07-24
申请号：US10858364
申请日：2004-06-01
申请人： E. Scott Priestley , Xiaojun Zhang
发明人： E. Scott Priestley , Xiaojun Zhang
IPC分类号： A61K31/24 , C07C229/52
CPC分类号： C07C257/18 , C07C311/05 , C07C311/06 , C07C2601/08 , C07C2601/14 , C07D213/75 , C07D231/40 , C07D277/44
摘要： The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel 3,4-disubstituted benzamidines and benzylamines, or a stereoisomer or pharmaceutically acceptable salt form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor Xa, factor XIa, factor IXa, and/or factor VIIa. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
摘要翻译： 本发明一般涉及抑制丝氨酸蛋白酶的化合物。 特别涉及可用作凝血级联丝氨酸蛋白酶的选择性抑制剂的新型3,4-二取代苯甲酰胺和苄胺或其立体异构体或药学上可接受的盐形式。 例如凝血酶，因子Xa，因子XIa，因子IXa和/或因子VIIa。 特别地，它涉及作为因子VIIa抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物及其使用方法。
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公开(公告)号：US07122627B2
公开(公告)日：2006-10-17
申请号：US10010184
申请日：2001-12-06
IPC分类号： C07K5/08
CPC分类号： C07F5/025 , A61K38/00 , C07F5/022 , C07K5/06191
摘要： The present invention relates to lactams of Formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
摘要翻译： 本发明涉及可用作HCV NS3蛋白酶抑制剂的式（I）的内酰胺或其立体异构形式，立体异构体混合物或其药学上可接受的盐形式，以及包含其的药物组合物和诊断试剂盒及其制备方法 使用它们来治疗病毒感染或作为测定标准或试剂。
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公开(公告)号：US06939854B2
公开(公告)日：2005-09-06
申请号：US10759725
申请日：2004-01-15
申请人： E. Scott Priestley
发明人： E. Scott Priestley
CPC分类号： C07K7/06 , A61K38/00 , C07F5/025 , C07K5/06191
摘要： This invention relates to a novel class of peptides having the Formula (I): which are useful as serine protease inhibitors, and more particularly as Hepatitis C virus (HCV) NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same in the treatment of HCV infection.
摘要翻译： 本发明涉及一类具有式（I）的肽，它们可用作丝氨酸蛋白酶抑制剂，更具体地说，涉及丙型肝炎病毒（HCV）NS3蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物及其用于治疗HCV感染的方法。
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公开(公告)号：US06120997A
公开(公告)日：2000-09-19
申请号：US6597
申请日：1998-01-13
申请人： Chi-Huey Wong , Martin Hendrix , Phil Alper , E. Scott Priestley
发明人： Chi-Huey Wong , Martin Hendrix , Phil Alper , E. Scott Priestley
IPC分类号： C07B61/00 , C07H15/04 , C07H15/203 , C07H17/02 , C12Q1/68
CPC分类号： C07H17/02 , C07H15/04 , C07H15/203 , C40B40/00
摘要： The invention relates to the combination of hydroxyamines with nucleic acid binding motifs to generate molecules and libraries of molecules targeting specific nucleic acid sequences. In particular, a series of libraries are constructed which contain hydroxyamine functionalities that are attached to various template backbones which display varying degrees of molecular recognition to phosphodiesters and varying degrees of sequence specific recognition to nucleic acids.
摘要翻译： 本发明涉及羟胺与核酸结合基序的组合以产生靶向特异性核酸序列的分子和分子文库。 特别地，构建了一系列文库，它们含有连接到各种模板骨架上的羟胺官能团，其显示出对磷酸二酯的不同程度的分子识别和对核酸的不同程度的序列特异性识别。
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