公开(公告)号：US20090274650A1

公开(公告)日：2009-11-05

申请号：US12370175

申请日：2009-02-12

申请人： Michael R. Hale ,  Roger Tung ,  Stephen Price ,  Robin David Wilkes ,  Wayne Carl Schairer ,  Ashley Nicholas Jarvis ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Vicente Samano ,  Istvan Kaldor ,  John Franklin Miller ,  Michael Stephen Brieger ,  Ronald George Sherrill

发明人： Michael R. Hale ,  Roger Tung ,  Stephen Price ,  Robin David Wilkes ,  Wayne Carl Schairer ,  Ashley Nicholas Jarvis ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Vicente Samano ,  Istvan Kaldor ,  John Franklin Miller ,  Michael Stephen Brieger ,  Ronald George Sherrill

IPC分类号： A61K31/443 ,  C07D493/04 ,  C07D413/12 ,  C07D317/46 ,  A61K31/5377 ,  A61K31/357 ,  A61K31/34 ,  A61K31/52 ,  A61K31/522 ,  A61K31/496 ,  A61K31/427 ,  A61K31/472 ,  A61K31/513 ,  A61K31/708 ,  A61K38/21 ,  A61K38/20 ,  A61P31/12 ,  A61P31/18

CPC分类号： C07D493/04 ,  A61K31/352 ,  A61K31/36 ,  A61K45/06 ,  C07D317/46 ,  A61K2300/00

摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

摘要翻译： 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶活性的方法和用于筛选抗HIV活性化合物的方法。

公开(公告)号：US08455497B2

公开(公告)日：2013-06-04

申请号：US12370175

申请日：2009-02-12

申请人： Michael R. Hale ,  Roger Tung ,  Stephen Price ,  Robin David Wilkes ,  Wayne Carl Schairer ,  Ashley Nicholas Jarvis ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Vicente Samano ,  Istvan Kaldor ,  John Franklin Miller ,  Michael Stephen Brieger ,  Ronald George Sherrill

发明人： Michael R. Hale ,  Roger Tung ,  Stephen Price ,  Robin David Wilkes ,  Wayne Carl Schairer ,  Ashley Nicholas Jarvis ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Vicente Samano ,  Istvan Kaldor ,  John Franklin Miller ,  Michael Stephen Brieger ,  Ronald George Sherrill

IPC分类号： C07D493/04 ,  A61K31/34 ,  A61K31/357 ,  A61K31/36 ,  A61P31/18 ,  C07C311/16 ,  C07C311/29

CPC分类号： C07D493/04 ,  A61K31/352 ,  A61K31/36 ,  A61K45/06 ,  C07D317/46 ,  A61K2300/00

摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：US06878728B1

公开(公告)日：2005-04-12

申请号：US09591464

申请日：2000-06-09

申请人： Michael R. Hale ,  Roger Tung ,  Stephen Price ,  Robin David Wilkes ,  Wayne Carl Schairer ,  Ashley Nicholas Jarvis ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Vicente Samano ,  Istvan Kaldor ,  John Franklin Miller ,  Michael Stephen Brieger

发明人： Michael R. Hale ,  Roger Tung ,  Stephen Price ,  Robin David Wilkes ,  Wayne Carl Schairer ,  Ashley Nicholas Jarvis ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Vicente Samano ,  Istvan Kaldor ,  John Franklin Miller ,  Michael Stephen Brieger

IPC分类号： A61K31/352 ,  A61K31/36 ,  A61K45/06 ,  A61K31/454 ,  A61K31/422 ,  C07D413/14 ,  C07D417/12

CPC分类号： C07D493/04 ,  A61K31/352 ,  A61K31/36 ,  A61K45/06 ,  C07D277/24 ,  C07D317/62 ,  C07D407/12 ,  A61K2300/00

摘要： The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.

摘要翻译： 本发明提供新的式（I）化合物，其中所有变量如说明书中所定义，可用作天冬氨酰蛋白酶抑制剂。