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。

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：US20090042973A1

公开(公告)日：2009-02-12

申请号：US12217517

申请日：2008-07-02

申请人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Francois Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

发明人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Francois Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

IPC分类号： A61K31/343 ,  C07C255/03 ,  C07D307/78 ,  A61K31/352 ,  A61P31/18 ,  C07D319/16 ,  A61K31/277

CPC分类号： C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C317/18 ,  C07D307/20 ,  C07D319/06 ,  C07D493/04 ,  C07F9/6561

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：US06617350B2

公开(公告)日：2003-09-09

申请号：US09927271

申请日：2001-08-09

申请人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  François Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

发明人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  François Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

IPC分类号： A61K3134

CPC分类号： C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C317/18 ,  C07D307/20 ,  C07D319/06 ,  C07D493/04 ,  C07F9/6561

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：US07919523B2

公开(公告)日：2011-04-05

申请号：US12217517

申请日：2008-07-02

申请人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Francois Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

发明人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Francois Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

IPC分类号： A61K31/357 ,  C07D319/06

CPC分类号： C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C317/18 ,  C07D307/20 ,  C07D319/06 ,  C07D493/04 ,  C07F9/6561

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：US06319946B1

公开(公告)日：2001-11-20

申请号：US09500781

申请日：2000-02-09

申请人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Francois Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

发明人： Michael R. Hale ,  Christopher T. Baker ,  Timothy A. Stammers ,  Ronald George Sherrill ,  Andrew Spaltenstein ,  Eric Steven Furfine ,  Francois Maltais ,  Clarence Webster Andrews, III ,  John Franklin Miller ,  Vicente Samano

IPC分类号： A61K31357

CPC分类号： C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C317/18 ,  C07D307/20 ,  C07D319/06 ,  C07D493/04 ,  C07F9/6561

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：US07442718B2

公开(公告)日：2008-10-28

申请号：US10613650

申请日：2003-07-02

申请人： Michael R Hale ,  Christopher T Baker ,  Timothy A Stammers ,  Ronald G Sherrill ,  Andrew Spaltenstein ,  Eric S Furfine ,  Francois Maltais ,  Clarence W Andrews, III ,  John F Miller ,  Vicente Samano

发明人： Michael R Hale ,  Christopher T Baker ,  Timothy A Stammers ,  Ronald G Sherrill ,  Andrew Spaltenstein ,  Eric S Furfine ,  Francois Maltais ,  Clarence W Andrews, III ,  John F Miller ,  Vicente Samano

IPC分类号： A61K31/357 ,  C07D317/46

CPC分类号： C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C317/18 ,  C07D307/20 ,  C07D319/06 ,  C07D493/04 ,  C07F9/6561

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：US20110118261A1

公开(公告)日：2011-05-19

申请号：US12747186

申请日：2008-12-10

申请人： Scott Allen ,  William C. Blackwell, III ,  Eric Boros ,  Jon L. Collins ,  Don Hertzog ,  Xi Liang ,  John Ray ,  Steven Michael Reister ,  Vicente Samano ,  Ron Sherrill

发明人： Scott Allen ,  William C. Blackwell, III ,  Eric Boros ,  Jon L. Collins ,  Don Hertzog ,  Xi Liang ,  John Ray ,  Steven Michael Reister ,  Vicente Samano ,  Ron Sherrill

IPC分类号： A61K31/5377 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  A61K31/444 ,  A61K31/4545 ,  A61P3/10 ,  A61P3/04 ,  A61P9/12 ,  A61P25/24 ,  A61P25/22 ,  A61P25/30

CPC分类号： C07D401/14 ,  C07D405/14

摘要： The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes.

摘要翻译： 本发明提供新颖的双吡啶基吡啶酮，它们是黑色素浓缩激素受体1（MCHR1）的拮抗剂，含有它们的药物组合物，其制备方法及其在治疗和治疗肥胖症和/或糖尿病中的用途。

公开(公告)号：US20050245596A1

公开(公告)日：2005-11-03

申请号：US10510469

申请日：2003-04-01

申请人： David Barrett ,  John Catalano ,  David Deaton ,  Aaron Miller ,  John Ray ,  Vicente Samano

发明人： David Barrett ,  John Catalano ,  David Deaton ,  Aaron Miller ,  John Ray ,  Vicente Samano

IPC分类号： A61K31/341 ,  A61K31/365 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/5377 ,  A61P19/00 ,  A61P19/10 ,  A61P43/00 ,  C07D207/12 ,  C07D207/26 ,  C07D207/263 ,  C07D207/27 ,  C07D207/273 ,  C07D207/48 ,  C07D307/20 ,  C07D307/33 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D43/02 ,  C07D45/02

CPC分类号： C07D207/27 ,  C07D207/12 ,  C07D207/273 ,  C07D207/48 ,  C07D307/20 ,  C07D307/33 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.

摘要翻译： 式（I）的杂环取代的酮酰胺衍生物，其中取代基A，D，A和R如权利要求中所定义，其可用作组织蛋白酶K抑制剂。 所描述的发明还包括制备这种杂环取代的酮酰胺衍生物的方法以及在制备用于治疗与骨吸收和形成之间不平衡的疾病（包括骨质疏松症）相关的药物的药物的方法，其可最终导致骨折 。