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公开(公告)号：US20100204200A1
公开(公告)日：2010-08-12
申请号：US12764772
申请日：2010-04-21
申请人： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
IPC分类号： A61K31/5377 , C07D413/12 , C07D295/145 , C07D413/14 , C07C245/00 , C07D401/12 , C07D403/12 , A61K31/5375 , A61K31/54 , A61K31/496 , A61K31/404
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.
摘要翻译： 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供了具有式1的化合物：其中Q是任选取代的氮杂环丁烷基，吡咯烷基，哌啶基和二氢吲哚基; 或Q为NR25R26; A，R 5，R 6，R 7，R 8，R 9，R 25，R 26和Ar为取代基。
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公开(公告)号：US20090075996A1
公开(公告)日：2009-03-19
申请号：US11995683
申请日：2006-07-14
申请人： Phillip B. Alper , Thomas Marsilje , Arnab Chatterjee , Wenshuo Lu , Daniel Mutnick , Michael Roberts , Yun He
发明人： Phillip B. Alper , Thomas Marsilje , Arnab Chatterjee , Wenshuo Lu , Daniel Mutnick , Michael Roberts , Yun He
IPC分类号： A61K31/5377 , C07D209/82 , C07D413/08 , A61K31/403
CPC分类号： C08J7/04 , C07D209/80 , C07D209/94 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D491/04 , C07D495/04 , C08J7/045 , C08J2369/00
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
摘要翻译： 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的TPO活性相关的疾病或病症的方法，特别是涉及血小板减少症的疾病或病症。
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公开(公告)号：US20070123523A1
公开(公告)日：2007-05-31
申请号：US11620608
申请日：2007-01-05
申请人： Hong Liu , David Tully , Phillip Alper , Robert Epple , Arnab Chatterjee , Michael Roberts
发明人： Hong Liu , David Tully , Phillip Alper , Robert Epple , Arnab Chatterjee , Michael Roberts
IPC分类号： A61K31/165 , A61K31/54 , A61K31/497 , A61K31/445
CPC分类号： C07D327/04 , C07D277/82 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
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公开(公告)号：US08268996B2
公开(公告)日：2012-09-18
申请号：US13161555
申请日：2011-06-16
申请人： Hong Liu , David C. Tully , Arnab Chatterjee , Phillip B. Alper , David H. Woodmansee , Daniel Mutnick
发明人： Hong Liu , David C. Tully , Arnab Chatterjee , Phillip B. Alper , David H. Woodmansee , Daniel Mutnick
IPC分类号： C07D413/12 , C07D295/185 , A61K31/5377 , A61K31/5375
CPC分类号： C07D263/56 , C07D211/66 , C07D273/02 , C07D277/64 , C07D295/185 , C07D307/30
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
摘要翻译： 本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与组织蛋白酶S活性相关的疾病或病症的方法。
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公开(公告)号：US07501408B2
公开(公告)日：2009-03-10
申请号：US11932679
申请日：2007-10-31
申请人： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
IPC分类号： C07D417/12 , C07D295/10 , A61K31/541
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula (I): wherein Q is thiomorpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.
摘要翻译： 本发明提供了用于选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供具有式（I）的化合物：其中Q是硫代吗啉基; A，R5，R6，R7，R8，R9和Ar为取代基。
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公开(公告)号：US20080108595A1
公开(公告)日：2008-05-08
申请号：US11932679
申请日：2007-10-31
申请人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
IPC分类号： C07D413/00 , A61K31/535 , C07D265/30 , A61K31/5377 , A61K31/54 , C07D279/12 , C07D241/04 , A61K31/495 , A61K31/397 , C07D205/04
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
摘要翻译： 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。
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公开(公告)号：US07307095B2
公开(公告)日：2007-12-11
申请号：US11620608
申请日：2007-01-05
申请人： Hong Liu , David Tully , Phillip Alper , Robert Epple , Arnab Chatterjee , Michael Roberts
发明人： Hong Liu , David Tully , Phillip Alper , Robert Epple , Arnab Chatterjee , Michael Roberts
IPC分类号： A61K31/423 , A61K31/403 , A61K31/428
CPC分类号： C07D327/04 , C07D277/82 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
摘要翻译： 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。
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公开(公告)号：US07173051B2
公开(公告)日：2007-02-06
申请号：US10868459
申请日：2004-06-10
申请人： Hong Liu , David Tully , Phillip Alper , Robert Epple , Arnab Chatterjee , Michael Roberts
发明人： Hong Liu , David Tully , Phillip Alper , Robert Epple , Arnab Chatterjee , Michael Roberts
IPC分类号： A61K31/423 , A61K31/403 , A61K31/428 , C07D263/58 , C07D227/04 , C07D417/02 , C07D498/02
CPC分类号： C07D327/04 , C07D277/82 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
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公开(公告)号：US20050113356A1
公开(公告)日：2005-05-26
申请号：US10922515
申请日：2004-08-18
申请人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
IPC分类号： A61K20060101 , A61K31/397 , A61K31/401 , A61K31/404 , A61K31/423 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/537 , A61K31/5375 , A61K31/54 , C07D209/04 , C07D209/08 , C07D261/14 , C07D265/30 , C07D295/13 , C07D295/18 , C07D295/20 , C07D411/12 , C07D413/12 , C07D417/12
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
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公开(公告)号：US07985749B2
公开(公告)日：2011-07-26
申请号：US11568459
申请日：2005-04-29
申请人： Hong Liu , David C. Tully , Arnab Chatterjee , Phillip B. Alper , David H. Woodmansee , Daniel Mutnick
发明人： Hong Liu , David C. Tully , Arnab Chatterjee , Phillip B. Alper , David H. Woodmansee , Daniel Mutnick
IPC分类号： A61K31/5355 , C07D413/12
CPC分类号： C07D263/56 , C07D211/66 , C07D273/02 , C07D277/64 , C07D295/185 , C07D307/30
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
摘要翻译： 本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与组织蛋白酶S活性相关的疾病或病症的方法。
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