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![Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors](/abs-image/US/2014/03/18/US08673924B2/abs.jpg.150x150.jpg)
1.发明授权Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors 有权取代的吡唑并[1,5-a]嘧啶作为细胞周期蛋白依赖性激酶抑制剂公开(公告)号：US08673924B2
公开(公告)日：2014-03-18
申请号：US11788847
申请日：2007-04-20
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent S. Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs , Paul Kirschmeier , Rajat Bannerji
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent S. Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs , Paul Kirschmeier , Rajat Bannerji
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： A61K31/33 , A61K31/4965 , A61K31/497 , A61K31/519 , A61K31/535 , A61K31/555 , A61K31/56 , A61K31/655 , A61K31/675 , A61K31/7004 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An example pyrazolo[1,5-a]pyrimidine compound useful in the present invention is shown below:
摘要翻译： 在其许多实施方案中，本发明提供了抑制患者中一种或多种细胞周期蛋白依赖性激酶的方法，包括向所述患者施用治疗有效量的至少一种吡唑并[1,5-a]嘧啶化合物或包含 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。 用于本发明的吡唑并[1,5-a]嘧啶化合物的实例如下所示：
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公开(公告)号：US08440443B1
公开(公告)日：2013-05-14
申请号：US11749550
申请日：2007-05-16
申请人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
发明人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
IPC分类号： C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00 , C07K2319/40
摘要： The present invention provides, inter alia, crystals of the MEK1 polypeptide which are particularly useful for structure based drug design as well as methods of use thereof.
摘要翻译： 本发明特别提供了特别可用于基于结构的药物设计的MEK1多肽的晶体及其使用方法。
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3.发明授权公开(公告)号：US06894072B2
公开(公告)日：2005-05-17
申请号：US10348094
申请日：2003-01-21
申请人： Ashok Arasappan , Frank Bennett , Stephane L. Bogen , Kevin X. Chen , Edwin Jao , Yi-Tsung Liu , Raymond G. Lovey , Vincent S. Madison , Latha G. Nair , F. George Njoroge , Anil K. Saksena , Mousumi Sannigrahi , Srikanth Venkatraman , Viyyoor M. Girijavallabhan
发明人： Ashok Arasappan , Frank Bennett , Stephane L. Bogen , Kevin X. Chen , Edwin Jao , Yi-Tsung Liu , Raymond G. Lovey , Vincent S. Madison , Latha G. Nair , F. George Njoroge , Anil K. Saksena , Mousumi Sannigrahi , Srikanth Venkatraman , Viyyoor M. Girijavallabhan
IPC分类号： A61K31/403 , A61K31/7052 , A61K38/21 , A61P1/16 , A61P31/12 , A61P31/14 , A61P43/00 , C07D207/16 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/70 , C07D213/75 , C07D217/26 , C07D233/68 , C07D243/12 , C07D253/06 , C07D271/06 , C07D277/06 , C07D277/46 , C07D277/56 , C07D295/15 , C07D307/68 , C07D317/58 , C07D335/10 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D209/02
CPC分类号： C07D207/27 , C07D207/16 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/70 , C07D213/75 , C07D217/26 , C07D233/68 , C07D243/12 , C07D253/06 , C07D271/06 , C07D277/06 , C07D277/46 , C07D277/56 , C07D295/15 , C07D307/68 , C07D317/58 , C07D335/10 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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公开(公告)号：US08088611B2
公开(公告)日：2012-01-03
申请号：US12784760
申请日：2010-05-21
申请人： Andrew J. Prongay , Thierry O. Fischmann , Chandra C. Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
发明人： Andrew J. Prongay , Thierry O. Fischmann , Chandra C. Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
IPC分类号： C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention provides, in part, AKT3 polypeptides and methods of use thereof along with nucleic acids encoding the polypeptides. For example, methods for screening for AKT3 inhibitors are provided herein.
摘要翻译： 本发明部分地提供AKT3多肽及其与编码多肽的核酸的使用方法。 例如，本文提供了用于筛选AKT3抑制剂的方法。
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5.发明授权Polynucleotides encoding polypeptide fragments of protein kinase B gamma (AKT3) 失效编码蛋白激酶Bγ（AKT3）多肽片段的多核苷酸公开(公告)号：US07776589B1
公开(公告)日：2010-08-17
申请号：US11847801
申请日：2007-08-30
申请人： Andrew J. Prongay , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
发明人： Andrew J. Prongay , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention provides, in part, AKT3 polypeptides and methods of use thereof along with nucleic acids encoding the polypeptides. For example, methods for screening for AKT3 inhibitors are provided herein.
摘要翻译： 本发明部分地提供AKT3多肽及其与编码多肽的核酸的使用方法。 例如，本文提供了用于筛选AKT3抑制剂的方法。
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6.发明授权Crystalline form of the catalytic domain of Aurora 2 kinase and methods of use thereof 失效Aurora 2激酶催化结构域的结晶形式及其使用方法公开(公告)号：US07422885B1
公开(公告)日：2008-09-09
申请号：US10943438
申请日：2004-09-17
申请人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
发明人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
CPC分类号： C12N9/12
摘要： The present invention discloses nucleic acids that encode an active human Aurora 2 kinase catalytic domain. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human Aurora 2 kinase catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human Aurora 2 kinase. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human Aurora 2 kinase in structure assisted drug design to identify compounds that can modulate the enzymatic activity of human Aurora 2 kinase.
摘要翻译： 本发明公开了编码活性人Aurora 2激酶催化结构域的核酸。 本发明还公开了生长包含活性人Aurora 2激酶催化结构域的多肽的X射线衍射晶体的方法。 本发明还公开了人Aurora 2激酶的催化结构域的结晶形式。 此外，本发明公开了在结构辅助药物设计中使用人Aurora 2激酶的X射线衍射晶体的方法来鉴定可调节人Aurora 2激酶的酶活性的化合物。
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7.发明授权公开(公告)号：US07824491B2
公开(公告)日：2010-11-02
申请号：US12184770
申请日：2008-08-01
申请人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
发明人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
CPC分类号： C12N9/12
摘要： The present invention discloses nucleic acids that encode an active human Aurora 2 kinase catalytic domain. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human Aurora 2 kinase catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human Aurora 2 kinase. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human Aurora 2 kinase in structure assisted drug design to identify compounds that can modulate the enzymatic activity of human Aurora 2 kinase.
摘要翻译： 本发明公开了编码活性人Aurora 2激酶催化结构域的核酸。 本发明还公开了生长包含活性人Aurora 2激酶催化结构域的多肽的X射线衍射晶体的方法。 本发明还公开了人Aurora 2激酶的催化结构域的结晶形式。 此外，本发明公开了在结构辅助药物设计中使用人Aurora 2激酶的X射线衍射晶体的方法来鉴定可调节人Aurora 2激酶的酶活性的化合物。
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公开(公告)号：US20100267053A1
公开(公告)日：2010-10-21
申请号：US12784760
申请日：2010-05-21
申请人： ANDREW J. PRONGAY , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
发明人： ANDREW J. PRONGAY , Thierry O. Fischmann , Chandra Kumar , Vincent S. Madison , Joseph E. Myers , Paul Reichert , Rosalinda Syto , William T. Windsor , Li Xiao , Todd W. Mayhood
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention provides, in part, AKT3 polypeptides and methods of use thereof along with nucleic acids encoding the polypeptides. For example, methods for screening for AKT3 inhibitors are provided herein.
摘要翻译： 本发明部分地提供AKT3多肽及其与编码多肽的核酸的使用方法。 例如，本文提供了用于筛选AKT3抑制剂的方法。
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公开(公告)号：US07511063B2
公开(公告)日：2009-03-31
申请号：US11504869
申请日：2006-08-16
申请人： Yongqi Deng , Patrick J. Curran , Gerald W. Shipps, Jr. , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
发明人： Yongqi Deng , Patrick J. Curran , Gerald W. Shipps, Jr. , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
IPC分类号： A61K31/47 , C07D215/14
CPC分类号： C07D409/04 , C07D215/48 , C07D215/50 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/10
摘要： Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
摘要翻译： 描述了基于喹啉的细胞周期蛋白依赖性激酶2抑制剂，包括抑制剂的组合物，以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法，抑制CDK-2的方法以及治疗疾病或疾病症状的方法。
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10.发明申请CRYSTALLINE FORM OF THE CATALYTIC DOMAIN OF AURORA 2 KINASE AND METHODS OF USE THEREOF 有权AURORA 2激酶的催化域的结晶形式及其使用方法公开(公告)号：US20090081706A1
公开(公告)日：2009-03-26
申请号：US12184770
申请日：2008-08-01
申请人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
发明人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
CPC分类号： C12N9/12
摘要： The present invention discloses nucleic acids that encode an active human Aurora 2 kinase catalytic domain. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human Aurora 2 kinase catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human Aurora 2 kinase. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human Aurora 2 kinase in structure assisted drug design to identify compounds that can modulate the enzymatic activity of human Aurora 2 kinase.
摘要翻译： 本发明公开了编码活性人Aurora 2激酶催化结构域的核酸。 本发明还公开了生长包含活性人Aurora 2激酶催化结构域的多肽的X射线衍射晶体的方法。 本发明还公开了人Aurora 2激酶的催化结构域的结晶形式。 此外，本发明公开了在结构辅助药物设计中使用人Aurora 2激酶的X射线衍射晶体的方法来鉴定可调节人Aurora 2激酶的酶活性的化合物。
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