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公开(公告)号：US09422292B2
公开(公告)日：2016-08-23
申请号：US14114983
申请日：2012-05-04
申请人： Brian K. Albrecht , Victor S. Gehling , Michael Charles Hewitt , Alexander M. Taylor , Jean-Christophe Harmange
发明人： Brian K. Albrecht , Victor S. Gehling , Michael Charles Hewitt , Alexander M. Taylor , Jean-Christophe Harmange
IPC分类号： A61K31/551 , C07D471/14 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
摘要翻译： 本发明涉及可用作含溴结构域蛋白质的抑制剂的化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。
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公开(公告)号：US09328117B2
公开(公告)日：2016-05-03
申请号：US14126877
申请日：2012-06-15
IPC分类号： A61K31/5025 , C07D487/04
CPC分类号： C07D487/04 , A61K31/5025
摘要： The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
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公开(公告)号：US20130310379A1
公开(公告)日：2013-11-21
申请号：US13988180
申请日：2011-11-21
申请人： Brian K. Albrecht , James Edmund Audia , Alexandre Gagnon , Jean-Christophe Harmange , Christopher G. Naveschuk
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Gagnon , Jean-Christophe Harmange , Christopher G. Naveschuk
IPC分类号： C07D211/58 , C07D451/04 , C07D471/04 , C07D207/14 , C07D401/12 , C07D405/12
CPC分类号： C07D211/58 , A61K31/4545 , C07D207/14 , C07D401/12 , C07D405/12 , C07D451/04 , C07D471/04
摘要： Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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公开(公告)号：US08198448B2
公开(公告)日：2012-06-12
申请号：US12287791
申请日：2008-10-14
申请人： Brian K. Albrecht , David Bauer , Alessandro Boezio , Deborah Choquette , Jean-Christophe Harmange , Richard T. Lewis , Julia Lohman , Michelle Potashman , Emily A. Peterson , Katrina W. Copeland , Karina Romero
发明人： Brian K. Albrecht , David Bauer , Alessandro Boezio , Deborah Choquette , Jean-Christophe Harmange , Richard T. Lewis , Julia Lohman , Michelle Potashman , Emily A. Peterson , Katrina W. Copeland , Karina Romero
IPC分类号： C07D487/04 , C07D403/12 , C07D403/14 , A61K31/53 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D519/00
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译： 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号：US08557996B2
公开(公告)日：2013-10-15
申请号：US12716187
申请日：2010-03-02
IPC分类号： C07D487/04 , A61K31/437 , A61P35/00
CPC分类号： C07D213/74 , C07D213/81 , C07D215/14 , C07D239/42 , C07D241/42 , C07D401/06 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症，癌症和相关病症的化合物。 化合物具有通式I，其中A1，A2，A3，A4，R1和R2如本文所定义。 因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US20110118250A1
公开(公告)日：2011-05-19
申请号：US12909566
申请日：2010-10-21
申请人： Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
发明人： Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC分类号： A61K31/538 , C07D405/12 , A61K31/4433 , A61K31/444 , C07D405/14 , A61K31/4439 , A61K31/506 , A61K31/497 , C07D413/12 , A61K31/5377 , A61K31/4178 , A61K31/4545 , A61K31/453 , C07D311/96 , A61K31/352 , C07D407/12 , A61K31/4709 , C07D401/12 , C07D409/12 , A61K31/422 , A61K31/4025 , C07D471/04 , A61K31/501 , A61P25/28 , A61P25/00 , A61P25/16
CPC分类号： C07D405/12 , C07D413/12
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默氏病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US08163766B2
公开(公告)日：2012-04-24
申请号：US12909566
申请日：2010-10-21
申请人： Wenge Zhong , Stephen A. Hitchcock , Vinod F. Patel , Yuan Cheng , Michael Croghan , Randall W. Hungate , Daniel La , Patricia Lopez , Matthew K. Kaller , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Lewis Pennington , Matthew Weiss , Ted Judd , Russell Graceffa , Qiufen Xue , Charles Kreiman , Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Scott Harried , Craig Masse , Bryant Yang
发明人： Wenge Zhong , Stephen A. Hitchcock , Vinod F. Patel , Yuan Cheng , Michael Croghan , Randall W. Hungate , Daniel La , Patricia Lopez , Matthew K. Kaller , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Lewis Pennington , Matthew Weiss , Ted Judd , Russell Graceffa , Qiufen Xue , Charles Kreiman , Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Scott Harried , Craig Masse , Bryant Yang
IPC分类号： A61K31/436
CPC分类号： C07D405/12 , C07D413/12
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US07973047B2
公开(公告)日：2011-07-05
申请号：US12779858
申请日：2010-05-13
申请人： Wenge Zhong , Stephen Hitchcock , Brian K. Albrecht , Michael D. Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig E. Masse , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Holger Monenschein , Thomas Nguyen
发明人： Wenge Zhong , Stephen Hitchcock , Brian K. Albrecht , Michael D. Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig E. Masse , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Holger Monenschein , Thomas Nguyen
IPC分类号： A61K31/438 , C07D471/00
CPC分类号： C07D405/12 , C07D311/68 , C07D413/12 , C07D491/052
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，W，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US07838676B2
公开(公告)日：2010-11-23
申请号：US11599901
申请日：2006-11-14
申请人： Qiufen Xue , Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Bryant Yang , Wenge Zhong
发明人： Qiufen Xue , Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Bryant Yang , Wenge Zhong
IPC分类号： C07D498/02 , C07D401/00
CPC分类号： C07D405/12 , C07D413/12
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, W, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中R 1，W，B，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US20100222338A1
公开(公告)日：2010-09-02
申请号：US12779858
申请日：2010-05-13
申请人： Wenge Zhong , Stephen Hitchcock , Brian K. Albrecht , Michael D. Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig E. Masse , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Holger Monenschein , Thomas Nguyen
发明人： Wenge Zhong , Stephen Hitchcock , Brian K. Albrecht , Michael D. Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig E. Masse , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Holger Monenschein , Thomas Nguyen
IPC分类号： A61K31/165 , C07D307/78 , C07D409/02 , C07D311/04 , C07C255/49 , C07C237/00 , C07D491/052 , C07D215/00 , C07D405/02 , C07D413/02 , A61K31/343 , A61K31/4025 , A61K31/352 , A61K31/47 , A61K31/5377 , A61P25/28 , A61P25/00 , A61P25/16
CPC分类号： C07D405/12 , C07D311/68 , C07D413/12 , C07D491/052
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，W，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。
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