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1.发明申请Amino-Oxazines and Amino-Dihydrothiazine Compounds as Beta-Secretase Modulators and Methods of Use 有权氨基 - 恶嗪和氨基 - 二氢噻嗪化合物作为β-分泌酶调节剂和使用方法公开(公告)号：US20110251186A1
公开(公告)日：2011-10-13
申请号：US13047693
申请日：2011-03-14
申请人： Jian J. CHEN , Wenge ZHONG , Bryant YANG , Wenyuan QIAN , Patricia LOPEZ , Ryan WHITE , Matthew WEISS , Ted JUDD , Timothy POWERS , Yuan CHENG , Thomas DINEEN , Oleg EPSTEIN , Jonathan LOW , Isaac MARX , Ana Elena MINATTI , Michele POTASHMAN , Nick A. PARAS
发明人： Jian J. CHEN , Wenge ZHONG , Bryant YANG , Wenyuan QIAN , Patricia LOPEZ , Ryan WHITE , Matthew WEISS , Ted JUDD , Timothy POWERS , Yuan CHENG , Thomas DINEEN , Oleg EPSTEIN , Jonathan LOW , Isaac MARX , Ana Elena MINATTI , Michele POTASHMAN , Nick A. PARAS
IPC分类号： A61K31/547 , A61P25/28 , C07D513/10 , C07D498/20 , A61K31/5386
CPC分类号： C07D513/10 , C07D498/10 , C07D498/20 , C07D513/20
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 A1, A2, A3, A4, A5, A6, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
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，其中式I中的A1，A2，A3，A4，A5，A6，R2，R7，X，Y和Z如本文所定义。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。
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公开(公告)号：US20120190666A1
公开(公告)日：2012-07-26
申请号：US13319683
申请日：2010-05-12
申请人： Christiane Bode , Alessandro Boezio , Alan C. Cheng , Deborah Choquette , James Robert Coats , Katrina Woodin Copeland , Hongbing Huang , Daniel La , Richard Thomas Lewis , Hongyu Liao , Michele Potashman , John Stellwagen , Shuyan Yi , Mark H. Norman , Markian M. Stec , Emily Anne Peterson , Russell Graceffa
发明人： Christiane Bode , Alessandro Boezio , Alan C. Cheng , Deborah Choquette , James Robert Coats , Katrina Woodin Copeland , Hongbing Huang , Daniel La , Richard Thomas Lewis , Hongyu Liao , Michele Potashman , John Stellwagen , Shuyan Yi , Mark H. Norman , Markian M. Stec , Emily Anne Peterson , Russell Graceffa
IPC分类号： A61K31/52 , C07D401/14 , A61K31/506 , A61P35/02 , A61K31/53 , C07D487/04 , A61K31/5377 , A61P35/00 , C07D473/40 , C07D471/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译： 本发明提供了PIKK抑制剂，更具体地，mTOR和/或PI3Kα激酶抑制剂的化合物，因此可用于治疗通过抑制激酶可治疗的疾病，特别是PI3激酶，更具体地，mTOR和/或PI3Kα，例如 癌症。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。
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公开(公告)号：US20120148531A1
公开(公告)日：2012-06-14
申请号：US13309488
申请日：2011-12-01
申请人： Brian K. ALBRECHT , David Bauer , Steven Bellon , Christiane M. Bode , Shon Booker , Alessandro Boezio , Deborah Choquette , Derin D'Amico , Jean-Christophe Harmange , Satoko Hirai , Randall W. Hungate , Tae-Seong Kim , Richard T. Lewis , Longbin Liu , Julia Lohman , Mark H. Norman , Michele Potashman , Aaron C. Siegmund , Stephanie Springer , Markian Stec , Ning Xi , Kevin Yang
发明人： Brian K. ALBRECHT , David Bauer , Steven Bellon , Christiane M. Bode , Shon Booker , Alessandro Boezio , Deborah Choquette , Derin D'Amico , Jean-Christophe Harmange , Satoko Hirai , Randall W. Hungate , Tae-Seong Kim , Richard T. Lewis , Longbin Liu , Julia Lohman , Mark H. Norman , Michele Potashman , Aaron C. Siegmund , Stephanie Springer , Markian Stec , Ning Xi , Kevin Yang
IPC分类号： A61K31/5025 , A61K31/5377 , A61K38/21 , A61P35/00 , A61P35/04 , C07D487/04 , A61K31/538
CPC分类号： A61K31/538 , A61K31/437 , A61K31/497 , A61K31/5025 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D403/12 , C07D471/04 , C07D473/34 , 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：US08088794B2
公开(公告)日：2012-01-03
申请号：US12945575
申请日：2010-11-12
申请人： Tae-Seong Kim , David Bauer , Steven Bellon , Alessandro Boezio , Shon Booker , Deborah Choquette , Derin C. D'Amico , Noel D'Angelo , Celia Dominguez , Ingrid M. Fellows , Julie Germain , Russell Graceffa , Jean-Christophe Harmange , Satoko Hirai , Daniel La , Matthew Lee , Longbin Liu , Mark H. Norman , Michele Potashman , Philip Roveto , Aaron C. Siegmund , Ning Xi , Kevin Yang
发明人： Tae-Seong Kim , David Bauer , Steven Bellon , Alessandro Boezio , Shon Booker , Deborah Choquette , Derin C. D'Amico , Noel D'Angelo , Celia Dominguez , Ingrid M. Fellows , Julie Germain , Russell Graceffa , Jean-Christophe Harmange , Satoko Hirai , Daniel La , Matthew Lee , Longbin Liu , Mark H. Norman , Michele Potashman , Philip Roveto , Aaron C. Siegmund , Ning Xi , Kevin Yang
IPC分类号： A61K31/47 , C07D453/02
CPC分类号： C07D413/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
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：US07531553B2
公开(公告)日：2009-05-12
申请号：US10804915
申请日：2004-03-19
申请人： Lucian V. Di Pietro , Jean-Christophe Harmange , Benny C. Askew, Jr. , Daniel Elbaum , Julie Germain , Gregory J. Habgood , Joseph L. Kim , Vinod F. Patel , Michele Potashman , Simon van der Plas
发明人： Lucian V. Di Pietro , Jean-Christophe Harmange , Benny C. Askew, Jr. , Daniel Elbaum , Julie Germain , Gregory J. Habgood , Joseph L. Kim , Vinod F. Patel , Michele Potashman , Simon van der Plas
IPC分类号： A61K31/47 , C07D215/00
CPC分类号： C07D401/12 , C07D235/30 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis 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血管生成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：US07435823B2
公开(公告)日：2008-10-14
申请号：US11042634
申请日：2005-01-24
申请人： Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , Gregory J. Habgood , David C. McGowan , Douglas A. Whittington , Daniel La , Vinod F. Patel
发明人： Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , Gregory J. Habgood , David C. McGowan , Douglas A. Whittington , Daniel La , Vinod F. Patel
IPC分类号： C07D215/38 , C07D265/34
CPC分类号： C07D213/64 , C07D213/81 , C07D215/233 , C07D215/38 , C07D215/48 , C07D215/54 , C07D237/34 , C07D239/34 , C07D239/47 , C07D239/84 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
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：US08217177B2
公开(公告)日：2012-07-10
申请号：US12009123
申请日：2008-01-15
申请人： Brian K. Albrecht , David Bauer , Steven Bellon , Christiane M. Bode , Alessandro Boezio , Deborah Choquette , Jean-Christophe Harmange , Julia Lohman , Michele Potashman
发明人： Brian K. Albrecht , David Bauer , Steven Bellon , Christiane M. Bode , Alessandro Boezio , Deborah Choquette , Jean-Christophe Harmange , Julia Lohman , Michele Potashman
IPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61P35/00
CPC分类号： A61K31/538 , A61K31/437 , A61K31/497 , A61K31/5025 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D403/12 , C07D471/04 , C07D473/34 , 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.
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公开(公告)号：US08178557B2
公开(公告)日：2012-05-15
申请号：US12157303
申请日：2008-06-09
申请人： Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , David C. McGowan , Douglas A. Whittington , Gregory J. Habgood , Vinod F. Patel , Daniel La
发明人： Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , David C. McGowan , Douglas A. Whittington , Gregory J. Habgood , Vinod F. Patel , Daniel La
IPC分类号： A61K31/04
CPC分类号： C07D213/64 , C07D213/81 , C07D215/233 , C07D215/38 , C07D215/48 , C07D215/54 , C07D237/34 , C07D239/34 , C07D239/47 , C07D239/84 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
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：US07759344B2
公开(公告)日：2010-07-20
申请号：US12008241
申请日：2008-01-09
申请人： Shon Booker , Noel D'Angelo , Julie Germain , Jean-Christophe Harmange , Tae-Seong Kim , Michele Potashman
发明人： Shon Booker , Noel D'Angelo , Julie Germain , Jean-Christophe Harmange , Tae-Seong Kim , Michele Potashman
IPC分类号： A61K31/495 , A61K31/4725 , A61K31/416 , C07D487/04 , C07D217/00 , C07D231/54
CPC分类号： C07D403/12 , C07D231/22 , C07D231/56 , C07D401/12 , C07D471/04
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as c-Met 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c-Met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：US20060040966A1
公开(公告)日：2006-02-23
申请号：US11185556
申请日：2005-07-19
申请人： Chester Yuan , Kevin Yang , Simon Van Der Plas , Babak Riahi , Michele Potashman , Vinod Patel , Rana Nomak , Aiwen Li , Qi Huang , Jean-Christophe Harmange , Benny Askew
发明人： Chester Yuan , Kevin Yang , Simon Van Der Plas , Babak Riahi , Michele Potashman , Vinod Patel , Rana Nomak , Aiwen Li , Qi Huang , Jean-Christophe Harmange , Benny Askew
IPC分类号： A61K31/517 , A61K31/4433 , C07D405/02 , C07D401/02
CPC分类号： C07D401/12 , C07D217/02 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II wherein R, R1 and R2 for each formula are defined herein. The invention further includes analogs, prodrugs and pharmaceutically acceptable salts and derivatives of Formulas I and II, as well as pharmaceutical compositions, medicaments and methods thereof 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： 选择的胺对于预防和治疗疾病如血管生成介导的疾病是有效的。 本发明包括式I和II的新型化合物，其中R 1，R 1和R 2各自在本文中定义。 本发明还包括式I和II的类似物，前药和药学上可接受的盐和衍生物，以及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，药物及其方法。 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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