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公开(公告)号：WO2016055028A1
公开(公告)日：2016-04-14
申请号：PCT/CN2015/091614
申请日：2015-10-10
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC. , ROMERO, F. Anthony , MAGNUSON, Steven R. , PASTOR, Richard , TSUI, Vickie Hsiao-Wei , MURRAY, Jeremy , CRAWFORD, Terry , BURDICK, Daniel J. , ALBRECHT, Brian K. , COTE, Alexandre , TAYLOR, Alexander M. , NASVESCHUK, Christopher G. , LEBLANC, Yves , HEWITT, Michael Charles , LAI, Kwong Wah , CHEN, Kevin
发明人： ROMERO, F. Anthony , MAGNUSON, Steven R. , PASTOR, Richard , TSUI, Vickie Hsiao-Wei , MURRAY, Jeremy , CRAWFORD, Terry , BURDICK, Daniel J. , ALBRECHT, Brian K. , COTE, Alexandre , TAYLOR, Alexander M. , NASVESCHUK, Christopher G. , LEBLANC, Yves , HEWITT, Michael Charles , LAI, Kwong Wah , CHEN, Kevin
IPC分类号： C07D223/16 , C07D243/12 , C07D267/14 , C07D281/10 , A61K31/551 , A61K31/553 , A61K31/554 , A61P29/00 , A61P37/00 , A61P35/00
CPC分类号： A61K31/55 , A61K31/337 , A61K31/5513 , A61K45/06 , C07D223/16 , C07D243/12 , C07D243/24 , C07D267/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/10 , C07D471/04 , C07D495/04 , A61K2300/00
摘要： The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
摘要翻译： 本发明涉及式（I）的化合物及其盐，其中A具有说明书中定义的任何值，以及其组成和用途。 该化合物可用作CBP和/或EP300的抑制剂。 还包括包含式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种CBP和/或EP300介导的病症中使用这些化合物和盐的方法。
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公开(公告)号：WO2012075456A1
公开(公告)日：2012-06-07
申请号：PCT/US2011/063173
申请日：2011-12-02
申请人： CONSTELLATION PHARMACEUTICALS , ALBRECHT, Brian, K. , AUDIA, James, Edmund , CÔTÉ, Alexandre , GEHLING, Victor, S. , HARMANGE, Jean-Christophe , HEWITT, Michael, Charles , NAVESCHUK, Christopher, G. , TAYLOR, Alexander, M. , VASWANI, Rishi, G.
发明人： ALBRECHT, Brian, K. , AUDIA, James, Edmund , CÔTÉ, Alexandre , GEHLING, Victor, S. , HARMANGE, Jean-Christophe , HEWITT, Michael, Charles , NAVESCHUK, Christopher, G. , TAYLOR, Alexander, M. , VASWANI, Rishi, G.
CPC分类号： C07D513/20 , C07D487/10 , C07D495/14 , C07D495/20 , C07D495/22 , C07D498/04 , C07D498/10 , C07D498/14 , C07D513/14
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以及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：WO2012068589A3
公开(公告)日：2012-05-24
申请号：PCT/US2011/061740
申请日：2011-11-21
申请人： CONSTELLATION PHARMACEUTICALS , ALBRECHT, Brian, K. , AUDIA, James, Edmund , GAGNON, Alexandre , HARMANGE, Jean-Christophe , NASVESCHUK, Christopher, G.
发明人： ALBRECHT, Brian, K. , AUDIA, James, Edmund , GAGNON, Alexandre , HARMANGE, Jean-Christophe , NASVESCHUK, Christopher, G.
IPC分类号： A01N57/00
摘要： Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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公开(公告)号：WO2009091374A2
公开(公告)日：2009-07-23
申请号：PCT/US2008/011724
申请日：2008-10-14
申请人： AMGEN INC. , ALBRECHT, Brian K. , BAUER, David , BELLON, Steven , BODE, Christiane M. , BOOKER, Shon , BOEZIO, Alessandro , CHOQUETTE, Deborah , D'AMICO, Erin , HARMANGE, Jean-christophe , HIRAI, Satoko , HUNGATE, Randall W. , KIM, Tae-seong , LEWIS, Richard T. , LIU, Longbin , LOHMAN, Julia , NORMAN, Mark H. , POTASHMAN, Michelle , SIEGMUND, Aaron C. , SPRINGER, Stephanie , STEC, Markian , XI, Ning , YANG, Kevin , PETERSON, Emily, A. , ROMERO, Karina , COPELAND, Katrina, W.
发明人： ALBRECHT, Brian K. , BAUER, David , BELLON, Steven , BODE, Christiane M. , BOOKER, Shon , BOEZIO, Alessandro , CHOQUETTE, Deborah , D'AMICO, Erin , HARMANGE, Jean-christophe , HIRAI, Satoko , HUNGATE, Randall W. , KIM, Tae-seong , LEWIS, Richard T. , LIU, Longbin , LOHMAN, Julia , NORMAN, Mark H. , POTASHMAN, Michelle , SIEGMUND, Aaron C. , SPRINGER, Stephanie , STEC, Markian , XI, Ning , YANG, Kevin , PETERSON, Emily, A. , ROMERO, Karina , COPELAND, Katrina, W.
IPC分类号： C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , A61K31/4355
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：WO2007061670A1
公开(公告)日：2007-05-31
申请号：PCT/US2006/044058
申请日：2006-11-13
申请人： AMGEN INC. , ZHONG, Wenge , HITCHCOCK, Stephen , ALBRECHT, Brian K , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HICKMAN, Dean , HORNE, Daniel , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod F. , PENNINGTON, Lewis , WEISS, Matthew , XUE, Qiufen , YANG, Bryant
发明人： ZHONG, Wenge , HITCHCOCK, Stephen , ALBRECHT, Brian K , BARTBERGER, Michael , BROWN, James , BROWN, Ryan , CHAFFEE, Stuart C. , CHENG, Yuan , CROGHAN, Michael , GRACEFFA, Russell , HARRIED, Scott , HICKMAN, Dean , HORNE, Daniel , HUNGATE, Randall , JUDD, Ted , KALLER, Matthew , KREIMAN, Charles , LA, Daniel , LOPEZ, Patricia , MASSE, Craig E. , MONENSCHEIN, Holger , NGUYEN, Thomas , NIXEY, Thomas , PATEL, Vinod F. , PENNINGTON, Lewis , WEISS, Matthew , XUE, Qiufen , YANG, Bryant
IPC分类号： C07D405/12 , C07D413/12 , A61K31/44 , A61P25/28
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, R 3 , R 4 , R 5 , 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，通过施用式（I）化合物或其组合物，包括它们， 到一个主题。 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：WO2006044823A3
公开(公告)日：2006-06-15
申请号：PCT/US2005037299
申请日：2005-10-17
申请人： AMGEN INC , CHAFFEE STUART C , ALBRECHT BRIAN K , HODOUS BRIAN L , MARTIN MATTHEW W , MCGOWAN DAVID C , DIMAURO ERIN F , REDDY GADE , CEE VICTOR J , OLIVIERI PHILIP R , REED ANTHONY , ROMERO KARINA
发明人： CHAFFEE STUART C , ALBRECHT BRIAN K , HODOUS BRIAN L , MARTIN MATTHEW W , MCGOWAN DAVID C , DIMAURO ERIN F , REDDY GADE , CEE VICTOR J , OLIVIERI PHILIP R , REED ANTHONY , ROMERO KARINA
IPC分类号： C07D239/42 , A61K31/505 , 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，癌症和相关病症的一类新化合物。 该化合物具有通式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：WO2005113494A2
公开(公告)日：2005-12-01
申请号：PCT/US2005/016346
申请日：2005-05-09
申请人： AMGEN INC. , GEUNS-MEYER, Stephanie, D. , HODOUS, Brian, L. , CHAFFEE, Stuart, C. , TEMPEST, Paul, A. , OLIVIERI, Philip, R. , JOHNSON, Rebecca, E. , ALBRECHT, Brian, K. , PATEL, Vinod, F. , CEE, Victor, J. , KIM, Joseph, L. , BELLON, Steven , ZHU, Xiaotian , CHENG, Yuan , XI, Ning , ROMERO, Karina , NGUYEN, Hanh, Nho , DEAK, Holly, L.
发明人： GEUNS-MEYER, Stephanie, D. , HODOUS, Brian, L. , CHAFFEE, Stuart, C. , TEMPEST, Paul, A. , OLIVIERI, Philip, R. , JOHNSON, Rebecca, E. , ALBRECHT, Brian, K. , PATEL, Vinod, F. , CEE, Victor, J. , KIM, Joseph, L. , BELLON, Steven , ZHU, Xiaotian , CHENG, Yuan , XI, Ning , ROMERO, Karina , NGUYEN, Hanh, Nho , DEAK, Holly, L.
IPC分类号： C07D1/04
CPC分类号： C07D213/73 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H 1-5 and R 1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
摘要翻译： 本发明涉及具有通式I的化合物，其中A，B，D，E，G，H 1-5和R 1-4如本文所定义，以及合成中间体，其能够调节各种 蛋白激酶受体酶，从而影响与这些激酶的活性相关的各种疾病状态和状况。 例如，这些化合物能够调节激酶，从而影响血管生成过程并治疗血管生成相关疾病和其它包括癌症和炎症的复发性疾病。 本发明还包括药物组合物，包括该化合物，以及治疗与蛋白激酶活性有关的疾病状态的方法。
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公开(公告)号：WO2012174487A8
公开(公告)日：2014-01-16
申请号：PCT/US2012042825
申请日：2012-06-15
申请人： CONSTELLATION PHARMACEUTICALS INC , ALBRECHT BRIAN K , HARMANGE JEAN-CHRISTOPHE , COTE ALEXANDRE , TAYLOR ALEXANDER M
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00 , C07D403/04
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.
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：WO2012174487A3
公开(公告)日：2013-04-25
申请号：PCT/US2012042825
申请日：2012-06-15
申请人： CONSTELLATION PHARMACEUTICALS INC , ALBRECHT BRIAN K , HARMANGE JEAN-CHRISTOPHE , COTE ALEXANDRE , TAYLOR ALEXANDRE M
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00 , C07D403/04
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.
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：WO2012174487A2
公开(公告)日：2012-12-20
申请号：PCT/US2012/042825
申请日：2012-06-15
申请人： CONSTELLATION PHARMACEUTICALS, INC. , ALBRECHT, Brian, K. , HARMANGE, Jean-christophe , CÔTÉ, Alexandre , TAYLOR, Alexandre, M.
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.
摘要翻译： 本发明涉及可用作含溴结构域蛋白抑制剂的化合物。 本发明还提供了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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