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1.发明申请HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS 有权羟基和甲氧基吡咯烷酮作为AKT蛋白激酶抑制剂公开(公告)号：US20080051399A1
公开(公告)日：2008-02-28
申请号：US11773949
申请日：2007-07-05
申请人： Ian Mitchell , James Blake , Rui Xu , Nicholas Kallan , Dengming Xiao , Keith Spencer , Josef Bencsik , Eli Wallace , Stephen Schlachter , Anna Banka , Jun Liang , Brian Safina , Birong Zhang , Christine Chabot , Steven Do
发明人： Ian Mitchell , James Blake , Rui Xu , Nicholas Kallan , Dengming Xiao , Keith Spencer , Josef Bencsik , Eli Wallace , Stephen Schlachter , Anna Banka , Jun Liang , Brian Safina , Birong Zhang , Christine Chabot , Steven Do
IPC分类号： A61K31/519 , A61K31/535 , A61P29/00 , C07D239/00 , C07D413/00
CPC分类号： A61K31/517 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。
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公开(公告)号：US08853216B2
公开(公告)日：2014-10-07
申请号：US12811983
申请日：2009-01-09
申请人： Josef Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith L. Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang , James Graham
发明人： Josef Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith L. Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang , James Graham
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00 , A61P29/00 , A61P25/00 , A61P9/00 , A61P15/02 , A61P17/00
CPC分类号： C07D239/70
摘要： The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供了包含式I的化合物及其药学上可接受的盐。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US20100292244A1
公开(公告)日：2010-11-18
申请号：US12811983
申请日：2009-01-09
申请人： Josef Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mtchell , Keith L. Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang
发明人： Josef Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mtchell , Keith L. Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang
IPC分类号： A61K31/517 , C07D403/04 , A61P29/00 , A61P35/00 , A61P9/00 , A61P25/00 , A61P17/00 , A61P15/02
CPC分类号： C07D239/70
摘要： The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供了包含式I的化合物及其药学上可接受的盐。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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4.发明授权Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors 有权羟基化和甲氧基化的嘧啶基环戊烷作为AKT蛋白激酶抑制剂公开(公告)号：US08853199B2
公开(公告)日：2014-10-07
申请号：US13272079
申请日：2011-10-12
申请人： Ian S. Mitchell , James F. Blake , Rui Xu , Nicholas C. Kallan , Dengming Xiao , Keith Lee Spencer , Josef R. Bencsik , Eli M. Wallace , Stephen T. Schlachter , Anna L. Banka , Jun Liang , Brian Safina , Birong Zhang , Christine Chabot , Steven Do
发明人： Ian S. Mitchell , James F. Blake , Rui Xu , Nicholas C. Kallan , Dengming Xiao , Keith Lee Spencer , Josef R. Bencsik , Eli M. Wallace , Stephen T. Schlachter , Anna L. Banka , Jun Liang , Brian Safina , Birong Zhang , Christine Chabot , Steven Do
IPC分类号： C07D409/12 , C07D409/14 , C07D403/12 , C07D401/12 , C07D405/12 , C07D413/12 , A61K31/496 , A61P35/00 , A61P29/00 , A61P25/28 , C07D239/70
CPC分类号： A61K31/517 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。
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5.发明授权Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors 有权羟基化和甲氧基化的嘧啶基环戊烷作为AKT蛋白激酶抑制剂公开(公告)号：US08063050B2
公开(公告)日：2011-11-22
申请号：US11773949
申请日：2007-07-05
申请人： Ian S. Mitchell , James F. Blake , Rui Xu , Nicholas C. Kallan , Dengming Xiao , Keith Lee Spencer , Josef R. Bencsik , Eli M. Wallace , Stephen T. Schlachter , Anna L. Banka , Jun Liang , Brian Safina , Birong Zhang , Christine Chabot , Steven Do
发明人： Ian S. Mitchell , James F. Blake , Rui Xu , Nicholas C. Kallan , Dengming Xiao , Keith Lee Spencer , Josef R. Bencsik , Eli M. Wallace , Stephen T. Schlachter , Anna L. Banka , Jun Liang , Brian Safina , Birong Zhang , Christine Chabot , Steven Do
IPC分类号： C07D239/70 , A61K31/496 , A61P35/00
CPC分类号： A61K31/517 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。
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6.发明申请公开(公告)号：US20110065716A1
公开(公告)日：2011-03-17
申请号：US12811957
申请日：2009-01-09
申请人： Josef R. Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith Lee Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang
发明人： Josef R. Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith Lee Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang
IPC分类号： A61K31/517 , C07D403/04 , A61P35/00 , A61P25/28 , A61P9/00 , A61P29/00 , A61P15/00 , A61P17/00
CPC分类号： C07D239/70
摘要： The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供包含式（I）的化合物，包括其药学上可接受的盐：还提供使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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7.发明授权公开(公告)号：US08835434B2
公开(公告)日：2014-09-16
申请号：US12811957
申请日：2009-01-09
申请人： Josef R. Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith Lee Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang
发明人： Josef R. Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith Lee Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Steven Do , Jun Liang , Brian Safina , Birong Zhang
IPC分类号： A61K31/517 , C07D403/04 , A61P35/00 , A61P25/28 , A61P9/00 , A61P29/00 , A61P15/00 , C07D239/70
CPC分类号： C07D239/70
摘要： The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供包含式（I）的化合物，包括其药学上可接受的盐：还提供使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US07749994B2
公开(公告)日：2010-07-06
申请号：US11503405
申请日：2006-08-14
申请人： Thomas E. Rawson , Brian Safina , Jennafer Dotson , Aihe Zhou , Ignacio Aliagas-Martin , Jason Halladay , Jun Liang , Matthias Rueth , Bing-Yan Zhu , Frederick Brookfield , Michael Prime , Birong Zhang , Jun M. Li
发明人： Thomas E. Rawson , Brian Safina , Jennafer Dotson , Aihe Zhou , Ignacio Aliagas-Martin , Jason Halladay , Jun Liang , Matthias Rueth , Bing-Yan Zhu , Frederick Brookfield , Michael Prime , Birong Zhang , Jun M. Li
IPC分类号： A61K31/55 , A61K31/538 , A61K31/424 , A61K31/4188 , C07D498/22
CPC分类号： C07D487/04 , C07D491/04
摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.
摘要翻译： 本发明提供新的激酶抑制剂，其可用作例如治疗恶性肿瘤的治疗剂，其中化合物具有通式I，其中A，X，Y，Z，R a，R b，R c，R 1，R 2，R 3和m定义 这里。
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公开(公告)号：US20130096104A1
公开(公告)日：2013-04-18
申请号：US13635369
申请日：2011-03-15
申请人： Yingjie Lai , Jun Liang , Steven R. Magnuson , Kirk D. Robarge , Vickie H. Tsui , Birong Zhang , Aihe Zhou
发明人： Yingjie Lai , Jun Liang , Steven R. Magnuson , Kirk D. Robarge , Vickie H. Tsui , Birong Zhang , Aihe Zhou
IPC分类号： C07D471/04 , C07D473/00
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D519/00
摘要： The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illnesses, inflammatory bowel disease or psoriasis.
摘要翻译： 本发明提供式Ia-Ib的化合物，其立体异构体或其药学上可接受的盐，其中A，X，R 1，R 2，R 4，R 5和R 16如本文所定义，药物组合物包括式Ia-Ib的化合物和药学上可接受的盐 可接受的载体，佐剂或赋形剂，以及在治疗中使用该化合物或组合物作为TYK2激酶抑制剂和相关疾病如炎性疾病，炎症性肠病或银屑病的方法。
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公开(公告)号：US08697708B2
公开(公告)日：2014-04-15
申请号：US13232778
申请日：2011-09-14
申请人： Toby Jonathan Blench , Charles Ellwood , Simon Charles Goodacre , Yingjie Lai , Jun Liang , Calum Macleod , Steven R. Magnuson , Vickie H. Tsui , Karen Williams , Birong Zhang
发明人： Toby Jonathan Blench , Charles Ellwood , Simon Charles Goodacre , Yingjie Lai , Jun Liang , Calum Macleod , Steven R. Magnuson , Vickie H. Tsui , Karen Williams , Birong Zhang
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00
CPC分类号： A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/519 , C07D513/04
摘要： Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
摘要翻译： 提供式I化合物，立体异构体，互变异构体，溶剂合物，前药和药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义，药物组合物包括式I化合物和药学上可接受的 载体，佐剂或载体，在治疗中使用化合物或组合物的方法，以及制备式I化合物的方法。
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