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1.发明公开HYDROXYLATED AND METHOXYLATED CYCLOPENTA [D] PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 审中-公开羟肟酸甲氧基环戊二烯[D] - 吡啶ALS AKT-蛋白酶
公开(公告)号：EP2966065A2
公开(公告)日：2016-01-13
申请号：EP15178003.8
申请日：2007-07-05
发明人： MITCHELL, Ian, S. , BLAKE, James, F. , XU, Rui , KALLAN, Nicholas, C. , XIAO, Dengming , SPENCER, Keith, Lee , BENCSIK, Josef, R. , LIANG, Jun , SAFINA, Brian , ZHANG, Birong , CHABOT, Christine , DO, Steven , WALLACE, Eli, W. , BANKA, Anna, L. , SCHLACHTER, Stephen, T.
IPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I for use in oral dosage forms:
Also provided are oral dosage forms comprising these compounds, methods of using the compounds and oral dosage forms of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer. Further provided are intermediate compounds from the synthesis of these compounds.摘要翻译： 本发明提供包含拆分的对映异构体，分解的非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含用于口服剂型的式I：还提供包含这些化合物的口服剂型，使用该化合物的方法和口服剂型 的本发明作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病如癌症。 还提供了来自这些化合物的合成的中间体化合物。
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2.发明授权HYDROXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS 有权羟基化PYRIMIDYLCYCLOPENTANE AS AKT蛋白激酶抑制剂
公开(公告)号：EP2247578B1
公开(公告)日：2013-05-22
申请号：EP09700422.0
申请日：2009-01-09
发明人： BENCSIK, Josef R. , BLAKE, James F. , KALLAN, Nicholas C. , MITCHELL, Ian S. , SPENCER, Keith Lee , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70
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3.发明公开HYDROXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS 有权羟丙基吡嗪基胆碱酯酶AKT-PROTEINKINASEINHIBITOREN
公开(公告)号：EP2247578A1
公开(公告)日：2010-11-10
申请号：EP09700422.0
申请日：2009-01-09
发明人： BENCSIK, Josef R. , BLAKE, James F. , KALLAN, Nicholas C. , MITCHELL, Ian S. , SPENCER, Keith Lee , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00
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.
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4.发明授权HYDROXYLATED AND METHOXYLATED CYCLOPENTA [D] PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 有权羟基化和甲氧基化的CYCLO PENTA〔D]嘧啶类AS AKT蛋白激酶抑制剂的
公开(公告)号：EP2049501B1
公开(公告)日：2011-09-14
申请号：EP07799337.6
申请日：2007-07-05
发明人： MITCHELL, Ian, S. , BLAKE, James, F. , XU, Rui , KALLAN, Nicholas, C. , XIAO, Dengming , SPENCER, Keith, Lee , BENCSIK, Josef, R. , LIANG, Jun , SAFINA, Brian , ZHANG, Birong , CHABOT, Christine , DO, Steven , WALLACE, Eli, W. , BANKA, Anna, L. , SCHLACHTER, Stephen, T.
IPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14
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.
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5.发明公开HYDROXYLATED AND METHOXYLATED CYCLOPENTA [D] PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 有权羟肟酸甲氧基环戊二烯[D] - 吡啶ALS AKT-蛋白酶
公开(公告)号：EP2049501A1
公开(公告)日：2009-04-22
申请号：EP07799337.6
申请日：2007-07-05
发明人： MITCHELL, Ian, S. , BLAKE, James, F. , XU, Rui , KALLAN, Nicholas, C. , XIAO, Dengming , SPENCER, Keith, Lee , BENCSIK, Josef, R. , LIANG, Jun , SAFINA, Brian , ZHANG, Birong , CHABOT, Christine , DO, Steven , WALLACE, Eli, W. , BANKA, Anna, L. , SCHLACHTER, Stephen, T.
IPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14
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.
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6.发明公开HYDROXYLATED AND METHOXYLATED CYCLOPENTA [D] PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 审中-公开羟基化和甲氧基环戊二烯基[D]嘧啶作为AKT蛋白激酶抑制剂
公开(公告)号：EP2966065A3
公开(公告)日：2016-03-02
申请号：EP15178003.8
申请日：2007-07-05
发明人： MITCHELL, Ian, S. , BLAKE, James, F. , XU, Rui , KALLAN, Nicholas, C. , XIAO, Dengming , SPENCER, Keith, Lee , BENCSIK, Josef, R. , LIANG, Jun , SAFINA, Brian , ZHANG, Birong , CHABOT, Christine , DO, Steven , WALLACE, Eli, W. , BANKA, Anna, L. , SCHLACHTER, Stephen, T.
IPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I for use in oral dosage forms:
Also provided are oral dosage forms comprising these compounds, methods of using the compounds and oral dosage forms of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer. Further provided are intermediate compounds from the synthesis of these compounds.摘要翻译： 本发明提供了包含用于口服剂型的式I的化合物，包括拆分的对映体，拆分的非对映体，溶剂化物和药学上可接受的盐：还提供了包含这些化合物的口服剂型，使用该化合物的方法和口服剂型 作为AKT蛋白激酶抑制剂用于治疗过度增殖性疾病如癌症。 进一步提供了来自合成这些化合物的中间体化合物。
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7.发明授权HYDROXYLATED PYRIMIDYL CYCLOPENTANE AS AKT PROTEIN KINASE INHIBITOR 有权羟丙基吡咯烷基环丙烷酸AKT-PROTEINKINASEHEMMER
公开(公告)号：EP2240455B1
公开(公告)日：2012-12-26
申请号：EP09700629.0
申请日：2009-01-09
发明人： BENCSIK, Josef , BLAKE, James, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70
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8.发明公开HYDROXYLATED PYRIMIDYL CYCLOPENTANE AS AKT PROTEIN KINASE INHIBITOR 有权羟基化pyrimidylaminoquinoline环戊烷AS AKT蛋白激酶抑制剂
公开(公告)号：EP2240455A1
公开(公告)日：2010-10-20
申请号：EP09700629.0
申请日：2009-01-09
发明人： BENCSIK, Josef , BLAKE, James, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00
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.
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公开(公告)号：EP4320132A1
公开(公告)日：2024-02-14
申请号：EP22719149.1
申请日：2022-04-06
申请人： Genentech, Inc.
发明人： GAZZARD, Lewis J. , GREEN, Samantha Alyson , KELLEY, Elizabeth H. , LANDRY, Matthew Leo , MALHOTRA, Sushant , RAVETZ, Benjamin David , SIU, Michael , TERRETT, Jack Alexander , WEI, BinQing , DO, Steven , CHENG, Yun-Xing , CHENG, Limin , XIN, Jianfeng , HE, Mingtao , WU, Guosheng , SUN, Yinlei , SHAO, Cheng , LU, Aijun , ZHANG, Yulai
IPC分类号： C07D498/06 , C07D519/00 , A61P35/00 , A61K31/553
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公开(公告)号：EP3077401A1
公开(公告)日：2016-10-12
申请号：EP14827591.0
申请日：2014-12-03
申请人： Genentech, Inc.
发明人： KOLESNIKOV, Aleksandr , DO, Steven
IPC分类号： C07D498/16 , C07D471/16 , A61K31/4353
CPC分类号： A61K31/553 , A61K31/519 , A61K31/53 , A61K31/5365 , A61K31/542 , A61K31/55 , A61K45/06 , C07D471/16 , C07D498/16 , C07D513/16
摘要： Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
摘要翻译： 具有式I的化合物，其中如本文定义的R 1，X 1，X 2，X 3和X 4是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。
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