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公开(公告)号：US20140148436A1
公开(公告)日：2014-05-29
申请号：US14170272
申请日：2014-01-31
Applicant: Array BioPharma, Inc.
Inventor： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicolas C. Kallan , Mark Munson , Guy P.A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
IPC: C07D239/94 , C07D403/12 , C07D495/04 , C07D491/048 , C07D231/56 , C07D401/12 , C07D409/04 , C07D401/04 , C07D409/12 , C07D487/04
CPC classification number: C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. 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.
Abstract translation: 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 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：US20130143865A1
公开(公告)日：2013-06-06
申请号：US13753008
申请日：2013-01-29
Applicant: Array BioPharma Inc. , GENENTECH, INC.
Inventor： Josef R. Bencsik , James F. Blake , Nicholas C. Kallan , Ian S. Mitchell , Keith L. Spencer , Dengming Xiao , Rui Xu , Christine Chabot , Jun Liang , Brian S. Safina
IPC: C07D409/12 , C07D403/12 , C07D401/12 , C07D239/70
CPC classification number: C07D239/70 , A61K31/506 , C07D401/12 , C07D403/12 , C07D409/12
Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. 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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公开(公告)号：US10329288B2
公开(公告)日：2019-06-25
申请号：US14913635
申请日：2014-08-21
Applicant: Genentech, Inc. , Array BioPharma Inc.
Inventor： Chong Han , Keena Green , Francis Gosselin , Michelangelo Scalone , Paul J. Nichols , Weidong Liu , Keith L. Spencer , Zackary D. Crane , Peter J. Stengel , Sagar Shakya
IPC: C07D471/04
Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.
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公开(公告)号：US20180282324A1
公开(公告)日：2018-10-04
申请号：US15806650
申请日：2017-11-08
Applicant: Genentech, Inc. , Array Biopharma Inc.
Inventor： Jeffrey Stults , Christopher M. Lindemann , Keith L. Spencer , Weidong Liu , Joseph Lubach
IPC: C07D471/04 , A61K31/437 , A61K45/06
Abstract: Disclosed are crystalline forms of (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.
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公开(公告)号：US09416110B2
公开(公告)日：2016-08-16
申请号：US14401087
申请日：2013-05-17
Applicant: Array BioPharma Inc. , Genentech, Inc.
Inventor： David Askin , Chong Han , Jonathan W. Lane , Travis Remarchuk , Sagar Shakya , C. Gregory Sowell , Keith L. Spencer , Peter J. Stengel
IPC: C07D239/02 , C07D239/42 , C07D239/30 , C07D403/04 , C07D239/70
CPC classification number: C07D239/42 , C07D239/30 , C07D239/70 , C07D403/04
Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.
Abstract translation: 本发明提供制备式I化合物及其盐的方法，其中R 1在本文中定义，以及所述式的化合物和中间体。
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Patent Agency Ranking
公开(公告)号：US09309204B2
公开(公告)日：2016-04-12
申请号：US14401091
申请日：2013-05-17
Applicant: Array BioPharma Inc. , Genentech, Inc.
Inventor： Jonathan W. Lane , Travis Remarchuk , Sagar Shakya , Keith L. Spencer , Peter J. Stengel
IPC: C07D403/04 , C07D239/70 , C07D239/42
CPC classification number: C07D239/70 , C07D239/42 , C07D403/04
Abstract: The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
Abstract translation: 本发明提供了用于制备和纯化羟基化环戊二烯并[d]嘧啶化合物的新方法，其可用于治疗诸如癌症的疾病作为AKT蛋白激酶抑制剂，包括化合物（S）-2-（4-氯苯基）-1 - （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） -1。
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公开(公告)号：US20170247337A1
公开(公告)日：2017-08-31
申请号：US15593064
申请日：2017-05-11
Applicant: Array BioPharma Inc. , Genentech, Inc.
Inventor： David Askin , Chong Han , Jonathan W. Lane , Travis Remarchuk , Sagar Shakya , C. Gregory Sowell , Keith L. Spencer , Peter J. Stengel
IPC: C07D239/42
CPC classification number: C07D239/42 , C07D239/30 , C07D239/70 , C07D403/04
Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.
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公开(公告)号：US20160251350A1
公开(公告)日：2016-09-01
申请号：US15054611
申请日：2016-02-26
Applicant: Genentech, Inc. , Array Biopharma Inc.
Inventor： Jeffrey Stults , Christopher M. Lindemann , Keith L. Spencer , Weidong Liu , Joseph Lubach
IPC: C07D471/04 , A61K45/06 , A61K31/437
CPC classification number: C07D471/04 , A61K31/437 , A61K45/06
Abstract: Disclosed are crystalline forms of (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.
Abstract translation: 公开了（R）-N-（4-（3-氨基哌啶-1-基）-5-溴-1H-吡咯并[2,3-b]吡啶-3-基）环丙烷甲酰胺和盐，溶剂化物的结晶形式 及其水合物，以及药物组合物，制剂及其制造方法。
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公开(公告)号：US09409886B2
公开(公告)日：2016-08-09
申请号：US14086717
申请日：2013-11-21
Applicant: Array BioPharma Inc. , Genentech, Inc.
Inventor： Josef Bencsik , James F. Blake , James M. Graham , Martin F. Hentemann , Nicholas C. Kallan , Ian S. Mitchell , Stephen T. Schlachter , Keith L. Spencer , Dengming Xiao , Rui Xu , Mike Welch , Jun Liang , Brian S. Safina
IPC: C07D403/12 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D403/14 , A61P35/02 , A61P35/04 , A61P29/00 , A61P9/00 , A61P25/28 , A61P35/00 , A61P25/16 , A61P31/04 , A61P37/06 , A61P37/08 , A61P17/06 , A61P11/06
CPC classification number: C07D403/12 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12
Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. 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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公开(公告)号：US20160152576A9
公开(公告)日：2016-06-02
申请号：US14170272
申请日：2014-01-31
Applicant: Array BioPharma, Inc.
Inventor： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicolas C. Kallan , Mark Munson , Guy P.A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
IPC: C07D239/94 , C07D403/12 , C07D495/04 , C07D491/048 , C07D231/56 , C07D401/12 , C07D409/04 , C07D401/04 , C07D409/12 , C07D487/04
CPC classification number: C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. 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.
Abstract translation: 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 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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