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公开(公告)号：US11952375B2
公开(公告)日：2024-04-09
申请号：US17484564
申请日：2021-09-24
发明人： Siegfried H. Reich , Paul A. Sprengeler , Stephen E. Webber , Alan X. Xiang , Justin T. Ernst , Bennett C. Borer , Samuel Sperry , Jo Ann Z. Wilson
IPC分类号： C07D471/04 , A61K31/506 , A61P35/00
CPC分类号： C07D471/04 , C07B2200/13
摘要： The present invention provides crystalline solids of 6′-((6-aminopyrimidin-4-yl)amino)-8′-methyl-2′H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione:
The crystalline compounds of the present application are inhibitors of Mnk and finds utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.-
公开(公告)号：US20200339590A1
公开(公告)日：2020-10-29
申请号：US16804937
申请日：2020-02-28
发明人： Justin T. Ernst , Siegfried H. Reich , Paul A. Sprengeler , Chinh Viet Tran , Garrick Kenneth Packard , Alan X. Xiang , Christian Nilewski , Theo Michels
IPC分类号： C07D491/048 , C07D307/93 , C07D333/78 , C07D491/153 , C07D491/16 , C07D491/20 , C07D498/14 , C07D519/00
摘要： The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
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公开(公告)号：US10577378B2
公开(公告)日：2020-03-03
申请号：US15917973
申请日：2018-03-12
发明人： Justin T. Ernst , Siegfried H. Reich , Paul A. Sprengeler , Chinh Viet Tran , Garrick Kenneth Packard , Alan X. Xiang , Christian Nilewski , Theo Michels
IPC分类号： C07D491/048 , C07D307/93 , C07D333/78 , C07D491/153 , C07D491/16 , C07D491/20 , C07D498/14 , C07D519/00
摘要： The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
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公开(公告)号：US20180228803A1
公开(公告)日：2018-08-16
申请号：US15895523
申请日：2018-02-13
IPC分类号： A61K31/506 , A61P35/02 , A61P29/00
CPC分类号： A61K31/506 , A61P29/00 , A61P35/02
摘要： The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof wherein X1, X2, R1, R2, R3 and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.
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公开(公告)号：US20170266185A1
公开(公告)日：2017-09-21
申请号：US15611966
申请日：2017-06-02
IPC分类号： A61K31/506 , A61K31/52 , A61K31/519 , C07D487/04 , C07D473/34 , C07D519/00 , C07D495/20 , C07D491/20 , C07D471/20 , C07D471/10 , C07D471/04 , A61K31/551
CPC分类号： A61K31/506 , A61K31/519 , A61K31/52 , A61K31/551 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D491/20 , C07D495/20 , C07D519/00
摘要： The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula I compounds as well as methods for utilizing the compounds of Formula I and the pharmaceutically acceptable compositions of Formula I compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.
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6.发明申请公开(公告)号：US20170121346A1
公开(公告)日：2017-05-04
申请号：US15337184
申请日：2016-10-28
发明人： Paul A. Sprengeler , Siegfried H. Reich , Justin T. Ernst , Stephen E. Webber , Mike Shaghafi , Douglas Murphy , Chinh Tran
IPC分类号： C07D498/04 , C07D403/12 , C07D239/42 , C07D403/14 , C07D409/12 , C07D239/48 , C07D409/14 , C07D487/04 , C07D471/04 , C07D471/10 , C07D491/107 , C07D401/12 , C07D473/34 , C07D417/12
CPC分类号： C07D498/04 , C07D239/42 , C07D239/48 , C07D239/49 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D473/34 , C07D487/04 , C07D491/107
摘要： The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2, A3, A4, A5, W1, Y, R1, R2, R3, R4, R5, R6a, R6b, R7, R8, R8a, R8b, R9, R9a, R9b, and R10 and subscript “n” are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
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公开(公告)号：US20230381232A1
公开(公告)日：2023-11-30
申请号：US18158770
申请日：2023-01-24
发明人： Kevin R. WEBSTER , Rajesh SHARMA , Gary CHIANG
IPC分类号： A61K35/17 , C07K14/74 , A61P35/00 , C07K14/725 , C07K14/73 , C07K14/16 , C07K14/705 , C12N5/0783 , C07D471/04 , C07D487/04 , C07D495/20 , C07D491/20 , C07D471/20 , A61K31/501
CPC分类号： A61K35/17 , C07K14/70539 , A61P35/00 , C07K14/7051 , C07K14/70514 , C07K14/162 , C07K14/70517 , C07K14/70589 , C07K14/70564 , C12N5/0638 , C07D471/04 , C07D487/04 , C07D495/20 , C12N5/0636 , C07D491/20 , C07D471/20 , A61K31/501 , A61K45/06
摘要： The present disclosure relates to genetically modified T cells comprising a transgene encoding an engineered antigen specific receptor, wherein expression of an endogenous gene selected from MNK1, MNK2, or both are inhibited in the genetically modified T cell in order to enhance central memory T cell subsets in cellular immunotherapy compositions.
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公开(公告)号：US20210046074A1
公开(公告)日：2021-02-18
申请号：US16910921
申请日：2020-06-24
发明人： Kevin R. Webster , Vikas Goel
IPC分类号： A61K31/506 , A61K39/395 , A61K31/713 , A61K45/06
摘要： The present disclosure relates to the use MNK-specific inhibitors to inhibit immunosuppression components, such as immune checkpoint proteins PD-1, PD-L1, LAG3, and/or immunosuppressive cytokines, such as IL-10, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease.
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公开(公告)号：US20210010086A1
公开(公告)日：2021-01-14
申请号：US16881193
申请日：2020-05-22
IPC分类号： C12Q1/6886 , A61K31/506 , G01N33/574
摘要： The present disclosure relates to compositions and methods for identifying or diagnosing a human subject having or suspected of having a hyperproliferative disease and who would benefit from treatment with a MNK inhibitor.
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公开(公告)号：US10793551B2
公开(公告)日：2020-10-06
申请号：US16162459
申请日：2018-10-17
IPC分类号： C07D403/04 , C07D401/14 , A61P35/00
摘要： The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I or Formula II, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X1, X2, X3, X4, X5, Y1, Y2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification. The inventive Formula I and Formula II compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
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