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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：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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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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公开(公告)号：US20190209560A1
公开(公告)日：2019-07-11
申请号：US16178678
申请日：2018-11-02
IPC分类号： A61K31/506 , A61K31/551 , A61K31/52 , A61K31/519 , C07D519/00 , C07D495/20 , C07D471/04 , C07D471/20 , C07D471/10 , C07D487/04 , C07D473/34 , C07D491/20
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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公开(公告)号：US11440917B2
公开(公告)日：2022-09-13
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：US20180085368A1
公开(公告)日：2018-03-29
申请号：US15809011
申请日：2017-11-10
IPC分类号： A61K31/506 , A61K31/551 , C07D473/34 , C07D487/04 , C07D471/10 , C07D471/20 , C07D471/04 , C07D495/20 , C07D519/00 , A61K31/519 , A61K31/52 , C07D491/20
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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公开(公告)号：US09957277B2
公开(公告)日：2018-05-01
申请号：US15358761
申请日：2016-11-22
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： C07D491/00 , C07D491/048 , C07D307/93 , C07D333/78 , C07D491/153 , C07D491/16 , C07D491/20 , C07D498/14 , C07D519/00
CPC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：US20160317536A1
公开(公告)日：2016-11-03
申请号：US15187854
申请日：2016-06-21
IPC分类号： A61K31/506 , A61K31/52 , A61K31/551 , A61K31/519
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.
摘要翻译： 或其立体异构体，互变异构体或其药学上可接受的盐，其中R1，R2，R3，R4a，R4b，R5，R6，R7，R8，W1，W2，Y和n如本文所定义。 还描述了式I化合物的药学上可接受的组合物以及利用式I化合物和式I化合物的药学上可接受的组合物作为Mnk抑制剂以及用于治疗诸如癌症的疾病的治疗剂的方法。
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