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1.发明公开公开(公告)号：US20240083910A1
公开(公告)日：2024-03-14
申请号：US18257003
申请日：2021-12-14
申请人： Richard BERGER , Christopher Douglas COX , Brendan M. CROWLEY , Marc LABROLI , Michael Aaron PLOTKIN , Izzat Tiedje RAHEEM , Deyou SHA , Anthony SHAW , Jason W. SKUDLAREK , Ling TONG , Merck Sharp & Dohme LLC
发明人： Richard Thaddeus Berger, JR. , Christopher Douglas Cox , Brendan M. Crowley , Marc Labroli , Michael Aaron Plotkin , Izzat Tiedje Raheem , Deyou Sha , Anthony W. Shaw , Jason W. Skudlarek , Ling Tong
IPC分类号： C07D498/04 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/517 , A61P31/22 , C07D401/14 , C07D519/00
CPC分类号： C07D498/04 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/517 , A61P31/22 , C07D401/14 , C07D519/00
摘要： The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.
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公开(公告)号：US20070281951A1
公开(公告)日：2007-12-06
申请号：US11788856
申请日：2007-04-20
申请人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Marc Labroli , Kartik Keertikar
发明人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Marc Labroli , Kartik Keertikar
IPC分类号： A61K31/495
CPC分类号： A61K31/519 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的组合物，制备药物制剂的方法，包括 一种或多种这样的化合物，以及使用这些化合物或组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。
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![Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors](/abs-image/US/2009/10/20/US07605155B2/abs.jpg.150x150.jpg)
3.发明授权公开(公告)号：US07605155B2
公开(公告)日：2009-10-20
申请号：US11542920
申请日：2006-10-04
IPC分类号： C07D487/04 , C07D413/06 , C07D417/04 , C07D243/08 , A61K31/519 , A61K31/551 , A61K31/497 , A61K31/541 , A61K31/5355 , A61P35/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. All illustrative compound is shown below:
摘要翻译： 在其许多实施方案中，本发明提供了一类作为细胞周期蛋白依赖性激酶（CDK）抑制剂的吡唑并[1,5-a]嘧啶化合物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备方法 包含一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。 所有说明性化合物如下所示：
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4.发明授权Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权三取代和四取代的吡唑并嘧啶作为细胞周期蛋白依赖性激酶抑制剂公开(公告)号：US07196078B2
公开(公告)日：2007-03-27
申请号：US11245401
申请日：2005-10-06
IPC分类号： A61K31/5513 , A61K31/5355 , A61K31/519 , C07D487/04 , C07D413/04 , C07D417/04 , C07D243/08 , A61K31/541 , A61P19/02 , A61P29/00 , C07D413/06
CPC分类号： C07D487/04 , Y02P20/582
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。
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公开(公告)号：US20060247320A1
公开(公告)日：2006-11-02
申请号：US11369643
申请日：2006-03-07
申请人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Yushi Xiao , Angela Kerekes , Tao Yu , Sunil Paliwal , Hon-Chung Tsui , Neng-Yang Shih , Stuart McCombie , Vincent Madison , Charles Lesburg , Jose Duca
发明人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Yushi Xiao , Angela Kerekes , Tao Yu , Sunil Paliwal , Hon-Chung Tsui , Neng-Yang Shih , Stuart McCombie , Vincent Madison , Charles Lesburg , Jose Duca
IPC分类号： A61K31/12
CPC分类号： C07D519/00 , C07D493/10 , C07D495/04 , C07D495/06 , C07D495/14 , C07D495/20 , C07D513/04
摘要： The present invention provides compounds of Formula I (wherein R1, R3, X, W, Z and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
摘要翻译： 本发明提供式I化合物（其中R 1，R 3，X，W，Z和环Y如本文所定义）。 本发明还提供了包含这些化合物的组合物，其可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病或病症并抑制KSP驱动蛋白活性。
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6.发明公开公开(公告)号：US20240067657A1
公开(公告)日：2024-02-29
申请号：US18258903
申请日：2021-12-21
申请人： Kira A. ARMACOST , Richard Thaddeus BERGER , Andrew J. COOKE , Christopher Douglas COX , Brendan M. CROWLEY , Marc LABROLI , Michael Aaron PLOTKIN , Izzat Tiedje RAHEEM , Anthony W. SHAW , Kelly-Ann S. SCHLEGEL , Jason W. SKUDLAREK , Ling TONG , Merck Sharp & Dohme LLC
发明人： Kira A. Armacost , Richard Thaddeus Berger, Jr. , Andrew J. Cooke , Christopher Douglas Cox , Brendan M. Crowley , Marc Labroli , Michael Aaron Plotkin , Izzat Tiedje Raheem , Anthony W. Shaw , Kelly-Ann S. Schlegel , Jason W. Skudlarek , Ling Tong
IPC分类号： C07D498/04 , A61K31/517 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D519/00
CPC分类号： C07D498/04 , A61K31/517 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D519/00
摘要： The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R7, and R8 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compound, and methods of using the Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.
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![Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors](/abs-image/US/2013/11/19/US08586576B2/abs.jpg.150x150.jpg)
7.发明授权Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors 有权取代的吡唑并[1,5-a]嘧啶作为细胞周期蛋白依赖性激酶抑制剂公开(公告)号：US08586576B2
公开(公告)日：2013-11-19
申请号：US11710644
申请日：2007-02-23
IPC分类号： A61K31/5513 , A61K31/5377 , A61K31/541 , A61K31/519 , A61P35/04 , A61P35/02 , A61P35/00 , C07D487/04 , C07D295/04 , C07D243/14
CPC分类号： C07D487/04 , Y02P20/582
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。
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公开(公告)号：US20060281778A1
公开(公告)日：2006-12-14
申请号：US11369625
申请日：2006-03-07
申请人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Angela Kerekes , Tao Yu , Hon-Chung Tsui , Neng-Yang Shih , Yushi Xiao , Sunil Paliwal
发明人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Angela Kerekes , Tao Yu , Hon-Chung Tsui , Neng-Yang Shih , Yushi Xiao , Sunil Paliwal
IPC分类号： A61K31/4745 , C07D498/02
CPC分类号： C07D495/04
摘要： The present invention provides compounds of Formula I (wherein R1, R3, X, W, Z and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
摘要翻译： 本发明提供式I化合物（其中R 1，R 3，X，W，Z和环Y如本文所定义）。 本发明还提供了包含这些化合物的组合物，其可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病或病症并抑制KSP驱动蛋白活性。
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公开(公告)号：US20060128725A1
公开(公告)日：2006-06-15
申请号：US11245401
申请日：2005-10-06
申请人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Marc Labroli , Kartik Keertikar
发明人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Marc Labroli , Kartik Keertikar
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , Y02P20/582
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
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公开(公告)号：US20130196986A1
公开(公告)日：2013-08-01
申请号：US13825161
申请日：2011-09-16
IPC分类号： C07D487/04 , A61K45/06 , A61K31/5377 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61K45/06
摘要： The invention provides certain 3,7-disubstituted-[1,2,4]triazolo[4,3-a]pyrazin-8(7H)-ones of the Formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R8, and X are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating pain or an inflammatory disease.
摘要翻译： 本发明提供了式（I）的某些3,7-二取代 - [1,2,4]三唑并[4,3-a]吡嗪-8（7H） - 及其药学上可接受的盐，其中R1，R2 ，R3，R8和X如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗疼痛或炎性疾病的方法。
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