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81. 发明授权

US07576085B2 Imidazopyrazines as cyclin dependent kinase inhibitors 失效
标题翻译：咪唑吡嗪作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07576085B2
公开(公告)日：2009-08-18
申请号：US11272392
申请日：2005-11-10
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Lianyun Zhao , Patrick J. Curran , David B. Belanger , Blake Hamann , Panduranga A. Reddy , M. Arshad Siddiqui
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Lianyun Zhao , Patrick J. Curran , David B. Belanger , Blake Hamann , Panduranga A. Reddy , M. Arshad Siddiqui
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D403/00 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine 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. An illustrative compound of the invention is shown below:
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的咪唑并[1,2-a]吡嗪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。本发明的说明性化合物如下所示：

82. 发明授权

US07205308B2 Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：三取代的7-氨基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：US07205308B2
公开(公告)日：2007-04-17
申请号：US11244772
申请日：2005-10-06
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P19/02 , A61P29/00
CPC分类号： C07D487/04
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。

83. 发明授权

US07196092B2 N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译： N-杂芳基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：US07196092B2
公开(公告)日：2007-03-27
申请号：US11244776
申请日：2005-10-06
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P19/02 , A61P29/00
CPC分类号： C07D487/04
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。

84. 发明授权

US07196078B2 Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：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
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Marc Labroli , Kartik M. Keertikar
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Marc Labroli , Kartik M. Keertikar
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。

85. 发明授权

US07074795B2 17β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases 失效
标题翻译： 17β-羟类固醇脱氢酶3型抑制剂用于治疗雄激素依赖性疾病
公开(公告)号：US07074795B2
公开(公告)日：2006-07-11
申请号：US10713828
申请日：2003-11-14
申请人： Kamil Paruch , Timothy J. Guzi
发明人： Kamil Paruch , Timothy J. Guzi
IPC分类号： A61K31/496 , C07D401/12
CPC分类号： C07D211/46 , C07D211/58
摘要： In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17 β-hydroxysteroid dehydrogenase, 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 type 3 17 β-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions. In one embodiment, the present invention discloses a compound having the general structure shown in Formula I:wherein the various moieties are as defined herein.
摘要翻译：在其许多实施方案中，本发明提供了一类新型化合物作为3β-17β-羟基类固醇脱氢酶的抑制剂，制备此类化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物制剂的方法，其包含一种或多种化合物，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3β17型羟基类固醇脱氢酶相关的一种或多种疾病的方法。在一个实施方案中，本发明公开了具有式I所示的一般结构的化合物：其中各种部分如本文所定义。

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