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51. 发明授权

US07038045B2 Pyrazolotriazines as kinase inhibitors 有权
标题翻译：吡唑啉三嗪作为激酶抑制剂
公开(公告)号：US07038045B2
公开(公告)日：2006-05-02
申请号：US11064044
申请日：2005-02-23
申请人： Timothy J. Guzi , Kamil Paruch
发明人： Timothy J. Guzi , Kamil Paruch
IPC分类号： C07D251/72 , A61K311/53 , A61P19/02
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, 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 kinases 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]三嗪化合物作为激酶抑制剂，例如细胞周期蛋白依赖性激酶，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物化合物，制备包含一种或多种这样的化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与激酶相关的一种或多种疾病的方法。

52. 发明授权

US07354921B2 Pyrazolotriazines as kinase inhibitors 有权
标题翻译：吡唑啉三嗪作为激酶抑制剂
公开(公告)号：US07354921B2
公开(公告)日：2008-04-08
申请号：US11546766
申请日：2006-10-12
申请人： Timothy J. Guzi , Kamil Paruch
发明人： Timothy J. Guzi , Kamil Paruch
IPC分类号： A61K31/53 , A61P35/00 , A61P19/02 , C07D251/72
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, 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 kinases 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]三嗪化合物作为激酶抑制剂，例如细胞周期蛋白依赖性激酶，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物化合物，制备包含一种或多种这样的化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与激酶相关的一种或多种疾病的方法。

53. 发明授权

US07166602B2 Pyrazolotriazines as kinase inhibitors 有权
公开(公告)号：US07166602B2
公开(公告)日：2007-01-23
申请号：US11335383
申请日：2006-01-19
申请人： Timothy J. Guzi , Kamil Paruch
发明人： Timothy J. Guzi , Kamil Paruch
IPC分类号： A61K31/53 , A61P19/02 , C07D251/72 , C07D487/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, 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 kinases using such compounds or pharmaceutical compositions.

54. 发明申请

US20100143384A1 NOVEL 4-CYANO, 4-AMINO, AND 4-AMINOMETHYL DERIVATIVES OF PYRAZOLO[1,5-a]PYRIDINES, PYRAZOLO[1,5-c]PYRIMIDINES AND 2H-INDAZOLE COMPOUNDS AND 5-CYANO, 5-AMINO, AND 5-AMINOMETHYL DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINES, AND IMIDAZO[1,5-a]PYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译：吡咯并[1,5-a]吡啶，吡唑并[1,5-c]吡嗪和2H-吲唑化合物和5-氰基，5-氨基和5的新4-氰基，4-氨基和4-氨基甲基衍生物咪唑并[1,2-a]吡啶的咪唑衍生物和作为循环依赖性激酶抑制剂的咪唑并[1,5-a]吡啶
公开(公告)号：US20100143384A1
公开(公告)日：2010-06-10
申请号：US12706551
申请日：2010-02-16
申请人： Alan K. Mallams , Vincent S. Madison , Kamil Paruch
发明人： Alan K. Mallams , Vincent S. Madison , Kamil Paruch
IPC分类号： A61K39/395 , A61K38/50 , A61K33/24 , A61K38/16 , A61K38/08 , A61K38/09 , A61K31/7048 , A61K31/7076 , A61K31/7068 , A61K31/568 , A61K31/5377 , A61K31/53 , A61K31/4985 , A61K31/437 , A61K31/4439 , C07D471/04 , C07D401/12 , A61K31/573 , A61P35/00 , C07D487/04 , A61K31/519 , A61K31/704
CPC分类号： C07D231/56 , C07D401/12 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-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.
摘要翻译：在其许多实施方案中，本发明提供了一类新的吡唑并[1,5-a]吡啶，吡唑并[1,5-c]嘧啶和2H-吡唑并[4,5-a]吡啶的4-氰基，4-氨基和4-氨基甲基衍生物，吲唑化合物和咪唑并[1,2-a]吡啶和咪唑并[1,5-a]吡嗪化合物的5-氰基，5-氨基和5-氨基甲基衍生物作为细胞周期蛋白依赖性激酶的抑制剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，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。

55. 发明授权

US08603998B2 Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors 有权
标题翻译：细胞周期检查点的调节剂及其与检查点激酶抑制剂的组合
公开(公告)号：US08603998B2
公开(公告)日：2013-12-10
申请号：US12744021
申请日：2008-11-05
申请人： Timothy J. Guzi , David A. Parry , Marc A. Labroli , Michael D. Dwyer , Kamil Paruch
发明人： Timothy J. Guzi , David A. Parry , Marc A. Labroli , Michael D. Dwyer , Kamil Paruch
IPC分类号： A61K31/70 , C07H19/00 , A61K31/535 , C07D487/00
CPC分类号： C07H19/067 , C07H19/073
摘要： In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的式（V）嘧啶类似物作为细胞周期检查点的靶向基于机制的调节剂。可以通过施用本发明的细胞周期检查点调节剂来治疗癌症和/或恶性肿瘤。还讨论了细胞周期检查点调节剂与检查点激酶抑制剂的合适组合，以在癌细胞中产生协同凋亡。本发明包括通过施用细胞周期检查点调节剂和检查点激酶抑制剂的组合，包含活化剂的药物组合物以及组合药物试剂盒来治疗癌症的方法。

56. 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。

57. 发明申请

US20060173016A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
公开(公告)号：US20060173016A1
公开(公告)日：2006-08-03
申请号：US11395824
申请日：2006-03-31
申请人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Ronald Doll , Viyyoor Girijavallabhan , Lawrence Dillard , Vinh Tran , Zhen He , Ray James , Haengsoon Park
发明人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Ronald Doll , Viyyoor Girijavallabhan , Lawrence Dillard , Vinh Tran , Zhen He , Ray James , Haengsoon Park
IPC分类号： A61K31/517 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519 , A61K31/52 , A61K31/704 , A61K31/7072 , 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, 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.

58. 发明授权

US07700773B2 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridines, pyrazolo[1,5-c]pyrimidines and 2H-indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridines, and imidazo[1,5-a]pyrazines as cyclin dependent kinase inhibitors 失效
标题翻译：吡唑并[1,5-a]吡啶，吡唑并[1,5-c]嘧啶和2H-吲唑化合物的4-氰基，4-氨基和4-氨基甲基衍生物和5-氰基，5-氨基和5- 咪唑并[1,2-a]吡啶的氨基甲基衍生物和咪唑并[1,5-a]吡嗪作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07700773B2
公开(公告)日：2010-04-20
申请号：US11514548
申请日：2006-08-31
申请人： Alan K. Mallams , Vincent S. Madison , Kamil Paruch
发明人： Alan K. Mallams , Vincent S. Madison , Kamil Paruch
IPC分类号： C07D491/02 , C07D498/02
CPC分类号： C07D231/56 , C07D401/12 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-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.
摘要翻译：在其许多实施方案中，本发明提供了一类新的吡唑并[1,5-a]吡啶，吡唑并[1,5-c]嘧啶和2H-吡唑并[4,5-a]吡啶的4-氰基，4-氨基和4-氨基甲基衍生物，吲唑化合物和咪唑并[1,2-a]吡啶和咪唑并[1,5-a]吡嗪化合物的5-氰基，5-氨基和5-氨基甲基衍生物作为细胞周期蛋白依赖性激酶的抑制剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，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。

59. 发明申请

US20060235025A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
公开(公告)号：US20060235025A1
公开(公告)日：2006-10-19
申请号：US11395974
申请日：2006-03-31
申请人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Ronald Doll , Viyyoor Girijavallabhan , Lawrence Dillard , Vinh Tran , Zhen He , Ray James , Haengsoon Park
发明人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Ronald Doll , Viyyoor Girijavallabhan , Lawrence Dillard , Vinh Tran , Zhen He , Ray James , Haengsoon Park
IPC分类号： A61K31/519 , C07D487/04
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.

60. 发明申请

US20060173017A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
标题翻译：新型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：US20060173017A1
公开(公告)日：2006-08-03
申请号：US11395965
申请日：2006-03-31
申请人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Ronald Doll , Viyyoor Girijavallabhan , Chad Knutson , Brian McKittrick , Lawrence Dillard , Vinh Tran , Zhen Min He , Ray James , Haengsoon Park
发明人： Timothy Guzi , Kamil Paruch , Michael Dwyer , Ronald Doll , Viyyoor Girijavallabhan , Chad Knutson , Brian McKittrick , Lawrence Dillard , Vinh Tran , Zhen Min He , Ray James , Haengsoon Park
IPC分类号： A61K31/519 , C07D487/04
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。

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