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51. 发明授权

US07511049B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
标题翻译：吡唑并嘧啶类作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07511049B2
公开(公告)日：2009-03-31
申请号：US11779050
申请日：2007-07-17
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park
IPC分类号： A61K31/519 , A61P35/00 , 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.
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。

52. 发明授权

US07449488B2 Pyrazolopyrimidines as protein kinase inhibitors 有权
标题翻译：吡唑并嘧啶作为蛋白激酶抑制剂
公开(公告)号：US07449488B2
公开(公告)日：2008-11-11
申请号：US11244628
申请日：2005-10-06
申请人： Kamil Paruch , Timothy J. Guzi , Michael P. Dwyer , Gerald W. Shipps, Jr.
发明人： Kamil Paruch , Timothy J. Guzi , Michael P. Dwyer , Gerald W. Shipps, Jr.
IPC分类号： C07D231/00 , C07D231/54 , A61K31/415 , A01N43/56
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 protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
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]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种这类化合物的药物组合物，制备包括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，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。本发明还涉及丙型肝炎病毒（HCV）复制的抑制。特别地，本发明的实施方案提供了用于抑制HCV RNA依赖性RNA聚合酶酶活性的化合物和方法。本发明还提供了预防和治疗HCV感染的组合物和方法。

53. 发明授权

US07309705B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
公开(公告)号：US07309705B2
公开(公告)日：2007-12-18
申请号：US11395824
申请日：2006-03-31
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： A61K31/519 , A61P35/00 , C07D484/04
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.

54. 发明申请

US20070066621A1 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 失效
标题翻译：吡唑并[1,5-a]吡啶，吡唑并[1,5-c]嘧啶和2h-吲唑化合物的新型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：US20070066621A1
公开(公告)日：2007-03-22
申请号：US11514548
申请日：2006-08-31
申请人： Alan Mallams , Vincent Madison , Kamil Paruch
发明人： Alan Mallams , Vincent Madison , Kamil Paruch
IPC分类号： A61K31/519 , A61K31/496 , C07D487/04 , C07D471/02 , A61K31/4745
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

US07161003B1 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：吡唑并嘧啶类作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07161003B1
公开(公告)日：2007-01-09
申请号：US10654546
申请日：2003-09-03
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
IPC分类号： 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。

56. 发明授权

US07138396B2 17 β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases 失效
标题翻译： 17β-羟基类固醇脱氢酶3型抑制剂用于治疗雄激素依赖性疾病
公开(公告)号：US07138396B2
公开(公告)日：2006-11-21
申请号：US11045967
申请日：2005-01-28
申请人： Timothy J. Guzi , Kamil Paruch , Alan K. Mallams , Jocelyn D. Rivera , Ronald J. Doll , Viyyoor M. Girijavallabhan , Jonathan A. Pachter , Yi-Tsung Liu , Anil K. Saksena
发明人： Timothy J. Guzi , Kamil Paruch , Alan K. Mallams , Jocelyn D. Rivera , Ronald J. Doll , Viyyoor M. Girijavallabhan , Jonathan A. Pachter , Yi-Tsung Liu , Anil K. Saksena
IPC分类号： A61K31/497
CPC分类号： C07D211/34 , C07D211/48 , C07D295/185 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/02 , C07D409/12 , C07D409/14 , C07D417/12
摘要： There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17β-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.
摘要翻译：公开了可用作3型17β-羟基甾体脱氢酶抑制剂的式（I）化合物：其前药或化合物或所述前药的药学上可接受的盐。还公开了含有所述化合物及其用于治疗或预防雄激素依赖性疾病的药物组合物。

57. 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。

58. 发明授权

US08673924B2 Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：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：US08673924B2
公开(公告)日：2014-03-18
申请号：US11788847
申请日：2007-04-20
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent S. Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs , Paul Kirschmeier , Rajat Bannerji
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent S. Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs , Paul Kirschmeier , Rajat Bannerji
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： A61K31/33 , A61K31/4965 , A61K31/497 , A61K31/519 , A61K31/535 , A61K31/555 , A61K31/56 , A61K31/655 , A61K31/675 , A61K31/7004 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An example pyrazolo[1,5-a]pyrimidine compound useful in the present invention is shown below:
摘要翻译：在其许多实施方案中，本发明提供了抑制患者中一种或多种细胞周期蛋白依赖性激酶的方法，包括向所述患者施用治疗有效量的至少一种吡唑并[1,5-a]嘧啶化合物或包含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。用于本发明的吡唑并[1,5-a]嘧啶化合物的实例如下所示：

59. 发明授权

US08586576B2 Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：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
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 , A61K31/5377 , 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。

60. 发明授权

US08580782B2 Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：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：US08580782B2
公开(公告)日：2013-11-12
申请号：US11788856
申请日：2007-04-20
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Marc A. Labroli , Kartik M. Keertikar
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Marc A. Labroli , Kartik M. Keertikar
IPC分类号： A61K31/519 , A61K31/5513 , A61K31/5377 , A61K31/541 , A61P35/02 , A61P35/04 , A61P35/00 , C07D487/04 , C07D295/04 , C07D243/14
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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