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1. 发明授权

US08318735B2 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors 有权
标题翻译： 2-氨基噻唑-4-羧酸酰胺作为蛋白激酶抑制剂
公开(公告)号：US08318735B2
公开(公告)日：2012-11-27
申请号：US12447710
申请日：2007-10-29
申请人： Gerald W. Shipps, Jr. , Cliff C. Cheng , Xiaohua Huang , Thierry O. Fischmann , Jose S. Duca , Matthew Richards , Hongbo Zeng , Binyuan Sun , Panduranga Adulla Reddy , Lianyun Zhao , Shuyi Tang , Tzu T. Wong , Praveen K. Tadikonda , Luis E. Torres , M. Arshad Siddiqui , Michael P. Dwyer , Kartik M. Keertikar , Timothy J. Guzi
发明人： Gerald W. Shipps, Jr. , Cliff C. Cheng , Xiaohua Huang , Thierry O. Fischmann , Jose S. Duca , Matthew Richards , Hongbo Zeng , Binyuan Sun , Panduranga Adulla Reddy , Lianyun Zhao , Shuyi Tang , Tzu T. Wong , Praveen K. Tadikonda , Luis E. Torres , M. Arshad Siddiqui , Michael P. Dwyer , Kartik M. Keertikar , Timothy J. Guzi
IPC分类号： A61K31/5355 , A61K31/496 , C07D401/14 , C07D403/14 , C07D413/14
CPC分类号： C07D277/56 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04 , A61K2300/00
摘要： The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
摘要翻译：本发明涉及式（I）的新型苯胺基哌嗪衍生物，包含苯胺基哌嗪衍生物的组合物，以及使用苯胺基哌嗪衍生物治疗或预防增殖性病症，抗增殖病症，炎症，关节炎，中枢神经系统疾病，心血管疾病，脱发，神经元疾病，缺血性损伤，病毒性疾病，真菌感染或与蛋白激酶活性相关的病症。

2. 发明申请

US20100130465A1 2-AMINOTHIAZOLE-4-CARBOXYLIC AMIDES AS PROTEIN KINASE INHIBITORS 有权
标题翻译：作为蛋白激酶抑制剂的2-氨基噻唑-4-羧酰胺
公开(公告)号：US20100130465A1
公开(公告)日：2010-05-27
申请号：US12447710
申请日：2007-10-29
申请人： Gerald W. Shipps, JR. , Cliff C. Cheng , Xiaohua Huang , Thierry O. Fischmann , Jose S. Duca , Matthew Richards , Hongbo Zeng , Binyuan Sun , Panduranga A. Reddy , Lianyun Zhao , Shuyi Tang , Tzu T. Wong , Praveen K. Tadikonda , Luis E. Torres , M. Arshad Siddiqui , Michael P. Dwyer , Kartik M. Keertikar , Timothy J. Guzi
发明人： Gerald W. Shipps, JR. , Cliff C. Cheng , Xiaohua Huang , Thierry O. Fischmann , Jose S. Duca , Matthew Richards , Hongbo Zeng , Binyuan Sun , Panduranga A. Reddy , Lianyun Zhao , Shuyi Tang , Tzu T. Wong , Praveen K. Tadikonda , Luis E. Torres , M. Arshad Siddiqui , Michael P. Dwyer , Kartik M. Keertikar , Timothy J. Guzi
IPC分类号： A61K31/438 , C07D417/14 , A61K31/497 , C07D471/10 , C07D413/14 , A61K31/5377 , A61K31/551
CPC分类号： C07D277/56 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04 , A61K2300/00
摘要： The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
摘要翻译：本发明涉及式（I）的新型苯胺基哌嗪衍生物，包含苯胺基哌嗪衍生物的组合物，以及使用苯胺基哌嗪衍生物治疗或预防增殖性病症，抗增殖病症，炎症，关节炎，中枢神经系统疾病，心血管疾病，脱发，神经元疾病，缺血性损伤，病毒性疾病，真菌感染或与蛋白激酶活性相关的病症。

3. 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。

4. 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：

5. 发明授权

US07119200B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
公开(公告)号：US07119200B2
公开(公告)日：2006-10-10
申请号：US10776988
申请日：2004-02-11
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. Hobbs , 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. Hobbs , Douglas Walsh Hobbs
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/495
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.

6. 发明授权

US07807683B2 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：US07807683B2
公开(公告)日：2010-10-05
申请号：US11396001
申请日：2006-03-31
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： A61K31/519 , A61P35/04 , A61P35/02 , C07D487/04 , A61P35/00
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。

7. 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：

8. 发明申请

US20120029204A1 SYNTHESIS OF SUBSTITUTED-3-AMINOPYRAZOLES 审中-公开
标题翻译：取代的3-氨基吡唑的合成
公开(公告)号：US20120029204A1
公开(公告)日：2012-02-02
申请号：US12602716
申请日：2008-06-04
申请人： Carmen S. Alvarez , Michael P. Dwyer , Timothy J. Guzi , Kartik M. Keertikar , Marc A. Labroli , Kamil Paruch , Cory Seth Poker
发明人： Carmen S. Alvarez , Michael P. Dwyer , Timothy J. Guzi , Kartik M. Keertikar , Marc A. Labroli , Kamil Paruch , Cory Seth Poker
IPC分类号： C07D403/04
CPC分类号： C07D231/38 , C07D401/04 , C07D417/04
摘要： The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1′H-4,4′-bispyrazole.
摘要翻译：本发明公开了制备式（I）化合物的方法：其中A，M和Z如本文所定义。式（I）化合物的实例是3-氨基-1-甲基-1H-1'H-4,4'-双吡唑。

9. 发明授权

US07452902B2 Imidazopyridines as cyclin dependent kinase inhibitors 有权
标题翻译：咪唑并吡啶类作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07452902B2
公开(公告)日：2008-11-18
申请号：US11238597
申请日：2005-09-29
申请人： Michael P. Dwyer , Timothy J. Guzi , Kamil Paruch , Ronald J. Doll , Kartik M. Keertikar , Viyyoor M. Girijavallabhan
发明人： Michael P. Dwyer , Timothy J. Guzi , Kamil Paruch , Ronald J. Doll , Kartik M. Keertikar , Viyyoor M. Girijavallabhan
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine 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咪唑并[1,2-a]吡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。

10. 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。

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