公开(公告)号：US20070054925A1

公开(公告)日：2007-03-08

申请号：US11396079

申请日：2006-03-31

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

IPC分类号： A61K31/519 ,  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.

公开(公告)号：US20070054906A1

公开(公告)日：2007-03-08

申请号：US11396001

申请日：2006-03-31

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

IPC分类号： A61K31/5377 ,  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。

公开(公告)号：US20070037824A1

公开(公告)日：2007-02-15

申请号：US10654546

申请日：2003-09-03

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

IPC分类号： A61K31/519 ,  C07D487/02

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]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.

公开(公告)号：US20080050384A1

公开(公告)日：2008-02-28

申请号：US11788847

申请日：2007-04-20

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhenmin He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs ,  Paul Kirschmeier ,  Rajat Bannerji

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhenmin He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs ,  Paul Kirschmeier ,  Rajat Bannerji

IPC分类号： A61K31/519 ,  A61K31/33 ,  A61K31/4965 ,  A61K31/56 ,  A61K31/675 ,  A61K33/24 ,  A61K38/46 ,  A61P19/02 ,  A61P35/00 ,  A61P43/00 ,  A61P29/00 ,  A61K39/395 ,  A61K33/36 ,  A61K31/7004 ,  A61K31/655 ,  A61K31/535 ,  A61K31/497

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 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。

公开(公告)号：US20060178371A1

公开(公告)日：2006-08-10

申请号：US11395676

申请日：2006-03-31

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Carmen Alvarez ,  Tin-Yau Chan ,  Chad Knutson ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Carmen Alvarez ,  Tin-Yau Chan ,  Chad Knutson ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park

IPC分类号： A61K31/519 ,  A61K31/7048 ,  A61K31/704 ,  A61K31/525 ,  A61K31/66 ,  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.

公开(公告)号：US20070083044A1

公开(公告)日：2007-04-12

申请号：US11542921

申请日：2006-10-04

申请人： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Carmen Alvarez

发明人： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Carmen Alvarez

IPC分类号： C07D487/12 ,  C07D487/04

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of amino-substituted 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.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的氨基取代的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备这些化合物的方法，药物组合物包括一种或多种这样的化合物 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，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

公开(公告)号：US06372747B1

公开(公告)日：2002-04-16

申请号：US09465553

申请日：1999-12-16

申请人： Arthur G. Taveras ,  Ronald J. Doll ,  Alan B. Cooper ,  Johan A. Ferreira ,  Timothy Guzi ,  Dinanath F. Rane ,  Viyyoor M. Girijavallabhan ,  Cynthia J. Aki ,  Jianping Chao ,  Carmen Alvarez ,  Joseph M. Kelly ,  Tarik Lalwani ,  Jagdish A. Desai ,  James J-S Wang

发明人： Arthur G. Taveras ,  Ronald J. Doll ,  Alan B. Cooper ,  Johan A. Ferreira ,  Timothy Guzi ,  Dinanath F. Rane ,  Viyyoor M. Girijavallabhan ,  Cynthia J. Aki ,  Jianping Chao ,  Carmen Alvarez ,  Joseph M. Kelly ,  Tarik Lalwani ,  Jagdish A. Desai ,  James J-S Wang

IPC分类号： A61K31496

CPC分类号： C07D401/04 ,  C07D401/14

摘要： Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

摘要翻译： 公开了下式的化合物：其中R 13表示咪唑环; R14表示氨基甲酸酯，脲，酰胺或磺酰胺基; 当酰胺基和R 13咪唑基之间的烷基链被取代时，R8表示H，或R8表示芳基烷基，杂芳基烷基或环烷基等取代基; 并且其余的取代基如本文所定义。 还公开了其中R 8为H，酰胺基和R 13咪唑基之间的烷基链未被取代的化合物。 还公开了使用所公开的化合物治疗癌症的方法和抑制法呢基蛋白转移酶的方法。

公开(公告)号：US06740661B2

公开(公告)日：2004-05-25

申请号：US10026999

申请日：2001-12-20

申请人： Arthur G. Taveras ,  Ronald J. Doll ,  Alan B. Cooper ,  Johan A. Ferreira ,  Timothy Guzi ,  Alan K. Mallams ,  Dinanath F. Rane ,  Viyyoor M. Girijavallabhan ,  Adriano Afonso ,  Cynthia J. Aki ,  Jianping Chao ,  Carmen Alvarez ,  Joseph M. Kelly ,  Tarik Lalwani ,  Jagdish A. Desai ,  James J-S Wang ,  Jay Weinstein

发明人： Arthur G. Taveras ,  Ronald J. Doll ,  Alan B. Cooper ,  Johan A. Ferreira ,  Timothy Guzi ,  Alan K. Mallams ,  Dinanath F. Rane ,  Viyyoor M. Girijavallabhan ,  Adriano Afonso ,  Cynthia J. Aki ,  Jianping Chao ,  Carmen Alvarez ,  Joseph M. Kelly ,  Tarik Lalwani ,  Jagdish A. Desai ,  James J-S Wang ,  Jay Weinstein

IPC分类号： A61K314545

CPC分类号： C07D401/04 ,  C07D401/14

摘要： Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

摘要翻译： 公开了下式的化合物：其中R 13表示咪唑环; R 14代表氨基甲酸酯，脲，酰胺或磺酰胺基团; 酰胺基和R 13咪唑基之间的烷基链被取代时，R 8表示H，或者R 8表示芳烷基，杂芳基烷基或环烷基等取代基。 其余的取代基如本文所定义。还公开了其中R 8为H，酰胺基和R 13咪唑基之间的烷基链未被取代的化合物。还公开了一种治疗癌症和 使用所公开的化合物抑制法呢基蛋白转移酶的方法。

公开(公告)号：US5861395A

公开(公告)日：1999-01-19

申请号：US927469

申请日：1997-09-11

申请人： Arthur G. Taveras ,  Alan K. Mallams ,  Adriano Afonso ,  Stacy W. Remiszewski ,  F. George Njoroge ,  Ronald Doll ,  Tarik Lalwani ,  Carmen Alvarez

发明人： Arthur G. Taveras ,  Alan K. Mallams ,  Adriano Afonso ,  Stacy W. Remiszewski ,  F. George Njoroge ,  Ronald Doll ,  Tarik Lalwani ,  Carmen Alvarez

IPC分类号： C07D221/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  A61K31/495 ,  A61K31/535

CPC分类号： C07D401/04 ,  C07D221/06 ,  C07D401/12 ,  C07D401/14

摘要： Novel compounds of the formula: ##STR1## are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: ##STR2## wherein R.sup.1, R.sup.3 and R.sup.4 are each independently selected from halo. Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.

摘要翻译： 公开了下式的新型化合物：（1.0）。 式1.0的化合物由下式的化合物表示：其中R 1，R 3和R 4各自独立地选自卤素。 还公开了抑制法呢基蛋白转移酶和异常细胞如肿瘤细胞生长的方法。

公开(公告)号：US06387905B2

公开(公告)日：2002-05-14

申请号：US09797081

申请日：2001-03-01

申请人： F George Njoroge ,  Arthur G. Taveras ,  Ronald J. Doll ,  Tarik Lalwani ,  Carmen Alvarez ,  Stacy W. Remiszewski

发明人： F George Njoroge ,  Arthur G. Taveras ,  Ronald J. Doll ,  Tarik Lalwani ,  Carmen Alvarez ,  Stacy W. Remiszewski

IPC分类号： A61K31496

CPC分类号： C07D401/14 ,  C07D221/06 ,  C07D221/16 ,  C07D401/04 ,  C07D401/12

摘要： Novel compounds of the formula: are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: wherein R1, R3 and R4 are each independently selected from halo. Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.

摘要翻译： 公开了新的式的化合物。 式1.0的化合物由下式化合物表示：其中R 1，R 3和R 4各自独立地选自卤素。还公开了抑制法呢基蛋白转移酶和异常细胞如肿瘤细胞生长的方法。