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：US06800636B2

公开(公告)日：2004-10-05

申请号：US10028251

申请日：2001-12-20

申请人： Timothy Guzi ,  Dinanath F. Rane ,  Alan K. Mallams ,  Alan B. Cooper ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Arthur G. Taveras ,  Corey Strickland ,  Joseph M. Kelly ,  Jianping Chao

发明人： Timothy Guzi ,  Dinanath F. Rane ,  Alan K. Mallams ,  Alan B. Cooper ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Arthur G. Taveras ,  Corey Strickland ,  Joseph M. Kelly ,  Jianping Chao

IPC分类号： A61K314545

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14

摘要： Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. 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 8表示与咪唑基烷基结合的环状部分; R 9表示氨基甲酸酯，脲，酰胺或磺酰胺基; 并且其余取代基如本文所定义。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：US06362188B1

公开(公告)日：2002-03-26

申请号：US09465523

申请日：1999-12-16

申请人： Timothy Guzi ,  Dinanath F. Rane ,  Alan K. Mallams ,  Alan B. Cooper ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Arthur G. Taveras ,  Corey Strickland ,  Joseph M. Kelly ,  Jianping Chao

发明人： Timothy Guzi ,  Dinanath F. Rane ,  Alan K. Mallams ,  Alan B. Cooper ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Arthur G. Taveras ,  Corey Strickland ,  Joseph M. Kelly ,  Jianping Chao

IPC分类号： A61K31496

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14

摘要： Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. 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R8表示结合有异唑基烷基的环状部分; R9表示氨基甲酸酯，脲，酰胺或磺酰胺基团; 并且其余的取代基如本文所定义。 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：US07432268B2

公开(公告)日：2008-10-07

申请号：US11273712

申请日：2005-11-14

申请人： Timothy Guzi ,  Kamil Paruch ,  Alan Mallams ,  Jocelyn D. Rivera ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Jonathan A. Pachter ,  Yi-Tsung Liu ,  Anil K. Saksena

发明人： Timothy Guzi ,  Kamil Paruch ,  Alan 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 ,  A61K31/445 ,  A01N43/40 ,  C07D241/02 ,  C07D211/70 ,  C07D211/82 ,  C07D213/06

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。

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：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：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：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.