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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.
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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。
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公开(公告)号：USD447161S1
公开(公告)日：2001-08-28
申请号：US29128833
申请日：2000-08-30
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公开(公告)号：US6030982A
公开(公告)日：2000-02-29
申请号：US927731
申请日：1997-09-11
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： A61P35/00 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , A61K31/445 , A61K31/535 , A61K31/54 , C07D411/14 , C07D413/14
CPC分类号： C07D401/14 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/12
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.
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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.
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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。
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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。
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公开(公告)号：US06440974B2
公开(公告)日：2002-08-27
申请号：US09788947
申请日：2001-02-20
申请人： Ronald J. Doll , Carmen Alvarez , Tarik Lalwani , Yi-Tsung Liu
发明人： Ronald J. Doll , Carmen Alvarez , Tarik Lalwani , Yi-Tsung Liu
IPC分类号： A61K31496
CPC分类号： C07D401/04 , C07D221/16 , C07D405/14 , C07D409/14
摘要： Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
摘要翻译： 公开了新的式的化合物。 在式1.0中，a表示N或NO，R 1和R 3是卤素，R 2和R 4独立地是H或卤素，条件是至少一个是H，X是C，CH或N，T代表五或六元杂环烷基环，其具有 选自S或O的一个或两个杂原子。还公开了抑制法呢基蛋白转移酶的方法和治疗肿瘤细胞的方法。
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公开(公告)号：US06228856B1
公开(公告)日：2001-05-08
申请号：US09417885
申请日：1999-10-14
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： A61K314545
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。
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公开(公告)号：US06211193B1
公开(公告)日：2001-04-03
申请号：US09094720
申请日：1998-06-15
IPC分类号： A61K314545
CPC分类号： C07D401/04 , A61K31/4545 , C07D401/14 , C07D405/14 , C07D491/10 , C07D495/10
摘要： Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and R represents a cycloalkyl or a heterocycloalkyl ring that is substitued. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
摘要翻译： 公开了新的式的化合物。 在式1.0中，a表示N或NO，R 1和R 3为卤素，R 2和R 4独立地为H或卤素，条件是至少一个为H，X为C，CH或N，R为环烷基或杂环烷基环， 还公开了抑制法呢基蛋白转移酶的方法和治疗肿瘤细胞的方法。
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