公开(公告)号：US20070191604A1

公开(公告)日：2007-08-16

申请号：US11636954

申请日：2006-12-11

申请人： Alan Cooper ,  Yongqi Deng ,  Gerald Shipps ,  Neng-Yang Shih ,  Hugh Zhu ,  Robert Sun ,  Joseph Kelly ,  Ronald Doll ,  Yang Nan ,  Tong Wang ,  Jagdish Desai ,  James Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  M. Siddiqui ,  Ahmed Samatar ,  Sunil Paliwal ,  Hon-Chung Tsui ,  Azim Celebi ,  Yiji Wu ,  Sobhana Boga

发明人： Alan Cooper ,  Yongqi Deng ,  Gerald Shipps ,  Neng-Yang Shih ,  Hugh Zhu ,  Robert Sun ,  Joseph Kelly ,  Ronald Doll ,  Yang Nan ,  Tong Wang ,  Jagdish Desai ,  James Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  M. Siddiqui ,  Ahmed Samatar ,  Sunil Paliwal ,  Hon-Chung Tsui ,  Azim Celebi ,  Yiji Wu ,  Sobhana Boga

IPC分类号： C07D417/14 ,  C07D413/14 ,  C07D403/14

CPC分类号： C07D405/14 ,  C07D231/56 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14

摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

摘要翻译： 公开了式1.0的ERK抑制剂及其药学上可接受的盐和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。 哌啶环可以在环中具有双键。 所有其他取代基如本文所定义。 还公开了使用式1.0化合物治疗癌症的方法。

公开(公告)号：US20070232610A1

公开(公告)日：2007-10-04

申请号：US11705709

申请日：2007-02-13

申请人： Yongqi Deng ,  Gerald Shipps ,  Alan Cooper ,  Yang Nan ,  Tong Wang ,  M. Siddiqui ,  Hugh Zhu ,  Robert Sun ,  Joseph Kelly ,  Ronald Doll ,  Jagdish Desai ,  James Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  Neng-Yang Shih

发明人： Yongqi Deng ,  Gerald Shipps ,  Alan Cooper ,  Yang Nan ,  Tong Wang ,  M. Siddiqui ,  Hugh Zhu ,  Robert Sun ,  Joseph Kelly ,  Ronald Doll ,  Jagdish Desai ,  James Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  Neng-Yang Shih

IPC分类号： A61K31/53 ,  A61K31/506 ,  A61K31/502 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/407 ,  A61K31/401 ,  C07D403/02

CPC分类号： C07D207/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08

摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

公开(公告)号：US07807672B2

公开(公告)日：2010-10-05

申请号：US11705709

申请日：2007-02-13

申请人： Yongqi Deng ,  Gerald W. Shipps, Jr. ,  Alan Cooper ,  Yang Nan ,  Tong Wang ,  M. Arshad Siddiqui ,  Hugh Zhu ,  Robert Sun ,  Joseph M. Kelly ,  Ronald Doll ,  Jagdish Desai ,  James J-S Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  Neng-Yang Shih

发明人： Yongqi Deng ,  Gerald W. Shipps, Jr. ,  Alan Cooper ,  Yang Nan ,  Tong Wang ,  M. Arshad Siddiqui ,  Hugh Zhu ,  Robert Sun ,  Joseph M. Kelly ,  Ronald Doll ,  Jagdish Desai ,  James J-S Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  Neng-Yang Shih

IPC分类号： A61K31/506 ,  A61K31/5377 ,  A61K31/4025 ,  A61K31/496 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12

CPC分类号： C07D207/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08

摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

摘要翻译： 公开了式1.0的ERK抑制剂及其药学上可接受的盐和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。 哌啶环可以在环中具有双键。 所有其它取代基如本文所定义。 还公开了使用式1.0化合物治疗癌症的方法。

公开(公告)号：US20050059672A1

公开(公告)日：2005-03-17

申请号：US10911340

申请日：2004-08-04

申请人： Hugh Zhu ,  Alan Cooper ,  Jagdish Desai ,  James Wang ,  Dinanath Rane ,  Ronald Doll ,  F. Njoroge ,  Viyyoor Girijavallabhan

发明人： Hugh Zhu ,  Alan Cooper ,  Jagdish Desai ,  James Wang ,  Dinanath Rane ,  Ronald Doll ,  F. Njoroge ,  Viyyoor Girijavallabhan

IPC分类号： A61P35/00 ,  C07D401/06 ,  A61K31/496 ,  C07D43/14

CPC分类号： C07D401/06

摘要： Disclosed are novel tricyclic compounds of the formula: and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are uses of the compounds of formula (I) for the manufacture of a medicament for the treatment of cancer.

摘要翻译： 公开了下式的新型三环化合物及其药学上可接受的盐或溶剂化物。 该化合物可用于抑制法呢基蛋白转移酶。 还公开了包含式（I）化合物的药物组合物。 还公开了式（I）化合物在制备用于治疗癌症的药物中的用途。

公开(公告)号：US20080004287A1

公开(公告)日：2008-01-03

申请号：US11769030

申请日：2007-06-27

申请人： Yao Ma ,  Brian Lahue ,  Gerald Shipps ,  Yaolin Wang ,  Stephane Bogen ,  Matthew Voss ,  Latha Nair ,  Yuan Tian ,  Ronald Doll ,  Zhuyan Guo ,  Corey Strickland ,  Rumin Zhang ,  Mark McCoy ,  Weidong Pan ,  Elise Siegel ,  Craig Gibeau

发明人： Yao Ma ,  Brian Lahue ,  Gerald Shipps ,  Yaolin Wang ,  Stephane Bogen ,  Matthew Voss ,  Latha Nair ,  Yuan Tian ,  Ronald Doll ,  Zhuyan Guo ,  Corey Strickland ,  Rumin Zhang ,  Mark McCoy ,  Weidong Pan ,  Elise Siegel ,  Craig Gibeau

IPC分类号： A61K31/497 ,  A61P43/00 ,  C07D401/14

CPC分类号： C07D409/14 ,  C07D401/06 ,  C07D401/14

摘要： In its many embodiments, the present invention discloses novel compounds, as inhibitors of HDM2 protein, methods for preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of treatment, prevention, inhibition, of one or more diseases associated with the HDM2 protein or P53 using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明公开了作为HDM2蛋白的抑制剂的新化合物，制备这些化合物的方法，包含一种或多种这样的化合物的药物组合物，治疗，预防，抑制与HDM2相关的一种或多种疾病的方法 蛋白质或P53使用这些化合物或药物组合物。

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：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：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：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。