公开(公告)号：US20050037383A1

公开(公告)日：2005-02-17

申请号：US10822254

申请日：2004-04-09

申请人： Shahriar Taremi ,  Gaolian Xie ,  Thomas Hesson ,  Jose Duca ,  Corey Strickland ,  William Windsor ,  Vincent Madison ,  Rumin Zhang ,  Paul Reichert

发明人： Shahriar Taremi ,  Gaolian Xie ,  Thomas Hesson ,  Jose Duca ,  Corey Strickland ,  William Windsor ,  Vincent Madison ,  Rumin Zhang ,  Paul Reichert

IPC分类号： C07D209/20 ,  C07H21/04 ,  C07K14/47 ,  C12Q1/68

CPC分类号： C07H21/04 ,  C07D209/20 ,  C07K14/47 ,  C07K2299/00

摘要： The present invention discloses modified Hdm2 proteins that are soluble. In addition, the present invention discloses nucleic acids that encode the modified Hdm2 proteins of the present invention. The invention also provides crystals of modified Hdm2 proteins that are suitable for X-ray crystallization analysis. The present invention also discloses methods of using the modified Hdm2 proteins and crystals thereof to identify, select and/or design compounds that may be used as anticancer agents. The present invention further discloses compounds that bind to modified Hdm2 proteins in protein-ligand complexes.

摘要翻译： 本发明公开了可溶性的修饰的Hdm2蛋白。 此外，本发明公开了编码本发明的修饰的Hdm2蛋白质的核酸。 本发明还提供了适用于X射线结晶分析的修饰的Hdm2蛋白晶体。 本发明还公开了使用修饰的Hdm2蛋白及其晶体鉴定，选择和/或设计可用作抗癌剂的化合物的方法。 本发明还公开了与蛋白质 - 配体复合物中的修饰的Hdm2蛋白结合的化合物。

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。

公开(公告)号：US20100137326A1

公开(公告)日：2010-06-03

申请号：US12706814

申请日：2010-02-17

申请人： Alan K. Mallams ,  Vincent Madison ,  Kamil Paruch

发明人： Alan K. Mallams ,  Vincent Madison ,  Kamil Paruch

IPC分类号： A61K31/4985 ,  C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D401/14 ,  A61K31/444 ,  A61K31/519 ,  A61K31/4439 ,  A61P35/00

CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-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.

公开(公告)号：US07067661B2

公开(公告)日：2006-06-27

申请号：US10653776

申请日：2003-09-03

申请人： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Carmen S. Alvarez ,  Tin-Yau Chan ,  Chad Knutson ,  Vincent Madison ,  Thierry O. Fischmann ,  Lawrence W. Dillard ,  Vinh D. Tran ,  Zhen Min He ,  Ray Anthony James ,  Haengsoon Park

发明人： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer ,  Ronald J. Doll ,  Viyyoor M. Girijavallabhan ,  Carmen S. Alvarez ,  Tin-Yau Chan ,  Chad Knutson ,  Vincent Madison ,  Thierry O. Fischmann ,  Lawrence W. Dillard ,  Vinh D. Tran ,  Zhen Min He ,  Ray Anthony James ,  Haengsoon Park

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.