公开(公告)号：US06291504B1

公开(公告)日：2001-09-18

申请号：US09692023

申请日：2000-10-19

申请人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Anup P. Vidwans ,  Eddy W. Yue

发明人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Anup P. Vidwans ,  Eddy W. Yue

IPC分类号： A61K31416

CPC分类号： C07D401/12 ,  C07D231/54 ,  C07D409/12

摘要： The present invention relates to the synthesis of a new lass of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

摘要翻译： 本发明涉及式（I）的茚并[1,2-c]吡唑-4-酮新型的合成：其是称为细胞周期依赖性激酶的酶类的有效抑制剂，其涉及 催化亚基cdk1-9及其调节亚基称为细胞周期蛋白AH.本发明还提供了一种通过施用治疗有效量的这些化合物之一或其药学上可接受的盐形式来治疗癌症或其它增殖性疾病的新方法。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。

公开(公告)号：US07250435B2

公开(公告)日：2007-07-31

申请号：US11064758

申请日：2005-02-24

申请人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Anup P. Vidwans ,  Eddy Yue

发明人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Anup P. Vidwans ,  Eddy Yue

IPC分类号： A61K31/415 ,  C07D231/54

CPC分类号： C07D401/04 ,  C07D231/54 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

摘要翻译： 本发明涉及新一类式（I）的茚并[1,2-c]吡唑-4-酮的合成：其是称为细胞周期蛋白依赖性激酶的酶类的有效抑制剂，其涉及 催化亚基cdk1-7及其调控亚基称为细胞周期蛋白AG。 本发明还提供了通过施用治疗有效量的这些化合物之一或其药学上可接受的盐形式来治疗癌症或其它增殖性疾病的新方法。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。

公开(公告)号：US06413957B1

公开(公告)日：2002-07-02

申请号：US09639618

申请日：2000-08-15

申请人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Eddy W. Yue

发明人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Eddy W. Yue

IPC分类号： A61K315377

CPC分类号： C07D405/12 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

摘要翻译： 本发明涉及新一类式（I）的茚并[1,2-c]吡唑-4-酮的合成：其是称为细胞周期蛋白依赖性激酶的酶类的有效抑制剂，其涉及 催化亚基cdk1-7及其调控亚基称为细胞周期蛋白AG。 本发明还提供了通过施用治疗有效量的这些化合物之一或其药学上可接受的盐形式来治疗癌症或其它增殖性疾病的新方法。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。

公开(公告)号：US06407103B2

公开(公告)日：2002-06-18

申请号：US09731304

申请日：2000-12-06

申请人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Eddy W. Yue

发明人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Eddy W. Yue

IPC分类号： A61K315377

CPC分类号： C07D403/14 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

摘要翻译： 本发明涉及新一类式（I）的茚并[1,2-c]吡唑-4-酮的合成：其是称为细胞周期蛋白依赖性激酶的酶类的有效抑制剂，其涉及 催化亚基cdk1-9及其调节亚基称为细胞周期蛋白AH.本发明还提供了一种通过施用治疗有效量的这些化合物之一或其药学上可接受的盐形式来治疗癌症或其它增殖性疾病的新方法。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。