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1.发明授权5-AMINOINDENO[1,2-C]PYRAZOL-4-ONES AS ANTI-CANCER AND ANTI-PROLIFERATIVE AGENTS 有权5- AMINOINDENO [1,2-c]吡唑-4-酮作为抗肿瘤和生长抑制剂
公开(公告)号：EP1071668B1
公开(公告)日：2009-06-03
申请号：EP99918695.0
申请日：1999-04-20
IPC分类号： C07D231/54 , A61K31/41 , C07D409/12 , C07D403/12 , C07D401/12 , C07D417/12 , C07D413/12 , C07D413/14
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 known as cyclines 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.
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2.发明公开ACYLSEMICARBAZIDES AND THEIR USE AS CYCLIN DEPENDENT KINASE (CDK) INHIBITORS 审中-公开ACYLSEMICARBAZIDE及其作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：EP1414804A1
公开(公告)日：2004-05-06
申请号：EP00973682.8
申请日：2000-10-20
IPC分类号： C07D231/54 , C07D401/12 , C07D409/12 , A61K31/416 , A61P35/00
CPC分类号： C07D409/12 , C07D231/54 , C07D401/12
摘要： The present invention realtes to the synthesis fo 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. The invention also provides a novel method of treating cancer or otehr profiferative disease 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 disease by administering a therapeutically effective combination of one of the compounds of teh present invention and one or more other known anti-cancer or anti-proliferative agents.
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3.发明公开PEPTIDASE-CLEAVABLE, TARGETED ANTINEOPLASTIC DRUGS AND THEIR THERAPEUTIC USE 审中-公开肽酶裂变，有针对性的抗肿瘤药物及其治疗用途
公开(公告)号：EP1263473A2
公开(公告)日：2002-12-11
申请号：EP01918798.8
申请日：2001-03-15
发明人： COPELAND, Robert, A. , ALBRIGHT, Charles, F. , COMBS, Andrew, P. , DOWLING, Radine, L. , GRACIANI, Nilsa, R. , HAN, Wei , HIGLEY, C., Anne , HUANG, Pearl, S. , YUE, Eddy, W. , DIMEO, Susan, V.
IPC分类号： A61K47/48 , A61K31/704 , A61P35/00
摘要： This invention is directed to antineoplastic agents conjugated to enzyme-cleavable peptides comprising the amino acid recognition sequence of a membrane-bound and/or cell-secreted peptidase, and to the use of such conjugated compounds as chemotherapeutic agents in the targeted treatment of cancers.
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