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    Methods for identifying compounds for inhibition of neoplastic lesions, and pharmaceutical compositions containing such compounds
    9.
    发明公开
    Methods for identifying compounds for inhibition of neoplastic lesions, and pharmaceutical compositions containing such compounds 审中-公开
    一种鉴定可用于肿瘤性变化的抑制的化合物的方法，和含有这些化合物的药物组合物

    公开(公告)号：EP1161943A3

    公开(公告)日：2003-12-10

    申请号：EP01119687.0

    申请日：1999-10-14

    申请人： Cell Pathways, Inc.

    发明人： Liu, Li ,  Zhu, Bing ,  Li, Han ,  Thompson, Joseph W. ,  Pamukeu, Rifat ,  Piazza, Gary A.

    IPC分类号： A61K31/00 ,  A61K31/165 ,  A61K31/192 ,  A61K31/4192 ,  A61K31/365 ,  A61K38/06 ,  G01N33/50 ,  C12Q1/00 ,  C12N9/16 ,  A61P35/00

    CPC分类号： G01N33/5011 ,  A61K31/00 ,  A61K31/165 ,  A61K31/192 ,  A61K31/365 ,  A61K31/4192 ,  A61K38/00 ,  C12Q1/26 ,  C12Q1/44

    摘要： There is disclosed a pharmaceutical composition for the treatment of neoplasia, comprising a pharmaceutically acceptable carrier and a compound selected by: determining the cyclooxyegenase (COX) inhibitory activity of the compound; determining the PDE inhibition activity of the compound wherein the PDE is characterized by: (a) cGMP specificity over cAMP; (b) positive cooperative kinetic behaviour in the presence of cGMP substrate; (c) submicromolar affinity for cGMP; and (d) insensitivity to incubation with purified cGMP-dependent protein kinase; and selecting the compound that has COX inhibitory activity lower than said PDE activity for treating neoplasia. Also provided by the invention is a method for selecting a compound the treatment of neoplasia, comprising determining the cyclooxygenase (COX) inhibitory activity of the compound; determining the PDE2 inhibition activity of the compound; and selecting the compound that has COX inhibitory activity lower than said PDE activity for treating neoplasia.

    摘要翻译： 有游离缺失盘的药物组合物用于治疗肿瘤的治疗，其包含药学上可接受的载体，并通过选择的化合物：确定性挖掘cyclooxyegenase（COX）的化合物的抑制活性; 确定性采矿worin所述PDE的化合物的PDE抑制活性，是由为特征：（a）中的cGMP特异性高于cAMP; （B）在cGMP的底物的存在下正协同动力学行为; （C）对于cGMP具有亚微摩尔的亲和性; 和（d）不敏感性与纯化的cGMP依赖性蛋白激酶的保温; 和选择化合物确实具有COX抑制活性比PDE所述活动下用于治疗肿瘤。 因此，通过本发明提供的是用于选择化合物治疗肿瘤的方法，包括确定开采环氧合酶（COX）的化合物的抑制活性; 确定性采矿化合物的PDE2抑制活性; 和选择化合物确实具有COX抑制活性比PDE所述活动下用于治疗肿瘤。