Novel method for the asymmetric synthesis of beta-lactone compounds
    3.
    发明申请
    Novel method for the asymmetric synthesis of beta-lactone compounds 失效
    β-内酯化合物的不对称合成的新方法

    公开(公告)号:US20060258620A1

    公开(公告)日:2006-11-16

    申请号:US11378961

    申请日:2006-03-16

    摘要: The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.

    摘要翻译: 本发明的特征在于通过向受试者施用有效量的β-内酯来治疗受试者的癌症的方法。 本发明还具有通过向受试者施用有效量的脂肪酸合酶抑制剂来抑制受试者血管生成的方法。 这些方法可用于治疗各种癌症和其他疾病和病症。 本发明还涉及鉴定可用于本发明治疗肿瘤,抑制血管发生以及涉及病理性血管生成的疾病和病症的治疗的β-内酯和其它化合物的方法。 本发明还具有合成β-内酯并具有新型β-内酯化合物特征的方法。

    Selective substrates for matrix metalloproteinases
    5.
    发明申请
    Selective substrates for matrix metalloproteinases 失效
    基质金属蛋白酶的选择性底物

    公开(公告)号:US20050181989A9

    公开(公告)日:2005-08-18

    申请号:US10243613

    申请日:2002-09-13

    摘要: The invention provides isolated MMP-2, MMP-9 and MT1-MMP selective substrate polypeptides or functional peptidomimetics. The selective substrate polypeptides contain the following sequences: MMP-2 selective substrate polypeptides contain SEQ ID NOS:1-27, MMP-9 selective substrate polypeptides contain SEQ ID NOS:28-35, and MT1-MMP selective substrate polypeptide contain SEQ ID NOS:36-40. In addition, the invention provides a method of preferentially directing a moiety to a site of MMP-2 activity by administering to a subject an effective amount of an isolated MMP-2 selective substrate polypeptide containing SEQ ID NOS:45-47 linked to a moiety. Also provided is a method of preferentially directing a moiety to a site of MMP-9 activity by administering to a subject an effective amount of an isolated MMP-9 selective substrate polypeptide containing SEQ ID NO:44 linked to a moiety, and preferentially directing a moiety to a site of MT1-MMP activity by administering to a subject an effective amount of an isolated MT1-MMP selective substrate polypeptide containing SEQ ID NOS:36-40 linked to a moiety.

    摘要翻译: 本发明提供分离的MMP-2,MMP-9和MT1-MMP选择性底物多肽或功能肽模拟物。 选择性底物多肽包含以下序列:MMP-2选择性底物多肽含有SEQ ID NO:1-27,含有SEQ ID NO:28-35的MMP-9选择性底物多肽,并且含有SEQ ID NOS的MT1-MMP选择性底物多肽 :36-40。 此外,本发明提供了通过向受试者施用有效量的与部分连接的含有SEQ ID NO:45-47的分离的MMP-2选择性底物多肽来优先将部分定向到MMP-2活性位点的方法 。 还提供了通过向受试者施用有效量的与部分连接的含有SEQ ID NO:44的分离的MMP-9选择性底物多肽,优先将一部分连接至部分MMP-9活性部位的方法, 通过向受试者施用有效量的与部分连接的含有SEQ ID NO:36-40的分离的MT1-MMP选择性底物多肽,从而部分到MT1-MMP活性的位点。