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    Derivatives of aminobenzoic and aminobiphenylcarboxylic acids useful as anti-cancer agents
    1.
    发明授权
    Derivatives of aminobenzoic and aminobiphenylcarboxylic acids useful as anti-cancer agents 失效
    用作抗癌剂的氨基苯甲酸和氨基联苯羧酸的衍生物

    公开(公告)号：US06228985B1

    公开(公告)日：2001-05-08

    申请号：US09082787

    申请日：1998-05-21

    申请人： Christine H. Blood ,  Bernard R. Neustadt ,  Elizabeth M. Smith

    发明人： Christine H. Blood ,  Bernard R. Neustadt ,  Elizabeth M. Smith

    IPC分类号： C07K200

    CPC分类号： C07C229/38 ,  A61K38/00 ,  C07C237/36 ,  C07D209/18 ,  C07D209/20

    摘要： The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. The compounds are useful for treating uPA- or uPAR-mediated disorders, e.g., tumor metastasis, tumor angiogenesis, restenosis, chronic inflammation, or corneal angiogenesis.

    摘要翻译： 本发明提供具有下式的化合物：其中n为0或1; R为-NH 2，其中R1和R2独立地选自H，烷基，芳烷基，杂芳烷基，羧基，羧基烷基和氨基甲酰基; Q为R3C （O） - 或其中R 5选自H，烷基，芳烷基，杂芳烷基和氨基甲酰基烷基，R 3和R 4选自H，烷基，烷氧基，芳基烷氧基，芳烷基，杂芳烷基和氨基甲酰基烷基; 式I化合物的Q-NH-（CH 2）n - 和-C（O）R取代基相对于形成所述取代基的两个苯基之间的键的碳原子独立地位于邻位，间位或对位 条件是所述取代基不都位于邻位; 和式II化合物的Q-NH-（CH 2）n和-C（O）R取代基彼此定位在间或其生物不稳定酯或其药学上可接受的盐中。 该化合物可用于治疗uPA或uPAR介导的病症，例如肿瘤转移，肿瘤血管发生，再狭窄，慢性炎症或角膜血管生成。