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Derivatives of aminobenzoic and aminobiphenylcarboxylic acids useful as anti-cancer agents

机译:可用作抗癌剂的氨基苯甲酸和氨基联苯羧酸的衍生物

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.
机译:本发明提供具有下式的化合物:<化学ID =“ CHEM-US-00001”> <图像文件=“ US06228985-20010508-C00001.GIF” id =“ EMI-C00001” imgContent =“ undefined” imgFormat =“ GIF “ /> ExternalFileRef file =” US06228985-20010508-C00001.MOL“ id =” CHEMMOL-00001“ /> ;其中n为 0 1; ; R是&mdash; NH 2 或<化学id =“ CHEM-US-00002”> <图像文件=“ US06228985-20010508-C00002.GIF” id =“ EMI-C00002 “ imgContent =” undefined“ imgFormat =” GIF“ /> ;其中R 1 和R 2 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R 3 C(O)&mdash;或 <图像文件=“ US06228985-20010508-C00003.GIF” id =“ EMI-C00003” imgContent =“ undefined” imgFormat =“ GIF” /> ;其中R 5 选自H,烷基,芳烷基,杂芳烷基和氨基甲酰基烷基,并且R 3 和R 4 选自以下组成的组: 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; Q Q(NH 2 n 且式I化合物的C(O)R取代基相对于形成所述取代基所键合的两个苯基之间的键的碳原子独立地位于邻,间或对位,条件是所述取代基不都位于邻位;式II化合物的Q NH(CH 2 n 和&C(O)R取代基彼此间或对位。 ;或其生物不稳定的酯,或其药学上可接受的盐。该化合物可用于治疗uPA或uPAR介导的疾病,例如肿瘤转移,肿瘤血管生成,再狭窄,慢性炎症或角膜血管生成。

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