公开(公告)号：US06218393B1

公开(公告)日：2001-04-17

申请号：US09284642

申请日：1999-06-09

申请人： Hamish Ryder ,  Philip Anthony Ashworth ,  Michael Bryan Roe ,  Julie Elizabeth Brumwell ,  Sukhjit Hunjan ,  Adrian John Folkes ,  Jason Terry Sanderson ,  Susannah Williams ,  Levi Michael Maximen

发明人： Hamish Ryder ,  Philip Anthony Ashworth ,  Michael Bryan Roe ,  Julie Elizabeth Brumwell ,  Sukhjit Hunjan ,  Adrian John Folkes ,  Jason Terry Sanderson ,  Susannah Williams ,  Levi Michael Maximen

IPC分类号： C07D21704

CPC分类号： C07D401/12 ,  C07D215/54 ,  C07D217/04 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

摘要： Anthranilic acids of formula (I): wherein each of R to R9 is an organic substituent, n is 0 or 1, m is 0 or an integer of 1 to 6, q is 0 or 1, X is a direct bond, O, S, —S—(CH2)p or —O—(CHO2)p— wherein p is from 1 to 6 and Ar is an unsaturated carbocyclic or heterocyclic group, and the pharmaceutically acceptable salts thereof, have activity as inhibitors of P-glycoprotein and may thus be used, inter alia, as modulators of multidrug resistance in the treatment of multidrug resistant cancers, for example to potentiate the cytotoxicity of a cancer drug.

摘要翻译： 式（I）的邻氨基苯甲酸：其中R至R9各自为有机取代基，n为0或1，m为0或1至6的整数，q为0或1，X为直接键， S，-S-（CH 2）p或-O-（CHO 2）p - ，其中p为1至6，Ar为不饱和碳环或杂环基团及其药学上可接受的盐，具有作为P-糖蛋白抑制剂的活性 因此可以特别地用作治疗多药耐药性癌症的多药耐药性的调节剂，例如增强癌症药物的细胞毒性。