公开(公告)号：EP1244624A1

公开(公告)日：2002-10-02

申请号：EP00985582.6

申请日：2000-12-15

申请人： BTG INTERNATIONAL LIMITED

发明人： MINCHER, David, John,Napier University ,  TURNBULL, Agnes,Napier University ,  KAY, Graeme, Gillies

IPC分类号： C07D211/46 ,  A61K31/4409 ,  C07D295/10 ,  C07D207/16 ,  A61P39/00

CPC分类号： C07D207/08 ,  A61K47/64 ,  C07C225/26 ,  C07C237/20 ,  C07C237/22 ,  C07C271/22 ,  C07C2601/14 ,  C07C2603/24 ,  C07D207/16 ,  C07D211/26 ,  C07D211/46 ,  C07D243/08 ,  C07D295/116 ,  C07D295/13 ,  C07D295/185

摘要： Use of compound of Formula (I): at least one of R?1, R2, R5 and R6¿ is a group -AB and the others are independently selected from hydrogen, hydroxy, alkoxy or acyloxy, a group -AB a group -amino-(R7)nX-Y wherein R7 is a divalent organic radical and n is 0 or 1; R?3 and R4¿ are independently oxo, hydroxy or hydrogen; the or each A is independently a spacer group of formula -amino-(R7)n-X- which is bonded to the anthracene ring via the amino group nitrogen and to B via -X-, X is independently selected from O, NH and C(O); B is an amino acid residue or a peptide group or isostere thereof and Y is hydrogen or a capping group, or a physiologically acceptable derivative of such compound for the manufacture of a medicament for the treatment of cancers or microbial infections having cells exhibiting topoisomerase I activity characterised in that the group -amino-(R7)n-X- incorporates an optionally substituted heterocyclic ring directly attached to the anthroquinone ring through an amino nitrogen in the heterocycclic ring, or an optionally substituted heterocyclic or carbocyclic ring that is spaced from the anthraquinone ring by no more than an amino nitrogen and up to four carbon atoms.

摘要翻译： 式（I）化合物的用途：R 1，R 2，R 5和R 6中的至少一个为-AB基团，其余各自独立地选自氢，羟基，烷氧基或酰氧基，基团-AB a基 - 氨基 - （ R7）nX-Y其中R7是二价有机基团，n是0或1; R3和R4独立地是氧代，羟基或氢; 该或每个A独立地是式 - 氨基 - （R7）nX-的间隔基，其通过氨基氮键合到蒽环，并且通过-X-与B键合，X独立地选自O，NH和C（ O）; B是一种氨基酸残基或其肽基团或等价基因，Y是氢或封端基，或该化合物的生理上可接受的衍生物，用于制备用于治疗具有展现拓扑异构酶I活性的细胞的癌症或微生物感染的药物 其特征在于基团 - 氨基 - （R 7）n X-包含通过杂环环中的氨基氮直接连接到蒽醌环的任选取代的杂环，或与蒽醌环间隔开的任选取代的杂环或碳环，所述杂环或碳环与 不超过氨基氮和最多四个碳原子。