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    • 4. 发明公开
    • Preparation of fused polycyclic alkaloids by ring closure of azomethine ylides, novel compounds thereof and their use as chemotherapeutic agents
    • 稠合多环生物碱通过甲亚胺叶立德,其衍生物的环合和它们作为化疗剂的制备使用
    • EP1621533A1
    • 2006-02-01
    • EP05024198.3
    • 1998-05-01
    • THE AUSTRALIAN NATIONAL UNIVERSITY
    • The designation of the inventor has not yet been filed
    • C07D217/24C07D491/052A61K31/47C07D217/10
    • C07D217/10C07D217/24C07D491/04C07D491/052C07D491/14
    • The invention provides compounds of general Formula (I)

      wherein,

      A is a cyclic group being an optionally substituted aryl group or an aromatic heterocyclic group; or
      A is a cyclic group R A1 R A2 C-CR A3 R A4 wherein R A2 and R A3 , together with the carbon atoms to which they are attached form an optionally substituted saturated or unsaturated carbocyclic or heterocyclic group and R A1 and R A4 are as defined below or together form a bond; or
      A is a non-cyclic group R A1 R A2 C-CR A3 R A4 wherein R A1 - R A4 are as defined below and R A2 and R A3 may optionally together form a bond;
      Z is a carbon or a heteroatom;
      n is selected from 0, 1, 2 or 3; and
      R A1-A4 , W, X and Y may be the same or different and each are selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally protected hydroxy, optionally substituted amino, optionally substituted alkoxy, optionally substituted alkenoxy, optionally substituted alkynoxy, optionally substituted aryl, optionally substituted heterocyclyl, carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, optionally substituted alkylthio, halogen, nitro, sulfate, phosphate and cyano, or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group;
      or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof;
      provided that the compound is not one selected from Lamellarin A-N, S-X; D, L, K, M, N-triacetate; I-acetate; G-trimethyl ether; or T, U, V, Y-20-sulphate. Such compounds are useful as chemotherapeutic agents.
    • 本发明提供了通式worin(I)的化合物中,A是被任选substituiertem芳基或芳香族杂环基的环状基团; 或A是一个环状基团R A1,R A2 C-CR A3 - [R A4 worin - [R A2和R A3,与碳原子一起与它们所连接形式在OPTIONALLY substituiertem饱和或不饱和碳环或杂环基,R A1和R A4 是下文定义的或一起形成一个键; 或A是一个非环状基R A1 A2 - [R C-CR A3 A4 - [R [R worin A1 - R的A4如下文所定义并且R A2和R A3可以任选地一起形成一个键; Z是碳或杂原子; n选自0,1,2或3中选择; 和R A1-A4,W,X和Y可以相同或不同,且各自选自氢,任选substituiertem烷基,任选substituiertem烯基,任选substituiertem炔基,任选保护的羟基,任选substituiertem氨基,任选substituiertem烷氧基,任选substituiertem 链烯氧基,任选substituiertem炔,任选substituiertem芳基,任选substituiertem杂环基,羧基,羧基酯,甲酰氨基,酰基,酰氧基,巯,任选substituiertem烷硫基,卤素,硝基,硫酸盐,磷酸盐和氰基,或W和X,的氮一起 和碳原子它们所连接,形成饱和或不饱和含氮其可以任选substituiertem或任选地稠合到杂环基团的饱和或不饱和的碳环基,芳基或杂环基团; 或药学上可接受的衍生物和盐,种族匹配,异构体和/或互变异构体; 提供DASS死化合物不是一个从片螺素A-N,S-X中选择; D,L,K,M,N-三乙酸酯; I-乙酸酯; G-三甲基醚; 或T,U,V,Y-20-硫酸盐。 搜索化合物作为化学治疗剂是有用的。