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Process for producing condensed polycyclic alkaloids by ring closure of azomethine ylide, novel compounds by the process and use of the compounds as chemotherapeutic agents

机译:通过将甲亚胺叶立德环闭环生产缩合多环生物碱的方法,该方法的新化合物以及该化合物作为化学治疗剂的用途

摘要

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.
机译:本发明提供通式(I)的化合物其中,A为环状基团,其为任选取代的芳基或芳族杂环基;或A是环状基团R A1 R A2 C-CR A3 R A4,其中R A2和R A3以及它们所连接的碳原子一起形成任选取代的饱和或不饱和碳环或杂环基,以及R A1和R A4定义如下或一起形成键;或A为非环状基团R A1 R A2 C-CR A3 R A4其中R A1- R A4如以下所定义,R A2和R A3可任选地一起形成键;或Z为碳或杂原子; n从0、1、2或3中选择; R A1-A4,W,X和Y可以相同或不同,并且各自选自氢,任选取代的烷基,任选取代的烯基,任选取代的炔基,任选保护的羟基,任选取代的氨基,任选取代的烷氧基,任选取代的烯氧基,任选取代的炔氧基,任选取代的芳基,任选取代的杂环基,羧基,羧基酯,羧酰胺基,酰基,酰氧基,巯基,任选取代的烷硫基,卤素,硝基,硫酸根,磷酸根和氰基,或W和X,以及氮与它们连接的碳原子形成饱和或不饱和的含氮杂环基,该杂环基可以任选地被取代或任选地稠合到饱和或不饱和的碳环基,芳基或杂环基上;或其药学上可接受的衍生物和盐,外消旋体,异构体和/或互变异构体;前提是该化合物不是选自Lamellarin A-N,S-X的化合物; D,L,K,M,N-三乙酸酯;乙酸乙酸酯; G-三甲醚;或T,U,V,Y-20硫酸盐。这样的化合物可用作化学治疗剂。

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