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straight biaryl - pyridochinazolinonderivate as anti-cancer agents

机译:直联芳基-吡啶并中国唑啉酮衍生物作为抗癌药

摘要

The invention provides a compound having the formula (1), wherein (A) n = 2-4; (B) R1 and R2 are the same or different and selected from the group consisting of H, (C1-C3) alkyl, -CH2CH2OH, -CH2CH2NH2, and -CH2CH2N(CH3)2 or R1 and R2 are alkyl moieties which are taken together to form a 4- to 7-membered ring; (C) R3 is selected from the group consisting of H, -CH3, -CH2CH3, and -CH2CH2NH2; (D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3-position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri-substituted with -OR4, -NR5R6, -CO2H, -CO2R4, or phenyl; R4 is H or (C1-C4) straight-chain alkyl; R5 and R6 are the same or different and are selected from the group consisting of H, (C1-C4) straight-chain alkyl, -CH2CH2OH, -CH2CH2NH2, and -CH2CH2N(CH3)2 or R5 and R6 are alkyl moieties which are taken together to form a 4-7 membered ring; or a pharmaceutically acceptable salt thereof which is useful as an antineoplastic agent.
机译:本发明提供了具有式(1)的化合物,其中(A)n = 2-4; (B)R 1和R 2相同或不同,并且选自H,(C 1 -C 3)烷基,-CH 2 CH 2 OH,-CH 2 CH 2 NH 2和-CH 2 CH 2 N(CH 3)2,或R 1和R 2为烷基部分。一起形成4至7元环; (C)R3选自H,-CH3,-CH2CH3和-CH2CH2NH2; (D)Y是位于吡啶并喹唑啉酮核的2-或3-位的具有5-14个原子的杂环基,其中1-3个杂环原子独立地为氮,氧或硫;其中Y可以任选地被-OR 4,-NR 5 R 6,-CO 2 H,-CO 2 R 4或苯基单,二或三取代; R4是H或(C1-C4)直链烷基; R 5和R 6相同或不同,并且选自H,(C 1 -C 4)直链烷基,-CH 2 CH 2 OH,-CH 2 CH 2 NH 2和-CH 2 CH 2 N(CH 3)2,或者R 5和R 6为烷基部分,它们是一起形成一个4-7元环;或其可用作抗肿瘤药的药学上可接受的盐。

著录项

  • 公开/公告号DE69713139D1

    专利类型

  • 公开/公告日2002-07-11

    原文格式PDF

  • 申请/专利权人 AMERICAN CYANAMID CO. MADISON;

    申请/专利号DE19976013139T

  • 发明设计人 TROVA PETER;ZHANG NAN;

    申请日1997-11-24

  • 分类号C07D471/04;A61K31/505;

  • 国家 DE

  • 入库时间 2022-08-22 00:24:53

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