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Pyrimidinic derivatives inhibitors of the Enzyme dihydrofolate reductase (DHFR)

机译:酶二氢叶酸还原酶(DHFR)的嘧啶衍生物抑制剂

摘要

Claim 1: A compound having the structure of formula (1) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R¹ is H, C₁₋₆ alkyl,C₃₋₆ cycloalkyl,C₄₋₈ cycloalkylalkyl or halogen; W is N or CR¹⁸ and Z is N or CR¹⁷,2. The condition is that at least one of W and Z is n;R3,R830808,R83099,R8310,R8311th,R8322,R8313,R1831181 and r831222 are independent from h, acquilo c83218c833126;C₃₋₆ cycloalkyl,Hydroxyl or fluorine, provided that there are at least four rivers,R3,R830808,R83099,R8310,R8311th,R831222 and r8313sean h; if W is n, then there is no R2,R3,R8310 and r8311;If Z is n, there is no r830808,R83099,R⁸ and R⁹ is hydroxyl; R¹⁰ is substituted or unsubstituted C₆₋₁₀ aryl or 5-10 membered heteroaryl.
机译:1,具有式(1)结构的化合物或其药学上可接受的盐或前药,其中:R 1是H,C 1-8烷基,C 1-7环烷基,C 1-7环烷基烷基或卤素; W是N或CR -1,Z是N或CR 1-2。条件是W和Z中至少一个是n; R3,R830808,R83099,R8310,R8311th,R8322,R8313,R1831181和r831222独立于h,acquilo c83218c833126;C₃₋₆环烷基,羟基或氟,条件是至少有四个河流,R3,R830808,R83099,R8310,R8311th,R831222和r8313如果W为n,则不存在R2,R3,R8310和r8311;如果Z为n,则不存在r830808,R83099,R 4和R 5为羟基。 R 10是取代或未取代的C 1-4芳基或5-10元杂芳基。

著录项

  • 公开/公告号AR107538A1

    专利类型

  • 公开/公告日2018-05-09

    原文格式PDF

  • 申请/专利权人 TURING PHARMACEUTICALS LLC;

    申请/专利号AR2017P100287

  • 发明设计人

    申请日2017-02-03

  • 分类号C07D403/12;A61K31/505;A61K31/506;A61P33/02;C07D239/48;C07D401/12;C07D405/12;

  • 国家 AR

  • 入库时间 2022-08-21 12:54:16

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