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    • 9. 发明公开
    • Thiatriazine derivatives
    • 噻三嗪衍生物
    • EP0159533A2
    • 1985-10-30
    • EP85103158.3
    • 1985-03-19
    • HOECHST UK LIMITED
    • Ross, Barry Clive, Dr.Michael, Jeffrey DanielCousins, Simon John
    • C07D285/00C07D417/12A61K31/54C07C161/00
    • C07D285/15C07C307/04C07C333/00C07C335/38C07D417/12
    • Compounds of formula I
      are valuable H-2 antagonists; R represents hydrogen, alkyl, phenyl or phenalkyl; W and Z represent groups E-(CH 2 ) n -X-(CH 2 ) m- NH with E being phenyl, imidazolyl, thiazolyl, furyl, thienyl or pyridyl; or W or Z is hydrogen, alkyl, phenyl, O-alkyl, NR 4 R 5 (R 4 /R 5 are hydrogen, alkyl or phenyl); X is O or S; n is 0 or 1, m is 2, 3 or 3.
      Moreover compounds XXXI are described
      in which R 31 /R 32 are H, alkyl, cycloalkyl, phenyl, phenylkyl or part of 4-to 7-membered ring: L 3 /L 4 are X-(alkyl-phenyl, -phenalkyl), compounds XXXI are versatile intermediates for the production of i.a. compounds I.
      ComDounds XXXV
      with R 42 /R 43 being hydrogen, alkyl, phenyl, phenyalkyl are also versatile intermediates inter alia for the preparation of compounds I.
      Processes for the preparation of these compounds are disclosed as well.
    • 式I化合物是有价值的H-2拮抗剂; R代表氢,烷基,苯基或苯基烷基; W和Z代表E-(CH2)n-X-(CH2)m-NH基团,其中E为苯基,咪唑基,噻唑基,呋喃基,噻吩基或吡啶基; 或W或Z为氢,烷基,苯基,O-烷基,NR 4 R 5(R 4 / R 5为氢,烷基或苯基)。 X是O或S; 此外,描述了其中R 31 / R 32是H,烷基,环烷基,苯基,苯基烷基或部分4-至7-元环的化合物XXXI:其中R 3 / L 4是X - (烷基 - 苯基, - 苯基烷基),化合物XXXI是用于生产ia的通用中间体 化合物I.化合物XXXV与R42 / R43是氢,烷基,苯基,苯基烷基也是用于制备化合物I的通用中间体。此外,还公开了制备这些化合物的方法。