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    • 8. 发明申请
    • THIAZOLIDINE DERIVATIVES AND THEIR USE AS ANTI-VIRAL COMPOUNDS
    • 噻唑烷衍生物及其作为抗病毒化合物的用途
    • WO1993001174A1
    • 1993-01-21
    • PCT/EP1992001494
    • 1992-07-03
    • GLAXO GROUP LIMITEDKITCHIN, JohnHOLMES, Duncan, StuartHUMBER, David, CedricSTORER, RichardDOLAN, Simon, CharlesHANN, Michael, MenteithMCMEEKIN, PeterMURRAY-RUST, PeterPATEL, BinakumariWEINGARTEN, Gordon, Gad
    • GLAXO GROUP LIMITED
    • C07D217/06
    • C07D417/12C07D277/06C07D417/14
    • The present invention provides compounds of formula (I), wherein R is hydrogen, alkyl or CH2alkyl where the alkyl portion is substituted by OH; A represents either a group CHR CHR OH or a group (II), where R is hydrogen, alkyl, cycloalkylalkyl or Aralkyl, R is hydrogen, alkyl, cycloalkylalkyl, aralkyl, CHR CONR R (where R is hydrogen, alkyl, cycloalkylalkyl or Aralkyl, R is hydrogen or methyl and R is hydrogen, alkyl optionnally substituted by one or two hydroxyl groups, aryl, heteroaryl, cycloalkylalkyl, Aralkyl wherein the alkyl portion is optionnally substituted by hydroxymethyl, or Hetalkyl) or CHR NHCOR (where R is alkyl, cycloalkylalkyl or an aralkyl), R is alkoxy or NR R (where R is hydrogen or methyl and R is hydrogen, alkyl, aryl, aralkyl or cycloalkylalkyl); X is a group -CHR (CHR )r(CHR )sCHR -, where R and R are hydrogen, r is 1, s is zero and R is hydroxyl or hydroxymethyl, or R and R are hydrogen, r and s are 1 and R and R are each hydrogen or hydroxyl provided that at least one of R and R is hydroxyl, or one of R and R is hydrogen and the other is hydroxymethyl and r and s are zero; useful in chemotherapy, particularly of viral infections.
    • 本发明提供式(I)化合物,其中R 1是氢,烷基或C 2烷基,其中烷基部分被OH取代; A代表基团CHR 21 CHR 22 OH或基团(II),其中R 21是氢,烷基,环烷基烷基或芳烷基,R 22是氢,烷基,环烷基烷基,芳烷基,CHR 24 R CONR 25 R 26(其中R 24是氢,烷基,环烷基烷基或芳烷基,R 25是氢或甲基,R 26是氢,烷基选择性地被一个或两个羟基取代 ,芳基,杂芳基,环烷基烷基,芳烷基,其中烷基部分选择性地被羟甲基或Hetalkyl取代)或CHR 24 NHCOR 27(其中R 27是烷基,环烷基烷基或芳烷基),R 23是 烷氧基或NR 28 R 29(其中R 28是氢或甲基,R 29是氢,烷基,芳基,芳烷基或环烷基烷基); X是基团-CHR 30(CHR 31)r(CHR 32)s CHR 33,其中R 30和R 33是氢,r是1,s是0,R 31是羟基或羟甲基,或R 30和R 33是氢,r和s是1,R 31和R 32各自是氢或羟基,条件是R 31中至少有一个 且R 32为羟基,R 30和R 33之一为氢,另一个为羟甲基,r和s为0; 可用于化疗,特别是病毒感染。