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    • 22. 发明公开
    • Aphidicolane derivatives, their preparation and pharmaceutical compositions comprising them
    • Aphidicolanderivate,ihre Herstellung und sie enthaltende pharmazeutische Zusammensetzungen。
    • EP0112603A1
    • 1984-07-04
    • EP83304118.9
    • 1983-07-15
    • IMPERIAL CHEMICAL INDUSTRIES PLC
    • Ratcliffe, Arnold Harry
    • C07C35/44C07C47/36C07C49/513C07C247/00C07C309/63C07C69/96C07C229/00C07C271/06C07D303/14C07D211/46C07D295/14
    • C07D317/72C07C229/08C07C271/22C07C2603/86C07D211/46C07D295/15C07D303/14C07D493/08C07F7/1856
    • Aphidicolane derivatives of the formula:
      wherein R 1 stands for hydrogen or a hydroxy radical, R 2 stands for a hydroxy or methyl radical, or the group CR 1 R 2 stands for a keto group; R 3 stands for a formyl or hydroxymethyl radical, or for the group -CH 2 0.CO.OR 6 , wherein R 6 stands for a defined radical or R 2 and R 3 are joined together to form the group -O.CO.OCH 2 -; R 4 stands for a hydroxy radical; R 5 stands for a formyl radical, a hydroxyalkyl radical -(CH 2 ) 1-3 OH, a radical -CHR 7 OH, wherein R 7 stands for a defined radical, or R 5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group -CH 2 0.CO.OR 8 , wherein R 8 stands for a defined radical, or R 5 stands for the group -CH 2 O.CO.(CH 2 )m.CR 11 R 12 .(CH 2 ) n .NR 9 R 10 . wherein m, n, R 9, R 10 , R 11 and R 12 have defined values, or R 5 stands for the group -CH 2 O.SO 2 .R 13 , wherein R 13 stands for a defined radical; or R 4 and R 5 are joined together to form the group -O.CH 2 - or -O.CO.OCH 2 -; and, where appropriate, pharmaceutically acceptable salts thereof. Processes for the preparation of said aphidicolane derivatives. Pharmaceutical compositions comprising one of thecompounds and a pharmaceutical diluent or carrier. The compounds exhibit inhibitory activity against DNA-containing viruses and they inhibit the growth of some tumours.
    • 其中R1代表氢或羟基,R2代表羟基或甲基,或基团CR1R2代表酮基; R3代表甲酰基或羟甲基或基团-CH2O.CO.OR6,其中R6表示定义的基团,或R2和R3连接在一起形成基团-O.CO.OCH 2 - ; R4代表羟基; R5代表甲酰基,羟基烷基 - (CH2)1-3OH,基团-CHR7OH,其中R7代表定义的基团,或R5代表叠氮基甲基或吡咯烷基羰基氧基甲基或基团-CH2O.CO. OR 8,其中R8代表定义的基团,或R5代表基团-CH2O.CO.(CH2)m.CR11R12。(CH2)n.NR9R10,其中m,n,R9,R10,R11和R12具有定义的值 或R5代表基团-CH 2 O.SO 2 R 13,其中R 13表示定义的基团; 或R 4和R 5连接在一起形成基团-O.CH 2 - 或-O.CO.OCH 2 - ; 及其适当的药学上可接受的盐。 制备所述蚜虫烷衍生物的方法。 包含化合物之一和药物稀释剂或载体的药物组合物。 该化合物对含DNA病毒表现出抑制活性,并抑制某些肿瘤的生长。