申请人:Imperial Chemical Industries PLC
公开号:US04803201A1
公开(公告)日:1989-02-07
Aphidicolane derivatives of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a hydroxy radical, R.sup.2 stands for a hydroxy or methyl radical, or the group CR.sup.1 R.sup.2 stands for a keto group; R.sup.3 stands for a formyl or hydroxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.6, wherein R.sup.6 stands for a defined radical or R.sup.2 and R.sup.3 are joined together to form the group --O.CO.OCH.sub.2 --; R.sup.4 stands for a hydroxy radical; R.sup.5 stands for a formyl radical, a hydroxyalkyl radical --(CH.sub.2).sub.1-3 OH, a radical --CHR.sup.7 OH, wherein R.sup.7 stands for a defined radical, or R.sup.5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.8, wherein R.sup.8 stands for a defined radical, or R.sup.5 stands for the group --CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10, wherein m, n, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 have defined values, or R.sup.5 stands for the group --CH.sub.2 O.SO.sub.2.R.sup.13, wherein R.sup.13 stands for a defined radical; or R.sup.4 and R.sup.5 are joined together to form the group --O.CH.sub.2 -- or --O.CO.OCH.sub.2 --; and, where appropriate, pharmaceutically-acceptable salts thereof. Processes for the preparation of said aphidicolane derivatives. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds exhibit inhibitory activity against DNA-containing viruses and they inhibit the growth of some tumors.
Aphidicolane衍生物的化学式为:##STR1## 其中R.sup.1代表氢或羟基自由基,R.sup.2代表羟基或甲基自由基,或者基团CR.sup.1 R.sup.2代表酮基;R.sup.3代表甲酰基或羟甲基自由基,或者基团--CH.sub.2 O.CO.OR.sup.6,其中R.sup.6代表定义的自由基或R.sup.2和R.sup.3连接在一起形成基团--O.CO.OCH.sub.2 --;R.sup.4代表羟基自由基;R.sup.5代表甲酰基自由基,羟基烷基自由基--(CH.sub.2).sub.1-3 OH,基团--CHR.sup.7 OH,其中R.sup.7代表定义的自由基,或者R.sup.5代表偶氮甲基或吡咯啉甲酰氧甲基自由基,或者基团--CH.sub.2 O.CO.OR.sup.8,其中R.sup.8代表定义的自由基,或者R.sup.5代表基团--CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10,其中m,n,R.sup.9,R.sup.10,R.sup.11和R.sup.12有定义的值,或者R.sup.5代表基团--CH.sub.2 O.SO.sub.2.R.sup.13,其中R.sup.13代表定义的自由基;或者R.sup.4和R.sup.5连接在一起形成基团--O.CH.sub.2 --或--O.CO.OCH.sub.2 --;必要时,其药学上可接受的盐。制备所述Aphidicolane衍生物的方法。包含其中一种化合物和药用稀释剂或载体的药物组合物。这些化合物对含有DNA的病毒具有抑制活性,它们抑制某些肿瘤的生长。