申请人:PHARMA MAR, S.A.
公开号:EP0687673A1
公开(公告)日:1995-12-20
New antitumoral compounds are of formula (I):
where R², R³, R⁴, R⁵, R⁶, and R¹⁰ are the same or different and each represents a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, a hydroxy group or an acyloxy group R-(C=O)-O- (where R-(C=O)- is an acyl group of 1 to 26 carbon atoms); provided that at least one of R², R³, R⁴, R⁵, R⁶, and R¹⁰ is an acyloxy group R-(C=O)-O- (where R-(C=O)- is an acyl group of 1 to 26 carbon atoms) and further provided that at least one of R², R³, R⁴, R⁵, R⁶, and R¹⁰ is an acyloxy group R-(C=O)-O- (where R-(C=O)- is an acyl group of 10 to 25 carbon atoms); with the exception of the tetraacetate of bengazole A and the tetraacetate of bengazole B. The lead to these compounds is provided by digonazole triacetate of formula (V), obtained from digonazole which may itself be extracted from Jaspis digonoxea.
新的抗肿瘤化合物为式 (I):
其中 R²、R³、R⁴、R⁵、R⁶ 和 R¹⁰ 相同或不同,且各自代表氢原子、1 至 6 个碳原子的烷基、羟基或酰氧基 R-(C=O)-O-(其中 R-(C=O)-是 1 至 26 个碳原子的酰基);条件是 R²、R³、R⁴、R⁵、R⁶ 和 R¹⁰ 中至少有一个是酰氧基 R-(C=O)-O-(其中 R-(C=O)-是 1 至 26 个碳原子的酰基),进一步条件是 R²、R³、R⁴、R⁵、R⁶和 R¹⁰ 中至少有一个是酰氧基 R-(C=O)-O-(其中 R-(C=O)-是 10 至 25 个碳原子的酰基);苯加唑 A 的四乙酸酯和苯加唑 B 的四乙酸酯除外。这些化合物的先导成分是式 (V) 的地高唑三乙酸酯,它是从地高唑中获得的,而地高唑本身可以从 Jaspis digonoxea 中提取。