申请人:Jefford, Charles W.
公开号:EP0286316A1
公开(公告)日:1988-10-12
1,2,4-trioxane derivatives of formula:
(wherein
each of the subscripts m and n is equal to 0 or 1;
the symbol Z represents an epoxide oxygen atom at the 5,6 or 6,7 positions, or a pair of electrons forming a double bond at the 5,6 or 6,7 positions;
each of the symbols Ar¹ and Ar², being the same or different, represents an aromatic group which is optionally substituted;
each of the symbols R¹ and R², being the same or different, represents a linear or branched alkyl group, which is optionally substituted, or R¹ and R², taken together with the carbon atom to which they are attached, form an alicyclic group which is optionally interrupted by one or more oxygen, sulphur or nitrogen atoms and which group is optionally substituted with one or more alkyl or aryl groups, or one or more functional groups; and
each of X and Y, being the same or different, represents a hydrogen atom or a functional group which contains oxygen, nitrogen or sulphur) are of use in the treatment of tropical diseases including malaria and have other physiological activities.
式中的 1,2,4-三氧杂环己烷衍生物:
其中
下标 m 和 n 分别等于 0 或 1;
符号 Z 代表位于 5、6 或 6、7 位的环氧氧原子,或位于 5、6 或 6、7 位的形成双键的一对电子;
符号 Ar¹ 和 Ar² (相同或不同)代表任选被取代的芳香基团;
符号 R¹ 和 R² 中的每个符号,无论相同或不同,均代表任选被取代的直链或支链烷基,或 R¹ 和 R² 与它们所连接的碳原子一起形成脂环族基团,该基团任选被一个或多个氧原子、硫原子或氮原子打断,且该基团任选被一个或多个烷基或芳基或一个或多个官能团取代;以及
X和Y(相同或不同)分别代表一个氢原子或一个含氧、氮或硫的官能团)可用于治疗热带疾病,包括疟疾,并具有其他生理活性。