21-Hydroxycorticosteroid esters which can have good solution stability and are therefore suitable for formulation into aqueous compositions for injection or infusion, have the formula
wherein St is the corticosteroid without its 21-hydroxy group;
Y is a bond. -O- or -S-;
Xis -CO-NR-, -NR-CO-, -O-, -S-, -SO- or-S02- and R is hydrogen or C1-4 alkyl;
m is an integer of from 1 to 5 and n is an integer of from 2 to 9, provided that m + n ≤ 10; and
either R, and R2 are each C1-4 alkyl optionally substituted by one hydroxyl group or -NR1R2 is a monocyclic heterocyclic group;
or a salt thereof.
21-羟基皮质类
固醇酯具有良好的溶液稳定性,因此适合配制成注射或输注用的
水性组合物,其结构式为
其中,St 是不含 21-羟基的皮质类
固醇;
Y 是键-O-或-S-;
X是-CO-NR-、-NR-CO-、-O-、-S-、-SO-或-S02-,R是氢或C1-4烷基;
m 是 1 至 5 的整数,n 是 2 至 9 的整数,但 m + n ≤ 10;以及
R和R2各自为被一个羟基任选取代的C1-4烷基,或-NR1R2为单环杂环基团;
或其盐。