A sterile, non-irritant, non toxic pharmaceutical composition adapted for topical administration to the eye is described which contains a compound of formula (I):
wherein X = Y is CR = N or N = CR where at least two of R, R', R2 and R3 are amino groups and the other groups of R, R', R2 and R3 are hydrogen atom, lower alkyl, aryl, carboxamido or lower alkoxycarbonyl groups except that when R', R2 and R3 are all amino and X = Y is CR = N, R is not phenyl. The composition may be used to treat ocular hypertension and glaucoma.
                            本发明描述了一种无菌、无刺激、无毒、适用于眼部局部用药的药物组合物,该组合物含有式 (I) 的化合物:
其中 X = Y 为 CR = N 或 N = CR,其中 R、R'、R2 和 R3 中至少有两个基团为
氨基,R、R'、R2 和 R3 中的其他基团为氢原子、低级烷基、芳基、羧酰胺基或低级烷氧羰基,但当 R'、R2 和 R3 均为
氨基且 X = Y 为 CR = N 时,R 不是苯基。该组合物可用于治疗眼压过高和青光眼。