申请人:SANKYO COMPANY LIMITED
公开号:EP0319316A2
公开(公告)日:1989-06-07
Monoester griseolic acid derivatives of formula (I):
(in which: R1 and R2 are the same or different and each represents a hydrogen atom, a hydroxy group or a protected hydroxy group; R3 and R4 each represents a hydrogen atom, or together represent an extra carbon-carbon bond between the two carbon atoms to which they are attached; one of RS and R6 represents a hydrogen atom and the other represents a carboxy-protecting group removable in the biochemical environment of the human eye); and pharmaceutically acceptable salts thereof have been found to have valuable properties in the treatment of ophthalmic disorders. They may be prepared by the selective esterification of the appropriate free acid.
式(I)的单酯格栅羧酸衍生物:
其中R1和R2相同或不同,各自代表一个氢原子、一个羟基或一个受保护的羟基;R3和R4各自代表一个氢原子,或共同代表它们所连接的两个碳原子之间的一个额外的碳-碳键;RS和R6中的一个代表氢原子,另一个代表可在人眼的生化环境中去除的羧基保护基团);以及它们的药学上可接受的盐类已被发现在治疗眼科疾病方面具有宝贵的特性。它们可以通过选择性酯化适当的游离酸来制备。