申请人:MITSUBISHI CHEMICAL CORPORATION
公开号:EP0810221A1
公开(公告)日:1997-12-03
An oxygen-containing heterocyclic derivative represented by the following formula (I) and its salt, and a solvate and a hydrate thereof:
wherein:
R1:hydrogen atom, R8-CO-, R8-O-CO- or other wherein R8 represents C1-C20 alkyl, aryl or other,
R2, R4 and, R6:a hydrogen atom, C1-C5 alkyl or other,
R3 and R5:a hydrogen atom, C1-C20 alkyl or other,
R7:a hydrogen atom, R9-CO- or other wherein R9 represents C1-C10 alkyl group or other,
A:C1-C3 alkylene group
n:0 or 1.
The oxygen-containing heterocyclic derivatives of the present invention have potent inhibitory activity against cysteine proteases and are excellent in oral absorbability, tissue distribution, and cellular membrane permeability. Therefore, they are useful as therapeutic medicament for diseases such as cerebral apoplexy, Alzheimer's disease and the like.
下式(I)所代表的含氧杂环衍生物及其盐,以及其溶液和水合物:
其中
R1:氢原子、R8-CO-、R8-O-CO-或其它,其中 R8 代表 C1-C20 烷基、芳基或其它、
R2、R4 和 R6:氢原子、C1-C5 烷基或其他、
R3 和 R5:一个氢原子、C1-C20 烷基或其他、
R7:氢原子、R9-CO- 或其他,其中 R9 代表 C1-C10 烷基或其他、
A:C1-C3 亚烷基
n:0 或 1。
本发明的含氧杂环衍生物对半胱氨酸蛋白酶具有很强的抑制活性,并且在口服吸收性、组织分布性和细胞膜渗透性方面都很出色。因此,它们可作为治疗药物用于脑中风、老年痴呆症等疾病。