1,3,2-dioxathiolane oxide derivative

C - Chemistry – Metallurgy – 07 – D

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C07D 327/10 (2006.01) C07C 237/22 (2006.01) C07D 237/22 (2006.01) C07D 295/185 (2006.01) C07D 317/32 (2006.01) C07D 405/12 (2006.01) C07D 411/12 (2006.01)

Patent

CA 2047226

ABSTRACT OF THE DISCLOSURE A 1,3,2-dioxathiolane oxide derivative having good inhibitory activity against thiol proteases such as calcium- dependent neutral protease (CANP) and cathepsins B, H and L, which is expected to be used in the cure, mitigation, treatment and prevention of myotonic dystrophy, inflammation, and renal hypertension. This derivative is represented by the following formula:. Image [I] wherein X means -S(O)- or -S(O)2; R1 means a hydrogen atom, an alkali metal atom, a benzyl group, or a lower alkyl group; R2 means a lower alkyl group which may be substituted with a methylthio group, or a benzyl group, R3 and R4 may be the same or different and independently mean a hydrogen atom, an alkyl group having one to ten carbon atoms, a lower alkyl group substituted with a guanidyl group, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group, or a phenethyl group, or together mean an alkylene group.

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