4h-3, 1-benzoxazin-4-one derivative

Details 4h-3, 1-benzoxazin-4-one derivative 4h-3, 1-benzoxazin-4-one derivative

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) C07D 207/16 (2006.01) C07D 413/12 (2006.01) C07K 5/062 (2006.01) C07K 5/065 (2006.01) C07K 5/08 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2056453

- 54 - A B S T R A C T 4H-3,1-benzoxazin-4-one derivatives represented by formula (I) below: Image (I) wherein R1 means a lower alkyl group, R2 means a lower alkyl group, a lower alkylthioalkyl group, or a lower alkanesulfinylalkyl group, R3 means a hydrogen atom, a hydroxyl group, a lower alkoxy group, or a lower acyloxy group, X means an amino acid residue selected from the group consisting of alanine, valine, and phenylalanine, n means an integer of 0, 1, or 2, and Y means a substi- tuent selected from the group consisting of an alkanoyl group having 2 to 6 carbon atoms which may be substituted by a phenyl group, a benzyloxycarbonyl group, a lower alkoxycarbonyl group, a cinnamoyl group, and a methoxysuccinyl group. These derivatives have strong serine protease inhibiting effect and are useful as effective components of agents for preventing and curing diseases caused by an excessive effect of serine protease, e.g., pneumonia, pulmonary emphysema, fibroid lung, bronchitis, arthritis, pancreatitis, nephritis, shock, sepsis, and arteriosclerosis.

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