申请人:JAPAN TOBACCO INC.
公开号:EP0533951A1
公开(公告)日:1993-03-31
Disclosed is a novel oxazinone derivative represented by formula (I) given below or a pharmaceutically acceptable acid-addition salt thereof, which is useful as an anti-inflammatory agent, an agent for suppressing neutrophil infiltration and as a serine protease inhibitor:
where A includes, for example,
in which W is -O-, -S-, -CH=CH- or -NR⁹- or means that (CH₂)n is directly bonded to (CH₂)n,
V² is =CR¹²- or =N-, and
D is 5 to 7-membered carbon ring or hetero ring;
X is -O-, -S-, -CO-, or -NR¹⁵ or means that A is directly bonded to (CH₂)l;
Y is -O-, -CH=CH- or NR¹⁶- or means that (CH₂)l is directly bonded to Z;
Z is -CH₂- or -CO-; and
l is an integer of 0 to 4.
Further, R and R¹ to R¹⁶ are hydrogen atom, lower alkyl group, etc.
本发明公开了一种由下式(I)代表的新型噁嗪酮衍生物或其药学上可接受的酸加成盐,该衍生物可用作抗炎剂、抑制中性粒细胞浸润的制剂和丝氨酸蛋白酶抑制剂:
其中 A 包括,例如
其中 W 是-O-、-S-、-CH=CH- 或-NR⁹- 或表示 (CH₂)n 与 (CH₂)n 直接键合、
V² 是 =CR¹²- 或 =N-,以及
D 是 5 至 7 元碳环或杂环;
X 是-O-、-S-、-CO-或-NR¹⁵,或表示 A 直接与 (CH₂)l 结合;
Y 是-O-、-CH=CH- 或 NR¹⁶- 或表示 (CH₂)l 直接与 Z 键合;
Z 是-CH₂- 或-CO-;以及
l 是 0 至 4 的整数。
此外,R 和 R¹ 至 R¹⁶ 是氢原子、低级烷基等。