申请人:Pharmacia & Upjohn S.p.A.
公开号:US06147073A1
公开(公告)日:2000-11-14
A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.
一种具有以下化学式(I)的四环亚甲基-2-噁啉酮衍生物
其中R、R.sub.1、R.sub.2和R.sub.3中的一个或两个(这两个可能相同也可能不同)被选择为:a)-X-(CH.sub.2).sub.m-NH.sub.2,-X-(CH.sub.2).sub.m-NR.sub.4 R.sub.5或-X-(CH.sub.2).sub.m-NHR.sub.6,在其中X为-O-、-S-或-NH-,m为2到4的整数,R.sub.4和R.sub.5中的一个为氢或C.sub.1-C.sub.6烷基,另一个为C.sub.1-C.sub.6烷基或R.sub.4和R.sub.5与它们连接的N原子一起形成5到7个成员的饱和杂环,R.sub.6为C.sub.2-C.sub.6烷酰基或含有1到3个氨基酸的C-末端连接的肽残基,其中末端氨基团是自由的、受保护的或烷基化形式,以提供一个--NR.sub.4 R.sub.5基团,其中R.sub.4和R.sub.5如上定义。