申请人:Satoh Shigeki
公开号:US20060229236A1
公开(公告)日:2006-10-12
A cyclic tetrapeptide compound of the formula (I): wherein R
1
is hydrogen; R
2
is lower alkyl, aryl, optionally substituted ar(lower)alkyl, heterocyclic(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, lower alkylcarbamoyl(lower)alkyl or arylcarbamoyl(lower)alkyl; R
3
and R
4
are each independently hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic(lower)alkyl or cyclo(lower)alkyl(lower)alkyl, or R
3
and R
4
are linked together to form lower alkylene or condensed ring, or one of R
3
and R
4
is linked to the adjacent nitrogen atom to form a ring; R
5
is lower alkylene or lower alkenylene, Y is [wherein R
Y1
is hydrogen, halogen or optionally protected hydroxy, R
Y2
is hydrogen, halogen, lower alkyl or phenyl, and R
Y3
is hydrogen or lower alkyl]; R
8
is hydrogen or lower alkyl; and n is an integer of 1 or 2, or a salt thereof.
公式(I)的环状四肽化合物:其中R1为氢;R2为低碳基、芳基、可选取代的芳基(较低)烷基、杂环(较低)烷基、环(较低)烷基(较低)烷基、低碳基氨基(较低)烷基或芳基氨基(较低)烷基;R3和R4各自独立地为氢、低碳基、可选取代的芳基(较低)烷基、可选取代的杂环(较低)烷基或环(较低)烷基(较低)烷基,或者R3和R4结合形成低碳基亚烷基或缩合环,或者R3和R4中的一个与相邻的氮原子结合形成环;R5为低碳基亚烷基或低碳基烯烃基,Y为[其中RY1为氢、卤素或可选保护的羟基,RY2为氢、卤素、低碳基或苯基,RY3为氢或低碳基];R8为氢或低碳基;n为1或2的整数,或其盐。