GLYCOPEPTIDE ANTIBIOTIC DERIVATIVE

摘要

The present invention provides a novel glycopeptide antibiotic derivative. These derivatives are represented by the formula (I)
or a pharmaceutically acceptable salt or solvate thereof,
wherein
R A is
€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-X 1 -Ar 1 -X 2 -Y-X 3 -Ar 2
wherein
X 1 , X 2 and X 3 are single bond; heteroatom-containing group selected from the group consisting of -N=, =N-, - NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group;
Y is -NR 2 CO-, -CONR 2 - (R 2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R 3 is alkylene;
Ar 1 and Ar 2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond;
R B is
€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-NHNR X R Y or -NR Z OR W
wherein
R X is hydrogen or lower alkyl;
R Y is hydrogen, optionally substituted lower alkyl, C(=NH)NH 2 , CSNH 2 , COCONH 2 , CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl;
R Z is hydrogen or lower alkyl;
R W is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl;
R C is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N=, =N-, -NR 1 - (R 1 is hydrogen or lower alkyl), -O-, -S-, -SO- and -SO 2 -; and
R is optionally substituted alkyl.