Oligooxopiperazines and methods of making and using them

摘要

The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed.

主权项

1. An oligooxopiperazine of Formula I:wherein:
each of R1, R2, R3, and R4 is independently an amino acid side chain, H, N(R)2, OR, halogen, an alkyl, or an aryl; wherein each R is independently H, an alkyl, or an aryl; each R6 is independently H, N(R)2, OR, halogen, an alkyl, or an aryl; wherein each R is independently H, an alkyl, or an aryl; A is X1 wherein:
X1 is H, COR′, CO2R′, CONHR′, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a protecting group for protection of an amine, a targeting moiety, or a tag; wherein R′ is H, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a targeting moiety, or a tag; and B is Y or D, wherein:
Y is OR′, COR′, N(R′″)2, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a protecting group for protection of a carboxylic acid, a targeting moiety, or a tag;
wherein:R′ is H, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a targeting moiety, or a tag; andeach R′″ is independently H, CO2R′, CONHR′, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a targeting moiety, or a tag; andD is a moiety of the formula  wherein:
R5 is an amino acid side chain, H, N(R)2, OR, halogen, an alkyl, or an aryl;
wherein each R is independently H, an alkyl, or an aryl;R6 is H, N(R)2, OR, halogen, an alkyl, or an aryl; wherein each R is independently H, an alkyl, or an aryl; andE is X2 or F, wherein:
X2 is H, COR′, CO2R′, CONHR′, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a protecting group for protection of an amine, a targeting moiety, or a tag; wherein R′ is H, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a targeting moiety, or a tag; andF is a moiety of the formula  wherein: R6 is H, N(R)2, OR, halogen, an alkyl, or an aryl; wherein each R is independently H, an alkyl, or an aryl; R7 is an amino acid side chain; and Y is OR′, COR′, N(R′″)2, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a protecting group for protection of a carboxylic acid, a targeting moiety, or a tag; wherein: R′ is H, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a targeting moiety, or a tag; and each R′″ is independently H, CO2R′, CONHR′, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, a targeting moiety, or a tag.