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1. A pharmaceutical formulation comprising:
(i) 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 or C, 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; andC is a moiety of the formula wherein:
each X′ is independently H, COR′, CO2R′, CONHR′, N(R″)2, an alkyl, an aryl, an arylalkyl, a cycloalkyl, a heteroaryl, 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;R0 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; andR6 is H, N(R)2, OR, halogen, an alkyl, or an aryl; wherein each R is independently H, an alkyl, or an aryl; 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; with the proviso that A and B are not both, respectively, C and D, and (ii) a pharmaceutically acceptable vehicle. |
