Short-chain peptide indocyanine dye conjugates used as contrast agents for optical diagnostics

摘要

Cyanine dyes are described by formula XVIII wherein: p is 1, 2 or 3; n is 1, 2, 3, 4, or 10; R1 and R2 are 4-sulfobutyl, 3-sulfopropyl, 2-sulfoethyl, 3- mehtyl-3-sulfopropyl, methyl, ethyl, or propyl radical; R3 is H or the radicals -COOE1, -CONE1E2, NHCOE1, - NHCONHE1, -NE1E2, OE1, -OSO3E1, -SO3E1, -SO2NHE1 E1 and E2 are H, methyl, ethyl or a C3-C6 alkyl radical which is interrupted by 0 to 2 oxygen atoms and/or by 0 to 1 carbonyl groups and/or is substituted by 5 to 5 hydroxy groups. Formulas XIX or XX wherein: R1 and R2 are 4-sulfobutyl, 3-sulfopropyl, 2-sulfoethyl radical R3 is -COOH or -CONH-(CH2)n-COOH with n=2 or 3, -CONH-(CH2)n- NCS with n= 2 or 3, -CONH-(CH2)n-NHCO-CH2-X1 with n=2 or 3 and X1= Cl, Br or formula (A) R4 and R5 are H, methyl radical or a hydroxylated alkyl radical R6 is -(CH2)m-COOH with m=0 to 2, (CH2)m-NCS with m= 0 to 2, -(CH2)m-CONH-peptide with m=0 to 2, -(CH2)m-NH-CS-NH-peptide with m= 0 to 2 And X stands for O or S And by formula XXI wherein: R1 and R2 are 4-sulfobutyl, 3-sulfopropyl radical R3 is -COOH or -CONH-(CH2)n-COOH with n=2 or 3, -CONH-(CH2)n- NCS with n= 2 or 3, -CONH-(CH2)n-NHCO-CH2-X1 with n=2 or 3 and X1= Cl, Br or formula (A) R4 and R5 are H, methyl radical or a hydroxylated alkyl radical.