Patent ID: 6545162
Filing Date: 2003-04-08
Classification: A61K,C07D,C07K,C08G,C12Q

Abstract:
A polyamide-oligonucleotide conjugate of the formula: or a pharmaceutically acceptable salt thereof, wherein:n is 1-11; each Y is independently selected from the group consisting of: wherein p is 0 to 3; each X is independently selected from the group consisting of N and Câ€”R1, wherein each R1 is independently selected from the group consisting of H, CH3, OH, NH2, Cl, and CF3; each R2 is independently selected from the group consisting of H, C1-10 alkyl, C1-10 alkene, and C1-10 alkyne; R3 is selected from the group consisting of: H, or NHâ€”R6, wherein R6 is selected from the group consisting of H, &ggr;-aminobutyric acid, &bgr;-alanine, glycine, ethylenediamine, 3,3â€²-diamino-N-methylpropylamine, tert-butoxycarbonyl (Boc), dimethylaminopropylamine (Dp), and ethylenediaminetetraacetic acid, wherein if R6 is &ggr;-aminobutyric acid, &bgr;-alanine, or glycine, R6 is optionally substituted at its amino terminus with &ggr;-aminobutyric acid, &bgr;-alanine, glycine, ethylenediamine, 3,3â€²-diamino-N-methylpropylamine, tert-butoxycarbonyl (Boc), dimethylaminopropylamine (Dp), or ethylenediaminetetraacetic acid; R4 is a covalent linking group; and R5 is an oligonucleotide.