Patent ID: 6395474
Filing Date: 2002-05-28
Classification: A61K,A61P,C07H,C07K,C12Q

Abstract:
A compound having the formula: wherein: n is at least 2, at least one of L1-Ln is a naturally occuring nucleobase, a non-naturally occurring nucleobase, a DNA intercalator, or a nucleobase-binding group, with the remainder of L1-Ln being independently selected from the group consisting of hydrogen, hydroxy, (C1-C4)alkanoyl, naturally occurring nucleobases, non-naturally occurring nucleobases, aromatic moieties, DNA intercalators, nucleobase-binding groups, heterocyclic moieties, and reporter ligands; each of A1-An is a single bond, a methylene group or a group of formula: where:X is O, S, Se, NR3, CH2 or C(CH3)2; p1 Y is a single bond, O, S or NR4; each of p and q is zero or an integer from 1 to 5; each of r and s is zero or an integer from 1 to 5, provided that s is not zero in any A1-An in which Y is NR4; each R1 and R2 is independently selected from the group consisting of hydrogen, (C1-C4)alkyl which may be hydroxy- or alkoxy- or alkylthio-substituted, hydroxy, alkoxy, alkylthio, amino and halogen; and each R3 and R4 is independently selected from the group consisting of hydrogen, (C1-C4)alkyl, hydroxy- or alkoxy- or alkylthio-substituted (C1-C4)alkyl, hydroxy, alkoxy, alkylthio and amino; each of B1-Bn is N or R3N+, where R3 is as defined above; each of T1-Tn is CR6R7, CHR6CHR7 or CR6R7CH2, where R6 is hydrogen and R7 is selected from the group consisting of the side chains of aspartic acid, glutamic acid, tryrosine, asparagine, glutamine, threonine, serine, cysteine, arginine, tryptophan, alanine, phenylalanine, proline, methionine, valine, leucine, and isoleucine, or R6 and R7 are independently selected from the group consisting of hydrogen, (C2-C6)alkyl, aryl, aralkyl, heteroaryl, hydroxy, (C1-C6)alkoxy, (C1-C6)alkylthio, NR3R4 and SR5, where R3 and R4 are as defined above, and R5 is hydrogen, (C1-C6)alkyl, hydroxy-, alkoxy-, or alkylthio-substituted (C1-C6)alkyl, or R6 and R7 taken together complete an alicyclic or heterocyclic system; each of D1-Dn is CR6R7, CH2CR6R7 or CHR6CHR7, where R6 and R7 are as defined above; each of G1-Gnâˆ’1 is â€”NR3COâ€”, â€”NR3l CSâ€”, â€”NR3SO2â€” or â€”NR3SO2â€”, in either orientation, where R3 is as defined above; Q is â€”CO2H, â€”CONRâ€²Râ€³, â€”SO3H or â€”SO2NRâ€²Râ€³ or an activated derivative of â€”CO2H or â€”SO3H; and I is â€”NHRâ€²â€³Râ€³â€³ or â€”NRâ€²â€³C(O)Râ€³â€³, where Râ€², Râ€³, Râ€²â€³ and Râ€³â€³ are independently selected from the group consisting of hydrogen, alkyl, amino protecting groups, reporter ligands, intercalators, chelators, peptides, proteins, carbohydrates, lipids, steroids, oligonucleotides and soluble and non-soluble polymers.