Patent ID: 6710163
Filing Date: 2004-03-23
Classification: A61K,A61P,C07H,C07K,C12Q

Abstract:
A compound having one of the following formulas: wherein:L is a naturally occurring nucleobase, a non-naturally occurring nucleobase, a DNA intercalator, or a nucleobase-binding group, and amino groups are, optionally, protected by amino protecting groups; A is a single bond or a group of the formula: â€ƒwhere: X is O, S, Se, NR3, CH2 or C(CH3)2; Y is: a single bond, O or S when s or q is zero; or a single bond, O, S or NR4 when s or q is an integer from 1 to 5; each of p and q is zero or an integer from 1 to 5, the sum p+q being not more than 10; each of r and s is zero or an integer from 1 to 5, the sum r+s being not more than 10; each R1 and R2 is independently selected from the group consisting of hydrogen, (C1-C4)alkyl, hydroxy- or alkoxy- or alkylthio-substituted (C1-C4)alkyl, 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; B is N or R3N+, where R3 is as defined above; each T is CR6R7, CHR6CHR7 or CR6R7CH2, where R6 is hydrogen and R7 is selected from the group consisting of the side chains of naturally occurring alpha amino acids, 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 or (C1-C6)alkyl, hydroxy-, alkoxy-, or alkylthio-substituted (C1-C6)alkyl, or R6 and R7 taken together complete an alicyclic or heterocyclic system; D is CR6R7, CH2CR6R7 or CHR6CHR7, where R6 and R7 are as defined above; each E is, independently, COON or CSOH, or an activated or protected derivative thereof; and each G is, independendy, NHR3 or NPgR3, where R3 is as defined above, and Pg is an amino protecting group.