| abstract |
Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1) wherein R<SUP>1 </SUP>is a binding partner, a linker or H; a and b are 0 or 1, provided that the total of a and b is 0 or 1; A is N or C; X is S, O, -C(O)-, NH or NCH<SUB>2</SUB>R<SUP>6</SUP>; Y is -C(O)-; Z is taken together with A to form an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R<SUP>6 </SUP>or -O; R<SUP>6 </SUP>is independently H, C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl, C<SUB>2</SUB>-C<SUB>6 </SUB>alkenyl, C<SUB>2</SUB>-C<SUB>6 </SUB>alkynyl, NO<SUB>2</SUB>, N(R<SUP>3</SUP>)<SUB>2</SUB>, C≡N or halo, or an R<SUP>6 </SUP>is taken together with an adjacent R<SUP>6 </SUP>to complete a ring containing 5 or 6 ring atoms; R<SUP>3 </SUP>is a protecting group or H; and tautomers, solvates and salts thereof; and provided that where a is 0, b is 1, and R<SUP>1 </SUP>is in which D<SUP>2 </SUP>is independently hydroxyl, blocked hydroxyl, mono, di or triphosphate, or an oligodeoxyribonucleotide otherwise containing only the bases A, G, T and C; and D<SUP>3 </SUP>is H or OH; then Z is not unsubstituted phenyl. Also provided are novel intermediates and methods for the preparation and use of the structure (1) compounds. |