Nucleic acid-binding oligomers possessing N-branching for therapy and diagnostics

Claim 1

A compound of the formula I ##STR13## in which A represents --(CH 2 ) n - or --CO--, B represents all natural or unnatural nucleobases, or derivatives derived therefrom by chemical modification, or halogenated precursors thereof, optionally substituted on the amino groups by protective groups selected from the group consisting of acetyl, trifluoroacetyl, trichloroacetyl, benzoyl, phenylacetyl, benzyloxycarbonyl, tertbutyloxycarbonyl, allyloxycarbonyl or (9-fluorenyl)methoxycarbonyl, or other protective groups which are customary in peptide and nucleic acid chemistry, or possessing free amino groups, D represents --(CO) p --, E and G, independently of each other, represent --CHR--, where R represents H or a residue of a natural or unnatural amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, cysteine, methionine, phenylalanine, tyrosine, histidine, tryptophan, lysine, ornithine, asparagine, aspartic acid, glutamine, glutamic acid, arginine, proline, hydroxyproline or sarcosine, dehydroamino acids selected from the group consisting of dehydroalanine or dehydro-α-aminobutyric acid, phenylglycine, 4-nitrophenylalanine, 3-nitrophenylalanine, 2-nitrophenylalanine, 2-, 3- or 4-aminophenylalanine, 3,4-dichlorophenylalanine, 4-iodophenylalanine, 4-methoxyphenylalanine, 1-triazolylalanine, 2-pyridylalanine, 3-pyridylalanine, 4-pyridylalanine, 1-naphthylalanine or 2-naphthylalanine, optionally possessing protective groups, in their D or L form, or, optionally, E and G are linked together via an alkyl chain --(CH 2 ) q --, K represents --CO--, --SO 2 -- or --CH 2 --, L can be a carrier system, reporter ligand, a solubility-mediating group or hydrogen, M can, independently of L, be a carrier system, reporter ligand, a solubility-mediating group or hydrogen, m can be 0, 1, 2 or 3, n can be 0, 1, 2, 3 or 4, p can be 0, 1 or 2, q can be 0, 1 or 2, and s can assume values of between 1 and 30 containing the radical of a compound selected from the group consisting of 4-tert-butyloxycarbonylamino-N-[(thymin-1-yl)acetyl]-L-cis-proline, N-[(N 4 -benzoylcytosin-1-yl)acetyl]-4-tert-butyloxycarbonylamino-L-cis-proline, 4-tert-butyloxycarbonylamino-N-[(thymin-1-yl)-acetyl]-L-trans-proline, 4-tert-butyloxycarbonylamino-N-[(N 6 -benzyloxycarbonyl-adenin-9-yl)acetyl]-L-cis-proline, 4-tert-butyloxycarbonylamino-N-[(N 6 -benzyloxycarbonyl-adenin-9-yl)acetyl]-L-trans-proline, and 4-tert-butyloxycarbonylamino-N-[(N 4 -benzyloxycarbonyl-cytosin-1-yl)acetyl]-L-trans-proline.