Patent ID: 7084125

Claim:
An oligomer comprising at least one nucleoside analogue (Xylo-LNA) of the general formula I wherein X is —O—, and the sugar group of formula I is xylofuranosyl; B is selected from hydrogen, hydroxy, optionally substituted C 1-4 -alkoxy, optionally substituted C 1-4 -alkyl, optionally substituted C 1-4 -acyloxy, nucleobases, DNA intercalators, photochemically active groups, thermochemically active groups, chelating groups, reporter groups, and ligands; P designates the radical position for an internucleoside linkage to a succeeding monomer, or a 5′-terminal group, such internucleoside linkage or 5′-terminal group optionally including the substituent R 5 or equally applicable the substituent R 5* ; P* designates an internucleoside linkage to a preceding monomer, or a 3′-terminal group; R 2* and R 4* together designate a biradical consisting of 1–4 groups/atoms selected from —(CR*R*) r —Y—(CR*R*) s —, —(CR*R*) r —Y—(CR*R*) s —Y—, —Y—(CR*R*) r+s —Y—, —Y—(CR*R*) r —Y—(CR*R*) s —, —(CR*R*) r+s —, —Y—, —Y—Y—, wherein each Y is —O—, —S—, —N(R N* )—, each R* is independently selected from hydrogen, halogen, hydroxy, mercapto, amino, optionally substituted C 1-6 -alkoxy, optionally substituted C 1-6 -alkyl, and/or two adjacent (non-geminal) R* may together designate a double bond, and each of r and s is 0–4 with the proviso that the sum r+s is 1–4, each of the substituents R 1* , R 2 , R 3* , R 5 , R 5* , which are present is independently selected from hydrogen, optionally substituted C 1-12 -alkyl, optionally substituted C 2-12 -alkenyl, optionally substituted C 2-12 -alkynyl, hydroxy, C 1-12 -alkoxy, C 2-12 -alkenyloxy, carboxy, C 1-12 -alkoxycarbonyl, C 1-12 -alkylcarbonyl, formyl, aryl, aryloxy-carbonyl, aryloxy, arylcarbonyl, heteroaryl, heteroaryloxy-carbonyl, heteroaryloxy, heteroarylcarbonyl, amino, mono- and di(C 1-6 -alkyl)amino, carbamoyl, mono- and di(C 1-6 -alkyl)-amino-carbonyl, amino-C 1-6 -alkyl-aminocarbonyl, mono- and di(C 1-6 -alkyl)amino-C 1-6 -alkyl-aminocarbonyl, C 1-6 -alkyl-carbonylamino, carbamido, C 1-6 -alkanolyloxy, sulphono, C 1-6 -alkylsulphonyloxy, nitro, azido, sulphanyl, C 1-6 -alkylthio, halogen, DNA intercalators, photochemically active groups, thermochemically active groups, chelating groups, reporter groups, and ligands, where aryl and heteroaryl may be optionally substituted, and where two geminal substituents together may designate oxo, thioxo, imino, or optionally substituted methylene, or together may form a spiro biradical consisting of a 1–5 carbon atoms(s) alkylene chain which is optionally interrupted and/or terminated by one or more heteroatoms/groups selected from —O—, —S—, and —(NR N )— where R N is selected from hydrogen and C 1-4 -alkyl, and where two adjacent (non-geminal) substituents may designate an additional bond resulting in a double bond; and R N* , when present is selected from hydrogen and C 1-4 -alkyl; and basic salts and acid addition salts thereof.