Patent ID: 6794499
Filing Date: 2004-09-21
Classification: C07H

Abstract:
An oligomer comprising at least one LNA nucleoside of the general formula I whereinX is selected from â€”Oâ€”; B is selected from hydrogen, hydroxy, optionally substituted C1-4-alkoxy, optionally substituted C1-4-alkyl, optionally substituted C1-4-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 5â€²-terminal group, such internucleoside linkage or 5â€²-terminal group optionally including the substituent R5; one of the substituents R2, R2*, R3, and R3* is a group P* which designates an internucleoside linkage to a preceding monomer, or a 3â€²-terminal group, one pair of non-geminal substituents R4*, and R2*, designating a biradical consisting of 2-5 groups/atoms selected from â€”(CR*R*)râ€”Yâ€”(CR*R*)sâ€”, â€”(CR*R*)râ€”Yâ€”(CR*R*)sâ€”Yâ€”, â€”Yâ€”(CR*R*)r+sâ€”Yâ€”, â€”Yâ€”(CR*R*)râ€”Yâ€”(CR*R*)sâ€”, â€”(CR*R*)r+sâ€”, each R* is independently selected from hydrogen, halogen, hydroxy, mercapto, amino, optionally substituted C1-6-alkoxy, optionally substituted C1-6-alkyl, DNA intercalators, photochemically active groups, thermochemically active groups, chelating groups, reporter groups, and ligands, Y is â€”Oâ€”, â€”Sâ€”, 0 (zero) or â€”N(RN)â€”, and each of r and s is 0-4 with the proviso that the sum r+s is 1-4, and provided that when the biradical is â€”(CR*R*)râ€”Yâ€”(CR*R*)sâ€”, then Y is â€”Sâ€” or â€”N(RNâ€²)â€”; and each of the substituents R1*, R2, R3, R5, and R5*, which are present and not involved in P, P* is independently selected from hydrogen, optionally substituted C1-12-alkyl, optionally substituted C2-12-alkenyl, optionally substituted C2-12-alkynyl, hydroxy, C1-12-alkoxy, C2-12-alkenyloxy, carboxy, C1-12-alkoxycarbonyl, C1-12-alkylcarbonyl, formyl, aryl, aryloxy-carbonyl, aryloxy, arylcarbonyl, heteroaryl, heteroaryloxy-carbonyl, heteroaryloxy, heteroarycarbonyl, amino, mono- and di(C1-6-alkyl)amino, carbamoyl, mono- and di(C1-6-alkyl)-amino-carbonyl, amino-C1-6-alkyl-aminocarbonyl, mono- and di(C1-6-alkyl)amino-C1-6-alkyl-aminocarbonyl, C1-6-alkyl-carbonylamino, carbamido, C1-6-alkanoyloxy, sulphono, C1-6-alkylsulphonyloxy, nitro, azido, sulphanyl, C1-6-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 basic salts and acid addition salts thereof.