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Oligonucleotide analogues

  • US 6,794,499 B2
  • Filed: 09/11/1998
  • Issued: 09/21/2004
  • Est. Priority Date: 09/12/1997
  • Status: Expired due to Term
First Claim
Patent Images

1. An oligomer comprising at least one LNA nucleoside of the general formula I embedded imagewhereinX is selected from —

  • O—

    ;

    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 5′

    -terminal group, such internucleoside linkage or 5′

    -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 3′

    -terminal group, one pair of non-geminal substituents R4*, and R2*, designating a biradical consisting of 2-5 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—

    , 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 —

    O—

    , —

    S—

    , 0 (zero) or —

    N(RN)—

    , 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 —

    (CR*R*)r—

    Y—

    (CR*R*)s—

    , then Y is —

    S—

    or —

    N(RN′

    )—

    ; 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.

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