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Amine-derivatized nucleosides and oligonucleosides

  • US 6,900,297 B1
  • Filed: 06/05/1995
  • Issued: 05/31/2005
  • Est. Priority Date: 01/11/1990
  • Status: Expired due to Term
First Claim
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1. A compound which hybridizes with a nucleic acid and comprises a plurality of linked nucleosides, wherein:

  • each nucleoside includes a pentofuranosyl sugar portion and a base portion; and

    at least one of said nucleosides bears at a 2′

    -O-position, a 3′

    -O-position, or a 5′

    -O-position of said pentofuranosyl sugar, a terminal substituent having formula;




    RA

    N(R1a)(R1b) where;

    RA is alkyl having from 1 to about 10 carbon atoms or (CH2

    CH2

    Q)x;

    R1a and R1b, independently, are H, R2, or an amine protecting group or have formula C(X)—

    R2, C(X)—

    RA

    R2, C(X)—

    Q—

    RA

    R2, C(X)—

    Q—

    R2; and

    R2 is a peptide;

    X is O or S;

    each Q is, independently, is NH, O, or S; and

    x is 1 to about 200.

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