Boronic acid conjugates of oligonucleotide analogs

Boronic acid conjugates of oligonucleotide analogs

  • CN 104,411,831 B
  • Filed: 03/07/2013
  • Issued: 08/11/2020
  • Est. Priority Date: 03/20/2012
  • Status: Active Grant
First Claim
Patent Images

1. An oligonucleotide analog comprising a backbone, a 3 '"'"'end, and a 5'"'"' end, the backbone comprising a sequence of morpholine ring structures joined by intersubunit linkages joining the 3 '"'"'end of one morpholine ring structure to the 5'"'"' end of an adjacent morpholine ring structure, wherein each morpholine ring structure is joined to a base pairing moiety such that the oligonucleotide analog can bind to a target nucleic acid in a sequence specific manner, wherein at least one of the intersubunit linkages, the 3 '"'"'end, or the 5'"'"' end comprises a boronic acid or boronic ester moiety covalently bound thereto, wherein the boronic acid or boronic ester moiety independently at each occurrence has one of the following structures (I) or (II):

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