US2018195062A1PendingUtilityA1

Pharmaceutical Composition

Assignee: ROCHE INNOVATION CT COPENHAGEN ASPriority: Apr 3, 2006Filed: Sep 13, 2017Published: Jul 12, 2018
Est. expiryApr 3, 2026(expired)· nominal 20-yr term from priority
A61P 3/06A61P 43/00A61P 9/10A61P 37/02A61P 35/02A61P 3/10A61P 3/00A61P 25/00A61P 31/14A61P 31/04A61P 31/12A61P 35/00A61P 29/00C12N 15/113C12N 2310/321C12N 2310/322C12N 2310/113A61P 15/00C12N 2310/3231C12N 2310/3515A61P 21/00A61P 11/00A61P 1/16C12N 2310/3533C12N 2310/3521C12N 15/11A61K 48/00
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Claims

Abstract

The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 17 nucleobases which are complementary to human microRNAs. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical composition comprising a single stranded oligonucleotide, or a conjugate of said oligonucleotide, having a length of between 8 and 17 nucleobase units, and a pharmaceutically acceptable diluent, carrier, or adjuvant; wherein at least one of the nucleobase units of the single stranded oligonucleotide is a Locked Nucleic Acid (LNA) nucleobase unit, and wherein the single stranded oligonucleotide is complementary to a human microRNA sequence. 
     
     
         2 .- 95 . (canceled)

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