IP Library Granted Patent US 9,447,412
Granted Patent B2
US 9,447,412 · App. 14/011,808 · Granted Sep 20, 2016

Oligomeric compounds and compositions for use in modulation of small non-coding RNAS

Inventors: Bridget Gordon (Encinitas, CA); C. Frank Bennett (Carlsbad, CA); Susan M. Freier (San Diego, CA); Richard H. Griffey (Vista, CA); Eric E. Swayze (Carlsbad, CA); Ravi Jain (Carlsbad, CA); Balkrishen Bhat (Carlsbad, CA)
Assignee: Regulus Therapeutics Inc.
C12N15/113C12N15/111C12N2310/11C12N2310/113C12N2310/14C12N2310/31C12N2310/315C12N2310/317C12N2310/3181C12N2310/32C12N2310/321C12N2310/3231C12N2310/3341C12N2310/341C12N2310/346C12N2310/351C12N2310/3515C12N2320/11C12N2320/30C12N2320/50
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Quick Facts
Patent No.
US 9,447,412
App. No.
14/011,808
Granted
Sep 20, 2016
Kind
B2
Abstract

Compounds, compositions and methods are provided for modulating the expression and function of small non-coding RNAs. The compositions comprise oligomeric compounds, targeted to small non-coding RNAs. Methods of using these compounds for modulation of small non-coding RNAs as well as downstream targets of these RNAs and for diagnosis and treatment of disease associated with small non-coding RNAs are also provided.

Claims (17)

1. A method of mimicking miR-16 in a cell comprising contacting the cell with a compound comprising a first oligomeric compound and a second oligomeric compound, wherein:

a) the first oligomeric compound consists of 15 to 30 monomeric subunits and is at least 90% identical to the sequence of miR-16 (SEQ ID NO: 196); and

b) the second oligomeric compound consists of 15 to 30 monomeric subunits and is complementary to the first oligomeric compound, and

c) at least one monomeric subunit of the second oligomeric compound is a modified nucleoside.

2. The method of claim 1 , wherein the compound induces apoptosis in the cell.

3. The method of claim 2 , wherein the cell is in vivo.

4. The method of claim 2 , wherein the cell is in vitro.

5. The method of claim 1 , wherein the first oligomeric compound is at least 95% identical to the sequence of miR-16 (SEQ ID NO: 196).

6. The method of claim 1 , wherein the first oligomeric compound and/or the second oligomeric compound comprises a 5′-terminal modification.

7. The method of claim 1 , wherein the second oligomeric compound comprises a 5′-terminal modification.

8. The method of claim 7 , wherein the 5′-terminal modification is a 5′-modified phosphate.

9. The method of claim 1 , wherein the first oligomeric compound and/or the second oligomeric compound comprises a two-nucleobase overhang at the 3′ end.

10. The method of claim 9 , wherein the first oligomeric compound and the second oligomeric compound each comprises a two-nucleobase overhang at the 3′ end.

11. The method of claim 1 , wherein the second oligomeric compound comprises at least one modified sugar moiety.

12. The method of claim 11 , wherein at least one modified sugar moiety is selected from 2′-F, 2′-O-methyl, 2′-O-methoxyethyl, and a bicyclic sugar moiety.

13. The method of claim 1 , wherein the second oligomeric compound comprises at least one modified internucleoside linkage.

14. The method of claim 13 , wherein at least one modified internucleoside linkage is a phosphorothioate linkage.

Assignments (2)
RELEASE OF SECURITY INTEREST Recorded May 14, 2024
From: OXFORD FINANCE LLC, AS COLLATERAL AGENT AND LENDER
To: REGULUS THERAPEUTICS INC.
Reel/Frame 067402/0782 →
SECURITY INTEREST Recorded Aug 8, 2018
From: REGULUS THERAPEUTICS INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT AND LENDER
Reel/Frame 046748/0561 →
Continuity (8)
Continuation 13359271 · Jan 26, 2012
Continuation 12346940 · Dec 31, 2008
Division 10909125 · Jul 30, 2004
Provisional Application 60492056 · Jul 31, 2003
Provisional Application 60516303 · Oct 31, 2003
Provisional Application 60531596 · Dec 19, 2003
Provisional Application 60562417 · Apr 14, 2004
Related Publication 20140057963A1 · Feb 27, 2014