IP Library Granted Patent US 9,267,138
Granted Patent B2
US 9,267,138 · App. 14/705,580 · Granted Feb 23, 2016

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

Inventors: C. Frank Bennett (Carlsbad, CA); Susan M. Freier (San Diego, CA); Richard H. Griffey (Vista, CA)
Assignee: Regulus Therapeutics Inc.
C12N15/113C12N2310/315C12N2310/321C12N2310/3341C12N2310/351C12N2310/3515
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Quick Facts
Patent No.
US 9,267,138
App. No.
14/705,580
Granted
Feb 23, 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 (27)

1. A method of inhibiting the activity, function, or amount of miR-103 (SEQ ID NO: 225) and/or miR-107 (SEQ ID NO: 229), comprising contacting a cell with a compound comprising a modified oligonucleotide, wherein:

the modified oligonucleotide consists of 8, 9, 10, 11, or 12 linked monomeric subunits;

each monomeric subunit of the modified oligonucleotide comprises a modified sugar moiety; and

the modified oligonucleotide is complementary to miR-103 and/or miR-107 with no more than one mismatch.

2. The method of claim 1 wherein the modified oligonucleotide consists of 8 monomeric subunits.

3. The method of claim 1 wherein the modified oligonucleotide consists of 9 monomeric subunits.

4. The method of claim 1 wherein the modified oligonucleotide consists of 10 monomeric subunits.

5. The method of claim 1 wherein the modified oligonucleotide consists of 11 monomeric subunits.

6. The method of claim 1 wherein the modified oligonucleotide consists of 12 monomeric subunits.

7. The method of claim 1 , wherein each modified sugar moiety is independently selected from a 2′-F sugar moiety, a 2′-O-methyl sugar moiety, a 2′-O-methoxyethyl sugar moiety, and a bicyclic sugar moiety.

8. The method of claim 7 , wherein the bicyclic sugar moiety has a 4′-CH 2 —O-2′ bridge.

9. The method of claim 1 , wherein the modified oligonucleotide comprises at least one modified internucleoside linkage.

10. The method of claim 9 , wherein the modified internucleoside linkage is a phosphorothioate linkage.

11. The method of claim 1 , wherein each internucleoside linkage of the modified oligonucleotide is a phosphorothioate linkage.

12. The method of claim 1 , wherein the oligonucleotide comprises two or more chemically distinct regions.

13. The method of claim 12 , wherein the sugar moiety of each nucleoside of a first chemically distinct region is the same and is selected from a 2′-fluoro nucleoside, a 2′-O-methyl nucleoside, a 2′-O-methoxyethyl nucleoside, and a bicyclic sugar nucleoside.

14. The method of claim 13 , wherein the bicyclic nucleoside has a 4′-CH 2 —O-2′ bridge.

15. The method of claim 1 , wherein the oligonucleotide comprises at least one 5-methylcytosine.

16. The method of claim 1 , wherein the modified oligonucleotide is attached to a conjugate group.

17. The method of claim 16 , wherein the conjugate group is cholesterol.

18. The method of claim 16 , wherein the conjugate group comprises a carbohydrate.

19. The method of claim 1 , wherein each modified sugar moiety is a bicyclic sugar moiety.

20. The method of claim 19 , wherein each bicyclic sugar moiety has a 4′-CH 2 —O-2′ bridge.

21. The method of claim 1 , wherein the modified oligonucleotide is complementary to a target region comprising nucleobases 1 to 8 of miR-103 and/or miR-107.

22. The method of claim 1 , wherein the modified oligonucleotide is complementary to a target region comprising nucleobases 2 to 9 of miR-103 and/or miR-107.

23. The method of claim 1 , wherein the modified oligonucleotide is complementary to a target region comprising nucleobases 3 to 10 of miR-103 and/or miR107.

24. The method of claim 1 , wherein the contacting comprises administering the compound to a subject.

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 (10)
Division 14245535 · Apr 4, 2015
Division 13540097 · Jul 2, 2012
Division 13359271 · Jan 26, 2012
Continuation 12346940 · Dec 31, 2008
Continuation 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 20150337305A1 · Nov 26, 2015