IP Library Granted Patent US 8,133,876
Granted Patent B2
US 8,133,876 · App. 12/345,891 · Granted Mar 13, 2012

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

Assignee: Regulus Therapeutics Inc.
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Quick Facts
Patent No.
US 8,133,876
App. No.
12/345,891
Granted
Mar 13, 2012
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 (26)

1. A method of treating or preventing a disease or disorder associated with a microRNA comprising:

contacting an animal having or predisposed to the disorder with a therapeutically effective amount of compound comprising an oligomeric compound consisting of 15 to 30 monomeric subunits,

wherein the oligomeric compound is at least 90% complementary to the microRNA, and at least one monomeric subunit is a modified nucleoside;

and thereby treating or preventing the disease or disorder;

wherein the disease or disorder is diabetes or hypertension, and the oligomeric compound reduces one or more markers of insulin response.

2. A method of modulating one or more phenotypic outcomes comprising:

contacting a cell with a compound comprising an oligomeric compound consisting of 15 to 30 monomeric subunits,

wherein the oligomeric compound is at least 90% complementary to a microRNA, and

wherein at least one monomeric subunit is a modified nucleoside;

and thereby modulating one or more phenotypic outcomes;

wherein the one or more phenotypic outcomes is insulin response, and wherein the method further comprises detecting the modulation by a change in one or more markers of insulin response.

3. The method of claim 2 wherein the one or more markers of insulin response is selected from insulin-like growth factor binding protein-1 (IGFBP-1) expression, cytosolic PEPCK (PEPCK-C) expression, and follistatin expression.

4. The method of claim 1 wherein the microRNA is a let-7 homolog.

5. The method of claim 4 , wherein the oligomeric compound is at least 95% complementary to a let-7homolog.

6. The method of claim 4 , wherein the oligomeric compound is 100% complementary to a let-7homolog.

7. The method of claim 4 , wherein the oligomeric compound is 100% complementary to at least an 8-nucleobase portion of let-7homolog.

8. The method of claim 1 , wherein the oligomeric compound consists of an oligonucleotide.

9. The method of claim 1 , wherein at least one monomeric subunit comprises a modified sugar moiety.

10. The method of claim 9 , wherein the modified sugar moiety is selected from a 2′-F sugar moiety, a 2′-O-methyl sugar moiety, a 2′-O-methoxyethyl sugar moiety, and a bicyclic sugar moiety.

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

12. The method of claim 11 wherein the modified internucleoside linkage is a phosphorothioate linkage.

13. The method of claim 2 , wherein the oligomeric compound consists of an oligonucleotide.

14. The method of claim 2 , wherein at least one monomeric subunit comprises a modified sugar moiety.

15. The method of claim 14 , wherein the modified sugar moiety is selected from a 2′-F sugar moiety, a 2′-O-methyl sugar moiety, a 2′-O-methoxyethyl sugar moiety, and a bicyclic sugar moiety.

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

17. The method of claim 16 wherein the modified internucleoside linkage is a phosphorothioate linkage.

Assignments (5)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2010
From: ESAU, CHRISTINE; LOLLO, BRIDGET; BENNETT, C. FRANK; FREIER, SUSAN M.; GRIFFEY, RICHARD H.; BAKER, BRENDA F.; VICKERS, TIMOTHY A.; MARCUSSON, ERIC G.; KOLLER, ERICH; SWAYZE, ERIC E.; JAIN, RAVI; BHAT, BALKRISHEN; PERALTA, EIGEN R.
To: ISIS PHARMACEUTICALS, INC.
Reel/Frame 024361/0782 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2010
From: ISIS PHARMACEUTICALS, INC.
To: REGULUS THERAPEUTICS, LLC
Reel/Frame 024361/0870 →
CHANGE OF NAME Recorded May 10, 2010
From: REGULUS THERAPEUTICS, LLC
To: REGULUS THERAPEUTICS INC.
Reel/Frame 024362/0224 →
Continuity (6)
Continuation 10909125 · Jul 30, 2004
Provisional Application 60562417 · Apr 14, 2004
Provisional Application 60531596 · Dec 19, 2003
Provisional Application 60516303 · Oct 31, 2003
Provisional Application 60492056 · Jul 31, 2003
Related Publication 20090291907A1 · Nov 26, 2009