IP Library Granted Patent US 8,946,179
Granted Patent B2
US 8,946,179 · App. 13/412,307 · Granted Feb 3, 2015

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.
C12N15/113C12N15/111C12N2310/113C12N2310/14C12N2310/315C12N2310/317C12N2310/3181C12N2310/321C12N2310/341C12N2310/346C12N2320/11C12N2320/50
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Quick Facts
Patent No.
US 8,946,179
App. No.
13/412,307
Granted
Feb 3, 2015
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 (30)

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

contacting an animal having or predisposed to the disease or 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;

thereby treating or preventing the disease or disorder;

wherein the disease or disorder is selected from cancer, diabetic retinopathy, cardiovascular disease, rheumatoid arthritis, and psoriasis, and wherein the oligomeric compound inhibits or reduces one or more markers of angiogenesis selected from integrin beta3 expression, endoglin expression, TEM5 expression, MMP14 expression, MMP activity, and endothelial tube formation.

2. The method of claim 1 wherein the microRNA is selected from miR-29a, miR-30b, miR-123/126as, miR-133b, miR-183, miR-187, miR-192, miR-210, miR-217, miR-220, and miR-222.

3. The method of claim 2 , wherein the oligomeric compound is at least 95% complementary to the microRNA.

4. The method of claim 2 , wherein the oligomeric compound is 100% complementary to the microRNA.

5. The method of claim 2 , wherein the oligomeric compound is 100% complementary to at least an 8-nucleobase portion of the microRNA.

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

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

8. The method of claim 7 , 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.

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

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

11. A method of inhibiting angiogenesis 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 or a nucleoside mimetic;

wherein the oligomeric compound inhibits or reduces one or more markers of angiogenesis selected from integrin beta3 expression, endoglin expression, TEM5 expression, MMP14 expression, MMP activity, and endothelial tube formation;

thereby inhibiting angiogenesis.

12. The method of claim 11 , wherein the method further comprises detecting a change in one or more markers of angiogenesis.

13. The method of claim 11 wherein the microRNA is selected from miR-29a, miR-30b, miR-123/126as, miR-133b, miR-183, miR-187, miR-192, miR-210, miR-217, miR-220, and miR-222.

14. The method of claim 13 , wherein the oligomeric compound is at least 95% complementary to the microRNA.

15. The method of claim 13 , wherein the oligomeric compound is 100% complementary to the microRNA.

16. The method of claim 13 , wherein the oligomeric compound is 100% complementary to at least an 8-nucleobase portion of the microRNA.

17. The method of claim 11 , wherein the oligomeric compound consists of an oligonucleotide.

18. The method of claim 11 , wherein at least one monomeric subunit comprises a modified sugar moiety.

19. The method of claim 18 , 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.

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

21. The method of claim 20 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 Jun 28, 2012
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
To: ISIS PHARMACEUTICALS INC.
Reel/Frame 028459/0194 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 28, 2012
From: ISIS PHARMACEUTICALS INC.
To: REGULUS THERAPEUTICS, LLC
Reel/Frame 028459/0229 →
CHANGE OF NAME Recorded Jun 28, 2012
From: REGULUS THERAPEUTICS, LLC
To: REGULUS THERAPEUTICS INC.
Reel/Frame 028459/0541 →
Continuity (7)
Division 12345891 · Dec 30, 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 20120157514A1 · Jun 21, 2012