IP Library Granted Patent US 7,759,319
Granted Patent B2
US 7,759,319 · App. 11/329,992 · Granted Jul 20, 2010

Oligomeric compounds and compositions for use in modulation of pri-mirnas

Assignee: Regulus Therapeutics Inc.
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Quick Facts
Patent No.
US 7,759,319
App. No.
11/329,992
Granted
Jul 20, 2010
Kind
B2
Abstract

Compounds, compositions and methods are provided for modulating the levels expression, processing and function of pri-miRNAs. In particular, methods and compounds are provided for the modulation of the levels, expression, processing or function of polycistronic pri-miRNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs and pri-miRNAs. Further provided are methods for selectively modulating pri-miRNA levels in a cell. Also provided are methods for identifying oligomeric compounds that result in increase pri-miRNA levels when contacted with a cell.

Claims (22)

1. A method of increasing the amounts of pri-miR-15 and pri-miR-16 in a cell comprising:

contacting the cell with an oligomeric compound comprising an oligonucleotide consisting of 15 to 30 linked nucleosides and having a nucleobase sequence at least 90% complementary to a target region within nucleobases 257 to 308 of SEQ ID NO: 102, whereby the amounts of pri-miR-15 and pri-miR-16 in the cell are increased.

2. The method of claim 1 wherein the nucleobase sequence of the oligonucleotide is at least 95% complementary to a target region within nucleotides 257 to 308 of SEQ ID NO: 102.

3. The method of claim 1 wherein the nucleobase sequence of the oligonucleotide is 100% complementary to a target region within nucleobases 257 to 308 of SEQ ID NO 102.

4. The method of claim 1 wherein the oligonucleotide consists of 17 to 25 linked nucleosides.

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

6. The method of claim 1 wherein at least one nucleoside of the oligonucleotide comprises a sugar modification.

7. The method of claim 6 wherein each nucleoside of the oligonucleotide comprises a sugar modification.

8. The method of claim 7 wherein the sugar modification is 2′-O-methoxyethyl.

9. The method of claim 1 wherein at least one internucleoside linkage is a modified internucleoside linkage.

10. The method of claim 1 wherein each internucleoside linkage is a modified internucleoside linkage.

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

12. The method of claim 1 wherein the oligonucleotide comprises at least one cytosine, wherein the cytosine is a 5-methylcytosine.

13. The method of claim 12 wherein each cytosine is a 5-methylcytosine.

14. The method of claim 1 wherein the oligonucleotide has a nucleobase sequence selected from the group consisting of SEQ ID NOs 92, 93, 94, and 95.

15. A method of increasing the amounts of pri-miR-15 and pri-miR-16 in a cell comprising:

contacting the cell with an oligonucleotide consisting of 17 to 25 linked nucleosides and having a nucleobase sequence at least 90% complementary to a target region within nucleobases 257 to 308 of SEQ ID NO: 102, whereby the amounts of pri-miR-15 and pri-miR-16 in the cell are increased.

16. The method of claim 15 wherein each nucleoside comprises a sugar modification.

17. The method of claim 15 wherein each nucleoside comprises a 2′-O-methoxyethyl sugar modification.

18. The method of claim 17 wherein each internucleoside linkage is a phosphorothioate internucleoside linkage.

19. The method of claim 18 wherein the oligonucleotide comprises at least one cytosine and the cytosine is a 5-methylcytosine.

20. The method of claim 19 wherein the oligonucleotide has a nucleobase sequence selected from the group consisting of SEQ ID NOs 92, 93, 94, and 95.

Assignments (6)
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 →
CHANGE OF NAME Recorded Feb 12, 2009
From: REGULUS THERAPEUTICS, LLC
To: REGULUS THERAPEUTICS, INC.
Reel/Frame 022260/0041 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 8, 2007
From: ISIS PHARMACEUTICALS, INC.
To: REGULUS THERAPEUTICS, LLC
Reel/Frame 020085/0730 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 2, 2006
From: LOLLO, BRIDGET; JAIN, RAVI
To: ISIS PHARMACEUTICALS, INC.
Reel/Frame 017245/0001 →
Continuity (7)
Continuation In Part 1090912500 · Jul 30, 2004
Provisional Application 6049205600 · Jul 31, 2003
Provisional Application 6051630300 · Oct 31, 2003
Provisional Application 6053159600 · Dec 19, 2003
Provisional Application 6056241700 · Apr 14, 2004
Provisional Application 6064280700 · Jan 10, 2005
Related Publication 20060252722A1 · Nov 9, 2006