IP Library Granted Patent US 10,941,404
Granted Patent B2
US 10,941,404 · App. 17/012,524 · Granted Mar 9, 2021

Treatment of angiopoietin like 7 (ANGPTL7) related diseases

Inventors: Omri Gottesman (San Diego, CA); Shannon Bruse (San Diego, CA); Paul Buske (Madison, WI); Brian Cajes (San Diego, CA); David Lewis (Madison, WI); David Rozema (Cross Plains, WI)
Assignee: EMPIRICO INC.
C12N15/1136A61P27/06C12N2310/14C12N2310/315C12N2310/321C12N2310/322C12N2310/3515
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Quick Facts
Patent No.
US 10,941,404
App. No.
17/012,524
Granted
Mar 9, 2021
Kind
B2
Abstract

Provided herein are oligonucleotide compositions that inhibit ANGPTL7 and reduce intraocular pressure when administered to an eye. The oligonucleotide compositions contain nucleoside modifications.

Claims (22)

1. A composition comprising an oligonucleotide that targets Angiopoietin like 7 (ANGPTL7) and when administered to a cell decreases expression of ANGPTL7, wherein the oligonucleotide comprises a small interfering RNA (siRNA) comprising a sense strand and an antisense strand, wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NOs: 1424, 1541, or 2091 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, or an oligonucleotide sequence comprising 1 or 2 nucleoside substitutions, additions, or deletions of SEQ ID NOs: 1424, 1541, or 2091 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, and wherein the antisense strand comprises an oligonucleotide sequence of SEQ ID NOs: 3630, 3747, or 4297 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, or an oligonucleotide sequence comprising 1 or 2 nucleoside substitutions, additions, or deletions of SEQ ID NOs: 3630, 3747, or 4297 in which at least one internucleoside linkage is modified and at least one nucleoside is modified.

2. The composition of claim 1 , wherein the at least one nucleoside is modified comprises a 2′-fluoro modified nucleoside.

3. The composition of claim 1 , wherein the at least one nucleoside is modified comprises a 2′-O-methyl modified nucleoside.

4. The composition of claim 1 , wherein the oligonucleotide comprises 15-23 modified nucleosides.

5. The composition of claim 4 , wherein the 15-23 modified nucleosides comprises 2′-fluoro modified nucleosides and 2′-O-methyl modified nucleosides.

6. The composition of claim 1 , wherein the at least one internucleoside linkage is modified comprises a phosphorothioate linkage.

7. The composition of claim 1 , wherein the oligonucleotide comprises a lipid attached at a 3′ or 5′ terminus of the oligonucleotide.

8. The composition of claim 7 , wherein the lipid comprises cholesterol, myristoyl, palmitoyl, stearoyl, lithocholoyl, docosanoyl, docosahexaenoyl, myristyl, palmityl stearyl, or a-tocopherol, or a combination thereof.

9. The composition of claim 8 , wherein the lipid is attached to the 3′ terminus of the sense strand.

10. The composition of claim 9 , wherein the lipid comprises cholesterol.

11. The composition of claim 10 , wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NO: 11186 and the antisense strand comprises an oligonucleotide sequence of SEQ ID NO: 11306.

12. The composition of claim 10 , wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NO: 11200 and the antisense strand comprises an oligonucleotide sequence of SEQ ID NO: 11320.

13. The composition of claim 10 , wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NO: 11211 and the antisense strand comprises an oligonucleotide sequence of SEQ ID NO: 11331.

14. A pharmaceutical composition comprising

(a) an oligonucleotide that targets Angiopoietin like 7 (ANGPTL7) and when administered to a cell decreases expression of ANGPTL7, wherein the oligonucleotide comprises a small interfering RNA (siRNA) comprising a sense strand and an antisense strand, wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NOs: 1424, 1541, or 2091 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, or an oligonucleotide sequence comprising 1 or 2 nucleoside substitutions, additions, or deletions of SEQ ID NOs: 1424, 1541, or 2091 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, and wherein the antisense strand comprises an oligonucleotide sequence of SEQ ID NOs: 3630, 3747, or 4297 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, or an oligonucleotide sequence comprising 1 or 2 nucleoside substitutions, additions, or deletions of SEQ ID NOs: 3630, 3747, or 4297 in which at least one internucleoside linkage is modified and at least one nucleoside is modified; and

(b) a pharmaceutically acceptable carrier.

15. A composition comprising an oligonucleotide that targets Angiopoietin like 7 (ANGPTL7) and when administered to a subject in an effective amount decreases intraocular pressure, wherein the oligonucleotide comprises a small interfering RNA (siRNA) comprising a sense strand and an antisense strand, the antisense strand being complementary to a portion of a nucleic acid having the nucleoside sequence of SEQ ID NO: 11085, and each strand having 14 to 30 nucleotides, wherein the oligonucleotide comprises a lipid attached at a 3′ or 5′ terminus of the oligonucleotide, wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NOs: 1424, 1541, or 2091 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, or an oligonucleotide sequence comprising 1 or 2 nucleoside substitutions, additions, or deletions of SEQ ID NOs: 1424, 1541, or 2091 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, and wherein the antisense strand comprises an oligonucleotide sequence of SEQ ID NOs: 3630, 3747, or 4297 in which at least one internucleoside linkage is modified and at least one nucleoside is modified, or an oligonucleotide sequence comprising 1 or 2 nucleoside substitutions, additions, or deletions of SEQ ID NOs: 3630, 3747, or 4297 in which at least one internucleoside linkage is modified and at least one nucleoside is modified.

16. The composition of claim 15 , wherein the lipid is attached to the 3′ terminus of the sense strand.

17. The composition of claim 16 , wherein the lipid comprises cholesterol.

18. The composition of claim 17 , wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NO: 11186 and the antisense strand comprises an oligonucleotide sequence of SEQ ID NO: 11306.

19. The composition of claim 17 , wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NO: 11200 and the antisense strand comprises an oligonucleotide sequence of SEQ ID NO: 11320.

20. The composition of claim 17 , wherein the sense strand comprises an oligonucleotide sequence of SEQ ID NO: 11211 and the antisense strand comprises an oligonucleotide sequence of SEQ ID NO: 11331.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 29, 2020
From: GOTTESMAN, OMRI; BRUSE, SHANNON; BUSKE, PAUL; CAJES, BRIAN; LEWIS, DAVID; ROZEMA, DAVID
To: EMPIRICO INC.
Reel/Frame 054762/0822 →
Continuity (4)
Continuation PCTUS2020034063 · May 21, 2020
Provisional Application 62852813 · May 24, 2019
Provisional Application 62881906 · Aug 1, 2019
Related Publication 20200399640A1 · Dec 24, 2020
Cited By (2)
US 12,378,556 US 12,582,104