IP Library Granted Patent US 9,006,193
Granted Patent B2
US 9,006,193 · App. 12/992,536 · Granted Apr 14, 2015

Polymeric carrier

Inventors: Patrick S. Stayton (Seattle, WA); Allan S. Hoffman (Seattle, WA); Anthony J. Convertine (Seattle, WA); Craig L. Duvall (Nashville, TN); Danielle Benoit (Rochester, NY); Robert W. Overell (Shoreline, WA); Paul H. Johnson (Snohomish, WA); Anna S. Gall (Woodinville, WA); Mary G. Prieve (Lake Forest Park, WA); Amber E. E. Paschal (Redmond, WA); Charbel Diab (Seattle, WA); Priyadarsi De (Mohanpur, IN)
Assignees: University of Washington; PhaseRx, Inc.
C12N15/87A61K9/1075A61K47/48092A61K47/48176A61K47/48215C08F293/005
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Quick Facts
Patent No.
US 9,006,193
App. No.
12/992,536
Granted
Apr 14, 2015
Kind
B2
Abstract

Provided herein are polymeric carriers suitable for the delivery of polynucleotides (e.g. oligonucleotides) and/or other therapeutic agents into a living cell.

Claims (40)

1. A polymeric carrier comprising:

(a) a plurality of polymers that are block copolymers assembled into a polymeric carrier, the polymeric carrier comprising a core and a shell, the block copolymers having the chemical Formula I:

wherein

each of A 0 , A 1 , A 2 , A 3 and A 4 is —C—C—;

Y 0 is —C(O)O(1C-10C)alkyl-, optionally substituted with one or more fluorine groups;

Y 1 is —C(O)O(2C-10C)alkyl-;

Y 2 is —C(O)OCH 2 CH 2 —;

Y 3 is a covalent bond;

Y 4 is —C(O)O(CH 2 ) 3 CH 3 ;

wherein tetravalent carbon atoms of A 0 -A 4 that are not fully substituted with R 1 -R 5 and Y 0 -Y 4 are completed with an appropriate number of hydrogen atoms;

R 1 is (1C-3C)alkyl;

each of R 2 , R 3 , and R 5 is —CH 3 ;

R 4 is —CH 2 CH 2 CH 3 ;

Q 0 is a pyridyl disulfide residue;

Q 1 is a residue selected from the group consisting of polyoxylated alkyl, polyethylene glycol, and polypropylene glycol;

Q 2 is a dimethylamino residue;

Q 3 is a carboxyl residue;

m is greater than 0 to less than 1.0;

n is greater than 0 to less than 1.0, wherein m+n=1;

p is 0.1 to 0.9;

q is 0.1 to 0.9;

r is 0 to 0.8 wherein p+q+r=1;

v is 1 to 25 kDa; and

w is 1 to 50 kDa; and

(b) at least one polynucleotide,

wherein the polynucleotide is not in the core of the polymeric carrier.

2. The polymeric carrier of claim 1 , wherein the at least one polynucleotide is an oligonucleotide.

3. The polymeric carrier of claim 1 , further comprising a targeting moiety.

4. The polymeric carrier of claim 1 , wherein the targeting moiety is attached to the shell portion by a covalent bond to a polymer.

5. The polymeric carrier of claim 1 , wherein the plurality of polymers have spontaneously self-assembled into the polymeric carrier.

6. The polymeric carrier of claim 1 , wherein the shell of the polymeric carrier comprises the polynucleotide.

7. The polymeric carrier of claim 1 , wherein the at least one polynucleotide is attached to the block copolymer by a covalent bond, a non-covalent interaction, or a combination thereof.

8. The polymeric carrier of claim 1 , wherein the polynucleotide is an siRNA.

9. A composition comprising the polymeric carrier of claim 1 .

10. The polymeric carrier of claim 1 , wherein Q 1 is a polyethylene glycol residue.

11. The polymeric carrier of claim 1 , wherein

Y 1 is —C(O)OCH 2 CH 2 —.

12. The polymeric carrier of claim 1 , wherein

Y 0 is —C(O)OCH 2 CH 2 —.

13. The polymeric carrier of claim 1 , wherein v is 5 to 25 kDa.

Assignments (7)
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Apr 3, 2020
From: GENEVANT SCIENCES LTD.
To: ROIVANT SCIENCES LTD.
Reel/Frame 052312/0930 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2018
From: PHASERX, INC.
To: ROIVANT HEPATOLOGY GMBH
Reel/Frame 047649/0829 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2018
From: ROIVANT HEPATOLOGY GMBH
To: GENEVANT SCIENCES GMBH
Reel/Frame 047689/0406 →
CORRECTIVE ASSIGNMENT TO CORRECT THE MISSPELLING OF INVENTOR PASCHAL'S LAST NAME IN THE RECORDATION COVER SHEET FROM <PASCAL> TO <PASCHAL> PREVIOUSLY RECORDED ON REEL 025816 FRAME 0234. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT OF THEIR APPLICATION NO. 12/992,536, FILED FEBRUARY 25, 2011, TO PHASERX, INC.. Recorded Apr 13, 2011
From: OVERELL, ROBERT W.; JOHNSON, PAUL H.; GALL, ANNA S.; PRIEVE, MARY G.; PASCHAL, AMBER E.E.; DIAB, CHARBEL; DE, PRIYADARSI
To: PHASERX, INC.
Reel/Frame 026122/0357 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 16, 2011
From: OVERELL, ROBERT W.; JOHNSON, PAUL H.; GALL, ANNA S.; PRIEVE, MARY G.; PASCAL, AMBER E.E.; DIAB, CHARBEL; DE, PRIYADARSI
To: PHASERX, INC.
Reel/Frame 025816/0234 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 16, 2011
From: STAYTON, PATRICK S.; HOFFMAN, ALLAN S.; CONVERTINE, ANTHONY J.; DUVALL, CRAIG L.; BENOIT, DANIELLE
To: WASHINGTON, UNIVERSITY OF
Reel/Frame 025816/0135 →
CONFIRMATORY LICENSE Recorded Dec 1, 2010
From: UNIVERSITY OF WASHINGTON, CENTER FOR COMMERCIALIZATION
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 025433/0942 →
Continuity (7)
Provisional Application 61052914 · May 13, 2008
Provisional Application 61052908 · May 13, 2008
Provisional Application 61091294 · Aug 22, 2008
Provisional Application 61112054 · Nov 6, 2008
Provisional Application 61140779 · Dec 24, 2008
Provisional Application 61171358 · Apr 21, 2009
Related Publication 20110143435A1 · Jun 16, 2011