IP Library Patent Application 14630477
Patent Application
App. No. 14/630,477

POLYMERIC CARRIER

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Quick Facts
Patent No.
US None
App. No.
14/630,477
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 (47)

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—;

each of Y 0 and 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 1 S—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;

each of R 1 , R 2 , R 3 , and R 5 is (1C-5C)alkyl;

R 4 is —CH 2 CH 2 CH 3 ;

Q 0 is a residue selected from the group consisting of polyoxylated alkyl, polyethylene glycol, and polypropylene glycol;

Q 1 is a residue selected from the group consisting of amino, alkylamino, ammonium, alkylammonium, and guanidine;

Q 2 is a dimethylamino residue;

Q 3 is a carboxyl residue;

m is 0 to less than 1.0;

n is greater than 0 to 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 Q 0 is a polyethylene glycol residue.

3 . The polymeric carrier of claim 1 , wherein Q 1 is an alkylamino residue.

4 . The polymeric carrier of claim 3 , wherein Q 1 is a dimethylamino residue.

5 . The polymeric carrier of claim 1 , wherein

Y 0 is —C(O)OCH 2 CH 2 —; and

R 1 is —CH 3 .

6 . The polymeric carrier of claim 1 , wherein

Y 1 is —C(O)OCH 2 CH 2 —; and

R 2 is —CH 3 .

7 . The polymeric carrier of claim 1 , wherein R 3 is —CH 3 .

8 . The polymeric carrier of claim 1 , wherein R 5 is —CH 3 .

9 . The polymeric carrier of claim 1 , wherein m is 0.

10 . The polymeric carrier of claim 9 , wherein Q 1 is an alkylamino residue.

11 . The polymeric carrier of claim 10 , wherein Q 1 is a dimethylamino residue.

12 . The polymeric carrier of claim 1 , wherein the polynucleotide is an oligonucleotide.

13 . The polymeric carrier of claim 12 , wherein the polynucleotide is an siRNA.

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

15 . The polymeric carrier of claim 14 , wherein the targeting moiety is attached to the shell portion by a covalent bond to a polymer.

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

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

18 . The polymeric carrier of claim 1 , wherein w is 5 to 50 kDa.

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

20 . A method for intracellular delivery of a polynucleotide to a cell, the method comprising contacting a cell with the polymeric carrier of claim 1 .

Assignments (3)
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 →