IP Library Granted Patent US 11,684,584
Granted Patent B2
US 11,684,584 · App. 16/475,006 · Granted Jun 27, 2023

Branched peg molecules and related compositions and methods

Inventors: Debashish Roy (Seattle, WA); Jean-Rene E. Ella-Menye (Seattle, WA); Sean D. Monahan (Middleton, WI); Pierrot Harvie (Vancouver, CA); Anna Galperin (Seattle, WA); Michael E. Houston (Kirkland, WA); Mary G. Prieve (Lake Forest Park, WA)
Assignee: Genevant Sciences GmbH
A61K9/5123A61K38/1816A61K47/34A61K48/0041A61K49/0093
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Quick Facts
Patent No.
US 11,684,584
App. No.
16/475,006
Granted
Jun 27, 2023
Kind
B2
Abstract

Disclosed are branched PEG molecules, including branched PEG-lipids and branched-PEG proteins, as well as related compositions and methods for making branched PEG molecules. Also disclosed are related compositions, systems, and methods for in vivo delivery of therapeutic and diagnostic agents.

Claims (30)

1. A pH-sensitive polymer of Formula IXh:

GalNAc-C5-PEG 12 - [PEGMA300 0.75 —HMA 0.25 ] 4.2KDA -[DMAEMA 0.36 -PAA 0.13 -BMA 0.51 ]4.93KDa, wherein

GalNAc is an N-acetylgalactosamine residue;

C5 is an alkylene group containing 5 carbon atoms;

PEG 12 is a link moiety comprising a polyethylene glycol having 12 ethylene glycol units;

PEGMA300 is polyethyleneglycol methacrylate residue having 4-5 ethylene glycol units;

HMA is hexyl methacrylate residue;

DAEMA is dimethylaminoethyl methacrylate residue;

PAA is propyl acrylic acid residue; and

BMA is butyl methacrylate residue.

2. A composition comprising a pH-sensitive polymer of Formula IXh:

GalNAc-C5-PEG 12 - [PEGMA300 0.75 —HMA 0.25 ] 4.2KDa -[DMAEMA 0.36 -PAA 0.13 -BMA 0.51 ] 4.93KDa ; and

a therapeutic or diagnostic agent,

wherein

GalNAc is an N-acetylgalactosamine residue;

C5 is an alkylene group containing 5 carbon atoms;

PEG 12 is a link moiety comprising a polyethylene glycol having 12 ethylene glycol units;

PEGMA300 is polyethyleneglycol methacrylate residue having 4-5 ethylene glycol units;

HMA is hexyl methacrylate residue;

DAEMA is dimethylaminoethyl methacrylate residue;

PAA is propyl acrylic acid residue; and

BMA is butyl methacrylate residue.

3. The composition of claim 2 , wherein the therapeutic agent is a polynucleotide, a protein, or a peptide.

4. The composition of claim 3 , wherein the polynucleotide is an oligonucleotide.

5. The composition of claim 4 , wherein the oligonucleotide is an siRNA, an antisense oligonucleotide, an anti-miR, a locked nucleic acid-based oligonucleotide, a dicer substrate, an miRNA, an aiRNA, an shRNA, a ribozyme, or a nucleic acid aptamer.

6. The composition of claim 4 , wherein the oligonucleotide is an mRNA.

7. The composition of claim 6 , wherein the mRNA encodes a secreted protein.

8. The composition of claim 7 , wherein the secreted protein is a hormone, a cytokine, an growth factor, a clotting factor, an anti-protease protein, an angiogenic protein, an antiangiogenic protein, a chemokine, or an antibody.

9. A method for delivering a therapeutic or diagnostic agent to a subject, the method comprising: administering to a subject in need of thereof an effective amount of the composition of claim 2 .

10. The method of claim 9 , wherein the therapeutic agent is a polynucleotide, a protein, or a peptide.

Assignments (5)
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 Jan 21, 2020
From: ROY, DEBASHISH; ELLA-MENYE, JEAN-RENE E.; MONAHAN, SEAN D.; HARVIE, PIERROT; GALPERIN, ANNA; HOUSTON, MICHAEL E.; PRIEVE, MARY G.
To: PHASERX, INC.
Reel/Frame 051566/0358 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 21, 2020
From: ROY, DEBASHISH; ELLA-MENYE, JEAN-RENE E.; MONAHAN, SEAN D.; HARVIE, PIERROT; GALPERIN, ANNA; HOUSTON, MICHAEL E.; PRIEVE, MARY G.
To: PHASERX, INC.
Reel/Frame 051566/0409 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 21, 2020
From: ROIVANT HEPATOLOGY GMBH
To: GENEVANT SCIENCES GMBH
Reel/Frame 051655/0057 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 21, 2020
From: PHASERX, INC.
To: ROIVANT HEPATOLOGY GMBH
Reel/Frame 051655/0401 →
Continuity (3)
Provisional Application 62446186 · Jan 13, 2017
Provisional Application 62440941 · Dec 30, 2016
Related Publication 20200078313A1 · Mar 12, 2020