IP Library Granted Patent US 10,059,681
Granted Patent B2
US 10,059,681 · App. 15/166,482 · Granted Aug 28, 2018

Disubstituted maleic anhydrides with altered kinetics of ring closure

Inventors: Andrei V. Blokhin (Fitchburg, WI); David B. Rozema (Cross Plains, WI); Jonathan D. Benson (Stoughton, WI); Jeffrey C. Carlson (Madison, WI)
Assignee: Arrowhead Pharmaceuticals, Inc.
C07D307/89C07D307/60C07D307/66C07D307/88C07H15/08C07H15/26
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Quick Facts
Patent No.
US 10,059,681
App. No.
15/166,482
Granted
Aug 28, 2018
Kind
B2
Abstract

We describe anhydride compounds suitable for physiologically labile modification of amine-containing molecules. The described anhydrides form reversible linkages having desirable kinetics for in vivo delivery of biologically active molecules. Also described are endosomolytic polymers formed by modification of membrane active polyamines with the described anhydrides.

Claims (10)

1. An anhydride comprising the structure represented by:

wherein n is an integer from 1 to 8; and

Z comprises a carboxyl group, a hydroxyl group, an ester group, an amide group, an ether group, a tertiary amine group, a protected amine group, a targeting group, or a steric stabilizer group.

2. The anhydride of claim 1 , wherein:

Z is selected from the group consisting of: hydroxyl group, targeting group, and steric stabilizer group.

3. The anhydride of claim 1 , wherein the targeting group is an N-acetylgalactosamine.

4. The anhydride of claim 1 , wherein the steric stabilizer is a polyethyleneglycol.

5. The anhydride of claim 1 , wherein Z comprises polyethylene glycol.

6. The anhydride of claim 1 , wherein n is 1.

7. The anhydride of claim 1 , wherein n is 2.

Assignments (2)
SECURITY INTEREST Recorded Aug 7, 2024
From: ARROWHEAD PHARMACEUTICALS, INC.
To: SIXTH STREETLENDING PARTNERS, AS THE ADMINISTRATIVE AGENT
Reel/Frame 068510/0363 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 10, 2016
From: BLOKHIN, ANDREI V.; BENSON, JONATHAN D.; ROZEMA, DAVID B.; CARLSON, JEFFREY C.
To: ARROWHEAD PHARMACEUTICALS, INC.
Reel/Frame 039978/0610 →
Continuity (3)
Division 14119074
Provisional Application 61498025 · Jun 17, 2011
Related Publication 20160272605A1 · Sep 22, 2016
Cited By (2)
US 12,611,465 US 12,702,718