IP Library Granted Patent US 8,889,635
Granted Patent B2
US 8,889,635 · App. 12/570,977 · Granted Nov 18, 2014

Dendrimer conjugates

Inventors: James R. Baker, Jr. (Ann Arbor, MI); Xue-min Cheng (Ann Arbor, MI); Abraham F. L. Van Der Spek (Ann Arbor, MI); Baohua Mark Huang (Ann Arbor, MI); Thommey P. Thomas (Dexter, MI)
Assignee: The Regents of The University of Michigan
A61K47/483A61K47/48207A61K31/485
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Quick Facts
Patent No.
US 8,889,635
App. No.
12/570,977
Granted
Nov 18, 2014
Kind
B2
Abstract

The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.

Claims (8)

1. A composition comprising pain relief complexes and pain relief antagonist complexes;

wherein said pain relief complexes consist of dendrimers separately conjugated with 1) a pain relief agent via an ester linkage agent, wherein said pain relief agent is morphine, 2) a locking agent, wherein said locking agent is trigonelline, and 3) a targeting agent, wherein said targeting agent is transferrin;

wherein said pain relief antagonist complexes consist of dendrimers separately conjugated with 1) a pain relief agent antagonist via an indolequinone trigger agent, wherein said pain relief agent antagonist is naloxone, 2) a locking agent, wherein said locking agent is trigonelline, and 3) a targeting agent, wherein said targeting agent is transferrin;

wherein said pain relief antagonist complexes are configured to prevent respiratory depression caused said pain relief complexes;

wherein said dendrimers within said pain relief complexes and pain relief antagonist complexes are separate within said composition.

2. The composition of claim 1 , wherein said dendrimers are selected from the group consisting of a polyamideamine (PAMAM) dendrimer, a polypropylamine (POPAM) dendrimer, and a PAMAM-POPAM dendrimer.

3. The composition of claim 1 , wherein the linkage agent comprises a spacer comprising between 1 and 8 straight or branched carbon chains, wherein said straight or branched chains are selected from the group consisting of i) unsubstituted, and ii) substituted with alkyls.

4. The composition of claim 1 , wherein said dendrimers are acetylated.

Assignments (2)
CONFIRMATORY LICENSE Recorded May 6, 2010
From: UNIVERSITY OF MICHIGAN
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 024345/0346 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2010
From: BAKER, JAMES R., JR.; CHENG, XUE-MIN; VAN DER SPEK, ABRAHAM F.L.; HUANG, BAOHUA MARK; THOMAS, THOMMEY P.
To: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Reel/Frame 024007/0024 →
Continuity (2)
Provisional Application 61101461 · Sep 30, 2008
Related Publication 20100160299A1 · Jun 24, 2010