IP Library Granted Patent US 10,046,024
Granted Patent B2
US 10,046,024 · App. 15/195,366 · Granted Aug 14, 2018

Cyclic-GluR6 analogs, methods of treatment and use

Inventors: Mark Spaller (Lebanon, NH); John Marshall (Providence, RI); Dennis J. Goebel (Detroit, MI)
Assignee: The United States of America, as represented by National Institutes of Health (NIH), U.S. Dept of Health and Human Services (DHHS), NIH Division of Extramural Inventions and Technology Resource (DEITR
A61K38/12A61K9/006A61K9/0019A61K9/0034A61K9/0085A61K31/135A61K31/198A61K31/395A61K31/401A61K31/42A61K45/06C07K7/56A61K38/00Y10T428/2982
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Quick Facts
Patent No.
US 10,046,024
App. No.
15/195,366
Granted
Aug 14, 2018
Kind
B2
Abstract

A composition which is reversible inhibitor of at least one neuron-specific PDZ domain comprising wherein R is a molecular transporter with or without a linker amino acid; R 1 is at least about one amino acid covalently bound; and, R 2 is isoleucine, leucine, alanine, phenylalanine, or valine, and methods of use.

Claims (12)

1. A composition which is reversible inhibitor of at least one neuron-specific PDZ domain comprising

wherein

R is a molecular transporter with or without a linker amino acid;

R 1 is at least about one amino acid covalently bound; and,

R 2 is isoleucine, leucine, alanine, phenylalanine, or valine

and wherein the P −4 position is indicated.

2. The composition of claim 1 wherein R 1 is β-alanine.

3. The composition of claim 1 wherein R 2 is valine.

4. The composition of claim 1 wherein the P −4 position is lysine, aspartic acid, glutamic acid or arginine.

5. The composition of claim 1 having the structure:

6. The composition of claim 1 wherein R comprises a liposome, steroid, polyamine, nanotube, nanoparticle, dendrimer, cell-penetrating peptide, protein-transduction domain amino acid, peptoid, N-substituted glycine, oligogcarbamate, arginine oligomer of about 6-20 units (SEQ ID NO: 2), D-arginine oligomer, spaced arginine oligomer, N-arginine peptoid, oligoarbamate transporter, or tetrameric dendrimer.

7. The inhibitor of claim 1 wherein R comprises (SEQ ID NO: 3):

Assignments (1)
CONFIRMATORY LICENSE Recorded Aug 4, 2016
From: BROWN UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039562/0326 →
Continuity (2)
Continuation 13320848 · May 22, 2012
Related Publication 20160303186A1 · Oct 20, 2016