Cyclic-GluR6 analogs, methods of treatment and use

Patent metadata

Field	Value
Publication number	US-10046024-B2
Application number	US-201615195366-A
Country	US
Kind code	B2
Filing date	Jun 28, 2016
Priority date	May 18, 2009
Publication date	Aug 14, 2018
Grant date	Aug 14, 2018

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.

First claim

The invention claimed is:

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):

Assignees

• Univ Brown
• The United States Of America As Represented By National Institutes Of Health Nih U S Dept Of Health

Inventors

• Spaller Mark
• Marshall John
• Goebel Dennis J

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P25/08

  Antiepileptics; Anticonvulsants · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title