IP Library Granted Patent US 10,201,539
Granted Patent B2
US 10,201,539 · App. 15/445,833 · Granted Feb 12, 2019

Composition for reducing nervous system injury and method of making and use thereof

Inventors: Zhigang Xiong (Atlanta, GA); Roger P. Simon (Atlanta, GA)
Assignee: MOREHOUSE SCHOOL OF MEDICINE
A61K31/4965A61K9/00A61K9/0019A61K9/0085A61K31/155A61K31/40A61K31/55C07K14/43518
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Quick Facts
Patent No.
US 10,201,539
App. No.
15/445,833
Granted
Feb 12, 2019
Kind
B2
Abstract

This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof.

Claims (14)

1. A method for reducing nerve injury in a subject, comprising:

administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising an amiloride analog or a pharmaceutically acceptable salt thereof,

wherein the amiloride analog is selected from the group consisting of benzamil, a methylated analog of benzamil, phenamil, 5-(N-ethyl-N-isobutyl)-amiloride (EIPA), KB-R7943, 5-(N,N-hexamethylene) amiloride and 5-(N,N-dimethyl) amiloride hydrochloride, or

wherein the amiloride analog comprises—a water solubilizing group formed on a guanidine group, wherein the water solubilizing group is a N,N-dimethyl amino group or a sugar group, and

wherein the pharmaceutical composition is administered orally.

2. The method of claim 1 , wherein the amiloride analog is benzamil or a methylated analog of benzamil.

3. The method of claim 1 , wherein the amiloride analog is phenamil.

4. The method of claim 1 , wherein the amiloride analog is 5-(N-ethyl-N-isobutyl)-amiloride (EIPA).

5. The method of claim 1 , wherein the amiloride analog is KB-R7943.

6. The method of claim 1 , wherein the amiloride analog comprises 5-(N,N-hexamethylene) amiloride or 5-(N,N-dimethyl) amiloride hydrochloride.

7. The method of claim 1 , wherein the amiloride analog or a pharmaceutically acceptable salt thereof is given in a dose range of 0.1 mg-10 mg/kg body weight.

8. The method of claim 1 , wherein the pharmaceutical composition is administered within one hour of the onset of an ischemic event.

9. The method of claim 1 , wherein the pharmaceutical composition is administered between one hour and five hours of the onset of an ischemic event.

10. The method of claim 1 , wherein the nerve injury is a nervous system injury.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 13, 2017
From: XIONG, ZHIGANG; SIMON, ROGER P.
To: MOREHOUSE SCHOOL OF MEDICINE
Reel/Frame 041562/0018 →
Continuity (5)
Continuation 13972558 · Aug 21, 2013
Continuation In Part 13284166 · Oct 28, 2011
Continuation 11724859 · Mar 16, 2007
Provisional Application 60611241 · Sep 16, 2004
Related Publication 20170182041A1 · Jun 29, 2017