IP Library Granted Patent US 12,503,425
Granted Patent B2
US 12,503,425 · App. 18/537,093 · Granted Dec 23, 2025

Methods of treating or controlling cytotoxic cerebral edema

Inventors: Marc F. Pelletier (Shaker Heights, OH); George William Farr (Rocky River, OH); Paul Robert McGuirk (Spring Hill, FL); Christopher H. Hall (Shaker Heights, OH); Walter F. Boron (Shaker Heights, OH)
Assignee: Aeromics, Inc.
C07C235/64A61K31/167A61K31/24A61K31/5375A61K31/661A61K31/6615C07D295/185C07F9/12
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Quick Facts
Patent No.
US 12,503,425
App. No.
18/537,093
Granted
Dec 23, 2025
Kind
B2
Abstract

The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors.

Claims (8)

1 . A method of treating or controlling cytotoxic cerebral edema consequent to an ischemic stroke in a human patient in need thereof, wherein the method comprises administering to the human patient a pharmaceutical composition for intravenous administration comprising

in free or pharmaceutically acceptable salt form, and a pharmaceutically acceptable diluent or carrier,

and treating the human patient with intravenous thrombolysis and/or mechanical clot removal.

2 . The method of claim 1 , wherein the method comprises treating the human patient with intravenous thrombolysis and the intravenous thrombolysis is with rtPA.

3 . The method of claim 1 , wherein the pharmaceutical composition for intravenous administration is administered within 12 hours of the stroke.

4 . The method of claim 2 , wherein the pharmaceutical composition for intravenous administration is administered within 12 hours of the stroke.

5 . The method of claim 1 , wherein the pharmaceutical composition for intravenous administration is administered within 6 hours of the stroke.

6 . The method of claim 2 , wherein the pharmaceutical composition for intravenous administration is administered within 6 hours of the stroke.

Assignments (3)
CERTIFICATE OF CONVERSION Recorded Jul 20, 2024
From: AEROMICS, LLC
To: AEROMICS, INC.
Reel/Frame 068465/0128 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2023
From: PELLETIER, MARC F.; FARR, GEORGE WILLIAM; MCGUIRK, PAUL ROBERT; HALL, CHRISTOPHER H.; BORON, WALTER F.
To: AEROMICS, LLC
Reel/Frame 065887/0678 →
ASSIGNEE CHANGE OF ADDRESS Recorded Dec 15, 2023
From: AEROMICS, INC.
To: AEROMICS, INC.
Reel/Frame 066043/0810 →
Continuity (7)
Continuation 17443361 · Jul 26, 2021
Continuation 15982644 · May 17, 2018
Continuation 14398947
Provisional Application 61799606 · Mar 15, 2013
Provisional Application 61651778 · May 25, 2012
Provisional Application 61644268 · May 8, 2012
Related Publication 20240360077A1 · Oct 31, 2024
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