# US 10,945,995 B2 · Compositions and methods for channelopathy disorders-targeting fluid movement across membranes

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- Number: US 10,945,995 B2
- Document ID: US10945995B2
- Status: Granted
- Kind: B2
- Application number: 16/650,711
- Filed: 2018-09-25
- Published: 2020-09-10
- Granted: 2021-03-16
- Earliest claimed: 2017-09-26
- Assignees: Deha, LLC
- Applicants: Deha, LLC
- Inventors: Kumar Sripathirathan; Adhya Kumar
- Web page: https://patentgrep.com/patent/US10945995B2

## CPC

- A61K 31/4184: condensed with carbocyclic rings, e.g. benzimidazoles
- C07D 307/81: Radicals substituted by nitrogen atoms not forming part of a nitro radical
- A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
- A61K 31/4196: 1,2,4-Triazoles
- A61K 31/438: The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
- A61K 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- C07C 235/64: having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
- C07D 403/14: containing three or more hetero rings
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C07D 235/06: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D 235/26: Oxygen atoms
- C07D 249/08: 1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 409/06: linked by a carbon chain containing only aliphatic carbon atoms
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The present invention includes composition and methods for treating stroke comprising: identifying a subject in need of treatment for a stroke; and providing the subject with a therapeutically effective amount of an Aquaporin-4 inhibitor that blocks a filter portion of an Aquaporin-4 channel region, and identifying modulators of the different aquaporin specific splice variants.

## Claims

### Claim 1

A method of treating a subject in need of treatment for a disease or condition in which an Aquaporin-2, an Aquaporin-4, an Aquaporin-6, or an Aquaporin-11 is in need of modulation comprising:
providing the subject with a therapeutically effective amount of an Aquaporin-2, an Aquaporin-4, an Aquaporin-6, or an Aquaporin-11, inhibitor or modulator selected from at least one of:

### Claim 2 (depends on 1)

The method of claim 1, wherein the Aquaporin-2, Aquaporin-4, Aquaporin-6, or Aquaporin-11 inhibitor is adapted for oral, enteral, parenteral, intravenous, subcutaneous, intramuscular, pulmonary, or rectal administration.

### Claim 3 (depends on 1)

The method of claim 1, wherein the Aquaporin-2, Aquaporin-4, Aquaporin-6, or Aquaporin-11 inhibitor is provided in an amount of 1 microgram to 1 gram per dose.

### Claim 4 (depends on 1)

The method of claim 1, wherein the patient has been treated previously with at least one of an osmotic agent, barbiturates, steroids, or diuretics and the subject has become refractory to that treatment.

### Claim 5 (depends on 1)

The method of claim 1, wherein the Aquaporin-2, Aquaporin-4, Aquaporin-6, or Aquaporin-11 inhibitor has a potency in the range of 1-10 μM, 0.1-100 μM or 5-9 μM.

### Claim 6 (depends on 1)

The method of claim 1, wherein the Aquaporin-2, Aquaporin-4, Aquaporin-6, or Aquaporin-11 inhibitor inhibits perivascular astrocyte swelling.

### Claim 7 (depends on 1)

The method of claim 1, wherein the Aquaporin-2, Aquaporin-4, Aquaporin-6, or Aquaporin-11 inhibitor reduces brain edema and infarct size after stroke.

### Claim 8 (depends on 1)

The method of claim 1, wherein the Aquaporin-2, Aquaporin-4, Aquaporin-6, or Aquaporin-11 is an Aquaporin splice variant.