# US 10,766,936 B2 · Treatment of ischemia

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- Number: US 10,766,936 B2
- Document ID: US10766936B2
- Status: Granted
- Kind: B2
- Application number: 16/391,774
- Filed: 2019-04-23
- Published: 2019-09-05
- Granted: 2020-09-08
- Earliest claimed: 2004-09-16
- Assignees: Morehouse School of Medicine
- Applicants: Morehouse School of Medicine
- Inventors: Roger P. Simon; Zhigang Xiong
- Web page: https://patentgrep.com/patent/US10766936B2

## CPC

- C07K 14/43518: {from spiders}
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/4418: having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
- A61K 31/4965: Non-condensed pyrazines
- A61K 31/498: Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
- A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)}
- A61K 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)}
- A61K 38/1767: {from invertebrates}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A system, including methods and compositions, for treatment of ischemia.

## Claims

### Claim 1

A method of treating ischemia, comprising:
administering a therapeutically effective amount of an acid sensing ion channel 1a (ASIC1a) inhibitor to an ischemic subject in order to reduce injury resulting from ischemia, wherein the ion channel 1a (ASIC1a) inhibitor is a peptide that includes a cystine knot.

### Claim 2 (depends on 1)

The method of claim 1, wherein the step of administering includes a step of administering an ASIC1a inhibitor that inhibits ASIC1a selectively relative to one or more other acid sensing ion channel (ASIC) family members.

### Claim 3 (depends on 1)

The method of claim 1, wherein the step of administering includes a step of administering an inhibitor that is selective for ASICI a relative to every other member of the ASIC family.

### Claim 4 (depends on 1)

The method of claim 1, wherein the step of administering is performed on a subject that has suffered a stroke, in order to reduce injury resulting from the stroke.

### Claim 5 (depends on 1)

The method of claim 1, wherein the step of administering includes a step of administering the inhibitor nasally, intrathecally, and/or epidurally.

### Claim 6 (depends on 1)

The method of claim 1, wherein the step of administering includes a step of administering a peptide that is a derivative of PcTx1 (SEQ ID NO:1).

### Claim 7 (depends on 6)

The method of claim 6, wherein the peptide is a derivative that differs from PcTx1 by at least one deletion, substitution, and/or addition of one or more amino acids.

### Claim 8 (depends on 1)

The method of claim 1, the ASIC1a inhibitor being a first inhibitor, further comprising a step of administering a second inhibitor to the subject, the second inhibitor being configured to selectively inhibit at least one other channel that is not a member of the acid sensing ion channel family.

### Claim 9 (depends on 1)

The method of claim 1, wherein the step of administering includes a step of administering an inhibitor configured to inhibit ASIC1a channel activity at a concentration of inhibitor that is at least about ten-fold less than for inhibition of another ASIC family member.

### Claim 10 (depends on 1)

The method of claim 1, wherein the ischemia is stroke, and wherein the step of administering is performed at least about two hours after the onset of stroke on the ischemic subject to reduce injury induced by the stroke.