# US 11,439,615 B2 · Lipoxin and lipoxin analogue mediated neuroprotection and treatments

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- Number: US 11,439,615 B2
- Document ID: US11439615B2
- Status: Granted
- Kind: B2
- Application number: 16/492,494
- Filed: 2018-03-09
- Published: 2021-09-09
- Granted: 2022-09-13
- Earliest claimed: 2017-03-09
- Assignees: University Health Network; The Regents of the University of California
- Applicants: University Health Network; The Regents of the University of California
- Inventors: Jeremy M. Sivak; Izhar Livne-Bar; John G. Flanagan; Karsten Gronert; Jessica Wei
- Web page: https://patentgrep.com/patent/US11439615B2

## CPC

- A61K 31/202: having three or more double bonds, e.g. linolenic (eicosanoids, e.g. leukotrienes A61K31/557)
- A61P 25/00: Drugs for disorders of the nervous system
- A61K 31/557: Eicosanoids, e.g. leukotrienes {or prostaglandins}
- A61P 25/28: 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
- 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

Methods and compositions for inhibiting or preventing neurodegeneration, specifically hippocampal, cortical, and/or retinal ganglion cell neurons (RGC), and degeneration and/or cell loss or treating related disorders and diseases comprising administering to a subject an effective amount of one or more lipoxin compounds and/or lipoxin analogues such that degeneration and/or cell loss of neurons is inhibited or prevented.

## Claims

### Claim 1

A method for providing neuroprotection from and/or treating a chronic neurodegenerative retinal or brain disorder or condition comprising administering to a subject afflicted with said disorder or condition an effective amount of lipoxin B4 (LXB4) and/or an analog thereof, wherein the chronic retinal or brain neurodegenerative disorder or condition is selected from the group consisting of glaucoma, retinal ischemia, diabetic retinopathy, diabetic macular edema, age related macular degeneration, retinitis pigmentosa, Alzheimer's disease, multiple sclerosis, Parkinson's disease, and amyotrophic lateral sclerosis.

### Claim 2 (depends on 1)

The method of claim 1, wherein the chronic neurodegenerative retinal or brain disorder or condition comprises central nervous system neurodegeneration and/or neural cell loss and the effective amount of the LXB4 and/or an analog thereof is administered to the subject in need thereof such that the neurodegeneration and/or neural cell loss is inhibited or prevented.

### Claim 3 (depends on 1)

The method of claim 1, wherein the chronic neurodegenerative retinal or brain disorder or condition comprises hippocampal neuron, cortical neuron, optic neuron or retinal ganglion cell neurodegeneration and/or cell loss.

### Claim 4 (depends on 1)

The method of claim 1, wherein the chronic neurodegenerative retinal or brain disorder or condition comprises vision loss, reduced vision, or a chronic neurodegenerative retinal or brain disorder.

### Claim 5 (depends on 1)

The method of claim 1, wherein the chronic neurodegenerative retinal or brain disorder or condition comprises vision loss or reduced vision.

### Claim 6 (depends on 1)

The method of claim 1, wherein the LXB4 and/or an analog thereof is administered by parenteral, intravenous, subcutaneous, intramuscular, intraorbital, ophthalmic, intraocular, intravitreal, intracameral, subtenon, subconjunctival, intraperitoneal, aerosol or oral administration.

### Claim 7 (depends on 1)

The method of claim 1, wherein the LXB4 and/or an analog thereof is administered to an eye.

### Claim 8 (depends on 7)

The method of claim 7, wherein the LXB4 and/or an analog thereof is administered topically to the eye.

### Claim 9 (depends on 1)

The method of claim 1, wherein the concentration of the LXB4 and/or an analog thereof is at least 0.2 nM or 50 nM.

### Claim 10 (depends on 1)

The method of claim 1, wherein the concentration of the LXB4 and/or an analog thereof is less than 1 mM.

### Claim 11 (depends on 1)

The method of claim 1, wherein the LXB4 and/or an analog thereof is administered in a composition.

### Claim 12 (depends on 1)

The method of claim 1, wherein the LXB4 analog is LXB4 methyl ester.

### Claim 13 (depends on 1)

The method of claim 1, wherein the LXB4 analog is 15-epi-LXB4.

### Claim 14 (depends on 1)

The method of claim 1, wherein the LXB4 analog is benzo-LXB4.

### Claim 15 (depends on 1)

The method of claim 1, wherein the glaucoma is or comprises primary open angle glaucoma, secondary open angle glaucoma or normal tension glaucoma.

### Claim 16 (depends on 7)

The method of claim 7, wherein the LXB4 and/or analog thereof is administered to the eye by a sustained delivery device, topical gel or ointment, polymer, or intraocular gel, or sustained delivery device implant, polymer, or nanoparticles.

### Claim 17 (depends on 16)

The method of claim 16, wherein the sustained delivery device is a contact lens.