# US 11,077,151 B2 · Ascaroside treatment of autoimmune and inflammatory diseases

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- Number: US 11,077,151 B2
- Document ID: US11077151B2
- Status: Granted
- Kind: B2
- Application number: 16/327,659
- Filed: 2017-08-25
- Published: 2019-06-13
- Granted: 2021-08-03
- Earliest claimed: 2016-08-25
- Assignees: California Institute of Technology; Boyce Thompson Institute for Plant Research, Inc.
- Applicants: California Institute of Technology; Boyce Thompson Institute for Plant Research
- Inventors: Andrea Choe; Paul W. Sternberg; Frank C. Schroeder
- Web page: https://patentgrep.com/patent/US11077151B2

## CPC

- A61K 35/62: Leeches; Worms, e.g. cestodes, tapeworms, nematodes, roundworms, earth worms, ascarids, filarias, hookworms, trichinella or taenia
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/7028: Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K 31/7042: Compounds having saccharide radicals and heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- G01N 33/6869: {Interleukin}
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention relates to the use of ascr #7 for preventing or treating IL-6 and/or IL-1β-mediated diseases.

## Claims

### Claim 1

A method of preventing or treating an IL-6- and/or IL-1β-mediated disease in a subject, comprising administering to the subject a composition comprising ascr #7 or a pharmaceutically acceptable salt and/or prodrug thereof and a pharmaceutically acceptable carrier.

### Claim 2 (depends on 1)

The method of claim 1, wherein the IL-6- and/or IL-1β-mediated disease is an autoimmune disease or an inflammatory disease.

### Claim 3 (depends on 1)

The method of claim 1, wherein the subject has an elevated level of IL-6 and/or IL-1β.

### Claim 4 (depends on 1)

The method of claim 1, wherein the level of IL-6 and/or IL-10 in an affected tissue of the subject exceeds 200% of a normal level in the affected tissue.

### Claim 5 (depends on 1)

The method of claim 1, wherein the disease is Agammaglobulinemia, Amyloidosis, Ankylosing spondylitis, Anti-GBM/Anti-TBM nephritis, Antiphospholipid syndrome, Autoimmune hepatitis, Autoimmune inner ear disease, Atopic dermatitis, Asthma, Castleman disease, Celiac disease, Chagas disease, Chronic recurrent multifocal osteomyelitis, Cogan's syndrome, Cold agglutinin disease, CREST syndrome, Crohn's disease, Dermatomyositis, Devic's disease (neuromyelitis optica), Discoid lupus, Endometriosis, Eosinophilic esophagitis, Eosinophilic fasciitis, Evan's syndrome, Fibromyalgia, Giant cell arteritis, Giant cell myocarditis, Glomerulonephritis, Goodpasture's syndrome, Granulomatosis with polyangiitis, Graves' disease, Guillain-Barre syndrome, Hashimoto's thyroiditis, Hemolytic anemia, Henoch-Schonlein purpura, Hypogammaglobulinemia, Hypoproliferative anemia, IgA Nephropathy, Inclusion body myositis, Interstitial cystitis, Inflammatory Bowel Disease, Juvenile arthritis, Juvenile/Type 1 Diabetes, Juvenile myositis, Kawasaki syndrome, Lichen planus, Lichen sclerosus, Lupus (SLE), Meniere's disease, Multiple sclerosis, Myasthenia gravis, Microscopic polyangiitis, Optic neuritis, Pemphigus, Polyarteritis nodosa, Polymyalgia rheumatica, Polymyositis, Primary biliary cirrhosis, Primary sclerosing cholangitis, Psoriasis, Psoriatic arthritis, Rheumatic fever, Rheumatoid arthritis, Sarcoidosis, Sjogren's syndrome, Temporal arteritis/Giant cell arteritis, Transverse myelitis, Ulcerative colitis, Uveitis, Vasculitis, Vitiligo, Viral myocarditis, or Wegener's granulomatosis (Granulomatosis with Polyangiitis (GPA)).

### Claim 6 (depends on 5)

The method of claim 5, wherein the disease is asthma.

### Claim 7 (depends on 5)

The method of claim 5, wherein the disease is inflammatory bowel disease.

### Claim 8 (depends on 5)

The method of claim 5, wherein the disease is type 1 diabetes.

### Claim 9 (depends on 5)

The method of claim 5, wherein the disease is not eosinophilic esophagitis (EoE).

### Claim 10 (depends on 1)

The method of claim 1, further comprising administering an agent with an anti-inflammatory effect.

### Claim 11 (depends on 10)

The method of claim 10, wherein the agent with an anti-inflammatory effect is a corticosteroid.

### Claim 12 (depends on 11)

The method of claim 11, wherein the corticosteroid is selected from aldosterone, betamethasone, budesonide, corticosterone, cortisol, cortisone, dexamethasone, fluticasone, hydrocortisone, methylprednisolone, prednisolone, and prednisone.

### Claim 13 (depends on 1)

The method of claim 1, wherein the subject is a mammal.

### Claim 14 (depends on 13)

The method of claim 13, wherein the mammal is a mouse or a human.

### Claim 15 (depends on 14)

The method of claim 14, wherein the mammal is a human.

### Claim 16

A method of reducing IL-6 and/or IL-1β production from a cell, comprising contacting the cell with a composition comprising ascr #7 or a pharmaceutically acceptable salt and/or prodrug thereof and a pharmaceutically acceptable carrier.

### Claim 17 (depends on 1)

The method of claim 1, wherein the method is a method of treating the IL-6- and/or IL-1β-mediated disease in the subject.

### Claim 18 (depends on 1)

The method of claim 1, wherein the composition comprises ascr #7 or a pharmaceutically acceptable salt thereof.