# US 2021/0330616 A1 · Ameliorating agent for obesity-related metabolic disease

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- Number: US 2021/0330616 A1
- Document ID: US20210330616A1
- Status: Published application
- Kind: A1
- Application number: 17/272,998
- Filed: 2019-09-03
- Published: 2021-10-28
- Earliest claimed: 2018-09-03
- Assignees: Metabolic and Obese Research Science Corporation
- Applicants: Metabolic and Obese Research Science Corporation
- Inventors: Masatomo MORI
- Web page: https://patentgrep.com/patent/US20210330616A1

## CPC

- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/485: {Inorganic compounds}
- A61K 9/4858: {Organic compounds}
- A61K 9/4866: {Organic macromolecular compounds}
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/50: for increasing or potentiating the activity of insulin
- A61P 9/00: Drugs for disorders of the cardiovascular system
- 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 9/12: Antihypertensives
- A61P 13/12: of the kidneys
- A61P 19/06: Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

An object of the present invention is to provide a drug containing, as an active ingredient, a low-molecular-weight compound that ameliorates obesity-related metabolic diseases, for example, exhibits anti-obesity action without reduction of food intake through binding to Helz2 to lower its action, on the basis of the fact that Helz2 is intensely expressed in the liver both in humans and mice, and expression levels are significantly increased in the human liver with NAFLD, as an obesity-related metabolic disease, and in fatty liver in obese mice. The present invention provides an ameliorating agent for an obesity-related metabolic disease, in particular, an ameliorating agent for fatty liver, the ameliorating agent characterized by containing guanabenz or a salt of guanabenz as an active ingredient.

## Claims

### Claim at position 1

-14. (canceled)

### Claim 15

A method for ameliorating a fatty liver comprising administrating guanabenz or a salt of guanabenz to a patient in need thereof.

### Claim 16 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein guanabenz acetate is administered to a patient in need thereof.

### Claim 17 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein the fatty liver is non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).

### Claim 18 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein the fatty liver is caused by insulin resistance.

### Claim 19 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein the fatty liver is accompanied by obesity disease.

### Claim 20 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein the fatty liver is accompanied by hypertension.

### Claim 21 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein the fatty liver is accompanied by metabolic syndrome.

### Claim 22 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein guanabenz or the salt of guanabenz ameliorates the fatty liver through binding to Helz2 to lower its action.

### Claim 23 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein guanabenz or the salt of guanabenz exhibits anti-obesity action without reduction of appetite through binding to Helz2 to lower its action.

### Claim 24 (depends on 15)

The method for ameliorating a fatty liver according to claim 15, wherein the fatty liver is non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH), and wherein guanabenz or the salt of guanabenz ameliorates non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH) through binding to Helz2 to lower its action.

### Claim 25

A method for treating a fatty liver comprising administrating guanabenz or a salt of guanabenz to a patient in need thereof.

### Claim 26 (depends on 25)

The method for ameliorating a fatty liver according to claim 25, wherein guanabenz acetate is administered to a patient in need thereof.

### Claim 27 (depends on 25)

The method for ameliorating a fatty liver according to claim 25, wherein the fatty liver is non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).

### Claim 28 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein the fatty liver is caused by insulin resistance.

### Claim 29 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein the fatty liver is accompanied by obesity disease.

### Claim 30 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein the fatty liver is accompanied by hypertension.

### Claim 31 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein the fatty liver is accompanied by metabolic syndrome.

### Claim 32 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein guanabenz or the salt of guanabenz ameliorates the fatty liver through binding to Helz2 to lower its action.

### Claim 33 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein guanabenz or the salt of guanabenz exhibits anti-obesity action without reduction of appetite through binding to Helz2 to lower its action.

### Claim 34 (depends on 25)

The method for treating a fatty liver according to claim 25, wherein the fatty liver is non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH), and wherein guanabenz or the salt of guanabenz ameliorates non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH) through binding to Helz2 to lower its action.