# US 10,441,562 B2 · Aromatic farnesyl compound and application thereof

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- Number: US 10,441,562 B2
- Document ID: US10441562B2
- Status: Granted
- Kind: B2
- Application number: 15/518,698
- Filed: 2015-12-18
- Published: 2017-08-10
- Granted: 2019-10-15
- Earliest claimed: 2015-04-30
- Assignees: Institute of Microbiology, Chinese Academy of Sciences
- Applicants: Institute of Microbiology, Chinese Academy of Sciences
- Inventors: Hongwei Liu; Kai Wang; Li Bao; Junjie Han
- Web page: https://patentgrep.com/patent/US10441562B2

## CPC

- A61K 31/341: not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
- A23L 2/395: in a particular shape or form
- A23L 2/40: Effervescence-generating compositions
- A23L 2/52: Adding ingredients (adding preservatives A23B70/10)
- A23L 33/105: Plant extracts, their artificial duplicates or their derivatives
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/202: having three or more double bonds, e.g. linolenic (eicosanoids, e.g. leukotrienes A61K31/557)
- A61K 31/365: Lactones
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- 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 27/02: Ophthalmic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 57/03: Monocarboxylic acids
- C07D 307/33: in position 2, the oxygen atom being in its keto or unsubstituted enol form
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Aromatic farnesyl compound and application of a pharmaceutical salt thereof as an inhibitor of α-glucosidase, dipeptidyl peptidase-4, aldose reductase, protein tyrosine phosphatase-1B or HMG-CoA reductase, or use thereof in preparing medicine and functional healthcare products having a liver protective function and/or for treating and/or preventing type II diabetes, diabetic retinopathy, diabetic foot disease, and hyperlipidemia.

## Claims

### Claim 1

An aromatic farnesyl compound of formula (I) or pharmaceutically-acceptable salt thereof:
wherein, R1 is selected from H, C1-C5 alkyl group —NO2, F, Cl, Br, ester group, and acylamino group the number of R1 is 1, 2 or 3; configuration of 1′ is selected from R type and S type; R2 is H; X is O; the bond between 2′ and 3′ is a double bond; n=1, 2 or 3; and R3 is CH3.

### Claim 2

A compound or its pharmaceutically-acceptable salt selected from the group consisting of:

### Claim 3 (depends on 2)

A method for treating a condition in a subject in need thereof, comprising administering to the subject a composition comprising a compound of claim 2, wherein the condition is selected from the group consisting of diabetes type II; hyperlipidemia; hyperglycaemia; diabetic retinopathy; diabetic foot; non-alcohol fatty liver disease; and combinations thereof.

### Claim 4 (depends on 1)

A composition comprising metformin and at least one aromatic farnesyl compound or pharmaceutically-acceptable salt thereof according to claim 1.

### Claim 5 (depends on 3)

The method according to claim 3, wherein the composition is an injection, tablet, granule, powder, pill, capsule, oral liquid, ointment, cream or spray.

### Claim 6 (depends on 4)

The composition according to claim 4, wherein the composition is a food or functional health product selected from the group consisting of oral liquids, teas, tablets, capsules, drinks and effervescent tablets.

### Claim 7 (depends on 3)

The method according to claim 3, wherein the composition further includes one or more pharmaceutically-acceptable excipients.

### Claim 8 (depends on 7)

The method according to claim 7, wherein said excipients are selected from the group consisting of diluents, fillers, adhesives, wetting agents, disintegrating agents, absorption enhancers, surfactants, adsorption carriers, lubricants and sustained-release materials.

### Claim 9 (depends on 3)

The method according to claim 3, wherein the administration is by oral administration, gastrointestinal administration, injection, spray, or physical or chemical mediated administration.

### Claim 10 (depends on 2)

A composition comprising metformin and at least one compound according to claim 2.

### Claim 11 (depends on 1)

A method for treating a condition in a subject in need thereof, comprising administering to the subject a composition comprising a compound of claim 1, herein the condition is selected from the group consisting of diabetes type II, hyperlipidemia, hyperglycemia, diabetic retinopathy, diabetic foot, non-alcohol fatty liver disease, and combinations thereof.

### Claim 12 (depends on 11)

The method according to claim 11, wherein the composition is an injection, tablet, granule, powder, pill, capsule, oral liquid, ointment, cream or spray.

### Claim 13 (depends on 10)

The composition according to claim 10, wherein the composition is a food or functional health product selected from the group consisting of oral liquids, teas, tablets, capsules, drinks and effervescent tablets.

### Claim 14 (depends on 11)

The method according to claim 11, wherein the composition further includes one or more pharmaceutically-acceptable excipients.

### Claim 15 (depends on 14)

The method according to claim 14, wherein said excipients are selected from the group consisting of diluents, fillers, adhesives, wetting agents, disintegrating agents, absorption enhancers, surfactants, adsorption carriers, lubricants and sustained-release materials.

### Claim 16 (depends on 11)

The method according to claim 11, wherein the administration is by oral administration, gastrointestinal administration, injection, spray, or physical or chemical mediated administration.