# US 10,118,909 B2 · Monascuspurpurones, preparation and uses thereof

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- Number: US 10,118,909 B2
- Document ID: US10118909B2
- Status: Granted
- Kind: B2
- Application number: 14/511,136
- Filed: 2014-10-09
- Published: 2015-05-21
- Granted: 2018-11-06
- Earliest claimed: 2010-12-23
- Applicants: Food Industry Research and Development Institute
- Inventors: Ming-Jen Cheng; Ping-Hsun Yang; Ming-Der Wu; Shie-Jea Lin; Gwo-Fang Yuan; Yen-Lin Chen; Hsuen-Chun Liao; Kai-Ping Chen
- Web page: https://patentgrep.com/patent/US10118909B2

## CPC

- C07D 307/86: with an oxygen atom directly attached in position 7
- A61K 31/365: Lactones
- A61K 31/426: 1,3-Thiazoles
- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A61K 36/899: Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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 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
- B01D 15/18: relating to flow patterns
- B01D 15/424: {Elution mode}
- C12N 1/145: Fungi isolates
- C12P 17/04: containing a five-membered hetero ring, e.g. griseofulvin {, vitamin C}
- A61K 2236/19: involving fermentation using yeast, bacteria or both; enzymatic treatment
- C12R 2001/645: Fungi {; Processes using fungi}
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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
- B01D: SEPARATION (separating solids from solids by wet methods B03B, B03D; by pneumatic jigs or tables B03B; by other dry methods B07; magnetic or electrostatic separation of solid materials from solid materials or fluids, separation by high-voltage electric fields B03C; centrifuges, vortex apparatus B04; presses per se for squeezing-out liquid from liquid-containing material B30B9/02; treatment of water C02F, e.g. softening by ion-exchange C02F1/42; {arrangements of air intake cleaners in gas turbine plants F02C7/05} ; arrangements or mounting of filters in air-conditioning, air-humidification or ventilation F24F13/28)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12P: FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE {(brewing of beer C12C; producing vinegar C12J; producing specific peptides or proteins C07K; producing enzymes C12N9/00; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; measuring or testing processes involving enzymes or microorganisms C12Q; measuring or testing processes involving nucleic acid amplification reactions C12Q1/6844; fermentation processes to form a food composition, A21 or A23; compounds in general, see the relevant compound class, e.g. C01, C07)}
- C12R: INDEXING SCHEME ASSOCIATED WITH SUBCLASSES C12C - C12Q, RELATING TO MICROORGANISMS

## Abstract

The present invention relates to a monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPARγ and/or C/EBPα, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.

## Claims

### Claim 1

A method for preventing and/or treating a disease or disorder related to insulin resistance in a subject, which comprises administering to said subject a composition consisting of an effective amount of rel-(1S,7aR,3aR)-1-hexanoyl-5,13-dimethyl-6-(2-oxopentyl)-7a,7-dihydrobenzofuran-2,4-dione or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient.

### Claim 2

A method of increasing the activity of PPARγ and/or C/EBPα in a subject in need thereof, which comprises administering to said subject a composition consisting of an effective amount of rel-(1S,7aR,3aR)-1-hexanoyl-5,13-dimethyl-6-(2-oxopentyl)-7a,7-dihydrobenzofuran-2,4-dione or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient.

### Claim 3

A method of lowering blood glucose in a subject, which comprises administering to said subject a composition consisting of an effective amount of rel-(1S, 7aR,3aR)-1-hexanoyl-5,13-dimethyl-6-(2-oxopentyl)-7a,7-dihydrobenzofuran-2,4-dione or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient.

### Claim 4

A method of preventing and/or treating metabolic syndrome or its complication in a subject, which comprises administering to said subject a composition consisting of an effective amount of rel-(1S,7aR,3aR)-1-hexanoyl-5,13-dimethyl-6-(2-oxopentyl)-7a,7-dihydrobenzofuran-2,4-dione or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient.

### Claim 5 (depends on 4)

The method of claim 4, wherein the metabolic syndrome or its complication is selected from the group consisting of abdominal obesity, atherogenic dyslipidemia, elevated blood pressure, insulin resistance or glucose intolerance, type 2 diabetes and cardiovascular disease.

### Claim 6 (depends on 5)

The method of claim 5, wherein a second therapeutic agent for preventing or treating metabolic syndrome or its complication is administered to the subject.

### Claim 7 (depends on 6)

The method of claim 6, wherein the second therapeutic agent is selected from the group consisting of statins, fibrates, nicotinic acid; diuretics, angiotensin-converting enzyme (ACE) inhibitors; metformin, insulin, sulfonylurea (SU), biguanide, α-glucosidase inhibitors and thiazolidinediones (TZDs).