# US 7,608,630 B2 · Marasmius androsaceus L.es Fr extract, piperidone derivative, and their use for the preparation of hypertensives

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- Number: US 7,608,630 B2
- Document ID: US7608630B2
- Status: Granted
- Kind: B2
- Application number: 10/587,824
- Filed: 2004-09-29
- Published: 2007-07-12
- Granted: 2009-10-27
- Earliest claimed: 2004-01-30
- Assignees: Hainan Yangpu New Special Pharmaceutical Co., Ltd.; Beijing Toulin Medicine Science and Technology Co.
- Inventors: Jichu Yang; Nan Wang; Xing Yang; Jianping Ren
- Web page: https://patentgrep.com/patent/US7608630B2

## CPC

- C07D 211/46: having a hydrogen atom as the second substituent in position 4
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/12: Antihypertensives
- C07D 211/74: Oxygen atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to Marasmius androsaceus L.es Fr extract, a compound of formula I, or pharmaceutically acceptable salts thereof, and to methods for their preparation, pharmaceutical composition comprising the same as well as use of the extract or the compound in the preparation of a medicament for the prevention and/or treatment of hypertension and its related diseases.

## Claims

### Claim 1

A method for preparing Marasmius androsaceus L.es Fr extract, which comprises extracting fungi Marasmius androsaceus L.es Fr with an organic solvent, an aqueous organic solvent or water, and concentrating the obtained extractive.

### Claim 2 (depends on 1)

The method of claim 1, wherein the organic solvent is methanol, ethanol, propanol, butanol, dichloromethane, trichloromethane, methyl acetate, ethyl acetate, petroleum or diethyl ether.

### Claim 3

A method for preparing a compound of the following Formula I or a pharmaceutically acceptable salt thereof:
wherein,
R1 and each of R2, the same or different, independently represent hydrogen atom or C1-C5 alkyl;
represents a single bond or a double bond, when is a double bond, R3 is oxygen atom; when is a single bond, R3 is hydroxyl group, which comprises extracting fungi Marasmius androsaceus L.es Fr with an organic solvent, an aqueous organic solvent or water to obtain an extract, separating and purifying the extract thereby obtaining a compound monomer of the following Formula II,
and then deriving the compound of Formula I by reacting the compound monomer of Formula II with a calculated amount of alkyl halide under basic condition.

### Claim 4

A method for treating an individual with hypertension comprising administering the compound of the following Formula I to said individual:
wherein,
R1 and each of R2, the same or different, independently represent hydrogen atom or C1-C5 alkyl;
represents a single bond or a double bond, when is a double bond, R3 is oxygen atom; when is a single bond, R3 is hydroxyl group.

### Claim 5

A method for treating an individual with hypertension comprising administering the compound of the following Formula II to said individual:

### Claim 6 (depends on 4)

The method of claim 4 wherein said compound is 1-ethyl-3,3,5,5,-tetramethyl-4-piperidone.

### Claim 7 (depends on 4)

The method of claim 4 wherein said compound is 3,3,5,5-tetramethyl-4-piperidanol.

### Claim 8 (depends on 3)

The method of claim 3 wherein said compound is 1-ethyl-3,3,5,5-tetramethyl-4-piperidone.

### Claim 9 (depends on 3)

The method of claim 3 wherein said compound is 3,3,5,5-tetramethyl-4-piperidanol.