# US 2013/0158065 A1 · 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine, the preparation method and medical use thereof

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- Number: US 2013/0158065 A1
- Document ID: US20130158065A1
- Status: Published application
- Kind: A1
- Application number: 13/700,395
- Filed: 2011-09-02
- Published: 2013-06-20
- Earliest claimed: 2010-09-10
- Assignees: Jiangsu Shen Er Yang High Technology Co., Ltd; Changchun Huayang High Technology Co., Ltd
- Inventors: Tonghui Wang
- Web page: https://patentgrep.com/patent/US20130158065A1

## CPC

- C07D 219/10: attached in position 9
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/06: Antiarrhythmics
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Disclosed are 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine and the salt thereof, as well as the preparation method and medical use thereof. The compound can be useful for the preparation of medicaments for treating cardiovascular diseases, especially arrhythmia.

## Claims

### Claim 1

1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine comprising the following structural formula, and a pharmaceutical acceptable salt thereof:
molecular formula: C21H24N2O.H2O; molecular weight: 338.20; melting point (° C.): 234-236.

### Claim 2 (depends on 1)

The pharmaceutical acceptable salt according to claim 1, wherein the pharmaceutical acceptable salt is hydrochloride and comprises the following structural formula:
molecular formula: C21H24N2O.HCL.0.5H2O; molecular weight: 356.90; melting point (° C.) 231-234.

### Claim 3 (depends on 1)

A method for preparing the 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine according to claim 1, comprising:
weighting 5.0 g of 9-amino-1,2,3,4,5,6,7,8-octohydroacridine and 3.36 g of phenylacetic acid, and adding the same to a reaction bottle;
adding 25 ml polyphosphoric acid to the reaction bottle to provide a mixture;
heating the mixture to a temperature of 110-130° C. and allowing to react for 5 hours;
adding about 1000 ml water after the reaction;
adjusting pH to pH 5-6 with a KOH solution to generate a white precipitate;
filtering off and drying the white precipitate;
recrystallizing the white precipitate with methanol and acetone; and
filtering off the recrystallized precipitate to generate 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine.

### Claim 4 (depends on 2)

A method for preparing the hydrochloride of 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine according to claim 2, comprising:
dissolving 1.0 g of 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine in a minimal amount of HCL-methanol solution to provide a first solution;
adding diethyl ether to the first solution to generate a white precipitate; and
filtering off and drying the white precipitate at 90° C. to generate a white crystal, comprising the hydrochloride of 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine.

### Claim 5

(canceled)

### Claim 6

(canceled)

### Claim 7 (depends on 1)

A method of treating an arrhythmia disease in a subject in need of such treatment comprising:
administering a composition comprising 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine according to claim 1 to the subject.

### Claim 8 (depends on 2)

A method of treating an arrhythmia disease in a subject in need of such treatment comprising:
administering a composition comprising the pharmaceutical acceptable salt according to claim 2 to the subject.