# US 4,039,544 A · Azapurinones

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- Number: US 4,039,544 A
- Document ID: US4039544A
- Status: Granted
- Kind: A
- Application number: 05/680,444
- Filed: 1976-04-26
- Granted: 1977-08-02
- Earliest claimed: 1970-12-15
- Assignees: May & Baker Limited
- Inventors: Barbara Joyce Broughton; Bryan John Large; Stuart Malcolm Marshall; David Lord Pain; Kenneth Robert Harry Wooldridge
- Web page: https://patentgrep.com/patent/US4039544A

## CPC

- C07D 239/47: One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
- C07D 239/46: Two or more oxygen, sulphur or nitrogen atoms
- C07D 239/48: Two nitrogen atoms
- C07D 487/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The invention provides certain novel 8-azapurin-6-one derivatives substituted in the 2-position by a substituted phenyl group, preferably carrying an alkoxy in the 2-position, which possess valuable pharmacological properties especially in the treatment of respiratory disorders manifested by the interaction of tissue-fixed antibodies with specific antigens.

## Claims

### Claim 1

An 8-azapurin-6-one of the formula: ##STR17## wherein R.sup.3 is straight- or branched-chain alkoxy of from 1 to 4 carbon atoms and R.sup.1 is alkylthio of 1 to 6 carbon atoms, alkylsulphinyl of 1 to 6 carbon atoms, alkylsulphonyl of 1 to 6 carbon atoms, or alkoxycarbonyl of 2 to 7 carbon atoms, and pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(5-ethoxycarbonyl-2-propoxyphenyl)purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(5-methoxycarbonyl-2-propoxyphenyl)purin6-one or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(5-butoxycarbonyl)-2-propoxyphenyl)purin6-one or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-propylsulphonylphenyl)purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-methylsulphonylphenyl)purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-t-butylsulphonylphenyl)purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-t-butylthiophenyl)purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 9 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-t-butylsulphinylphenyl)-purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 10 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-isopropylsulphonylphenyl)-purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 1)

An 8-azapurin-6-one according to claim 1 which is 8-aza-2-(2-propoxy-5-isobutylsulphonylphenyl)-purin-6-one or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 1)

The 8-azapurin-6-one according to claim 1 which is the triethanolamine salt of 8-aza-2-(2-propoxy-5-propylsulphonylphenyl)purin-6-one.

### Claim 13 (depends on 1)

The 8-azapurin-6-one according to claim 1 which is the triethanolamine salt of 8-aza-2-(5-butoxy-carbonyl-2-propoxyphenyl)purin-6-one.