# US 4,393,053 A · Thiolic derivatives or erythromycin having therapeutic activity and pharmaceutical compositions containing them

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- Number: US 4,393,053 A
- Document ID: US4393053A
- Status: Granted
- Kind: A
- Application number: 06/344,961
- Filed: 1982-02-02
- Granted: 1983-07-12
- Earliest claimed: 1981-02-02
- Assignees: Refarmed S.A.
- Inventors: Jacques Gonella
- Web page: https://patentgrep.com/patent/US4393053A

## CPC

- C07H 17/08: Hetero rings containing eight or more ring members, e.g. erythromycins
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/10: Expectorants
- A61P 31/04: Antibacterial agents
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The thiolic salts of erythromycin and of the propionic ester of erythromycin with thenoyl alpha-mercaptopropionylglycine find therapeutical use in the cases in which erythromycin or its propionic ester are used and are generally endowed with very low toxicity and high hematic levels.

## Claims

### Claim 1

Thiolic derivatives of erythromycin and of the propionic ester of erythromycin having the formula
R--X (1)
wherein R is the radical of thenoyl alpha-mercaptopropionylglycine ##STR3## and X is the radical of erythromycin or of 3'-propionic ester of erythromycin having the formula ##STR4## in which R.sub.1 is H or CH.sub.3 --CH.sub.2 --CO.

### Claim 2 (depends on 1)

The erythromycin salt of thenoyl alpha-mercaptopropionylglycine, according to claim 1.

### Claim 3 (depends on 1)

The erythromycin 3'-propionic acid salt of propionic ester erythromycin with thenoyl alpha-mercaptopropionylglycine according to claim 1.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising as the active ingredient a thiolic derivative according to claim 1 in an amount effective to have an erythromycin activity together with a pharmaceutically acceptable carrier.

### Claim 5 (depends on 1)

A pharmaceutical composition having antibacterial and mucolytic activity containing, as the active ingredient, a thiolic derivative according to claim 1 in an amount effective to have antibacterial and mucolytic activity together with a pharmaceutical acceptable carrier.

### Claim 6 (depends on 5)

A pharmaceutical composition according to claim 5 in the form of a capsule or suspension suitable for oral administration.

### Claim 7 (depends on 5)

A pharmaceutical composition according to claim 5 in a form suitable for administration by the parenteral route or as an aerosol.