# US 5,705,529 A · N-benzoyl amino acid derivatives pharmaceutical compositions containing them and process for preparing same

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- Number: US 5,705,529 A
- Document ID: US5705529A
- Status: Granted
- Kind: A
- Application number: 08/540,924
- Filed: 1995-10-11
- Granted: 1998-01-06
- Earliest claimed: 1992-06-30
- Assignees: Gyogyszerkutato Intezet Kft.
- Inventors: Peter Matyus; Erzsebet Zara; Lajos Farkas; Agnes Papp; Antal Simay; Lajos Toldy; Ferenc Andrasi; Katalin Goldschmidt; Eszter Hodula; Ildiko Mathe; Klara Sutka; Zsuzsanna Fittler; Valeria Vitkoczi; Laszlo Sebestyen; Istvan Sziraki; Marta Rusz; Eva Gal
- Web page: https://patentgrep.com/patent/US5705529A

## CPC

- C07D 207/27: with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- A61P 3/06: Antihyperlipidemics
- C07C 235/60: having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C 237/22: having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated (peptides C07K)
- C07C 259/06: having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
- C07D 239/50: Three nitrogen atoms
- C07D 295/185: from aliphatic carboxylic acids
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The invention relates to novel N-benzoylamino acid derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C.sub.1-6 alkoxy group optionally substituted by a phenyl group; n means an integer from 2 to 15 as well as their tautomers, racemates and optically active individual (pure) isomers or mixtures thereof and the salts of these compounds and pharmaceutical compositions containing these compounds. The invention relates also to a process for the preparation of compounds of the general formula (I). The compounds of general formula (I) inhibit the peroxidation of lipids and therefore, they are expected to be useful for the treatment of diseases being in an indirect or direct connection with pathological oxidation processes, chiefly for the treatment and/or prevention of ischaemic and reperfusion tissue injuries, inflammatory reactions, atherosclerosis, various degenerative neurological disorders as well as for delaying the natural process of the ageing of cells.

## Claims

### Claim 1

An N-Benzoylamino acid compound of the formula (I), ##STR12## or a pharmaceutically acceptable salt thereof wherein
R.sup.3 is selected from the group consisting of a hydroxyl group and a C.sub.1 -C.sub.10 alkoxy group; and
n is an integer from 10 to 15.

### Claim 2 (depends on 1)

A pharmaceutical composition for the treatment of patients suffering from disorders being in an indirect or direct connection with pathological oxidation process occuring in an organism, which comprises a therapeutically effective amount of a compound as defined in claim 1, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.

### Claim 3 (depends on 2)

A pharmaceutical composition according to claim 2 wherein the disorders are ischaemic and reperfusion injuries, inflammations, atherosclerosis, or degenerative neurological disorders.