C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 235/52 (2006.01) A61K 31/165 (2006.01) A61K 31/195 (2006.01) A61K 31/22 (2006.01) A61K 31/40 (2006.01) A61K 31/495 (2006.01) C07C 235/60 (2006.01) C07C 237/22 (2006.01) C07C 259/06 (2006.01) C07D 207/12 (2006.01) C07D 207/263 (2006.01) C07D 239/50 (2006.01) C07D 295/185 (2006.01) C07D 403/14 (2006.01)
Patent
CA 2099453
ABSTRACT OF THE DISCLOSURE There are disclosed novel N-benzoylamino acid derivatives of the general formula (I), Image ( I ) wherein R1 and R2, which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C1-6 alkoxy group optionally substituted by a phenyl group; R3 represents a hydroxyl group; a C1-10 alkoxy; or a C1-4 alkoxy group optionally substituted by phenoxy group optionally bearing a nitrogen-containing substituent; or an -NR4R5 group, where R4 and R5, which are the same or different, designate hydrogen; a hydroxyl group; a C1-12 alkyl group; a C1-4 alkyl group optionally substituted by a hydroxyl group or an amino group; or R4 and R5 together with the adjacent nitrogen form an optionally substituted 5- or 6-membered heterocyclic group optionally containing an additional nitrogen atom, this heterocyclic group optionally being substituted by an oxo group or an optionally phenyl-substituted C1-4 alkyl group or a C3-5 alkenyl group; and R4 and R5 together represent piperazine, the latter may also be substituted by a diaminopyrimidinyl or di(pyrrolidino)-pyrimidinyl group; and n means an integer from 2 to 15 with the proviso that when R3 represents a hydroxyl group and n is 5, as well as one of R1 and R2 is a 4-hydroxyl group, then the other one of R1 and R2 is different from a 3-hydroxyl or 3-methoxy group; and when n is 2 or 3, then R1 and R2 cannot simultaneously stand for a 2- and a 3-methoxy group, as well as their tautomers, racemates and optically active 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 the compounds of 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 which are indirect by or direct by connected with pathological oxidation processes, and mainly 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.
Andrasi Ferenc
Farkas Lajos
Fittler Zsuzsanna
Gal Eva
Goldschmidt Katalin
Nisshin Flour Milling Co. Ltd.
Swabey Ogilvy Renault
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