Aromatic N-heterocycle derivatives for use as medicine

摘要

The invention relates to compounds, or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal thereof, wherein said compound is of formula A-B (I) wherein A is substitued or not aromatic N-heterocycle; and B is -[C(R 1 )(R 2 )] n -R 3 wherein n is an integer between 1 and 10, R 1 and R 2 represent independently in each of the n units a substituent selected from the group consisting of hydrogen, substituted or not C 1 -C 10 alkyl, halogen, oxy derivatives, thioderivatives, substituted or not C 3 -C 10 cycloalkyl, substituted or not C 6 -C 18 aryl, substituted or not C 2 -C 10 alkenyl, substituted or not C 2 -C 10 alkynyl, R 3 represents a substituent selected from the group consisting of hydrogen, substituted or not C 1 -C 10 alkyl, halogen, substituted or not C 3 -C 10 cycloalkyl, substituted or not C 6 -C 18 aryl, substituted or not C 2 -C 10 alkenyl, substituted or not C 2 -C 10 alkynyl, amino, heterocycle, thiocyanate, thio derivatives, hydroxylamine, amido, sulfonamide, amino sulfone derivatives, ether, thioether, ester, thioester, azido, azo, cyano, nitro, nitrooxy, carbamate, thiocarbamate, sulfinyl derivative, sulfonyl derivatives, acyl derivatives, oxy derivatives, ureido, thioureido, imino, oximino, hydrazino, thioamido, carboxylic, phosphate, phosphonate, carbamoyl phosphate; with the proviso that when A is 5-fluoroindole, B is bonded at position 3 of the 5-fluoroindole moiety, R 1 is hydrogen and n is between 2 and 10, R 3 is not -NR 4 R 5 wherein R 4 and R 5 independently represent a substituent selected from the group consisting of hydrogen, C 1 -C 10 alkyl, C 3 -C 10 cycloalkyl, aminoalkyl, or R 4 and R 5 taken together with the nitrogen atom to which they are attached to form a four to ten-membered heterocycle, and R 2 is not independently in each of the n units a substituent selected from the group consisting of hydrogen, C 1 -C 10 alkyl, halogen, alkoxy, aminoalkyl, and alkylamino; for the treatment or the prophylaxis of neurologic and/or inflammatory diseases or disorders. The present invention also provides pharmaceutical composition and in vitro method for inhibiting myeloperoxidase enzyme activity or low density lipoproteins oxidation.