| abstract |
This invention relates to compounds of general formula (I): wherein: (I) A carbonyl or hydroxymethylene piperidine; The formulas R1 are as follows; R 2 is hydrogen, alkyl, cycloalkyl (C 0-6 alkyl), Ar (C 0-6 alkyl), Het (C 0-6 alkyl), R 5 C (O) -, R 5 C (S) -, R5SO2-, R5OC (O) -, R5R'NC (O) -, R5R'NC (S) - adamantylcarbonyl or thorn; R '' is hydrogen, alkyl, Ar (C 0-6 alkyl) or Het (C 0-6 alkyl) piperidine; R '' 'is hydrogen, alkyl, cycloalkyl (C0-6alkyl), Ar (C0-6alkyl) alkyl or Het (C0-6alkyl) piperidine, R3hydrogen atom, alkenyl, alkynyl, Het, Ar or an alkyl moiety which in the precursor is -OR ', -SR', -NR'2, -N (R ') C (O) OR5, -CO2R', -CO2NR'2, Het, Ar or N (C = NH) substituted with NH2 piper; R4 is hydrogen, alkyl, cycloalkyl (C0-6) alkyl, Ar (C0-6 alkyl), Het (C0-6 alkyl), R5C (O) -, R5C (S) - , R5SO2-, R5OC (O) -, R5R'NC (O) -, R5R'NC (S) -, R'HNCH (R ') C (O) - or R5OC (O) NR'CH (R') C (O); R 5 is cycloalkyl (C 0 -C 6 alkyl), Ar (C 0 -C 6 alkyl), Het (C 0 -C 6 alkyl), Ar (C 0 -C 6 alkoxy), Het (0-6) (C 1 -C 6 alkoxy) - or alkyltube optionally optionally -OR ', -SR', -NR'2, -N (R ') C (O) OR 5, -CO 2 R', -CO 2 NR' 2, Het, Ar or N (C). = NH) substituted with NH2 piper; R 6 is hydrogen, alkyl, Ar (C 0 -C 6) alkyl, or Het (C 0 -C 6) alkyl; and R 7 is hydrogen, alkyl, cycloalkyl (C 0 -C 6) alkyl, Ar (C 0 -C 6) alkyl, Het (C 0 -C 6) alkyl, R 5 C (O) -, R 5 C (S) -, R5SO2-, R5OC (O) -, R5R'NC (O) -, R5R'NC (S) -, R'HNCH (R ') C (O) - or R5OC (O) NR'CH (R') C ( O); or R 6 and R 7 form a bonded naphthylpyrrolidine, piperidine or moose ring; R 'is hydrogen, alkyl, Ar (C 0 -C 6 alkyl) or Het (C 0 -C 6 alkyl) piperidine; R * is hydrogen, alkyl, cycloalkyl (C 0-6 alkyl), Ar (C0-6 alkyl) or Het (C0-6 alkyl) piperazin; Single bond or OX; Z is carbonyl or methylene pipette; and n is 0,1 or 2 - and their pharmaceutically acceptable salts. The present invention also relates to pharmaceutical compositions containing the compounds of the general formula (I) as active ingredient. The compounds and pharmaceutical compositions of the present invention are particularly useful for the treatment of pleural diseases in which cysteine proteases, in particular for the treatment of excessive rash and lupus erythematosus such as dandruff, peritonitis and arthritis, play an important role. ŕ |