Piperidine and pyrrolidine derivatives, process for their preparation, pharmaceutical compositions comprising them and their use

摘要

Piperidine and pyrrolidine derivatives of formula (I) wherein A is C(O) or CH(OH); R1 is a group of formula (a), (b), (c) or (d); R2 is H, C1-6alkyl optionally substituted independently by one or two halogens, SR, OR, N(R)2, C(O)N(R)2, carbamyl or C1-4alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R5C(O)-, R5C(S)-, R5SO2-, R5OC(O)-, R5R'NC(O)-, R5R'NC(S)-, R'HNCH(R')C(O)-, R5OC(O)NR'CH(R')C(O)-, adamantyl-C(O)- or a group of formula (e); R'' is H, C1-6alkyl optionally substituted independently by one or two halogens, SR, OR, N(R)2, C(O)N(R)2, carbamyl or C1-4alkyl, Ar-C0-6alkyl or Het-C0-6alkyl; R''' is H, C1-6alkyl optionally substituted independently by one or two halogens, SR, OR, N(R)2, C(O)N(R)2, carbamyl or C1-4alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl; and n is 0, 1 or 2. The compounds of formula (I) are inhibitors of cysteine proteases, particularly of cathepsin K, and are suitable for use in the treatment of diseases characterised by bone loss. Processes for preparing compounds of formula (I), their use for the manufacture of medicaments and pharmaceutical compositions comprising them are also described.