Cysteine Protease inhibitors of the Papain superfamily comprising cathepsin K protease inhibitors

摘要

A compound according to formula (I) wherein: R1 is R", R"C(O), R"C(S), R"SO2, R"OC(O), R"R'NC(O), or R"OC(O)NR'CH(R6)C(O); R is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R is H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R4 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; each R5 independently is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R6 is H, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl; R' is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R" is C1-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C2-6alkenyl; or Het-C2-6alkenyl; X is O or S; n is 1,2,or 3; or a pharmaceutically acceptable salt thereof. Also disclosed is the process for the preparation of the above compound and it's use in the treatment of disease in which inhibition of cysteine protease is a factor, inhibition of bone loss, osteoporosis, gingival or periodontal disease, osteoarthritis or rheumatoid arthritis.