4-Amino-azepan-3-one derivatives useful as protease inhibitors

摘要

A 4-amino-azepane-3-one derivative or pharmaceutically acceptable salts, hydrates and solvates thereof has the formula (I) wherein: R1 is R4-N(R')-CH(R3)-C(O)-, R5-X-CH(R3)-C(O)- or CH2(R3)- C(O)-; R2 is H, alkyl, cycloalkyl-alkyl, Ar-alkyl, Het-alkyl, R9C(O)-, R9C(S)-, R9SO2-, R9OC(O)-, R9(R11)NSO2-, R9(R11)NC(O)-, R9(R11)NC(S)-, R7-N(R6)-CH(R8)-Z-, pyridyl- phenyl-CH2-CO- or pyridyl-phenyl-(CH2)2-; R3, R4, R' R6 to R9, R11 and R12 are as defined in the specification; R" is H, alkyl, Ar-alkyl, or Het-alkyl; R"' is H, alkyl, cycloalkyl-alkyl, Ar-alkyl or Het-alkyl and X is CH2, S, or O and Z is C (O) or CH2. The compound are useful in treating a disease characterized by bone loss such as osteoporosis, periodontitis or gingivitis or in treating a disease characterized by excessive cartilage or matrix degradation such as osteoarthritis or rheumatoid arthritis