| 摘要 |
<p>This invention relates to compounds of formula (I) wherein: Y is Ar or NR1R2; R1 is R'', R''C(O), R''C(S), R''SO¿2?, R''OC(O), R''R'NC(O), or R''R'NC(S); R?2¿ is H, C¿1-6?alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R?3¿ is H, C¿2-6?alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl optionally substituted by OR', SR', NR'2, N(R')C(O)OR'', CO2R', CO2NR'2, N(C=NH)NH2, Het or Ar; R?4¿ is H, C¿1-6?alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R?5¿ is (a), Ar-C¿0-6?alkyl, Het-C0-6alkyl, adamantyl-C(O)-, Ar-C(O)-, Het-C(O)-; R?6¿ is R'', R''C(O), R''C(S), R''SO¿2?, R''OC(O), R''R'NC(O), R''R'NC(S), or R''OC(O)NR'CH(R*)C(O); R?7¿ is C¿3-6?cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, or C1-6alkyl optionally substituted by OR', SR', NR'2, N(R')C(O)OR'', CO2R', CO2NR'2, N(C=NH)NH2, Het or Ar; R* is H, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl-C0-6-alkyl, Ar-C0-6alkyl, Het-C0-6alkyl; each R' independently is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; each R'' independently is C1-6alkyl, C3-6cycloalkyl-C0-6-alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R''' is H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; Z is C(O) or CH2; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof, which are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor.</p> |
