| 摘要 |
The specification describes compounds of the formula I: wherein X is a single bond or a straight or branched, saturated or unsaturated chain containing 1 to 6 carbon atoms, wherein one or more of the carbon atoms are optionally independently replaced with O or S, and wherein one or more of the hydrogen atoms are optionally replaced with F; Y is a single bond, --CH(OH)--, or --C(O)--; R1 is H, an alkyl group, an aryl group, a heteroaryl group, a cycloalkyl group, or a heterocycloalkyl group; R2 is H, an alkyl group, an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, or C(O)R10 wherein R10 is H, an O-alkyl group, an alkyl group, an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, an O-aryl group, an O-alkyl group, or NR11 R12 ; wherein R11 is H, an alkyl group, an O-alkyl group, an aryl group, a heteroaryl group, a cycloalkyl group, or a heterocycloalkyl group, and wherein R12 is H, an alkyl group, an aryl group, a heteroaryl group, a cycloalkyl group, or a heterocycloalkyl group, or wherein R11 and R12 form, together with the nitrogen to which they are attached, a heteroaryl group or a heterocycloalkyl group; and R3 is H, an alkyl group, an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, NR11 R12, or OR11, wherein R11 and R12 are as defined above, or R2 and R3, together with the atom(s) to which they are attached, form a cycloalkyl group or a heterocycloalkyl group; R4 is H or any suitable organic moiety; R5 is C(O)NHOH, C(O)OR13, SH, N(OH)CHO, SC(O)R14, P(O)(OH)R15, or P(O)(OH)OR13 ; R13 is H, an alkyl group, or an aryl group, R14 is an alkyl group or an aryl group, and R15 is an alkyl group; and is a heteroaryl group having five ring atoms, including 1, 2 or 3 heteroatoms selected from O, S, and N. Methods of inhibiting matrix metalloproteinase activity that comprise contacting the protease with an effective amount of a compound of formula I or a pharmaceutically acceptable prodrug or a pharmaceutically acceptable salt or solvate thereof are also described
|
