PEPTIDYL COMPOUNDS AND THEIR THERAPEUTIC USE AS INHIBITORS OF METALLOPROTEINASES

摘要

A compound of formula (I), wherein R<1> is C1-6 alkyl, C2-6 alkenyl, aryl, (C1-6 alkyl)aryl or C1-6 alkyl-AR<9> where A is O, NR<9> or S(O)m, where m = 0-2, and the or each R<9> is H, C1-4 alkyl, aryl or (C1-4 alkyl)aryl; R<2> is H or C1-6 alkyl; either R<4> is H or C1-6 alkyl optionally substituted by amino (NH2), arylamino, protected amino, aryl, di(C1-6 alkyl)amino, mono(C1-6 alkyl)amino, CO2H, protected carboxyl, carbamoyl, mono(C1-6 alkyl)carbamoyl or di(C1-6 alkyl)carbamoyl, and R<5> is H or C1-6 alkyl, or NR4R5 is pyrrolidino, piperidino or morpholino; R<6> is optionally-substituted C3-6 cycloalkyl, C3-6 cycloalkenyl, C1-6 alkyl, benzyl, (C1-6 alkoxy)benzyl, benzyloxybenzyl or 3-indolylmethyl; Alk is C1-6 alkyl or C2-6 alkenyl and n = 0 or 1; R<7> is H or R<10>CO where R<10> is C1-4 alkyl, (C1-4 alkyl)aryl, C3-6 cycloalkyl, (C3-6 cycloalkyl)C1-4 alkyl, C2-6 alkenyl or (C2-6 alkenyl)aryl; and R<8> is H, C1-4 alkyl, (C1-4 alkyl)aryl or aryl; or a salt, solvate or hydrate thereof. Such compounds may be used to treat conditions associated with metalloproteinase, TNF and/or other activity.