of the formula (IV): 1
where:
R1=R'C(O), R'SO2,
R'=a bicyclic, saturated or unsaturated, 8-12 membered ring system
containing 0-4 hetero atoms selected from S, O and N, which is optionally
substituted with up to four substituents independently selected from
groups a), b) and c) below; or
R'=a monocyclic, saturated or unsaturated, 5-7 membered ring containing
0-3 hetero atoms selected from S, O and N, which monocyclic ring bears at
least one substituent selected from group a) and/or c) and which may
optionally bear one or two further substituents selected from group b);
R4=H, C1-7-alkyl, Ar--C1-7-alkyl, Ar, C3-7-cycloalkyl; C2-7alkenyl;
R3=C1-7-alkyl, C2-C7 alkenyl, C2-C7 alkenyl, C3-7-cycloalkyl,
Ar--C1-7-alkyl, Ar;
R5=C1-7-alkyl, halogen, Ar--C1-7-alkyl, CO-3-alkyl-CONR3R4 or a bulky
amine
R6 is H, C1-7-alkyl, Ar--C1-7-alkyl, C1-3-alkyl-SO.sub.2-R.sup.ix,
C1-3-alkyl-C(O)--NHR.sup.ix or CH.sub.2XAr
q is 0 or 1
have utility as inhibitors of cysteine proteases such as cathepsin K and
falcipain.
da fórmula (iv): 1 onde: R1=R'C(O), R'SO2, R'=a bicyclic, saturated ou unsaturated, 8-12 membered o sistema do anel que contem 0-4 átomos do hetero selecionados de S, de O e de N, que é substituído opcionalmente com os até quatro substituents selecionados independentemente dos grupos a), b) e c) abaixo; ou R'=a monocyclic, saturated ou unsaturated, 5-7 membered o anel que contem 0-3 átomos do hetero selecionados de S, de O e de N, que o anel monocyclic carrega ao menos um substituent selecionado do grupo a) e/ou c) e que podem opcionalmente carregar um ou dois substituents mais adicionais selecionados do grupo b); R4=H, C1-7-alkyl, Ar -- C1-7-alkyl, Ar, C3-7-cycloalkyl; C2-7alkenyl; R3=C1-7-alkyl, C2-C7 alkenyl, C2-C7 alkenyl, C3-7-cycloalkyl, Ar -- C1-7-alkyl, Ar; R5=C1-7-alkyl, halogênio, Ar -- C1-7-alkyl, CO-3-alkyl-CONR3R4 ou um amine volumoso R6 é H, C1-7-alkyl, Ar -- C1-7-alkyl, C1-3-alkyl-SO.sub.2-R.sup.ix, C1-3-c1-3-alkyl-C(O)-C(O) -- NHR.sup.ix ou CH.sub.2XAr q são 0 ou 1 tem a utilidade como inibidores de proteases do cysteine tais como o cathepsin K e o falcipain.
