MATRIX METALLOPROTEASE INHIBITORS

摘要

COMPOUNDS OF THE FORMULA: WHEREIN: N IS 0, 1 OR 2; Y IS HYDROXY OR XONH-, WHERE X IS HYDROGEN OR LOWER ALKYL; R1 IS HYDROGEN OR LOWER ALKYL; R2 IS HYDROGEN, LOWER ALKYL, HETEROALKYL, ARYL, ARALKYL, ARYLHETEROALKYL, CYCLOALKYL, CYCLOALKYLALKYL, HETEROARYL, HETEROARALKYL, HETEROARYLHETEROALKYL, HETEROCYCLO, HETEROCYLO-LOWER ALKYL, HETEROCYCLO-LOWER HETEROALKYL OR -NR6R7, WHEREIN: R6 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL OR CYCLOALKYLALKYL, ARYL, HETEROARYL AND HETEROARALKYL; R7 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL OR CYCLOALKYLALKYL, ARYL, ARALKYL, HETEROARYL, HETEROARALKYL, -C(O)R8, -C(O)NR8R9, -SO2NR8R9, -SO2R10, ARYLOXYCARBONYL, OR ALKOXYCARBONYL; OR R6 AND R7 TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED REPRESENT A HETEROCYCLO GROUP; WHEREIN R8 AND R9 ARE INDEPENDENTLY HYDROGEN, LOWER ALKYL, CYCLOALKYL, CYCLOALKYLALKYL, ARYL, ARALKYL, HETEROARYL, HETEROARALKYL OR HETEROALKYL; AND R10 IS LOWER ALKYL, CYCLOALKYL, CYCLOALKYLALKYL, ARYL, ARALKYL, HETEROARYL, HETEROARALKYL, HETEROALKYL OR HETEROCYCLO; OR R1 AND R2 TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED REPRESENT A CYCLOALKYL OR HETEROCYCLO GROUP; R3 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL, CYCLOALKYLALKYL, ARYL, ARALKYL, HETEROARY1, HETEROARALKY1, HETEROALKY1 OR LOWER ALKOXY; R4 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL OR CYCLOALKYLA1KY1; OR R2 AND R3 TOGETHER WITH THE CARBONS TO WHICH THEY ARE ATTACHED REPRESENT A CYCLOALKYL OR HETEROCYCLO GROUP; OR R3 AND R4 TOGETHER WITH THE CARBON TO WHICH THEY ARE ATTACHED REPRESENT A CYCLOA1KY1 OR HETEROCYCLO GROUP; AND R5 IS 1OWER ALKYL, CYCLOA1KY1, CYCLOALKYLALKY1, ARYL, ARALKYL, HETEROARYL, OR HETEROARALKYL; OR PHARMACEUTICA1LY ACCEPTABLE SALTS OR ESTERS THEREOF EXHIBIT USEFUL PHARMACOLOGICAL PROPERTIES, IN PARTICULAR FOR USE AS MATRIX METALLOPROTEASE INHIBITORS, PARTICULARLY FOR INTERSTITIAL COLLAGENASES.