Back to results
US 5,962,529 AGranted
Metalloproteinase inhibitors
AssigneeBritish Biotech Pharmaceuticals Limited
InventorsAndrew Miller, Mark Whittaker, Raymond Paul Beckett
Life of this patent
Estimating the term…
Abstract
Compounds of general formula (II) wherein X is a hydroxamic or carboxylic acid group, Y is carbonyl or sulphonyl and R.sub.1 and R.sub.2 are as defined in the claims, are matrix metalloproteinase inhibitors. ##STR1##
Claims11
A compound of formula (II) ##STR44## wherein R.sub.1 is selected from the group consisting of (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, phenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, substituted phenyl(C.sub.1 -C.sub.6)alkyl, amino(C.sub.1 -C.sub.6)alkyl;
- hydroxy-(C.sub.1 -C.sub.6)alkyl, mercapto(C.sub.1 -C.sub.6)alkyl and carboxy(C.sub.1 -C.sub.6)alkyl wherein the amino-, hydroxy-, mercapto-, or carboxyl-group is optionally protected or the carboxyl-group amidated;
- R.sub.2 represents (i) a group Z.sup.1 --Q--W--, or (ii) (Z.sup.1 --Q--W--).sub.2 CH-- in which each of the two groups Z.sup.1 --Q--W-- present may be the same or different, and wherein in both cases (i) and (ii):
- Z.sup.1 represents hydrogen or an optionally substituted aryl, cycloalkyl, or cycloalkenyl group, and
- --Q--W-- taken together represent a bond, or
- Q represents a bond or --O-- or --S-- and W represents a divalent C.sub.1 -C.sub.20 straight or branched alkyl or C.sub.2 -C.sub.20 alkenyl group which
- (a) may be interrupted by one or more non-adjacent ether or thioether linkages or --N(R.sub.x)-- groups wherein R.sub.x is hydrogen, or C.sub.1 -C.sub.6 alkyl, and/or
- (b) may carry one or more substituents selected from the group consisting of --OH, --SH, --O(Alk), --S(Alk), halogen, --NH2, --NH(Alk), --N(Alk).sub.2, --CO.sub.2 H, --CO.sub.2 (Alk), --CO(Alk), --CHO, --CHONH.sub.2, --CONH(Alk), --CON(Alk).sub.2, --(Alk)OH, --(Alk)SH, and --NHCO(Alk) where Alk represents C.sub.1 -C.sub.6 alkyl;
- z represents a group Z.sup.1 --Q--W-- wherein Z.sup.1 represents hydrogen or an optionally substituted cycloalkyl, or cycloalkenyl group and Q represents a bond or --O-- or --S-- and W represents a bond or --O-- or --S-- and W represents a divalent C.sub.1 -C.sub.20 straight or branched alkyl or C.sub.2 -C.sub.20 alkenyl group which
- (a) may be interrupted by one or more non-adjacent ether or thioether linkages or --N(R.sub.x)-- groups wherein R.sub.x is hydrogen, or C.sub.1 -C.sub.6 alkyl, and/or
- (b) may carry one or more substituents selected from the group consisting of --OH, --SH, --O(Alk), --S(Alk), halogen, --NH.sub.2, --NH(Alk), --N(Alk).sub.2, --CO.sub.2 H, --CO.sub.2 (Alk), --CO(Alk), --CHO, --CHONH.sub.2, --CONH(Alk), --CON(Alk).sub.2, --(Alk)OH, --(Alk)SH, and --NHCO(Alk) where Alk represents C.sub.1 -C.sub.6 alkyl;
- or a salt, hydrate or solvate thereof.
8 more elements
A compound selected from the group consisting of
- N-Hydroxy-2-((2-methoxy-benzyl)-(octane-1-sulfonyl)-amino)-acetamide;
- 2-((2-Ethoxy-benzyl)-(octane-1-sulfonyl)-amino)-N-Hydroxy-acetamide;
- N-Hydroxy-2-((naphthalen-2-yl-methyl)-(octane-1-sulfonyl)-amino)-acetamide;
- 2-((4-Chloro-benzyl)-(octane-1-sulfonyl)-amino)-N-hydroxy-acetamide;
- and salts, solvates or hydrates thereof.
2 more elements
Dependencies are inferred from the claim text.