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US 5,872,146 AGranted
Mercapto alkyl peptidyl compounds having MMP and TNF inhibitory activity
AssigneeChiroscience Limited
InventorsAndrew Douglas Baxter, John Gary Montana, David Alan Owen
Life of this patent
Estimating the term…
Abstract
Described herein are compounds of formula (I): ##STR1## which have MMP and TNF inhibitory activity.
Claims22
A compound of general formula (I):
- ##STR9## wherein:
- R.sup.1 is selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, (C.sub.1-6 alkyl)aryl, aryl, and C.sub.1-6 alkyl-AR.sup.9 where A is selected from the group consisting of O, NR.sup.9, and S(O).sub.m where m=0-2, and R.sup.9 is selected from the group consisting of H, C.sub.1-4 alkyl aryl, and (C.sub.1-4 alkyl)aryl;
- if A=NR.sup.9 the R.sup.9 groups may be the same or different;
- R.sup.2 is selected from the group consisting of hydrogen and C.sub.1-6 alkyl;
- R.sup.3 is selected from the group consisting of C.sub.1-6 alkyl-R.sup.6, aryl-R.sup.6, cyclo(C.sub.3-6)alkyl-R.sup.6, C.sub.1-6 alkyl-aryl-R.sup.6, and C.sub.1-6 alkyl-cyclo (C.sub.3-6) alkyl-R.sup.6, and R.sup.6 is an amidino or guanidino group;
- X is NR.sup.4 R.sup.5 where R.sup.4 is selected from the group consisting of hydrogen, aryl, cyclo(C.sub.3-6)alkyl, and C.sub.1-6 alkyl-cyclo(C.sub.3-6)alkyl;
- and R.sup.5 is hydrogen or C.sub.1-6 alkyl;
- or NR.sup.4 R.sup.5 is a ring;
- R.sup.7 is hydrogen or R.sup.10 CO where R.sup.10 is selected from the group consisting of C.sub.1-4 alkyl, C.sub.1-4 alkylaryl, cyclo(C.sub.3-6)alkyl, C.sub.1-4 alkyl-cyclo(C.sub.3-6)alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkenyl-aryl, and aryl;
- R.sup.8 is C.sub.1-4 alkyl-R.sup.11 ;
- R.sup.11 is phthalimido;
- R.sup.12 is hydrogen or is selected from the group consisting of COR.sup.9, CO.sub.2 R.sup.9 (where R.sup.9 is not H), CONHR.sup.9, and SO.sub.2 R.sup.9 (where R.sup.9 is not H);
- and
- R.sup.13 is selected from the group consisting of OH, OC.sub.1-4 alkyl, aryl, and C.sub.1-4 alkylaryl;
- or a salt, solvate, or hydrate thereof.
12 more elements
Dependencies are inferred from the claim text.