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US 5,039,706 AGranted
Antiinflammatory PLA.sub.2 inhibitors
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorWendell W. Wilkerson
Life of this patent
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Abstract
The invention relates to benzylamine phosphilipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylamine phospholipase A.sub.2 inhibitor.
Claims51
A substituted benzylamine phospholipase A.sub.2 inhibitor of the formula:
- ##STR155## or a pharmaceutically acceptable salt thereof, wherein Ar is ##STR156## and Z is H, F, Cl, Br, --OR.sup.1, or --S(O).sub.m R.sup.1, where R.sup.1 is H, --CH.sub.3, or --C.sub.2 H.sub.5, and m is 0, 1, or 2;
- n is 1 to 5;
- X is NH;
- and
- R is C.sub.7 -C.sub.25 alkyl, or a mono- or polycyclic benzoid aromatic system of the formula:
- ##STR157## where W is C.sub.1 -C.sub.20 alkyl, F, Cl, Br, --OR.sup.2, --S(O).sub.q R.sup.2, --C(CF.sub.3).sub.2 OH, or phenyl, and R.sub.2 is --CH.sub.3 or --C.sub.2 H.sub.5, and q is 0, 1, or 2;
- or
- R is benzhydryl, alkaryl or substituted alkaryl of 7 to 25 carbon atoms, where the substitution is on the aromatic moiety, and is F, Cl, Br, --OR.sup.3, --S(O).sub.r R.sup.3, or C.sub.1 -C.sub.10 alkyl, where R.sup.3 is --CH.sub.3 or --C.sub.2 H.sub.5, and r is 0, 1, or 2;
- provided that:
- a) when Z is H, X is NH, and n is 2, then R cannot be benzhydryl;
- b) when X is NH, then R cannot be phenyl or benzyl.
8 more elements
Dependencies are inferred from the claim text.