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US 5,290,817 AGranted
Substituted 1-benzylindanes and their use as inhibitors of phospholipase A.sub.2
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorJoseph J. Petraitis
Life of this patent
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Abstract
The invention relates to benzylindane phospholipase 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 benzylindane phospholipase A.sub.2 inhibitor including the representative example: ##STR1##
Claims27
A compound of formula I ##STR74## or a pharmaceutically acceptable salt thereof, wherein:
- R.sup.1 is H, halo, alkyl of 1-4 carbon atoms, OR.sup.3 or CO.sub.2 R.sup.4 ;
- R.sup.2 is H or when R.sup.1 is 6--OR.sup.3, then R.sup.2 may be 5--CO.sub.2 R.sup.4 ;
- X is COR.sup.3, CO.sub.2 R.sup.4, CN, NHR.sup.4, COCH.sub.2 R.sup.5, CHO, CH.sub.2 CHO, CH.sub.2 NH.sub.2, CF.sub.2 CHO, COCF.sub.3, C.sub.1 -C.sub.4 alkyl, halo, ##STR75## Y is H, or when X is --CHO, then Y may be ortho --OH relative to --CHO;
- R.sup.3 is alkyl of 1-4 carbon atoms;
- R.sup.4 is H or alkyl of 1-4 carbon atoms;
- and
- R.sup.5 is Cl, Br, or N.sub.3 ;
- provided that:
- (a) when X is COCH.sub.2 R.sup.5, then neither R.sup.1 nor R.sup.2 is CO.sub.2 H;
- (b) when R.sup.1 is OR.sup.3, then X is not OR.sup.3 ;
- (c) when X is CHO and Y is OH, then R.sup.1 is not OR.sup.3 ;
- (d) neither R.sup.1 nor R.sup.2, except when H, resides at the 7-position;
- (e) when X is CF.sub.2 CHO then neither R.sup.1 nor R.sup.2 is CO.sub.2 R.sup.4 ;
- (f) when R.sup.1 is 6--OR.sup.3 and R.sup.2 is 5--CO.sub.2 R.sup.4, then X is CH.sub.2 CHO, or ##STR76## (g) when R.sup.1 or R.sup.2 is CO.sub.2 R.sup.4 and X is CO.sub.2 R.sup.4, then R.sup.4 is the same in R.sup.1 or R.sup.2 and in X.
11 more elements
Dependencies are inferred from the claim text.