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US 5,877,200 AGranted
Cyclic amides
AssigneeCelgene Corporation
InventorGeorge W. Muller
Life of this patent
Estimating the term…
Abstract
Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.
Claims33
A compound of the formula:
- ##STR11## in which:
- n has a value of 1, 2, or 3;
- R.sup.5 is vic-naphthylene unsubstituted or substituted with 1 to 4 substituents each selected independently from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkylamino, dialkylamino, acylamino, alkyl of 1 to 10 carbon atoms, alkyl of 1 to 10 carbon atoms, alkoxy of 1 to 10 carbon atoms, and halo;
- R.sup.6 is CO or CH.sub.2 ;
- R.sup.7 is (i) phenyl or phenyl substituted with one or more substituents each selected independently of the other from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl of 1 to 10 carbon atoms, alkoxy of 1 to 10 carbon atoms, and halo, (ii) benzyl unsubstituted or substituted with 1 to 3 substituents selected from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl of 1 to 10 carbon atoms, alkoxy of 1 to 10 carbon atoms, and halo, (iii) naphthyl, and (iv) benzyloxy;
- R.sup.12 is --OH, alkoxy of 1 to 12 carbon atoms, or ##STR12## R.sup.8' is hydrogen or alkyl of 1 to 10 carbon atoms;
- and R.sup.9' is hydrogen, alkyl of 1 to 10 carbon atoms, --COR.sup.10, or --SO.sub.2 R.sup.10 in which
- R.sup.10 is hydrogen, alkyl of 1 to 10 carbon atoms, or phenyl.
5 more elements
Dependencies are inferred from the claim text.