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US 5,328,901 AGranted
Bis-arylphosphate ester antagonists of platelet activating factor
AssigneeAmerican Cyanamid Company
InventorsAllan Wissner, Kenneth Green, Robert E. Schaub
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Abstract
The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.
Claims10
A method of treating a malady selected from the group consisting of asthma, anaphylactic and septic shock, adult respiratory distress, transplant rejection, thrombosis, stroke and cardiac anaphylaxis in a mammal which comprises administering to the mammal an effective amount of a compound of the formula:
- ##STR12## wherein:
- X is a phenyl or naphthyl ring optionally substituted in any position with one to five substituents on the phenyl group and one to seven substituents to the naphthyl group of:
- (i) --R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, C.sub.1 -C.sub.25 alkoxy, C.sub.1 -C.sub.25 thioalkyl, C.sub.1 -C.sub.25 alkenyloxy, phenyl, phenoxy, substituted phenyl or substituted phenoxy wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen or trifluoromethyl;
- (ii) hydrogen halogen, trifluoromethyl, cyano and nitro;
- (iii) --CO.sub.2 R.sub.3, --CONHR.sub.3, --CHO, OCONHR.sub.3, and --NHCOR.sub.3
- wherein R.sub.3 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, phenyl or substituted phenyl wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen or trifluoromethyl;
- R.sub.1 is one or more substituents of the aromatic ring which may be in any position and are hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or halogen;
- --CH.sub.2 --Y is a single substituent or the aromatic ring which may occupy any position wherein Y is ##STR13## wherein R.sub.4 represents one or more substituents of the heterocyclic ring which may occupy a non-hetero atom position and is C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or hydrogen and;
- n is the integer 0 to 1.
6 more elements
Dependencies are inferred from the claim text.