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US 5,104,874 AGranted
Benzoquinone antiallergy and antinflammatory agents
AssigneePfizer Inc.
InventorsTakafumi Ikeda, Hiroaki Wakabayashi, Masami Nakane
Life of this patent
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Abstract
A series of 2-amino-5,6-dimethyl-1,4-benzoquinone derivatives, inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergic and antiinflammatory agents.
Claims12
A compound of the formula ##STR48## or the pharmaceutically acceptable salts thereof, wherein:
- R.sup.1 is hydrogen, alkyl having one to five carbon atoms, cycloalkyl having three to seven carbon atoms, phenylalkyl having from seven to nine carbon atoms, --COR.sup.4 where R.sup.4 is alkyl having from one to five carbon atoms, phenyl, hydroxy, amino, alkoxy having one to five carbon atoms, omega-carboxyalkyl having two to five carbon atoms, omega-alkoxycarbonylalkyl having from three to eight carbon atoms or --CH(OZ)R.sup.8 where R.sup.8 is hydrogen, alkyl having one to three carbon atoms, omega-carboxyalkyl having two to five carbon atoms or omega-alkoxycarbonyl having three to eight carbon atoms and Z is hydrogen or methoxyethoxymethyl;
- R.sup.2 is hydrogen or phenyl;
- R.sup.3 is (a) cycloalkyl having three to seven carbon atoms, (b) cycloalkylalkyl having five to seven carbon atoms (c) a moiety of the formula ##STR49## wherein m is an integer of 0 to 3 and R.sup.5 and R.sup.6 are each hydrogen, halo, carboxy, carbamoyl, carboalkoxy having two to four carbon atoms, alkoxycarbonylmethyl having three to five carbon atoms, or sulfamoyl or (d) substituted alkyl of the formula R.sup.7 -alkyl wherein said alkyl contains from five to twelve carbon atoms and R.sup.7 is hydroxy, carboxy, carboalkoxy having two to four carbon atoms, hydroxyalkoxy having two to four carbon atoms or furyl;
- and R.sup.2 and R.sup.3 when taken together with the nitrogen atom to which they are attached form a structure of the formula ##STR50##
1 more element
Dependencies are inferred from the claim text.