Fused ring heterocycles and pharmaceutical compositions containing same
AssigneeBiofor, Ltd.
InventorSung J. Lee
Life of this patent
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Abstract
A novel class of pyrrolidin-2-one and piperidin-2-one compounds in which the nitrogen atom is bonded to an oxyphenyl radical having tertiary-alkyl and tri-methylsilyl substituents. The compounds possess anti-inflammatory, immunomodulatory, analgesic and anti-pyretic activity and they may be combined with excipients to provide formulations which are useful in treating arthritis and conditions associated with that disease.
Claims20
A compound of the formula:
- ##STR13## wherein:
- R is a member selected from the group consisting of hydrogen, alkyl, alkanoyl and aroyl;
- R.sup.2 and R.sup.4 are joined to form an unsaturated hydrocarbylene chain having four carbon atoms between their points of attachment to the heterocyclic ring;
- R.sup.5 and R.sup.6 are the same or different and represent a member selected from the group consisting of hydrogen and lower alkyl;
- and
- X.sup.3 and X.sup.4 are the same or different and represent a member selected from the group consisting of tertiary-alkyl and trimethylsilyl;
- and the non-toxic pharmacologically acceptable salts thereof.
N-(3,5-Di-tert-butyl-4-hydroxyphenyl)isoindolinone.
A pharmaceutical composition comprising as the active ingredient a compound of the formula:
- ##STR15## wherein:
- R is a member selected from the group consisting of hydrogen, alkyl, alkanoyl and aroyl;
- R.sup.2 and R.sup.4 are joined to form an unsaturated hydrocarbylene chain having four carbon atoms between their points of attachment to the heterocyclic ring;
- R.sup.5 and R.sup.6 are the same or different and represent a member selected from the group consisting of hydrogen and lower alkyl;
- and
- X.sup.3 and X.sup.4 are the same or different and represent a member selected from the group consisting of tertiary-alkyl and trimethylsilyl;
- or a non-toxic pharmacologically acceptable salt thereof;
- in combination with a pharmaceutically acceptable carrier.
A method for treating inflammation in a mammal which comprises administering a safe and effective amount of an active ingredient of the formula:
- ##STR17## wherein:
- R is a member selected from the group consisting of hydrogen, alkyl, alkanoyl and aroyl;
- R.sup.2 and R.sup.4 are joined to form an unsaturated hydrocarbylene chain having four carbon atoms between their points of attachment to the heterocyclic ring;
- R.sup.5 -R.sup.6 are the same or different and represent a member selected from the group consisting of hydrogen and lower alkyl;
- and
- X.sup.3 and X.sup.4 are the same or different and represent a member selected from the group consisting of tertiary-alkyl and trimethylsilyl;
- or a non-toxic pharmacologically acceptable salt thereof.
Dependencies are inferred from the claim text.