Claims
- 1. 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.
- 2. The compound according to claim 1 wherein X.sup.3 and X.sup.4 represent tert-butyl.
- 3. The compound according to claim 1 wherein the unsaturated hydrocarbylene chain is 1,3-butadienylene.
- 4. A compound according to claim 1 of the formula: ##STR14## wherein: 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;
- R.sup.9 is selected from the group consisting of hydrogen, lower alkyl, alkanoyl and aroyl; and
- X.sup.3 and X.sup.4 are the same or different tertiary-lower alkyl moieties; and the non-toxic pharmacologically acceptable salts thereof.
- 5. The compound according to claim 4 wherein X.sup.3 and X.sup.4 represent tert-butyl.
- 6. The compound according to claim 4 wherein R.sup.5 and R.sup.6 represent hydrogen.
- 7. The compound according to claim 5 wherein R.sup.9 is hydrogen.
- 8. N-(3,5-Di-tert-butyl-4-hydroxyphenyl)isoindolinone.
- 9. 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.
- 10. The pharmaceutical composition according to claim 9 wherein the active ingredient is a compound in which X.sup.3 and X.sup.4 are tert-butyl.
- 11. A pharmaceutical composition according to claim 9 in which the active ingredient is a compound of the formula: ##STR16## wherein: 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;
- R.sup.9 is selected from the group consisting of hydrogen, lower alkyl, alkanoyl and aroyl; and
- X.sup.3 and X.sup.4 are the same or different tertiary-lower alkyl moieties; or a non-toxic pharmacologically acceptable salt thereof; in combination with a pharmaceutically acceptable carrier.
- 12. The pharmaceutical composition according to claim 11 wherein the active ingredient is a compound in which X.sup.3 and X.sup.4 are tert-butyl.
- 13. The pharmaceutical composition according to claim 12 wherein the active ingredient is a compound in which R.sup.2 and R.sup.4 are joined to form a 1,3-butadienylene chain.
- 14. The pharmaceutical composition according to claim 11 wherein the active ingredient is N-(3,5-di-tert-butyl-4-hydroxyphenyl)isoindolinone.
- 15. 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.
- 16. The method according to claim 15 wherein the active ingredient is administered orally.
- 17. The method according to claim 15 wherein R.sup.2 and R.sup.4 are joined to form a 1,3-butadienylene chain.
- 18. The method according to claim 15 wherein X.sup.3 and X.sup.4 represent tert-butyl.
- 19. The method according to claim 15 wherein the active ingredient is a compound of the formula: ##STR18## wherein: 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;
- R.sup.9 is selected from the group consisting of hydrogen, lower alkyl, alkanoyl and aroyl; and
- X.sup.3 and X.sup.4 are the same or different tertiary-lower alkyl moieties; or a non-toxic pharmacologically acceptable salt thereof.
- 20. The method according to claim 19 wherein the active ingredient is N-(3,5-di-tert-butyl-4-hydroxyphenyl)isoindolinone.
Parent Case Info
This is a division of application Ser. No. 248,942, filed Sep. 26, 1988, U.S. Pat. No. 4,958,482.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4166125 |
Kigasawa et al. |
Aug 1979 |
|
4954514 |
Kita et al. |
Sep 1990 |
|
Divisions (1)
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Number |
Date |
Country |
Parent |
248942 |
Sep 1988 |
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