16,17-Pyrazolino- and 16,17-isopyrazolino-1,4-pregnadiene derivatives
AssigneeLark S.p.A.
InventorsGaetano Palladino, Mario Micciarelli
Life of this patent
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Abstract
New 16,17-pyrazolino- and 16,17-isopyrazolino-1,4-pregnadiene-derivatives have been prepared, useful as antiinflammatory agents on topical and/or systemic administration. An analogy process for the preparation of 16,17-pyrazolino-1,4-pregnadiene derivatives and the quite surprising conversion of the latter ones to 16,17-isopyrazolino-1,4-pregnadiene derivatives are also disclosed. The results of pharmacological comparative trails of some new products of the present invention v. fluocinolone acetonide are reported.
Claims13
A pharmaceutical composition for treating inflammation and rheumatism comprising
- a pharmaceutically effective amount of a compound of the formula:
- ##STR6## wherein A is selected from the group consisting of H, Br, and Cl;
- X is selected from the group consisting of H, F, or Cl;
- Y is selected from the group consisting of .beta.-OH, keto, or Cl;
- Z is selected from the group consisting of .alpha.-F, .beta.-F, and .alpha.-CH.sub.3 ;
- and
- R is H or an acyl residue selected from the group consisting of a mono- or dicarboxylic organic acid having 2 to 8 carbon atoms, methasulfobenzoic acid, and phosphoric acid, admixed with a pharmaceutically acceptable carrier for topical, intraarticular, and systemic administration.
16.alpha.,17.alpha.-Pyrazolino-1,4-pregnadiene-6.alpha.,9.alpha .-difluoro-11.beta.,21-diol-3,20-dione-21-acetate.
16.alpha.,17.alpha.-Isopyrazolino-1,4-pregnadie ne-6.alpha.,9.alpha.-difluoro-11.beta.,21-diol-3,20-dione-21-acetate.
16.alpha.,17.alpha.-Pyrazolino-1,4-pregnadiene-11.beta.,21-diol-3, 20-dione, 21-acetate.
16.alpha.,17.alpha .-Isopyrazolino-1,4-pregnadiene-11.beta.,21-diol-3,20-dione-21-acetate.
16.alpha.,17.alpha.-Isopyrazolino-1,4-pregnadiene-6.alpha.,9.alpha.- difluoro-11.beta.,21-diol-3,20-dione.
16.alpha.,17.alpha.-Isopyrazolino- 1,4-pregnadiene-6.alpha.,9.alpha.-difluoro-11.beta.,21-diol-3,20-dione-21-b utyrate.
16.al pha.,17.alpha.-Isopyrazolino-1,4-pregnadiene-6.alpha.,9.alpha.-difluoro-11. beta.,21-diol-3,20-dione-21-valerate.
16.alpha.,17.alpha.-Isopyrazolino- 1,4-pregnadiene-6.alpha.,9.alpha.-difluoro-11.beta.,21-diol-3,20-dione-21-p ivalate.
A pharmaceutical composition for treating inflammation and rheumatism comprising
- a pharmaceutically effective amount of a compound of the formula:
- ##STR7## wherein A is selected from the group consisting of H, Br, and Cl;
- X is selected from the group consisting of H, F, or Cl;
- Y is selected from the group consisting of .beta.--OH, keto, or Cl;
- Z is selected from the group consisting of H, .alpha.-F, .beta.-F, and .alpha.-CH.sub.3 ;
- and
- R is H or an acyl residue selected from the group consisting of a mono- or dicarboxylic organic acid having 2 to 8 carbon atoms, methasulfobenzoic acid, and phosphoric acid, admixed with a pharmaceutically acceptable carrier for topical, intraarticular, and systemic administration.
A method for treating inflammation in a patient experiencing same comprising
- administering to said patient an inflammation reducing quantity of a compound of the formula ##STR8## wherein A is selected from the group consisting of H, Br, and Cl;
- X is selected from the group consisting of H, F, or Cl;
- Y is selected from the group consisting of .beta.-OH, keto, or Cl;
- Z is selected from the group consisting of H, .alpha.-F, .beta.-F, and .alpha.-CH.sub.3 ;
- and
- R is H or an acyl residue selected from the group consisting of a mono- or dicarboxyl organic acid having 2 to 8 carbon atoms, methasulfobenzoic acid, and phosphoric acid.
A method for treating inflammation in a patient experiencing same comprising
- administering to said patient an inflammation reducing quantity of a compound of the formula ##STR9## wherein A is selected from the group consisting of H, Br, and Cl;
- X is selected from the group consisting of H, F, or Cl;
- Y is selected from the group consisting of .beta.-OH, keto, or Cl;
- Z is selected from the group consisting of H, .alpha.-F, .beta.-F, and .alpha.-CH.sub.3 ;
- and
- R is H or an acyl residue selected from the group consisting of a mono- or dicarboxyl organic acid having 2 to 8 carbon atoms, methasulfobenzoic acid, and phosphoric acid.
Dependencies are inferred from the claim text.