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US 4,064,240 AGranted
21-Cyclic acetals of steroidal 21-aldehydes and methods of preparation
AssigneeSyntex (U.S.A.) Inc.
InventorsMichael Marx, Denis John Kertesz
Life of this patent
Estimating the term…
Abstract
21-Cyclic acetals of steroids of the corticoid series are prepared from the corresponding 21-hydroxy steroids. The products have utility as anti-inflammatory agents.
Claims22
A compound of the formula:
- ##STR10## wherein n is 0 or 1;
- each of R.sup.1 - R.sup.6 is independently hydrogen or lower alkyl containing 1 to 4 carbon atoms and when n is 0, any two of R.sup.1 14 R.sup.6 on adjacent carbon atoms, taken together, are lower alkylene containing 3 to 5 carbon atoms;
- R.sup.11 is chloro or hydroxy;
- X.sup.1 and X.sup.2 are independently hydrogen, chloro or fluoro, with the proviso that when R.sup.11 is chloro, X.sup.2 is chloro;
- and
- Z is a single or double bond.
3 more elements
A pharmaceutical composition useful for treating inflammatory disorders, comprising a pharmaceutically acceptable non-toxic carrier in admixture with an effective amount of a compound of the formula:
- ##STR14## wherein:
- n is 0 or 1;
- each of R.sup.1 - R.sup.6 is independently hydrogen or lower alkyl containing 1 to 4 carbon atoms and when n is 0, any two of R.sup.1 - R.sup.6 on adjacent carbon atoms, taken together, are lower alkylene containing 3 to 5 carbon atoms;
- R.sup.11 is chloro or hydroxy;
- X.sup.1 and X.sup.2 are independently hydrogen, chloro or fluoro, with the proviso that when R.sup.11 is chloro, X.sup.2 is chloro;
- and
- Z is a single or double bond.
4 more elements
A method for relieving symptoms associated with inflammatory disorders comprising, administering an effective amount of a compound of the formula:
- ##STR15## wherein:
- n is 0 or 1;
- each of R.sup.1 - R.sup.6 is independently hydrogen or lower alkyl containing 1 to 4 carbon atoms and when n is 0, any two of R.sup.1 - R.sup.6 on adjacent carbon atoms, taken together, are lower alkylene containing 3 to 5 carbon atoms;
- R.sup.11 is chloro or hydroxy;
- X.sup.1 and X.sup.2 are independently hydrogen, chloro or fluoro with the proviso that when R.sup.11 is chloro, X.sup.2 is chloro;
- and
- Z is a single or double bond;
- or a pharmaceutical composition same.
5 more elements
Dependencies are inferred from the claim text.