Topical administration of azaspiranes to prevent or treat skin conditions associated with hyperproliferation of keratinocytes
OwnerLawrence R. Bernsteininventor
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Abstract
A locally administrable topical pharmaceutical composition is provided for use in the prevention or treatment of skin conditions associated with hyperproliferation of keratinocytes and/or an immunologically mediated disorders, as psoriasis, atopic dermatitis, contact dermatitis, seborrheic dermatitis or actinic dermatitis. The composition contains a topical carrier and spirogermanium or a structurally related azaspirane.
Claims29
A locally administrable topical pharmaceutical composition comprising a carrier suitable for topical administration and an amount of an active agent effective to prevent or treat skin conditions associated with hyperproliferation of keratinocytes and/or an immunologically mediated hyperproliferative skin disorder, wherein the active agent is an azaspirane compound having the structure of formula (I) ##STR4## wherein:
- R.sup.1 and R.sup.2 may be the same or different and are each selected from the group consisting of hydrogen and lower alkyl;
- X is selected from the group consisting of Ge, Si and Sn;
- Y.sup.1 and Y.sup.2 are the same and are either CH.sub.2 or C.dbd.O;
- m is zero or one;
- Z is CH.sub.2 when m is 1 and CH.sub.2 or C.dbd.O when m is zero;
- R.sup.3 is alkylene or alkenylene;
- n is an integer in the range of 2 to 6 inclusive when R.sup.3 is alkylene and 3 to 6 inclusive when R.sup.3 is alkenylene;
- and
- R.sup.4 and R.sup.5 are independently selected from the group consisting of lower alkyl or lower alkenyl, or are linked together to form a heterocyclic group selected from morpholino, pyrrolidino, piperidino and lower alkyl substituted piperazino in which the lower alkyl group is attached to a terminal nitrogen atom,
- or a pharmaceutically acceptable acid addition salt thereof,
- wherein the effective amount of the active agent represents less than approximately 1.0 wt. % of the composition,
- and further wherein the composition is in the form of an ointment, lotion, cream, gel or shampoo.
A method for preventing or treating a skin condition associated with hyperproliferation of keratinocytes in an individual prone to or afflicted with such a condition, comprising administering to the affected area of the individual's skin a therapeutically effective amount of a locally administrable topical pharmaceutical composition comprising a carrier suitable for topical administration and an active agent, wherein the active agent is an azaspirane compound having the structure of formula (I) ##STR5## wherein:
- R.sup.1 and R.sup.2 may be the same or different and are each selected from the group consisting of hydrogen and lower alkyl;
- X is selected from the group consisting of Ge, Si and Sn;
- Y.sup.1 and Y.sup.2 are the same and are either CH.sub.2 or C.dbd.O;
- m is zero or one;
- Z is CH.sub.2 when m is 1 and CH.sub.2 or C.dbd.O when m is zero;
- R.sup.3 is allylene or alkenylene;
- n is an integer in the range of 2 to 6 inclusive when R.sup.3 is alkylene and 3 to 6 inclusive when R.sup.3 is alkenylene;
- and
- R.sup.4 and R.sup.5 are independently selected from the group consisting of lower alkyl or lower alkenyl, or are linked together to form a heterocyclic group selected from morpholino, pyrrolidino, piperidino and lower alkyl substituted piperazino in which the lower alkyl group is attached to a terminal nitrogen atom,
- or a pharmaceutically acceptable acid addition salt thereof,
- wherein the condition is psoriasis, atopic dermatitis, contact dermatitis, seborrheic dermatitis, or actinic keratosis.
Dependencies are inferred from the claim text.