Schering Corporation

Charles J Casmer

Richard W Draper

Michael J Green

1,3,5(10),6,8-19-Nor-pregnapentaene-20-ones exhibit anti-mitotic activity with minimal or no hormonal activity. They are particularly useful in the treatment and control of psoriasis when applied topically, preferred anti-psoriatic compounds being 1,3,5(10),6,8-19-nor-pregnapentaene-3,17.alpha.,21-triol-20-one 21-acetate and the 16.alpha.-methyl and 16.beta.-methyl analogs thereof. The 1,3,5(10),6,8-19-nor-pregnapentaene-20-ones are also useful as intermediates in the preparation of the corresponding 14-dehydro compounds which also exhibit anti-mitotic activity as described and claimed in copending application Ser. No. 819,182 filed July 26, 1977 of Richard W. Draper and Charles J. Casmer of common assignee as this application, and now abandoned.

1,3,5(10),6,8-19-Nor-pregnapentaenes, their use as anti-psoriatic

1,3,5(10),6,8,14-19 Nor-pregnahexaene-20-ones exhibit anti-mitotic activity with minimal or no hormonal activity. They are particularly useful in the treatment and control of psoriasis when applied topically, a preferred anti-psoriatic compound being 16.alpha.-methyl-1,3,5(10),6,8,14-19-nor-pregnahexaene-3,17.alpha.,21-trio l-20-one 21-acetate.

1,3,5(10),6,8,14-19-Nor-pregnahexaenes, their use as anti-psoriatic

Novel retinoic acid esters of anti-inflammatory steroids of the pregnane series are described and their use in the treatment and control of acne vulgaris via the topical or intralesional route. A preferred mode of the invention comprises treating acne by applying topically to the affected area hydrocortisone 21-all-trans-retinoate in concentrations of from about 0.05 to about 0.15 percent. Pharmaceutical formulations and methods for the manufacture of the novel steroidal retinoates are also described.

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Rahway, NJ, United States of America

Charles J Casmer