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Last Updated: May 6, 2024

Claims for Patent: 8,143,240

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Summary for Patent: 8,143,240

Title:	17.alpha., 21-dihydroxypregnene esters as antiandrogenic agents
Abstract:	17.alpha.,21-Dihydroxypregna-4,9-diene-3,20-dione and 17.alpha.,21-dihydroxypregna-4-ene-3,20-dione 17 and/or 21 esters of having remarkable antiandrogenic activity, and the processes for the preparation thereof.
Inventor(s):	Ajani; Mauro (Lainate, IT), Moro; Luigi (Cairate, IT)
Assignee:	Cosmo S.p.A. (Lainate (Milan), IT)
Application Number:	12/457,870
Patent Claims:	1. A method of treating a patient suffering from a condition selected from the group consisting of acne, seborrhea, hirsutism and alopecia, comprising administering to said patient topically or systemically an effective amount of a compound of formula (I) ##STR00003## wherein: R.sub.1 is hydrogen and R.sub.2 is a C.sub.3-C.sub.18 acyl group. 2. A method of treating a patient suffering from a condition selected from the group consisting of acne, seborrhea, hirsutism, and alopecia, said method comprising administering to said patient an effective amount of a compound of formula (II) ##STR00004## wherein: R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or a C.sub.3-C.sub.18 acyl group, with the proviso that at least one of R.sub.1 and R.sub.2 is different from hydrogen. 3. The method as claimed in claim 2 wherein R.sub.1 is hydrogen and R.sub.2 is propionyl. 4. The method as claimed in claim 2 wherein R.sub.1 and R.sub.2 are butanoyl. 5. A method of treating a patient suffering from a condition selected from the group consisting of acne, seborrhea, hirsutism and alopecia, comprising administering to said patient topically or systemically an effective amount of a pharmaceutical composition comprising as active ingredient a compound of formula (I) ##STR00005## wherein: R.sub.1 is hydrogen and R.sub.2 is a C.sub.3-C.sub.18 acyl group, in admixture with an acceptable carrier, wherein said active ingredient is present in an amount of 0.1 to 1.0% by weight. 6. The method as claimed in claim 2, wherein the compound of formula (II) is administered topically or systemically. 7. A method as claimed in claim 1 wherein the compound of formula (I) is as defined in claim 1, wherein R.sub.1 is hydrogen and R.sub.2 is propionate. 8. A method as claimed in claim 1 wherein the compound of formula (I) is as defined in claim 1, wherein R.sub.1 is hydrogen and R.sub.2 is butyrate. 9. A method as claimed in claim 5 wherein the active ingredient is present in an amount of 0.2-0.8% by weight.

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