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Details for Patent: 3,995,060

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Details for Patent: 3,995,060

Title: Antiandrogenic agents and method for the treatment of androgen dependent disease states
Abstract:This application relates to certain 4'-substituted and to 3',4'-disubstituted anilides, to methods for their preparation and to methods for their use as antiandrogens. These substituted anilides are useful in the treatment of androgen dependent disease states, such as benign prostatic hypertrophy, hirsutism, acne and the like.
Inventor(s): Neri; Rudolph O. (Hawthorne, NJ), Topliss; John G. (West Caldwell, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Filing Date:Sep 11, 1974
Application Number:05/505,116
Claims:1. A method for the treatment of benign prostatic hypertrophy which comprises administering to mammals suffering from benign prostatic hyperstrophy, an effective quantity for treating benign prostatic hypertrophy of a compound having the structural formula: ##SPC26##

or the non-toxic pharmaceutically acceptable salts thereof, wherein X is a member of the group consisting of nitro, trifluoromethyl, chloro, bromo and iodo; Y is a member of the group consisting of hydrogen, halogen, nitro, lower alkyl, lower alkoxy, lower alkanoyl, polyfluoroloweralkoxy, polyfluoroloweralkyl, and trifluoromethylthio, with the proviso that when Y and R' are both hydrogen, X is other than iodo; R' is a member of the group consisting of hydrogen and alkyl having less than 5 carbon atoms and R is cyclopropyl, cyclobutyl or branched chain alkyl having up to 8 carbon atoms.

2. A method according to claim 1 wherein R is isopropyl.

3. A method according to claim 2 wherein R' is hydrogen. Y is trifluoromethyl and X is nitro, said compound being 4'-nitro-3'-trifluoromethylisobutyranilide.

4. A method according to claim 2 wherein R' is hydrogen, Y is trifluoromethyl and X is iodo, said compound being 4'-iodo-3'-trifluoromethylisobutyranilide.

5. A method according to claim 1 wherein R is cyclopropyl.

6. A method according to claim 5 wherein R' is hydrogen, Y is trifluoromethyl, and X is nitro, said compound being 4'-nitro-3'-trifluoromethylcyclopropylcarbanilide.
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