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Last Updated: March 30, 2025

Claims for Patent: 5,846,976

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Summary for Patent: 5,846,976

Title:	Androstenone derivative
Abstract:	The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.
Inventor(s):	Batchelor; Kenneth William (Chapel Hill, NC), Frye; Stephen Vernon (Durham, NC), Dorsey, Jr.; George F. (Raleigh, NC), Mook, Jr.; Robert A. (Chapel Hill, NC)
Assignee:	Glaxo Wellcome Inc. (Research Triangle Park, NC)
Application Number:	08/708,167
Patent Claims:	1. A method of treating an androgen responsive or mediate condition in a mammal suffering from said condition comprising administering to said mammal a safe and effective amount of 17.beta.-N-(2,5-bis(Trifluoromethyl)) phenylcarbamoyl-4-aza-5.alpha.-andro st-1-en-3-one or a pharmaceutically acceptable solvate thereof. 2. A method of claim 1 wherein the androgen responsive or mediated condition is benign prostatic hypertrophy, prostate cancer, acne, male pattern baldness and hirsutism. 3. A method of treating an androgen responsive or mediated condition in a mammal suffering from said condition comprising administering to said mammal a safe and effective amount of a pharmaceutical formulation comprising a safe and effective amount of 17.beta.-N-(2,5-bis(Trifluoromethyl)) phenylcarbamoyl-4-aza-5.alpha.-androst-1-en-3-one or a pharmaceutically acceptable solvate thereof. 4. The method of claim 3 wherein said formulation further comprises an alpha 1 adrengergic receptor blocker. 5. The method of claim 3 wherein said formulation further comprises an anti-estrogen selected from the group consisting of: clomiphene and tamoxifen. 6. The method of claim 5 wherein said anti-estrogen is tamoxifen. 7. The method of claim 3 wherein said formulation further comprises an anti-androgen. 8. The method of claim 6 wherein said anti-androgen is flutamide.

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