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Claims for Patent: 5,565,467

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Claims for Patent: 5,565,467

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 W. (Chapel Hill, NC), Frye; Stephen V. (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:08/405,120
Patent Claims: 1. 17.beta.-N-(2,5- bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-androst-1-en-3-one or a pharmaceutically acceptable solvate thereof.

2. A pharmaceutical formulation comprising the compound of claim 1 and a pharmaceutically acceptable carrier thereof.

3. A pharmaceutical formulation comprising a safe and effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier thereof.

4. The pharmaceutical formulation of claim 3 further comprising an alpha 1 adrenergic receptor blocker.

5. The pharmaceutical formulation of claim 4 wherein the alpha 1 adrenergic receptor blocker is selected from the group consisting of: prazosin, terazosin, doxazosin, indoramin, trimazosin and tamsolosin.

6. The pharmaceutical formulation of claim 5 wherein the alpha 1 adrenergic receptor blocker is terazosin.

7. The pharmaceutical formulation of claim 3 further comprising an anti-estrogen selected from the group consisting of: clomiphene and tamoxifen.

8. The pharmaceutical formulation of claim 7 wherein an the anti-estrogen is tamoxifen.

9. The pharmaceutical formulation of claim 3 further comprising an anti-androgen.

10. The pharmaceutical formulation of claim 9 wherein the anti-androgen is flutamide.
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