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Details for Patent: 6,169,082

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Details for Patent: 6,169,082

Title: Salts of 8,9-dehydroestrone sulfate ester
Abstract:This invention presents alkali metal salts of 8,9-dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.
Inventor(s): Raveendranath; Panolil C. (Plattsburgh, NY), Wichtowski; John A. (Middletown, CT)
Assignee: American Home Products Corporation (Madison, NJ)
Filing Date:Feb 18, 1993
Application Number:08/019,387
Claims:1. A pharmaceutically acceptable alkaline earth metal, ammonium or amine salt of 8,9-dehydroestrone-3-sulfate ester free from other estrogenic steroids, wherein the amine of said salt is selected from the group consisting of an alkylamine of 1 to 6 carbon atoms and a dialkylamine in which each alkyl group has, independently, 1 to 6 carbon atoms.

2. A compound of claim 1 which is calcium 8,9-dehydroestrone-3-sulfate.

3. A compound of claim 1 which is magnesium 8,9-dehydroestrone-3-sulfate.

4. A compound of claim 1 which is ammonium 8,9-dehydroestrone-3-sulfate.

5. A compound of claim 1 which is an alkylamine salt of 8,9-dehydroestrone-3-sulfate in which the alkyl moiety of the amine contains 1 to 6 carbon atoms.

6. A compound of claim 5 which is the ethylamine salt of 8,9-dehydroestrone-3-sulfate.

7. A compound of claim 1 which is a dialkylamine salt of 8,9-dehydroestrone-3-sulfate in which each of the alkyl moieties of the amine contain 1 to 6 carbon atoms.

8. A compound of claim 7 which is the dimethylamine salt of 8,9-dehydroestrone-3-sulfate.

9. A method for the treatment of atherosclerosis which comprises administering to a patient in need of anti-atherosclerotic treatment, an effective amount of a salt of 8,9-dehydroestrone sulfate ester.

10. A method of claim 9 in which said salt of 8,9-dehydroestrone sulfate ester is the calcium, magnesium, ammonium, alkylamine or dialkylamine salt in which each of the alkyl groups of said amines contain from 1 to 6 carbon atoms.

11. A method of removing arterial lesions attending the development of atherosclerosis which comprises administering, orally, or parenterally, to a patient suffering from atherosclerosis, a pharmaceutical composition containing an anti-atherosclerotic amount of a salt of 8,9-dehydroestrone sulfate ester.

12. A method of claim 11 in which said salt of 8,9-dehydroestrone sulfate ester is the calcium, magnesium, ammonium, alkylamine or dialkylamine salt in which each of the alkyl groups of said amines contain from 1 to 6 carbon atoms.
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