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Last Updated: March 29, 2024

Claims for Patent: 4,808,616


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Summary for Patent: 4,808,616
Title: 6-substituted androsta-1,4-diene-3,17-diones
Abstract:The invention relates to 6-alkylidenandrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
Inventor(s): Buzzetti; Franco (Monza, IT), Barbugian; Natale (Milan, IT), Lombardi; Paolo (Milan, IT), di Salle; Enrico (Milan, IT)
Assignee: Farmitalia Carlo Erba S.r.l. (Milan, IT)
Application Number:06/882,364
Patent Claims: 1. 6-methylenandrosta-1,4-diene-3,17-dione.

2. A compound selected from the group consisting of:

1-methyl-6-methylenandrosta-1,4-diene-3,17-dione;

1-ethyl-6-methylenandrosta-1,4-diene-3,17-dione;

4-methyl-6-methylenandrosta-1,4-diene-3,17-dione;

4-ethyl-6-methylenandrosta-1,4-diene-3,17-dione;

4-fluoro-6-methylenandrosta-1,4-3,17-dione;

4-chloro-6-methylenandrosta-1,4-diene-3,17-dione;

6-ethylidenandrosta-1,4-diene-3,17-dione;

6-propylidenandrosta-1,4-diene-3,17-dione;

4-fluoro-1-methyl-6-methylenandrosta-1,4-diene-3,17-dione;

4-chloro-1-methyl-6-methylenandrosta-1,4-diene-3,17-dione;

1-methyl-6-ethylidenandrosta-1,4-diene-3,17-dione, and

4-fluoro-6-ethylidenandrosta-1,4-diene-3,17-dione.

3. A pharmaceutical composition containing a suitable carrier and/or diluent and, as an active principle, a therapeutically effective amount of a compound of claim 1 or 2, or a pharmaceutically acceptable salt thereof.

4. A pharmaceutically composition, suitable for the treatment of advanced hormone-dependent breast, pancreatic, endometrial and ovarian cancers, comprising, as an active principle, a therapeutically effective amount of a compound of claim 1 or 2, in association with a suitable carrier and/or diluent.

5. A pharmaceutical composition, suitable for the treatment of prostatic hypertrophy and prostatic hyperplasia, comprising, as an active principle, a therapeutically effective amount of a compound of claim 1 or 2, in association with a suitable carrier and/or diluent.

6. A method for the treatment of advanced hormone-dependent breast, pancreatic, endometrial or ovarian cancer comprising administering patients in need of such treatment an effective amount of a compound of claim 1 or 2.

7. A method for the treatment of prostatic hypertrophy or prostatic hyperplasia comprising administering to patients in need of such treatment an effective amount of a compound of claim 1 or 2.

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