Cecil Alfred Robinson

US Patent:

40874613, May 2, 1978

Filed:

Aug 22, 1977

Appl. No.:

5/826750

Inventors:

Cecil H. Robinson - Pylesville MD

Assignee:

The Johns Hopkins University - Baltimore MD

International Classification:

C07C 4944
C07C 4946
C07C 4954

US Classification:

260586E

Abstract:

6 (H)-5,10-seco-4,5-dieneketo steroids are disclosed which exhibit anti-ardrogenic properties.

US Patent:

40596303, Nov 22, 1977

Filed:

Feb 26, 1976

Appl. No.:

5/661792

Inventors:

Cecil H. Robinson - Pylesville MD

Assignee:

The Johns Hopkins University - Baltimore MD

International Classification:

C07C 4945

US Classification:

260586E

Abstract:

The present invention relates to certain new and useful steroids which demonstrate anti-androgenic properties. These steroids are 5,10-secosteroids that have been found to be potent irreversible inhibitors of the enzyme. DELTA. sup. 5 -3-ketosteroid isomerase which is involved in androgen biosynthesis. In addition, certain of the steroids of the invention compete reversibly with 5-. alpha. -dihydrotestosterone for binding to the prostatic cytoplasmic receptor protein while others inhibit the enzyme prostatic testosterone 5-. alpha. -reductase. The anti-androgenic properties of the present compounds indicate such utility as the control of abnormal growth of the human prostate, e. g. in the therapy of human prostatic cancer.