Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1984-08-20
1988-05-17
Schenkman, Leonard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
2603973, 2603974, 514177, A61K 3156, C07J 100
Patent
active
047451092
ABSTRACT:
Thiol-substituted synthetic steriod hormones or androgens having a testosterone ring system backbone are used to inhibit aromatase's catalyzed conversion of C.sub.19 androgens having a A.sup.4,3-ketone group to estrogens in the treatment of estrogen-dependent tumors, such as metastatic breast cancer in postmenopausal females.
The compounds have the general formula: ##STR1## wherein R.sub.1 =a thiol, such as --SH or --CH.sub.2 SH, and R.sub.2 =OH or =O. The preferred synthetic hormones are 17.beta.-hydroxy-10.beta.-mercaptoestr-4-en-3-one, 19-mercaptoandrost-4-en-3,17-dione, and 10.beta.-mercaptoandrost-4-en-3,17-dione.
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Bednarski Patrick J.
Nelson Sidney D.
Porubek David J.
Lipovsky Joseph A.
Schenkman Leonard
Washington Research Foundation
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