An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R. sub. 1 is F, Br, NO. sub. 2, or H; R. sub. 2 is F, Br, NO. sub. 2, NH. sub. 2, or H; R is H or alkyl of 1-4 carbon atoms; R. sub. 3 is O or H. sub. 2 ; and R. sub. 4 is H. sub. 2, O, or. alpha. -H,. beta. -OH; R. sub. 5 is H. sub. 2,. alpha. -H and. beta. -OH or B-H and. alpha. -OH in admixture with a pharmaceutically acceptable carrier with the proviso that R. sub. 1, R. sub. 2 and R. sub. 3 cannot all be hydrogen and one of R. sub. 1 and R. sub. 2 is F.
Compounds And Compositions For Inhibiting Estrogen Sulfotransferase Transferase Activity, Process And Novel Intermediates Therein
Samuel C. Brooks - Orchard Lake MI Jerome P. Horwitz - Oak Park MI
Assignee:
Wayne State University - Detroit MI
International Classification:
A61K 3156
US Classification:
514182
Abstract:
The present invention concerns the novel compounds having fluoro, amino, nitro or hydroxy monosubstituted at the 2- or 4- position on deoxyestrone as well as deoxyestra-17-ol. The compounds are useful as estrogen sulfotransferase inhibitors. Such estrogen sulfotransferase inhibition provides the novel use for treating a female mammal to prevent implantation of a blastocyst. Additionally, the invention concerns the novel synthesis and novel intermediates in the synthesis of the estrogen sulfotransferase inhibiting compound of the present invention.
Samuel C. Brooks - Orchard Lake MI Jerome P. Horwitz - Oak Park MI
Assignee:
Wayne State University - Detroit MI
International Classification:
A61K 3156
US Classification:
514178
Abstract:
A compound of the formula ##STR1## wherein Z is alkoxy of 1-4 carbon atoms or hydroxyalkoxy of 2-4 carbon atoms and Y is nitro, inhibiting the growth of murine ductal carcinoma (MXT mammary tumors).
Samuel C. Brooks - Orchard Lake MI Jerome P. Horwitz - Oak Park MI
Assignee:
Wayne State University - Detroit MI
International Classification:
A61K 3156
US Classification:
514178
Abstract:
A compound of the formula ##STR1## wherein Z is alkoxy of 1-4 carbon atoms and Y is amino, inhibits the growth of murine ductal carcinoma (MXT mammary tumors). A compound wherein Z is OH and Y is nitro, administered orally, inhibits the growth of MXT mammary tumors.
An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R. sub. 1 is Br, NO. sub. 2, or H; R. sub. 2 is Br, NO. sub. 2, NH. sub. 2, or H; R is H or alkyl of 1-4 carbon atoms; R. sub. 3 is O or H. sub. 2 ; and R. sub. 4 is H. sub. 2, O, or. alpha. -H,. beta. -OH, in admixture with a pharmaceutically acceptable carrier. The specificity of the invention is believed targeted to the substituent at R. sub. 2 or C. sub. 4 and secondarily the OR group at C. sub. 3.
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Past: supervisor at Alpha metals, forman at federated metals asarco I am the oldest bro of Gloria,debra,laverne,clinton, richard,&walter Brooks. I live in New Jersey not far from Atlantic city.