The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jan. 23, 1996

Filed:

May. 02, 1994
Applicant:
Inventors:

Philip M Weintraub, Cincinnati, OH (US);

Cynthia A Gates, Fairfield, OH (US);

Michael R Angelastro, Cincinnati, OH (US);

Timothy T Curran, Cincinnati, OH (US);

J O'Neal Johnston, Milford, OH (US);

Assignee:

Merrell Dow Pharmaceuticals Inc., Cincinnati, OH (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ; C07J / ;
U.S. Cl.
CPC ...
514178 ; 514177 ; 514180 ; 514181 ; 552515 ;
Abstract

This invention is directed to 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C.sub.17-20 lyase and 5.alpha.-reductase inhibitory activity, the use of the present compounds as C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and also to a method for using such compounds in the treatment of androgen and/or estrogen dependent disorders, including bengin prostatic hyperplasia, breast cancer and prostatic cancer. The 4-amino compounds are prepared by the reaction of the appropriate 4,5-epoxide with sodium azide in an inert solvent in the presence of a catalytic amount of strong acid under appropriate reaction conditions. Alternatively, the 4-amino compounds are prepared by first nitration and then reduction of the appropriate steroid under appropriate reaction conditions.


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