Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders

Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders

United States Patent	5,510,351
Graham, et. al.	* Apr. 23, 1996

Inventors:	Graham; Donald W. (Mountainside, NJ); Aster; Susan D. (Teaneck, NJ); Tolman; Richard L. (Warren, NJ).
Assignee:	Merck & Co., Inc. (Rahway, NJ).
*[]**Notice:	The portion of the term of this patent subsequent to Nov. 10, 2014 has been disclaimed.
Appl. No.:	338,490
Filed:	Nov. 14, 1994
PCT Filed:	May 17, 1993
PCT No:	PCT/US93/04630
371 Date:	Nov. 14, 1994
102(e) Date:	Nov. 14, 1994
PCT Pub. No.:	WO93/23051
PCT Pub. Date:	Nov. 25, 1993

Related U.S. Application Data

Continuation-in-part of Ser No. 886,050, May 20, 1992, abandoned.

Intl. Cl. :	A61K 31/58
Current U.S. Cl.:	514/253; 514/241; 514/261; 514/269; 514/284; 544/198; 544/242; 544/264; 544/336; 546/77
Field of Search:	546/77; 514/284, 253; 544/336

References Cited | [Referenced By:]

U.S. Patent Documents

4,220,775	Sept., 1980	Rasmusson et al.	546/77
4,337,584	Mar., 1983	Rasmusson et al.	546/77
4,596,812	Jun., 1986	Chidsey, III et al.
4,732,897	Mar., 1988	Cainelli et al.	546/77
4,760,071	Jul., 1988	Rasmusson et al.	546/71
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5,049,562	Sept., 1991	Rasmusson et al.	546/77
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Foreign Patent Documents

0004949	Oct., 1979	EP
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1465544	Nov., 1965	FR
WO93/23039	Nov., 1993	WO
94/00125	Jan., 1994	WO

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Geldof "Consideration of the use of 17Beta-N,N-diethylcarbamoyl-4-methyl-4-aza-5 alpha androstan-3-one (4MA) a 5 alpha-reductase inhibitor in prostate cancer therapy" J. Cancer Res. Clin. Oncol. 118: 50-55 (1992).

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Primary Examiner: Daus; Donald G.
Attorney, Agent or Firm: Fitch; Catherine D., Giesser; Joanne M., Winokur; Melvin

Abstract

Described are delta 17 and delta 20 olefinic and saturated 17 Beta-substituted 4-aza-5 alpha-androstan-3-ones and related compounds having 5 alpha reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.

14 Claims, No Drawings