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

17-Ethers and thioethers of 4-aza-steroids. Asteroids as 5A-reductase inhibitors.

 

Inventors:

Graham; Donald W. (Mountainside, NJ); Aster; Susan D. (Teaneck, NJ); Hagmann; William (Westfield, 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

 

Related U.S. Application Data:

Continuation-in-part of Ser No. 886,021, 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

 

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

References Cited:

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

4,859,681      Aug., 1989      Rasmusson et al.      546/77

4,882,319      Nov., 1989      Holt et al.      514/71

4,888,336      Dec., 1989      Holt et al.      546/77

4,910,226      Mar., 1990      Holt et al.      514/319

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Other References

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