17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders

Patent 5620986 Issued on April 15, 1997. Estimated Expiration Date:

March 1, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Abstract Claims Description Full Text

Patent References

2227876

3239417

3264301

3285918

Preparation of 4-aza-17-substituted-5଱-androstan-3-ones useful as 5଱-reductase inhibitors
Patent #: 4220775
Issued on: 09/02/1980
Inventor: Rasmusson , et al.

Novel steroid 5଱-reductase inhibitors
Patent #: 4317817
Issued on: 03/02/1982
Inventor: Blohm , et al.

4-Aza-17ଲ-substituted-5଱-androstan-3-one-reductase inhibitors
Patent #: 4377584
Issued on: 03/22/1983
Inventor: Rasmusson , et al.

Methods and solutions for treating male pattern alopecia
Patent #: 4596812
Issued on: 06/24/1986
Inventor: Chidsey, III , et al.

Steroidic 5଱-reductase inhibitors
Patent #: 4732897
Issued on: 03/22/1988
Inventor: Cainelli , et al.

17ଲ-N-monosubstituted carbamoyl-4-aza-5଱-androst-1-en-3-ones which are active as testosterone 5଱-reductase inhibitors
Patent #: 4760071
Issued on: 07/26/1988
Inventor: Rasmusson , et al.

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Inventors

Assignee

Merck & Co., Inc.

Application

No. 338574 filed on 03/01/1995

US Classes:

514/284, Tetracyclo ring system having the six-membered hetero ring as one of the cyclos514/253.02, Polycyclo ring system having the additional six-membered nitrogen hetero ring as one of the cyclos514/269, Pyrimidines with chalcogen bonded directly to a ring carbon of said pyrimidine moiety544/238, 1,2-diazines which contain an additional hetero ring544/242, 1,3-diazines544/243, Phosphorus attached directly or indirectly to the diazine ring by nonionic bonding544/336, 1,4-diazines544/337, Phosphorus attached directly or indirectly to the diazine ring by nonionic bonding546/77The six-membered hetero ring shares ring members with one other cyclo only

Examiners

Primary: Daus, Donald G.

Attorney, Agent or Firm

Foreign Patent References

970692 CA. 07/12/1975
0004949 EP. 10/12/1979
0155096 EP. 09/12/1985
0200859 EP. 11/12/1986
0277002 EP. 06/12/1988
0289327 EP. 11/12/1988
0314199 EP. 05/12/1989
0343954 EP. 11/12/1989
0375349 EP. 06/12/1990
0375347 EP. 06/12/1990
0375345 EP. 06/12/1990
0375344 EP. 08/12/1990
0572166A1 EP. 12/12/1993
1465544 FR. 11/12/1965
WO91/12261 WO. 08/12/1991
WO93/23053 WO. 11/12/1993
9323048 WO. 11/12/1993

International Classes

A61K 031/45
C07D 221/02

Abstract

Novel substituted 4-azasteroid 5-଱-reductase inhibitors of formula (I), wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These compounds are effective inhibitors of testosterone 5଱-reductase(s) and are thus useful in the treatment of a number of hyperandrogenic conditions including benign prostatic hypertrophy, acne, seborrhea, female hirsutism, and male and female pattern baldness (alopecia).

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