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US Patent 5620986 - 17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders

US Patent Issued on April 15, 1997
Estimated Patent Expiration Date: Icon_subject March 1, 2015Estimated 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.
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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).

Other References

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Inventors

Assignee

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

Field of Search

514/284, Tetracyclo ring system having the six-membered hetero ring as one of the cyclos546/77The six-membered hetero ring shares ring members with one other cyclo only

Examiners

Primary: Daus, Donald G.

Attorney, Agent or Firm

US Patent References

2227876, 3239417, 3264301, 3285918, 4220775, Preparation of 4-aza-17-substituted-5଱-androstan-3-ones useful as 5଱-reductase inhibitors
Issued on: 09/02/1980
Inventor: Rasmusson ,   et al.4317817, Novel steroid 5଱-reductase inhibitors
Issued on: 03/02/1982
Inventor: Blohm ,   et al.4377584, 4-Aza-17ଲ-substituted-5଱-androstan-3-one-reductase inhibitors
Issued on: 03/22/1983
Inventor: Rasmusson ,   et al.4596812, Methods and solutions for treating male pattern alopecia
Issued on: 06/24/1986
Inventor: Chidsey, III ,   et al.4732897, Steroidic 5଱-reductase inhibitors
Issued on: 03/22/1988
Inventor: Cainelli ,   et al.4760071, 17ଲ-N-monosubstituted carbamoyl-4-aza-5଱-androst-1-en-3-ones which are active as testosterone 5଱-reductase inhibitors
Issued on: 07/26/1988
Inventor: Rasmusson ,   et al.4845104, Oxidized analogs of 17ଲ-N-monosubstituted-carbamoyl-4-aza-5-଱-androstan-3-ones
Issued on: 07/04/1989
Inventor: Carlin ,   et al.4859681, 17 ଱-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
Issued on: 08/22/1989
Inventor: Rasmusson ,   et al.4882319, Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-଱-reductase
Issued on: 11/21/1989
Inventor: Holt, et al.4910226, Steroid 5-alpha-reductase inhibitors
Issued on: 03/20/1990
Inventor: Holt, et al.5049562, 17ଲ-acyl-4-aza-5଱-androst-1-ene-3-ones as 5଱-reductase inhibitors
Issued on: 09/17/1991
Inventor: Rasmusson, et al.5110939, Intermediates in the preparation of steriod 5-alpha-reductase inhibitors
Issued on: 05/05/1992
Inventor: Holt, et al. 5116983, 5494914Inhibitors for testosterone 5଱-reductase activity
Issued on: 02/27/1996
Inventor: Labrie, et al.

Foreign Patent References

  • 970692 CA. 07/21/1975
  • 0004949 EP. 10/21/1979
  • 0155096 EP. 09/21/1985
  • 0200859 EP. 11/21/1986
  • 0277002 EP. 06/21/1988
  • 0289327 EP. 11/21/1988
  • 0314199 EP. 05/21/1989
  • 0343954 EP. 11/21/1989
  • 0375349 EP. 06/21/1990
  • 0375347 EP. 06/21/1990
  • 0375345 EP. 06/21/1990
  • 0375344 EP. 08/21/1990
  • 0572166A1 EP. 12/21/1993
  • 1465544 FR. 11/21/1965
  • WO91/12261 WO. 08/21/1991
  • WO93/23053 WO. 11/21/1993
  • 9323048 WO. 11/21/1993

International Classes

A61K 031/45
C07D 221/02

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