U.S. patents available from 1976 to present.
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17ଲ-acyl-4-aza-5଱-androst-1-ene-3-ones as 5଱-reductase inhibitors

Patent 5049562 Issued on September 17, 1991. Estimated Expiration Date: Icon_subject August 21, 2009. 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.

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.

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

Oxidized analogs of 17ଲ-N-monosubstituted-carbamoyl-4-aza-5-଱-androstan-3-ones
Patent #: 4845104
Issued on: 07/04/1989
Inventor: Carlin ,   et al.

17 ଱-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors Patent #: 4859681
Issued on: 08/22/1989
Inventor: Rasmusson ,   et al.

Inventors

Assignee

Application

No. 396184 filed on 08/21/1989

US Classes:

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: Rivers, Diana G.

Attorney, Agent or Firm

Foreign Patent References

  • 970692 CA. 07/13/1975
  • 0004949 EP. 10/13/1979
  • 155096 EP. 09/13/1985
  • 1465544 FR. 11/13/1965

International Classes

A61K 031/58
C07J 073/00

Abstract

17ଲ-Acyl-4-aza-5଱-androst-1-ene-3-ones of the formula ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR2 is monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents;and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulation of the above compounds are active as testosterone 5଱-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, androgenic alopecia, prostatic carcinoma and benign prostatic hypertrophy.

Other References

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  • JNCI, vol. 74, No. 2, pp. 475-481, Feb. 1985
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  • Brooks et al., Prostate (1986) 9(1):65-75
  • Brooks et al., Steroids (1986) 47(1):1-19
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