.

BioPharmaceutical Business Intelligence

  • Analyze global market entry opportunities
  • Uncover prior art in expired and abandoned patents
  • Obtain formulation and manufacturing information

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving leading biopharmaceutical companies globally:

Johnson and Johnson
Farmers Insurance
Cerilliant
Covington
Dow
Healthtrust
Citi
Medtronic
UBS
Queensland Health

Generated: November 18, 2017

DrugPatentWatch Database Preview

Details for Patent: ► Subscribe

« Back to Dashboard

Details for Patent: ► Subscribe

Title: 17.beta.-acyl-4-aza-5.alpha.-androst-1-ene-3-ones as 5.alpha. reductase inhibitors
Abstract:17.beta.-Acyl-4-aza-5.alpha.-androst-1-en-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and R.sup.2 is a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or 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, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl; and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
Inventor(s): Rasmusson; Gary H. (Watchung, NJ), Reynolds; Glenn F. (Westfield, NJ)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Sep 23, 1991
Application Number:07/764,047
Claims:1. A compound of formula: ##STR8## wherein R is selected from hydrogen, methyl and ethyl; and

R.sup.2 is a monovalent radical selected from benzyl and phenethyl or heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl, and

R', R", R'" are each selected from hydrogen or methyl.

2. A compound of claim 1 wherein the compound is 17.beta.(2-pyrrolylcarbonyl)-4-aza-5.alpha.-androst-1-en-3-one.

3. A compound of claim 1 wherein the compound is 4-methyl-17.beta.-(2-pyrrolylcarbonyl)-4-aza-5.alpha.-androst-1-en-3-one.

4. A method of treating the hyperandrogenic condition of acne vulgaris, seborrhea, female hirsutism, and benign prostatic hypertrophy comprising parenteral administration to a patient in need of such treatment of a therapeutically effective amount of a compound of formula: ##STR9## wherein R and R.sup.2 are defined as in claim 1.

5. A method of inhibiting testosterone 5.alpha.-reductase in a patient in need of such inhibiting treatment, comprising administration to such a patient of a therapeutically effective amount of a compound of the formula: ##STR10## wherein R and R.sup.2 are defined as in claim 1,

R' is hydrogen or methyl,

R" is hydrogen of .beta.-methyl,

R"' is hydrogen, .alpha.-methyl or .beta.-methyl.

6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of formula: ##STR11## wherein R and R.sup.2 are defined as in claim 1.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Serving leading biopharmaceutical companies globally:

Healthtrust
Cerilliant
Argus Health
Dow
Harvard Business School
Medtronic
US Army
US Department of Justice
Cipla
Covington

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted
Privacy and Cookies
Terms & Conditions

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot