Drug patents …
… from Kazakhstan to Kalamazoo
Proactively manage your pharmacy inventory
Find generic entry opportunities
Anticipate generic drug launch
Manage your formulary budget
Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Flat-rate pricing for predictable budgeting
Short-term plans for project- or client-based billing
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|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|
|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.
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.