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US 5,510,485 AGranted
17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5A-reductase inhibitors
AssigneeMerck & Co., Inc.
InventorsDonald W. Graham, Susan D. Aster, William Hagmann, Richard L. Tolman
Life of this patent
Estimating the term…
Abstract
Described are new 17.beta.-ester, amide and ketone 4-aza-5a-androstan-3-ones and related compounds and their use as 5a-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenetic related disorders.
Claims3
A compound of the formula:
- ##STR97## wherein:
- dashed line "a" can represent a double bond when present;
- R is selected from hydrogen, methyl and ethyl;
- R.sub.20 is selected from hydrogen and methyl;
- n is an integer from 0 to 10;
- R.sub.4 is selected from:
- (a) COR.sub.1, where R.sub.1 is C.sub.6 -C.sub.10 aryl, substituted C.sub.6 -C.sub.10 aryl, and heteroaryl;
- (b) CONHR.sub.2, where R.sub.2 is substituted phenyl, heteroaryl, substituted heteroaryl, or C.sub.7 -C.sub.12 cycloalkyl;
- and
- (c) CO.sub.2 R.sub.3, where R.sub.3 is C.sub.6 -C.sub.10 aryl, substituted C.sub.6 -C.sub.10 aryl, or C.sub.7 -C.sub.12 cycoalkyl;
- wherein aryl is selected from phenyl, benzyl, 1-and 2-phenethyl and naphthyl;
- wherein heteroaryl is selected from pyridyl, pyrryl, thienyl, isothiazolyl, thiazolyl, imidazolyl, tetrazolyl, pyrazinyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, pyrazolyl, indolyl, isoxazolyl, triazolyl, furanyl, oxazolyl, and thiadiazolyl;
- wherein cycloalkyl is selected from 1- and 2-adamantyl, norbomyl, and bicyclo(2.2.2)octyl;
- wherein the above aryl or heteroaryl radical can further be substituted with one or two substituents;
- and the pharmaceutically acceptable salts thereof.
12 more elements
Dependencies are inferred from the claim text.