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US 5,510,351 AGranted
Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
AssigneeMerck & Co., Inc.
InventorsDonald W. Graham, Susan D. Aster, Richard L. Tolman
Life of this patent
Estimating the term…
Abstract
Described are delta 17 and delta 20 olefinic and saturated 17 Beta-substituted 4-aza-5 alpha-androstan-3-ones and related compounds having 5 alpha reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.
Claims14
A compound of the formula:
- ##STR34## wherein:
- Alk is C.sub.1-4 straight or branched chain alkyl or alkenyl;
- dashed lines "a", "e" and "f" each can independently represent a double bond when present, with the proviso that double bonds formed by "e" and "f" are not both present concurrently;
- R is selected from hydrogen, methyl and ethyl;
- R.sup.2 is
- (a) C.sub.6-10 aryl;
- or
- (b) heteroaryl;
- wherein aryl is selected from phenyl, benzyl, 1- and 2-phenethyl and naphthyl;
- wherein heteroaryl is selected from pyridyl, pyrryl, imidazolyl, tetrazolyl, pyrazinyl, pyrazolyl, triazolyl, thienyl, furanyl, isothiazolyl, thiazolyl, isoxazolyl, oxazolyl, oxadiazolyl, thiadiazolyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, and indolyl;
- wherein the above aryl or heteroaryl radical can be substituted with one or two or three substituents;
- and the pharmaceutically acceptable salts thereof.
9 more elements
A compound of the formula:
- ##STR38## wherein:
- Alk is C.sub.1-4 straight or branched chain alkyl;
- dashed line "a" can represent a double bond when present;
- R is selected from hydrogen, methyl and ethyl;
- R.sup.2 is
- (a) C.sub.6-10 aryl;
- or
- (b) heteroaryl;
- wherein aryl is selected from phenyl, benzyl, 1- and 2-phenethyl and naphthyl;
- wherein heteroaryl is selected from pyridyl, pyrryl, imidazolyl, tetrazolyl, pyrazinyl, pyrazolyl, triazolyl, thienyl, furanyl, isothiazolyl, thiazolyl, isoxazolyl, oxazolyl, oxadiazolyl, thiadiazolyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, and indolyl;
- wherein the above aryl or heteroaryl radical can be substituted with one or two or three substituents;
- and the pharmaceutically acceptable salts thereof.
9 more elements
Dependencies are inferred from the claim text.