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US 5,912,357 AGranted
Indole derivatives as 5-.alpha.-reductase-1-inhibitors
AssigneePfizer Inc.
InventorsJulian Blagg, Graham Nigel Maw, David James Rawson
Life of this patent
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Abstract
A compound of formula (I): ##STR1## and the pharmaceutically acceptable base salts thereof, wherein: R is CO.sub.2 R.sup.12 where R.sup.12 is H or a biolabile ester-forming group, or R is tetrazol-5-yl, and either (a) R.sup.1 is ##STR2## and R.sup.2 is F, Cl, Br, I, CH.sub.3 or CF.sub.3, or (b) R.sup.1 is C.sub.3 -C.sub.6 alkyl and R.sup.2 is C.sub.2 -C.sub.4 alkyl, useful as steroid 5-.alpha.-reductase inhibitors.
Claims9
A compound of formula (I):
- ##STR32## and the pharmaceutically acceptable base salts thereof, wherein:
- R is CO.sub.2 R.sup.12 where R.sup.12 is H or a C.sub.1 -C.sub.6 alkyl ester, and either (a) R.sup.1 is ##STR33## and R.sup.2 is F, Cl, Br, I, CH.sub.3 or CF.sub.3, or (b) R.sup.1 is C.sub.3 -C.sub.6 alkyl and R.sup.2 is C.sub.2 -C.sub.4 alkyl.
A compound selected from:
- 4-3-(2,2-p-chlorophenyl-1,3-benzodioxolan-5-yl!carbonyl)-2-methylindol-1- yl!butanoic acid;
- 4-3-(2-butyl-(4-n-propylphenyl)-1,3-benzodioxolan-5-yl!carbonyl)2-methyli ndol-1-yl!butanoic acid;
- 4-3-(2-butyl-2-(4-ethylphenyl)-1,3-benzodioxolan-5-yl!carbonyl)2-methylin dol-1-yl!butanoic acid;
- ethyl-4-3-(2,2-p-chlorophenyl-1,3-benzodioxolan-5-yl)carbonyl)2-methylind ol-1-yl!butanoate;
- ethyl-4-3-(2-butyl-2-{4-n-propylphenyl)-1,3-benzodioxolan-5-yl!carbonyl)2 -methylindol-1-yl!butanoate;
- and
- ethyl-4-3-(2-butyl-2-(4-ethylphenyl)-1,3-benzodioxolan-5-yl!carbonyl)2-me thylindol-1-yl!butanoate,
- and pharmaceutically acceptable base salts thereof.
5 more elements
Dependencies are inferred from the claim text.