Inhibitors of 5-.alpha.-testosterone reductase

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United States of America Patent

PATENT NO 5543406
SERIAL NO

08244875

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) ##STR1## wherein R.sup.1 and R.sup.2 are i) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, or ii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond; R.sup.3c is hydrogen; R.sup.4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, --(CH.sub.2).sub.m CO.sub.2 R.sup.16, --(CH.sub.2).sub.m Ar.sup.a, --(CH.sub.2).sub.n 'CONR.sup.17 R.sup.18, --(CH.sub.2).sub.n 'NR.sup.17 R.sup.18 or --(CH.sub.2).sub.n 'OR.sup.16, wherein R.sup.16 is hydrogen, lower alkyl or lower alkenyl; R.sup.17 and R.sup.18 are independently hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ar.sup.a is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5; R.sup.19 and R.sup.20 are independently hydrogen or lower alkyl, or taken together R.sup.19 and R.sup.20 form a carbonyl group (.dbd.O); R.sup.5c is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR.sup.21 R.sup.22, wherein R.sup.21 and R.sup.22 are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations.

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Patent Owner(s)

Patent OwnerAddress
GLAXO INCLEGAL-PATENT GROUP 5 MOORE DRIVE RTP NC 27709

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Andrews, Robert C Durham, NC 42 713
Cribbs, Cynthia M Raleigh, NC 1 3
Frye, Stephen V Durham, NC 11 76
Haffner, Curt D Cary, NC 1 3
Maloney, Patrick R Durham, NC 6 47

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