Heterocyclic inhibitors of 5-.alpha.-testosterone reductase

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United States of America Patent

PATENT NO 5302589
SERIAL NO

07927091

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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): ##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; X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl, p and q are independently either 0 or 1; R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are i) independently, hydrogen or lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl or ii) taken together with the linking nitrogen to form a 4 to 8 atom heterocyclic group, ##STR3## wherein; Y represents O, CH.sub.2, --N.dbd., NH or N(lower alkyl) optionally substituted with one or more lower alkyl groups; Ar is an aromatic group of 6 to 12 carbons; R.sup.4 is hydrogen or methyl; Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N----CH.dbd.N-- or --N.dbd.CH--; n and m are independently 0, 1 or 2; 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
Fang, Francis G Durham, NC 63 1220
Frye, Stephen V Durham, NC 11 76
Middlemiss, David Ware, GB 43 328

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