Phenylimidazolidines having antiandrogenic activit

专利名称：Phenylimidazolidines having antiandrogenic

activity

发明人：Martine Gaillard-Kelly,Francois

Goubet,Daniel Philibert,Jean-GeorgesTeutsch

申请号：US08/064257申请日：19930518公开号：US05411981A公开日：19950502

摘要：A compound of the formula ##STR1## wherein R.sub.1 is --CN, -- NO.sub.2 orhalogen, R.sub.2 is --CF.sub.3 or halogen, --A-B-- is of ##STR2## X is --O-- or --S--, R.sub.3 ishydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy ofup to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms thearyl and aralkyl being optionally substituted by halogen, --CF.sub.3, alkyl, alkoxy, alkenyl,alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone orsulfoxide, free, esterified, amidified or salified carboxy, -- NH.sub.2, mono anddialkylamino and heterocyclic of 3 to 6 ring members and containing at least one

heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl,alkenyl and alkynyl being optionally interrupted by at least one oxygen, nitrogen orsulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atomsand Y is --O--, --S-- or --NH--, except the compounds wherein --A-B-- is ##STR3## X is

oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen andR.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acidaddition salts.

申请人：ROUSSEL UCLAF

代理机构：Bierman and Muserlian

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