Androgenic directed compositions
AssigneeBiophysica, Inc.
InventorsMilos Sovak, Jerome C. Bressi, James Gordon Douglass, III, Brian Campion, Wolfgang Wrasidlo
Life of this patent
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Abstract
Substituted phenylthiohydantoins are provided for use in detecting the presence of tumor cells having androgenic receptors and providing for cytostatic and cytotoxic activity toward such cells. The subject compounds provide for vehicles for specific targeting to the androgenic receptor containing cells of cytostatic and/or cytotoxic agents, heavy or light radioactive or radioopaque atoms, and the like for detection and treatment of cancer cells involving androgenic receptors or blocking androgenic receptors.
Claims7
A compound selected from the group consisting of:
- (a) 4-[3'-(2"-propenyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl]-2-t rifluoromethyl-benzonitrile;
- (b) 7{5",5"-dimethyl-4"-oxo-3"-[4'"-cyano-3'"-trifluoromethylphenyl-1'-imidazo lidinyl]-2"-thioxo-1"-ethylcarbamoxy}paclitaxel;
- (c) 4-[3'-(2"-propynyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl]-2-t rifluoromethyl-benzonitrile;
- (d) 4-[3'-(2"-{4'"-imidazolyl}ethyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidaz olidinyl]-2-trifluoromethyl-benzonitrile;
- (e) 4-[3'-{2"-N-(.rho.-hydroxy phenethyl) amidoethyl}-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl]-2-trifluoro methyl-benzonitrile;
- (f) 4-[3'-(2",2"-dimethyl-1",3"-dioxolane-4"-methyl)-4',4'-dimethyl-5'-oxo-2'- thioxo-1'-imidazolidinyl]-2-trifluoromethyl-benzonitrile;
- (g) 4-[3'-(2",3"-dihydroxypropyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazoli dinyl]-2-trifluoromethyl-benzonitrile;
- (h) 4-[3'-(2"-N-(t-butoxycarbonyl)-aminoethyl)-4',4'-dimethyl-5'-imino-2'-thio xo-1'-imidazolidinyl]-2-trifluoromethyl-benzonitrile;
- (i) 4-[3'-(2"-N-(t-butoxycarbonyl)-aminoethyl)-4',4'-dimethyl-5'-oxo-2'-thioxo -1'-imidazolidinyl]-2-trifluoromethyl-benzonitrile;
- (j) 4-[3'-(2"-aminoethyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl]-2 -trifluoromethyl-benzonitrile;
- (k) 4-[3'-(2"-N-acetylaminoethyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazoli dinyl]-2-trifluoromethyl-benzonitrile;
- (l) 4-[3'-(2",2"-dimethyl-1",3"-dioxolane-4"-methyl)-4',4'-dimethyl-5'-imino-2 '-thioxo-1'-imidazolidinyl]-2-trifluoromethyl-benzonitrile;
- (m) 4- [3'-(4"-fluorobutyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl]-2- trifluoromethyl-benzonitrile;
- (n) 4-[3'-trans-(2"-propenyl-3"-iodo)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imida zolidinyl]-2-trifluoromethyl-benzonitrile;
- (o) 4-[3'-gem-(2"-propenyl-2"-iodo)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazo lidinyl]-2-trifluoromethyl-benzonitrile;
- (p) 4-[3'-cis-(2"-propenyl-3"-iodo)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazo lidinyl]-2-trifluoromethyl-benzonitrile;
- (q) 4-[3'-methylcyclopropyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidazolidinyl ]-2-trifluoromethyl-benzonitrile;
- (r) 4-[3'-cis-(2"-propenyl-3"-bromo)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imidaz olidinyl]-2-trifluoromethyl-benzonitrile;
- (s) 4-[3'-trans-(2"-propenyl-3"-chloro)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-imi dazolidinyl]-2-trifluoromethyl-benzonitrile;
- and
- (t) 4-[3'-trans-(propanyl-3"-carboranyl)-4',4'-dimethyl-5'-oxo-2'-thioxo-1'-im idazolidinyl]-2-trifluoromethyl-benzonitrile.
Dependencies are inferred from the claim text.