Patent ID: 6225308
Filing Date: 2001-05-01
Classification: A61K,A61P,C07D

Abstract:
A method of treating prostate cancer or benign prostate hypertrophy in a mammal, the method comprising administering to a mammal in need thereof an effective amount of a compound of the formulae: ##STR181##wherein:R.sub.1 is selected from H, OH, --O--C(O)--C.sub.1 -C.sub.12 alkyl (straight chain or branched), --O--C.sub.1 -C.sub.12 alkyl (straight chain or branched or cyclic), or halogens; or C.sub.1 -C.sub.4 halogenated ethers.R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently selected from H, OH, --O--C(O)--C.sub.1 -C.sub.12 (straight chain or branched), --O--C.sub.1 -C.sub.12 (straight chain or branched or cyclic), halogens, or C.sub.1 -C.sub.4 halogenated ethers, cyano, C.sub.1 -C.sub.6 alkyl (straight chain or branched), or trifluoromethyl, with the proviso that, when R.sub.1 is H, R.sub.2 is not OH;X is selected from H, C.sub.1 -C.sub.6 alkyl, cyano, nitro, trifluoromethyl, halogen;n is 2 or 3;Y is the moiety: ##STR182##wherein:a) R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.6 alkyl, or phenyl optionally substituted by CN, C.sub.1 -C.sub.6 alkyl (straight chain or branched), C.sub.1 -C.sub.6 alkoxy (straight chain or branched), halogen, --OH, --CF.sub.3, or --OCF.sub.3 ; orb) R.sub.7 and R.sub.8 are concatenated to form a five-membered saturated heterocycle containing one nitrogen heteroatom, the heterocycle being optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H, --CN--, --CONHR.sub.1, --NH.sub.2, --NH(C.sub.1 -C.sub.4 alkyl), --N(C.sub.1 -C.sub.4 alkyl).sub.2, --NHSO.sub.2 R.sub.1, --NHCOR.sub.1, --NO.sub.2, or phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; orc) R.sub.7 and R.sub.8 are concatenated to form a six-membered saturated heterocycle containing one nitrogen heteroatom, the heterocycle being optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H, --CN, --CONHR.sub.1, --NH.sub.2, --NH(C.sub.1 -C.sub.4 alkyl), --N(C.sub.1 -C.sub.4 alkyl).sub.2, --NHSO.sub.2 R.sub.1, --NHCOR.sub.1, --NO.sub.2, or phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; ord) R.sub.7 and R.sub.8 are concatenated to form a seven-membered saturated heterocycle containing one nitrogen heteroatom, the heterocycle being optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H, --CN, --CONHR.sub.1, --NH.sub.2, --NH(C.sub.1 -C.sub.4 alkyl), --N(C.sub.1 -C.sub.4 alkyl).sub.2, --NHSO.sub.2 R.sub.1, --NHCOR.sub.1, --NO.sub.2, or phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; ore) R.sub.7 and R.sub.8 are concatenated to form an eight-membered saturated heterocycle containing one nitrogen heteroatom, the heterocycle being optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H, --CN, --CONHR.sub.1, --NH.sub.2, --NH(C.sub.1 -C.sub.4 alkyl), --N(C.sub.1 -C.sub.4 alkyl).sub.2, --NHSO.sub.2 R.sub.1, --NHCOR.sub.1, --NO.sub.2, or phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; orf) R.sub.7 and R.sub.8 are concatenated to form a saturated bicyclic heterocycle containing from 6-12 carbon atoms either bridged or fused and containing one nitrogen heteroatom, the heterocycle being optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H, --CN, --CONHR.sub.1, --NH.sub.2, --NH(C.sub.1 -C.sub.4 alkyl), --N(C.sub.1 -C.sub.4 alkyl).sub.2, --NHSO.sub.2 R.sub.1, --NHCOR.sub.1, --NO.sub.2, or phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4) alkyl;or a pharmaceutically acceptable salt thereof.