Patent ID: 6291451
Filing Date: 2001-09-18
Classification: A61K,A61P,C07D

Abstract:
A method of treating or inhibiting breast cancer in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound of formula I or II, having the structures ##STR183##R.sub.1 is selected from H, OH or the C.sub.1 -C.sub.12 esters (straight chain or branched) or C.sub.1 -C.sub.12 (straight chain or branched or cyclic) alkyl ethers thereof, or halogens; or C.sub.1 -C.sub.4 halogenated ethers including triflouromethyl ether and trichloromethyl ether;R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently selected from H, OH or the C.sub.1 -C.sub.12 esters (straight chain or branched) or C.sub.1 -C.sub.12 alkyl ethers (straight chain or branched or cyclic) thereof, halogens, or C.sub.1 -C.sub.4 halogenated ethers including triflouromethyl ether and trichloromethyl ether, 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 selected from:a) the moiety: ##STR184##wherein 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;b) a five-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.m --, wherein m is an integer of from 0-2, 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 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl;c) a six-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.m --, wherein m is an integer of from 0-2, 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 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl;d) a seven-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.m --, wherein m is an integer of from 0-2, 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 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; ore) a bicyclic heterocycle containing from 6-12 carbon atoms either bridged or fused and containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, and --S(O).sub.m --, wherein m is an integer of from 0-2, 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 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4) alkyl; or a pharmaceutically acceptable salt thereof.