Patent ID: 6835729
Filing Date: 2004-12-28
Classification: A61K,A61P,C07D

Abstract:
A method of lowering cholesterol levels 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 wherein:R1 is selected from H, OH or the C1-C12 esters (straight chain or branched) or C1-C12 (straight chain or branched or cyclic) alkyl ethers thereof, or halogens; or C1-C4 halogenated ethers including triflouromethyl ether and trichloromethyl ether, R2, R3, R4, R5, and R6 are independently selected from H, OH or the C1-C12 esters (straight chain or branched) or C1-C12 alkyl ethers (straight chain or branched or cyclic) thereof, halogens, or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether, cyano, C1-C6 alkyl (straight chain or branched), or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH, X is selected from H, C1-C6 alkyl, cyano, nitro, trifluoromethyl, halogen; n is 2 or 3; Y is selected from: a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl optionally substituted by CN, C1-C6 alkyl (straight chain or branched), C1-C6 alkoxy (straight chain or branched), halogen, â€”OH, â€”CF3 or â€”OCF3; b) a five-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of â€”Oâ€”, â€”NHâ€”, â€”N(C1C4 alkyl)â€”, â€”N&boxH;, and â€”S(O)mâ€”, 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, C1-C4 alkyl, trihalomethyl, C1-C4 acyloxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 akylsulfonyl, hydroxy (C1-C4)alkyl, â€”CO2Hâ€”, â€”CNâ€”, â€”CONHR1â€”, â€”NH2â€”, C1-C4 alkylamino, di(C1-C4)alkylamino, â€”NHSO2R1â€”, â€”NHCOR1â€”, â€”NO2, and phenyl optionally substituted with 1-3 (C1-C4)alkyl; c) a six-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of â€”Oâ€”, â€”NHâ€”, â€”N(C1C4 alkyl)â€”, â€”N&boxH;, and â€”S(O)mâ€”, 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, C1-C4 alkyl, trihalomethyl, C1-C4 alkoxy, trihalomethoxy, C1-C4 acyloxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, hydroxy (C1-C4)alkyl, â€”CO2Hâ€”, â€”CNâ€”, â€”CONHR1â€”, â€”NH2â€”, C1-C4 alkylamino, di(C1-C4)alkylamino, â€”NHSO2R1â€”, â€”NHCOR1â€”, â€”NO2, and phenyl optionally substituted with 1-3 (C1-C4)alkyl; d) a seven-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of â€”Oâ€”, â€”NHâ€”, â€”N(C1C4 alkyl)â€”, â€”N&boxH;, and â€”S(O)mâ€”, 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, C1-C4 alkyl, trihalomethyl, C1-C4 alkoxy, trihalomethoxy, C1-C4 acyloxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, hydroxy (C1-C4)alkyl, â€”CO2Hâ€”, â€”CNâ€”, â€”CONHR1â€”, â€”NH2â€”, C1-C4 alkylamino, di(C1-C4)alkylamino, â€”NHSO2R1â€”, â€”NHCOR1â€”, â€”NO2, and phenyl optionally substituted with 1-3 (C1-C4)alkyl; or e) 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 â€”Oâ€”, â€”NHâ€”, â€”N(C1C4 alkyl)â€”, and â€”S(O)mâ€”, 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, C1-C4 alkyl, trihalomethyl, C1-C4 alkoxy, trihalomethoxy, C1-C4 acyloxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, hydroxy (C1-C4)alkyl, â€”CO2Hâ€”, â€”CNâ€”, â€”CONHR1â€”, â€”NH2â€”, C1-C4 alkylamino, di(C1-C4)alkylamino, â€”NHSO2R1â€”, â€”NHCOR1â€”, â€”NO2, and phenyl optionally substituted with 1-3 (C1-C4) alkyl; or a pharmaceutically acceptable salt thereof.