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    • 9. 发明授权
    • 1-(4-(Substituted alkoxy)benzyl)naphthalene compounds having estrogen inhibitory activity
    • 具有雌激素抑制活性的1-(4-(取代烷氧基)苄基)萘化合物
    • US06509356B1
    • 2003-01-21
    • US09129119
    • 1998-08-04
    • Jeffrey Alan DodgeAndrew Lawrence GlasebrookCharles Willis Lugar, III
    • Jeffrey Alan DodgeAndrew Lawrence GlasebrookCharles Willis Lugar, III
    • A61K31445
    • C07D207/08C07C217/20C07C275/28C07C275/30C07C275/34C07D207/27C07D211/22C07D221/20C07D295/088C07D295/112C07D473/08
    • A class of substituted benzylnaphthylene compounds of the structure where R1 and R2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is —(CH2)1-6; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N′-(lower alkyl)ureido; or N, N′-(di-lower alkyl ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl) pyrrolidinyl]; 1- 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.5]undecan-3-yl; pyrrolidinon-1-yl; unsubstituted phenyl; or phenyl substituted with acyl of two to four carbon atoms, alkyl of one to four carbon atoms, halo, or alkoxy of one to four carbon atoms; with the proviso that n is not 2 or 3 when Z is 1-pyrrolidinyl, 1-piperidinyl, 1-azepinyl, 4-morpholinyl, N,N-dimethylamino or N,N-diethylamino; are selective estrogen receptor modulators useful in the prophylaxis or treatment of breast cancer.
    • 一类取代的苄基萘酚化合物,其中R 1和R 2独立地是氢,1至6个碳原子的烷基,2至6个碳原子的酰基或苯甲酰甲基; X是 - (CH 2)1-6; Y不存在或选自1,4-哌嗪基; 脲基 N-(低级烷基)脲基; N' - (低级烷基)脲基; 或N,N' - (二 - 低级烷基脲基; Z是1-,2-或3-吡咯烷基; 1-,2-或3- [1-(低级烷基)吡咯烷基] 3-或4-哌啶基; 1-,2-,3-或4- [1-低级烷基)哌啶基]; N,N-二烷基; 1-氮杂基; 1-或2-萘基氨基,4-吗啉基,二甲基-4-吗啉基,3-氮杂螺[5.5]十一烷-3-基; 吡咯烷酮-1-基; 未取代的苯基; 或被2-4个碳原子的酰基取代的苯基,1-4个碳原子的烷基,卤素或1-4个碳原子的烷氧基; 条件是当Z是1-吡咯烷基,1-哌啶基,1-氮杂基,4-吗啉基,N,N-二甲基氨基或N,N-二乙基氨基时,n不是2或3。 是可用于预防或治疗乳腺癌的选择性雌激素受体调节剂。