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    • 6. 发明授权
    • Acyclic amide and sulfonamide ligands for the estrogen receptor
    • 用于雌激素受体的非环酰胺和磺酰胺配体
    • US07053212B2
    • 2006-05-30
    • US10666811
    • 2003-09-17
    • Kimberly O. CameronRichard Chesworth
    • Kimberly O. CameronRichard Chesworth
    • C07D279/12C07D295/12C07D413/12C07D211/18C07D207/04
    • C07D249/08C07C233/60C07C311/21C07C311/29C07C2601/02C07C2601/08C07C2601/14C07D207/08C07D207/16C07D211/14C07D211/42C07D211/46C07D213/38C07D213/40C07D215/20C07D215/36C07D217/02C07D231/12C07D233/56C07D261/10C07D295/088C07D295/135C07D295/185C07D307/12C07D333/34
    • The present invention provides estrogen receptor (ER) ligands of structural formula (I) the pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, and the pharmaceutically acceptable salts of the prodrugs, wherein R1, R2, R3, R4, R5, X, and Q are as defined herein. The invention further provides pharmaceutical compositions comprising the compounds of formula (I), and methods for treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER which comprise administering to a mammalian subject in need of treatment therewith, an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug, or a pharmaceutical composition comprising a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug. The invention further provides pharmaceutical compositions comprising combinations of the compounds of formula (I) and one or more of sodium fluoride, estrogen, a bone anabolic agent, a growth hormone or growth hormone secretagogue, a prostaglandin agonist/antagonist, and a parathyroid hormone, and methods of treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER comprising the administration of an effective amount of such combination to a mammalian subject in need of treatment therewith.
    • 本发明提供结构式(I)的药学上可接受的盐,立体异构体和前药的雌激素受体(ER)配体和前药的药学上可接受的盐,其中R 1,R 2, R 3,R 3,R 4,R 5,X和Q如本文所定义。 本发明还提供包含式(I)化合物的药物组合物,以及用于治疗或预防由ER介导的疾病,病症,病状或症状的方法,其包括向需要治疗的哺乳动物受试者施用有效量的 式(I)化合物或其药学上可接受的盐,立体异构体或前药,或前药的药学上可接受的盐,或包含式(I)化合物或其药学上可接受的盐,立体异构体, 或前药,或前药的药学上可接受的盐。 本发明进一步提供包含式(I)化合物与一种或多种氟化钠,雌激素,骨合成代谢剂,生长激素或生长激素促分泌素,前列腺素激动剂/拮抗剂和甲状旁腺激素的组合的药物组合物, 以及治疗或预防由ER介导的疾病,病症,病症或症状的方法,包括向需要治疗的哺乳动物受试者施用有效量的这种组合。