Dihydro-dibenzo[B,E]oxepine based selective estrogen receptor modulators, compositions and methods
    37.
    发明授权
    Dihydro-dibenzo[B,E]oxepine based selective estrogen receptor modulators, compositions and methods 失效
    二氢二苯并[B,E]氧自由基的选择性雌激素受体调节剂,组合物和方法

    公开(公告)号:US07375229B2

    公开(公告)日:2008-05-20

    申请号:US11276203

    申请日:2006-02-17

    摘要: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC═CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation, and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

    摘要翻译: 本发明提供式(I)的化合物,其中R 1是-H,-OH,-O(C 1 -C 4) 烷基),-OCOC 6 H 5,-OCO(C 1 -C 6烷基),或 (C 2 -C 6烷基);和(C 2 -C 6)烷基)。 R 0,R 2和R 3各自独立地为-H,-OH,-O(C 1 H 3) -C≡C4烷基),-OCOC 6 H 5,-OCO(C 1 -C 4烷基) 6烷基),-OSO 2(C 2 -C 6烷基)或卤素; R4是1-哌啶基,1-吡咯烷基,甲基-1-吡咯烷基,二甲基-1-吡咯烷基,4-吗啉代,二甲基氨基,二乙基氨基,二异丙基氨基或1-六亚甲基亚氨基; n为2或3; X是-S-或-HC-CH-; G是-O - , - S-,-SO-,SO 2 - 或-N(R 5) - ,其中R 5, 是-H或C 1 -C 4烷基; 和Y是-O - , - S-,-NH-,-NMe - 或-CH 2 - ,或其药学上可接受的盐,其药物组合物,任选地与雌激素和孕激素组合 ; 抑制与雌激素剥夺相关的疾病的方法,以及抑制与内源性雌激素异常生理反应有关的疾病的方法。

    Derivative of dihydro-dibenzo (a) anthracenes and their use as selective estrogen receptor modulators
    38.
    发明授权
    Derivative of dihydro-dibenzo (a) anthracenes and their use as selective estrogen receptor modulators 失效
    二氢二苯并(a)蒽衍生物及其作为选择性雌激素受体调节剂的用途

    公开(公告)号:US07119206B2

    公开(公告)日:2006-10-10

    申请号:US10527527

    申请日:2003-09-22

    CPC分类号: C07D295/088 C07D333/50

    摘要: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is S— or —HC═CH—; and Y is O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen

    摘要翻译: 本发明提供式(I)的化合物,其中R 1是-H,-OH,-O(C 1 -C 4) 烷基),-OCOC 6 H 5,-OCO(C 1 -C 6烷基),或 (C 2 -C 6烷基);和(C 2 -C 6)烷基)。 R 0,R 2和R 3各自独立地为-H,-OH,-O(C 1 H 3) -C≡C4烷基),-OCOC 6 H 5,-OCO(C 1 -C 4烷基) 6烷基),-OSO 2(C 2 -C 6烷基)或卤素; R 4是1-哌啶基,1-吡咯烷基,甲基-1-吡咯烷基,二甲基-1-吡咯烷基,4-吗啉代,二甲基氨基,二乙基氨基,二异丙基氨基或1-六亚甲基亚氨基; n为2或3; X是S-或-HC-CH-; 和Y是O-,-S - , - NH - , - MeMe-或-CH 2 - 。 或其药学上可接受的盐; 其药物组合物,任选与雌激素和孕激素组合; 抑制与雌激素剥夺有关的疾病的方法; 以及用于抑制与内源性雌激素异常生理反应相关的疾病的方法