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    • 32. 发明授权
    • Dihydro-dibenzo[B,E]oxepine based selective estrogen receptor modulators, compositions and methods
    • 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
    • US07375229B2
    • 2008-05-20
    • US11276203
    • 2006-02-17
    • Owen Brendan Wallace
    • Owen Brendan Wallace
    • C07D409/00C07D411/00C07D417/00C07D211/06C07D419/00
    • C07D295/088C07D313/12C07D333/56C07D495/04
    • 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.
    • 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。
    • 33. 发明授权
    • Derivative of dihydro-dibenzo (a) anthracenes and their use as selective estrogen receptor modulators
    • 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
    • US07119206B2
    • 2006-10-10
    • US10527527
    • 2003-09-22
    • Owen Brendan Wallace
    • Owen Brendan Wallace
    • C07D211/66C07D265/30C07D207/04C07D333/54A61K31/435C07C309/65C07C211/19
    • C07D295/088C07D333/50
    • 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
    • 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