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    • 2. 发明授权
    • (3) and (6) substituted estrogenic compounds
    • (3)和(6)取代的雌激素化合物
    • US07179799B2
    • 2007-02-20
    • US10628057
    • 2003-07-23
    • Edward N. HillFrederick D. SancilioRobert R. Whittle
    • Edward N. HillFrederick D. SancilioRobert R. Whittle
    • A61K31/56C07J1/00
    • C07J1/00
    • Novel estrogenic compounds of Formula I are provided. wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower allyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an α or a β orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.
    • 提供式I的新型雌激素化合物。 其中由波浪线表示的键可以是单键或双键,使得当波浪线是单键时,R 1选自氢,硫酸根和葡糖醛酸酯或其它酯 ,并且当波浪线是双键时,R 1不存在; R 2是低级烷基; R 3可以选自氢,硫酸盐或葡糖苷酸或其它酯; 和R 4至R 13可以独立地选自氢,羟基,酮,低级烯丙基,低级烷氧基,卤素和羰基,R 14 选自氢,硫酸根和葡萄糖醛酸和其它酯。 当R 1是羟基时,羟基或酯取代基可具有α或β取向。 还提供包括本发明化合物的物质组合物,其方法是使用本发明化合物治疗需要治疗的哺乳动物。
    • 5. 发明授权
    • Estrogenic compounds, pharmaceutical compositions thereof, and methods of using same
    • 雌激素化合物,其药物组合物及其使用方法
    • US06660726B2
    • 2003-12-09
    • US09800614
    • 2001-03-08
    • Edward N. HillFrederick D. SancilioRobert R. Whittle
    • Edward N. HillFrederick D. SancilioRobert R. Whittle
    • A61K3156
    • C07J1/00
    • Novel estrogenic compounds of Formula I are provided. wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R1 is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R1 does not exist; R2 is lower alkyl; R3 may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R4 through R13 may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R14 is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R1 is hydroxy, the hydroxy or ester substituent may have either an &agr; or a &bgr; orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.
    • 提供式I的新型雌激素化合物,其中由波浪线表示的键可以是单键或双键,使得当波浪线是单键时,R 1选自氢,硫酸根和葡糖醛酸酯或其它 酯,当波浪线为双键时,R1不存在; R2是低级烷基; R3可以选自氢,硫酸盐或葡糖苷酸或其他酯; R 4至R 13可以独立地选自氢,羟基,酮,低级烷基,低级烷氧基,卤素和羰基,R 14选自氢,硫酸根和葡萄糖醛酸和其它酯。 当R 1是羟基时,羟基或酯取代基可具有α或β取向。 还提供包括本发明化合物的物质组合物,其方法是使用本发明化合物治疗需要治疗的哺乳动物。