发明授权
- 专利标题： Pentacyclic oxepines and derivatives thereof, compositions and methods
- 专利标题（中）： 五环氧基及其衍生物，组合物和方法
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申请号： US10521998申请日： 2003-07-18
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公开(公告)号： US07271264B2公开(公告)日： 2007-09-18
- 发明人: Ronald Jay Hinklin , Owen Brendan Wallace
- 申请人： Ronald Jay Hinklin , Owen Brendan Wallace
- 申请人地址： US IN Indianapolis
- 专利权人： Eli Lilly and Company
- 当前专利权人： Eli Lilly and Company
- 当前专利权人地址： US IN Indianapolis
- 代理商 John C. Demeter; Gilbert T. Voy
- 国际申请： PCT/US03/19561 WO 20030718
- 国际公布： WO2004/009578 WO 20040129
- 主分类号： C07D211/22
- IPC分类号： C07D211/22 ; C07D405/12 ; C07D409/12
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-pyrrolidiny, 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.
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