发明申请
- 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: US20050261277A1公开(公告)日: 2005-11-24
- 发明人: Ronald Hinklin , Owen Wallace
- 申请人: Ronald Hinklin , Owen Wallace
- 专利权人: ELI LILLY AND COMPANY
- 当前专利权人: ELI LILLY AND COMPANY
- 国际申请: PCT/US03/19561 WO 20030718
- 主分类号: C07D295/08
- IPC分类号: C07D295/08 ; A61K31/381 ; A61K31/4025 ; A61K31/4427 ; A61K31/4436 ; A61K31/4453 ; A61K31/453 ; A61K31/5377 ; A61K31/55 ; A61P9/10 ; A61P15/00 ; A61P15/12 ; A61P19/08 ; A61P35/00 ; A61P43/00 ; C07D313/06 ; C07D313/10 ; C07D333/56 ; C07D333/68 ; C07D409/10 ; C07D495/02 ; C07D495/04 ; C07D498/02
摘要:
The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC—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═H—; 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.