发明公开
- 专利标题： 2,1-BENZISOTHIAZOLINE 2,2-DIOXIDES
- 专利标题（中）： 2,1-苯并异噻唑-2,2-二氧
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申请号： EP00930286.0申请日： 2000-05-01
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公开(公告)号： EP1175413A1公开(公告)日： 2002-01-30
- 发明人: COLLINS, Mark, A. , MACKNER, Valerie, A. , ZHI, Lin , JONES, Todd, K. , TEGLEY, Christopher, M. , WROBEL, Jay, E. , EDWARDS, James, P.
- 申请人： American Home Products Corporation , LIGAND PHARMACEUTICALS INCORPORATED
- 申请人地址： Five Giralda Farms Madison, New Jersey 07840 US
- 专利权人： American Home Products Corporation,LIGAND PHARMACEUTICALS INCORPORATED
- 当前专利权人： American Home Products Corporation,LIGAND PHARMACEUTICALS INCORPORATED
- 当前专利权人地址： Five Giralda Farms Madison, New Jersey 07840 US
- 代理机构： Hale, Stephen Geoffrey
- 优先权： US183039P 19990504; US552630 20000419
- 国际公布： WO0066574 20001109
- 主分类号： C07D275/06
- IPC分类号： C07D275/06 ; C07D413/04 ; A61K31/428 ; A61P15/00 ; A61P35/00
摘要：
A progesterone receptor antagonist of formula (1) wherein R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, heteroarylalkyl, and alkynyl; or R1 and R2 are taken together to form a ring and together contain -CH2(CH2)nCH2-, -CH2CH2CMe2CH2CH2-, -O(CH2)pCH2-, O(CH2)qO-, -CH2CH2OCH2CH2-, -CH2CH2NR7CH2CH2-; or R1 and R2 are a double bond, said double bond having two methyl groups bonded to the terminal end, having a cycloalkyl group bonded to the terminal end, having an oxygen bonded to the terminal end, or having a cycloether bonded to the terminal end; R5 is a trisubstituted phenyl ring having structure (z), or R5 is a five or six membered heteroaryl ring containing 1, 2, or 3 heteroatoms selected from the group consisting of O, S, SO¿2? and NR?6¿ or pharmaceutically acceptable salt thereof.
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