发明公开
EP0740667A1 PROCESS AND INTERMEDIATES FOR PREPARING NAPHTHYRIDONECARBOXYLIC ACID SALTS
失效
过程和中间产品用于制备naphthyridonecarboxylic酸盐
- 专利标题: PROCESS AND INTERMEDIATES FOR PREPARING NAPHTHYRIDONECARBOXYLIC ACID SALTS
- 专利标题(中): 过程和中间产品用于制备naphthyridonecarboxylic酸盐
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申请号: EP95901569.0申请日: 1994-12-12
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公开(公告)号: EP0740667A1公开(公告)日: 1996-11-06
- 发明人: BRAISH, Tamim, F. , FOX, Darrell, E. , NORRIS, Timothy , ROSE, Peter, R.
- 申请人: PFIZER INC.
- 申请人地址: 235 East 42nd Street New York, N.Y. 10017 US
- 专利权人: PFIZER INC.
- 当前专利权人: PFIZER INC.
- 当前专利权人地址: 235 East 42nd Street New York, N.Y. 10017 US
- 代理机构: Wood, David John, et al
- 优先权: US19940181942 19940118
- 国际公布: WO1995019361 19950720
- 主分类号: A61K31
- IPC分类号: A61K31 ; A61P31 ; C07D209 ; C07D471
摘要:
This invention relates to novel processes for preparing compounds of formula (I), wherein R1H is as defined below, which is a salt of the naphthyridone antibiotic 7-(1α,5α,6α)-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carbocylic acid and a pharmaceutically acceptable acid. The salt and antibiotics have antibacterial activity. This invention also relates to novel intermediates, and processes for their preparation, of formulae (IV), (IIIB) or (IIIA). The compounds of formulae (IIIA), (IIIB) and (IV) are useful as intermediates in the syntheses of the azabicyclo naphthyridone carboxylic acid alkanesulfonic acid salts of formula (I).
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