发明公开
- 专利标题: N-FORMYL HYDROXYLAMINE COMPOUNDS
- 专利标题(中): N-甲酰基羟胺CONNECTIONS
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申请号: EP06770806.5申请日: 2006-05-22
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公开(公告)号: EP1896452A2公开(公告)日: 2008-03-12
- 发明人: BRACKEN, Kathryn Rene , BUSHELL, Simon , DEAN, Karl , FRANCAVILLA, Charles , JAIN, Rakesh K. , LEE, Kwangho , SEEPERSAUD, Mohindra , SHU, Lei , SUNDARAM, Arathia , YUAN, Zhengyu
- 申请人: Novartis Pharma AG , NOVARTIS-PHARMA GMBH , Vicuron Pharmaceuticals, Inc.
- 申请人地址: Lichtstrasse 35 4002 Basel CH
- 专利权人: Novartis Pharma AG,NOVARTIS-PHARMA GMBH,Vicuron Pharmaceuticals, Inc.
- 当前专利权人: Novartis Pharma AG,NOVARTIS-PHARMA GMBH,Vicuron Pharmaceuticals, Inc.
- 当前专利权人地址: Lichtstrasse 35 4002 Basel CH
- 代理机构: Crawley, Patrick Edward
- 优先权: US683655P 20050523
- 国际公布: WO2006127576 20061130
- 主分类号: C07D401/12
- IPC分类号: C07D401/12 ; C07D403/12 ; A61P31/04
摘要:
Novel N-formyl hydroxylamine compounds (I) and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes . The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed. wherein R1 is hydrogen, alkyl, heteroalkyi, heterocycloalkyl, aryl or heteroaryl.; R3 is hydrogen, halogen, or alkoxy; R4 is aryl, or heteroaryl; or n is 0 to 3 and provided that R1 is cycloalkyl and/or R4 is an optionally substituted 6 membered, monocyclic heteroaryl ring having 2, 3 or 4 nitrogen heteroatoms in the ring wherein one or more of the ring nitrogen heteroatoms is optionally oxidized.
公开/授权文献
- EP1896452B1 N-FORMYL HYDROXYLAMINE COMPOUNDS 公开/授权日:2011-11-16
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