发明公开
EP0700376A1 NITROBENZYL MUSTARD QUATERNARY SALTS AND THEIR USE AS HYPOXIA-SELECTIVE CYTOTOXIC AGENTS
失效
第四纪硝基芥子气盐及其用途HYPOXÄMIESELEKTIVE细胞毒性药物
- 专利标题: NITROBENZYL MUSTARD QUATERNARY SALTS AND THEIR USE AS HYPOXIA-SELECTIVE CYTOTOXIC AGENTS
- 专利标题(中): 第四纪硝基芥子气盐及其用途HYPOXÄMIESELEKTIVE细胞毒性药物
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申请号: EP94917204.0申请日: 1994-05-24
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公开(公告)号: EP0700376A1公开(公告)日: 1996-03-13
- 发明人: WILSON, William Robert, School of Medicine , TERCEL, Moana, School of Medicine , DENNY, William Alexander, School of Medicine
- 申请人: AUCKLAND UNISERVICES LIMITED
- 申请人地址: UniServices House, 58 Symonds Street Auckland 1001 NZ
- 专利权人: AUCKLAND UNISERVICES LIMITED
- 当前专利权人: AUCKLAND UNISERVICES LIMITED
- 当前专利权人地址: UniServices House, 58 Symonds Street Auckland 1001 NZ
- 代理机构: Dearing-Lambert, Peter Richard, et al
- 优先权: NZ19930245270 19930525
- 国际公布: WO1994027954 19941208
- 主分类号: A61K31
- IPC分类号: A61K31 ; A61K47 ; A61P35 ; A61P43 ; C07C209 ; C07C211 ; C07C217 ; C07C237 ; C07C309 ; C07C317 ; C07C323 ; C07D233
摘要:
Nitrobenzyl mustard quaternary salts of formula (I), and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain -CR1R2- or CR1=CR2- (where R1 and R2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO2R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or ether groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO2, SO2R, CONHR, R, OR, SR, CF3 and aza (ring -CH= replaced by -N=); with the proviso that when Y=Cl or Br, Q=Me, and X=-CH2- then Ar¸ 2-nitrophenyl or 4-nitrophenyl.
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