发明授权
US5100881A N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of
1-aminomethylphosphonic acid useful for the treatment of neoplastic
diseases
失效
用于治疗神经疾病的1-氨基乙基磷酸的N-(23-VINCRISTINOYL)和N-(5'-去甲基-23-VINBLASTINOYL)化合物
- 专利标题: N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of 1-aminomethylphosphonic acid useful for the treatment of neoplastic diseases
- 专利标题(中): 用于治疗神经疾病的1-氨基乙基磷酸的N-(23-VINCRISTINOYL)和N-(5'-去甲基-23-VINBLASTINOYL)化合物
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申请号: US561065申请日: 1990-08-01
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公开(公告)号: US5100881A公开(公告)日: 1992-03-31
- 发明人: Gilbert Lavielle , Patrick Hautefaye , Alain Pierre
- 申请人: Gilbert Lavielle , Patrick Hautefaye , Alain Pierre
- 申请人地址: FRX Courbevoie, Cedex
- 专利权人: Adir et Compagnie
- 当前专利权人: Adir et Compagnie
- 当前专利权人地址: FRX Courbevoie, Cedex
- 优先权: FRX8910554 19890804
- 主分类号: A61K31/675
- IPC分类号: A61K31/675 ; A61P35/00 ; C07F9/32 ; C07F9/6558 ; C07F9/6561
摘要:
The invention relates to the compounds of general formula I: ##STR1## in which: R.sub.1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkenyl radical containing from 2 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and which can bear a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidazolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each represents a linear or branched alkyl radical containing from 1 to 6 carbon atoms,n is equal to 1 or 2,R.sub.4 represents a hydrogen atom, a formyl radical or a methyl radical, with the proviso, however, that R.sub.4 is never the methyl radical when n is equal to 2, andeither R.sub.5 and R.sub.6 together form a double bond, or R.sub.5 represents a hydrogen atom and R.sub.6 a hydroxyl radical,in the form of a mixture of diastereoisomers or of pure isomers, their N.sub.b,-oxides and their addition salts with a pharmaceutically acceptable inorganic or organic acid.These compounds are antitumor agents.
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