发明名称 ACRYLONITRILE DERIVATIVE
摘要 PROBLEM TO BE SOLVED: To obtain a metallo-β-lactamase inhibitor capable of suppressing the deactivation of aβ-lactam antibiotic substance by including a specific acrylonitrile compound or its pharmacologically permissible salt. SOLUTION: An acrylonitrile compound of formula I [Ar1 and Ar2 are each a (substituted) 6-10C aryl or a (substituted) monocyclic to tricyclic aromatic heterocyclic group containing 1-3 N, O or S atoms] or its pharmacologically permissible salt is used as an active component. The compound of formula I is preferably a compound of formula II (R1 is n-propyl, n-butyl or the like; R2 is H, vinyl or methoxy; and X is O or NH) [e.g. (z)-3-(4-propylphenyl)-2-(3- indolyl)-acrylonitrile]. The compound of formula I can be produced by the thermal dehydrative condensation of an aromatic aldehyde compound of the formula, Ar1CHO with an aromatic acetonitrile compound of the formula, Ar2 CH2CN in a solvent in the presence of a base.
申请公布号 JP2000336075(A) 申请公布日期 2000.12.05
申请号 JP19990146511 申请日期 1999.05.26
申请人 SANKYO CO LTD 发明人 KAWAMOTO ISAO;KANEKO SATORU;SAKURAI MITSUYA;MURAMATSU YASUNORI
分类号 C07D307/79;A61K31/00;A61K31/34;A61K31/343;A61K31/40;A61K31/403;A61K31/404;A61P31/00;A61P31/04;A61P43/00;C07D209/18;(IPC1-7):C07D209/18 主分类号 C07D307/79
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