发明名称 1,3-diarylprop-2-en-1-ones, compositions containing same and use thereof
摘要 Disclosed is a compound according to formula (I) wherein: Y is a halogen, linear or branched C1-C7 Alkyl (substituted or unsubstituted), a substituted or unsubstituted cycloalkyl, NH2, NH(R4), N(R4)2, aralkyl, substituted aralkyl, COOH, COO(R4), CONH2, CONH(R4), CON(R4)2, CN in which R4 is an optionally substituted alkyl or cycloalkyl group; Ar2 is a phenyl substituted by R1 and R2 where: one of R1 and R2 is selected from NH2, NH2HZ, NHC(O)-amino acid, N(R5)2 in which R5 is a C1-C2 alkyl group, NH-(GP), N=(GP) where GP is a metabolisable substituent; the other of R1 and R2 is selected from the group consisting of CH3, C2H5, OCH3, OC2H5, SCH3, NH(R5), N(R5)2, N(R5)GP, N(R5)C(O)-amino acid in which R5 is an alkyl group; X is selected from the group consisting of O, NOH, NO(R3), in which R3 is selected from the group consisting of H, linear or branched alkyl, cycloalkyl, halogenated alkyl, substituted cycloalkyl, halogenated cycloalkyl, halogenated cycloalkyl, aralkyl or substituted aralkyl; Ar is selected from groups containing di-, tri- and tetra- methoxyphenyls, ethylene dioxies, or methylene dioxies. Also disclosed is a pharmaceutical composition of the above drug used in the preparation of a medicament inhibiting the polymerization of tubulin, thereby promoting tumour necrosis and treating cancer.
申请公布号 NZ533224(A) 申请公布日期 2006.03.31
申请号 NZ20020533224 申请日期 2002.12.03
申请人 AVENTIS PHARMA S 发明人 MAILLIET, PATRICK;COMBEAU, CECILE;BISSERY, MARIE-CHRISTINE;CHERRIER, MARIE-PIERRE;CAULFIELD, THOMAS;TIRABOSCHI, GILLES
分类号 A61K31/136;A61K31/167;A61K31/404;A61P9/00;A61P35/00;A61P43/00;C07C225/22;C07C237/04;C07C279/36;C07D207/16;C07D209/08;C07D405/06;(IPC1-7):C07C225/22;A61K31/137 主分类号 A61K31/136
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