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    • 6. 发明申请
    • CEPHALOSPORIN DERIVATIVES AS ANTI-CANCER AGENTS
    • CEPHALOSPORIN衍生物作为抗癌剂
    • WO2002096430A1
    • 2002-12-05
    • PCT/NL2002/000356
    • 2002-05-31
    • KYLIX B.V.BARKER, NicholasVON KRIES, Jens, PeterBROHM, Dirk, EckartKRäMER, Timo, AlexanderSTIEBER, Frank
    • BARKER, NicholasVON KRIES, Jens, PeterBROHM, Dirk, EckartKRäMER, Timo, AlexanderSTIEBER, Frank
    • A61K31/54
    • C07D501/00C07D279/06
    • The invention relates to a compound and/or pharmaceutically acceptable salts, esters, hydrates or solvates thereof, having the structural formula (1) or (2): (Please insert formulas 1 and 2)wherein:- X and Y are independently selected from the group comprising: H,C,N,O,S or alkyl,- W is selected from the group comprising: NH 2 , NH-R 1 , NH-CO-R 1 , NH-CO-Cn-O-R 1 , | R 4 NH-CO-Cn-R 1 , NH-CO-O-Cn-R 1 , NH-CO-Cn-S-R 1 , NH-CO-Cn-NH- R 1 | | | | R 4 R 4 R 4 R 4 wherein R 4 is optional, and n = 1-12, preferably 1-6 and more preferably 1-4- V is selected from the group comprising: H, C, N, O, S or a terminal alkyl group, whereby when V is a terminal alkyl group, X and R 2 are nothing,- Z is selected from the group comprising: S, S = O, O = S = O,- Q is selected from the group comprising: H, or R 1 , R 2 , R 3 , or R 4 - R 1 , R 2 , R 3 , or R 4 are independently selected from the group comprising: H, alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxycarbonyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl.
    • 本发明涉及具有结构式(1)或(2)的化合物和/或其药学上可接受的盐,酯,水合物或溶剂化物:(请插入式1和2)其中:-X和Y独立地选自 所述基团包括:H,C,N,O,S或烷基,-W选自:NH 2,NH-R 1,NH-CO-R 1,NH-CO-Cn-O-R 1, R4 NH-CO-Cn-R1,NH-CO-O-Cn-R1,NH-CO-Cn-S-R1,NH-CO-Cn-NH-R1 | | | | R4 R4 R4 R4其中R4是任选的,n = 1-12,优选1-6,更优选1-4-V选自H,C,N,O,S或末端烷基, 当V是末端烷基时,X和R 2不是-Z选自S,S = O,O = S = O,-Q选自H或R 1, R 2,R 3或R 4 -R 1,R 2,R 3或R 4独立地选自H,烷基,烯基,炔基,环烷基,烷氧基,烷氧基羰基,芳基,芳基烷基,杂芳基,杂环烷基。