Tubulysins, method for producing the same and tubulysin preparations
    8.
    发明授权
    Tubulysins, method for producing the same and tubulysin preparations 有权
    Tubulysins,其制备方法和tubulysin制剂

    公开(公告)号:US07754885B2

    公开(公告)日:2010-07-13

    申请号:US10535630

    申请日:2003-10-20

    IPC分类号: C07D417/00 A61K31/445

    摘要: The invention relates to a compound of the following general formula (tubulysin) having the following meanings for R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, S, T, U, V, W, X, Y and Z: R=H, alkyl, aryl, OR1, NR1R2 or R1=H, C1-6alkyl or aryl R2=H, C1-6alkyl or aryl S=H, Hal, NO2 or NHR3 U=H, Hal, NO2 or NHR3 R3=H, HCO or C1-4alkyl-CO T=H or OR4 R4=H, C1-4alkyl, aryl, COR5, P(O)(OR6)2 or SO3R6 R5=C1-6alkyl, alkenyl, aryl or heteroaryl R6=H, alkyl or a metal ion V=H, OR7, Hal or (for W=O) O R7=H, C1-4alkyl or COR8 R5=C1-4alkyl, alkenyl or aryl W=H or C1-4alkyl or (for V=O) O X=H, C1-4alkyl, alkenyl or CH2OR9 R9=H, C1-4alkyl, alkenyl, aryl or COR10 R10=C1-6alkyl, alkenyl, aryl or heteroaryl Y=(for Z=CH3 or COR11) free electron pair or (for Z=CH3)O R11=C1-4alkyl, CF3 or aryl and/or Z=(for Y=O or free electron pair) CH3 or (for Y=free electron pair) COR11.

    摘要翻译: 本发明涉及对R,R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9,R 10,R 11,S,T,U,V具有以下含义的下列通式(管状素)的化合物 ,W,X,Y和Z:R = H,烷基,芳基,OR1,NR1R2或R1 = H,C1-6烷基或芳基R2 = H,C1-6烷基或芳基S = H,Hal,NO2或NHR3 U = H,Hal,NO 2或NHR 3 R 3 = H,HCO或C 1-4烷基-CO T = H或OR 4 R 4 = H,C 1-4烷基,芳基,COR 5,P(O)(OR 6)2或SO 3 R 6 R 5 = ,烯基,芳基或杂芳基R6 = H,烷基或金属离子V = H,OR7,Hal或(对于W = O)O R7 = H,C1-4烷基或COR8 R5 = C1-4烷基,烯基或芳基W = H或C 1-4烷基或(对于V = O)O X = H,C 1-4烷基,烯基或CH 2 OR 9 R 9 = H,C 1-4烷基,烯基,芳基或COR 10 R 10 = C 1-6烷基,烯基,芳基或杂芳基Y = 对于Z = CH 3或COR 11)自由电子对或(对于Z = CH 3)O R 11 = C 1-4烷基,CF 3或芳基和/或Z =(对于Y = O或自由电子对)CH 3或(对于Y = 对)COR11。