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    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

    申请人： Gerhard Hoefle ,  Nicole Glaser ,  Heinrich Steinmetz ,  Thomas Leibold ,  Florenz Sasse

    发明人： Gerhard Hoefle ,  Nicole Glaser ,  Heinrich Steinmetz ,  Thomas Leibold ,  Florenz Sasse

    IPC分类号： C07D417/00 ,  A61K31/445

    CPC分类号： C07D417/12 ,  A61K38/00 ,  C07D417/14 ,  C07K5/021

    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。