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    5.
    发明专利
    未知

    公开(公告)号：MX9307011A

    公开(公告)日：1994-05-31

    申请号：MX9307011

    申请日：1993-11-10

    Applicant: GLAXO INC

    Inventor： BESTERMAN JEFFREY MARK ,  STERNBACH DANIEL DAVID ,  PEEL MICHAEL ROBERT ,  LACKEY KAREN ,  LUZZIO MICHAEL JOSEPH ,  EVANS MICHAEL GLENN

    IPC: A61K31/47 ,  A61K31/675 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07F9/6561

    Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (I). wherein A represents a moiety of the formula (IIA), (IIB) or (IIC): X is selected from the group consisting of alkyl, aryl, (CH2)mOR1, (CH2)mSR1 and (CH2)mNR1R2 wherein m is an integer of 0 to 6, and R1 and R2 are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.

    Pyrido[3,4-b]-pyridine antitumor compounds
    9.
    发明专利
    Pyrido[3,4-b]-pyridine antitumor compounds 未知

    公开(公告)号：GB2280674A

    公开(公告)日：1995-02-08

    申请号：GB9415663

    申请日：1994-08-03

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL JOSEPH ,  STERNBACH DANIEL DAVID ,  UEHLING DAVID E ,  PROFETA JUNIOR SALVATORE

    IPC: C07D491/22 ,  A61K31/435

    Abstract: Camptothecin derivatives of formula (I> wherein R is hydrogen, alkyl, alkenyl or phenyl; Q is hydrogen, halogen, cyano, 5-tetrazolo, -COOR , -CONR R , -C(NH2)=NR , -CH=NNH2, -(CH2)nR , -CH=CH(CH2)nR or -C=C(CH2)nR wherein n is 0, 1, 2 or 3; R is hydrogen or alkyl; R and R independently represent hydrogen, alkyl, aminoalkyl or dialkylaminoalkyl; R is hydrogen, alkyl, hydroxy, alkoxy or -COOCH2NHCOO Bu; R is hydrogen, hydroxy, -NR R , -NHCOR or a nitrogen heterocycle of formula wherein R and R independently represent hydrogen or alkyl; R is alkyl or O-alkyl; Y is O, S, NR , CH2 or a direct linkage; R is hydrogen or alkyl; T is hydrogen or when Q is halogen T may also represent halogen; and X is a free electron pair, oxygen or alkyl; and pharmaceutically acceptable salts thereof, are topoisomerase inhibitors useful in the treatment of cancer. Pyridines of formula (II> wherein R* is methyl or ethyl Q is Br and T is H or Br; and derivatives corresponding to formula (I) but with the E ring open are novel intermediates.

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