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    Water soluble camptothecin derivatives
    31.
    发明专利
    Water soluble camptothecin derivatives 未知

    公开(公告)号：AU657007B2

    公开(公告)日：1995-02-23

    申请号：AU2738592

    申请日：1992-10-28

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL JOSEPH ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER LESLIE

    IPC: A61K31/47 ,  A61K31/435 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07D498/22 ,  C07D405/10 ,  C07D413/10 ,  C07D417/10

    Abstract: The invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R and R represent independently, hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R represents hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R represents -COR wherein R represents hydrogen, lower alkyl, perhalo-lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or iii) R and R taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) wherein: Y represents O, S, CH , NR4 wherein R4 represents hydrogen, lower alkyl, perhalo-lower alkyl, aryl, aryl substituted with one or more lower alkyl, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl groups or; -COR5 wherein R5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups; and the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

    Pyrido[3,4-b]-pyridine antitumor compounds
    32.
    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.

    WATER-SOLUBLE DERIVATIVES OF CAMPTOTHECIN, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL PREPARATIONS IN WHICH THEY ARE COMPRISED
    37.
    发明专利
    WATER-SOLUBLE DERIVATIVES OF CAMPTOTHECIN, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL PREPARATIONS IN WHICH THEY ARE COMPRISED 未知

    公开(公告)号：CZ323792A3

    公开(公告)日：1993-10-13

    申请号：CS323792

    申请日：1992-10-27

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL JOSEPH ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER LESLIE

    IPC: A61K31/47 ,  A61K31/435 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07D498/22

    Abstract: The invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R and R represent independently, hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R represents hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R represents -COR wherein R represents hydrogen, lower alkyl, perhalo-lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or iii) R and R taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) wherein: Y represents O, S, CH , NR4 wherein R4 represents hydrogen, lower alkyl, perhalo-lower alkyl, aryl, aryl substituted with one or more lower alkyl, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl groups or; -COR5 wherein R5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups; and the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

    39.
    发明专利
    未知

    公开(公告)号：NO924158D0

    公开(公告)日：1992-10-28

    申请号：NO924158

    申请日：1992-10-28

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL JOSEPH ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER LESLIE

    IPC: A61K31/435 ,  A61K31/47 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07D498/22 ,  C07D

    Abstract: The invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R and R represent independently, hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R represents hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R represents -COR wherein R represents hydrogen, lower alkyl, perhalo-lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or iii) R and R taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) wherein: Y represents O, S, CH , NR4 wherein R4 represents hydrogen, lower alkyl, perhalo-lower alkyl, aryl, aryl substituted with one or more lower alkyl, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl groups or; -COR5 wherein R5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups; and the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

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