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    SUBSTITUTED PHENYL-1,3 DIOXOLOQUINOLINE DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS
    15.
    发明专利
    SUBSTITUTED PHENYL-1,3 DIOXOLOQUINOLINE DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS 未知

    公开(公告)号：AU1231492A

    公开(公告)日：1992-08-27

    申请号：AU1231492

    申请日：1992-01-24

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL J ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  ROSS JOHNSON M

    IPC: C07D491/04 ,  C07D491/056 ,  A61K31/47

    Abstract: The present invention relates to the compounds of formula (I), wherein: R is hydrogen, hydroxy or amino; R is hydrogen, hydroxy, methoxy or methoxymethoxy; R is hydrogen, hydroxy, amino, methoxy, methoxymethoxy or, taken together with R , methylenedioxy (also known as 1,3 dioxolo); R is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C1-4)alkylaminomethyl or, taken together with R , methylenedioxy; R is hydrogen or hydroxy; provided that at least one of R through R is other than hydrogen; and i) X is hydroxy or methoxy with X , X and X being hydrogen; or ii) X taken together with X , X taken together with X or X taken together with X , is methylenedioxy, provided that each of the remaining respective X , X , X and X substituents are hydrogen, intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.

    CAMPTOTHECIN DERIVATIVES, METHOD OF PRODUCING THE SAME, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, THEIR USE AND INTERMEDIATE PRODUCTS
    16.
    发明专利
    CAMPTOTHECIN DERIVATIVES, METHOD OF PRODUCING THE SAME, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, THEIR USE AND INTERMEDIATE PRODUCTS 未知

    公开(公告)号：SK323792A3

    公开(公告)日：1998-09-09

    申请号：SK323792

    申请日：1992-10-27

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL J ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER L

    IPC: A61K31/435 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/47 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07D498/22 ,  A61K31/33

    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.

    DERIVATIVES OF CAMPTOTHECIN, PROCESS OF THEIR PREPARATION INTERMEDIATES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE COMPRISED
    17.
    发明专利
    DERIVATIVES OF CAMPTOTHECIN, PROCESS OF THEIR PREPARATION INTERMEDIATES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE COMPRISED 未知

    公开(公告)号：CZ284023B6

    公开(公告)日：1998-07-15

    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.

    19.
    发明专利
    未知

    公开(公告)号：NO924158L

    公开(公告)日：1993-04-30

    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 ,  A61K31/4738 ,  A61K31/47 ,  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.

    WATER SOLUBLE CAMPTOTHECIN DERIVATIVES
    20.
    发明专利
    WATER SOLUBLE CAMPTOTHECIN DERIVATIVES 未知

    公开(公告)号：CA2081580A1

    公开(公告)日：1993-04-30

    申请号：CA2081580

    申请日：1992-10-28

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL J ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER L

    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 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54

    Abstract: GLX-76/AC155 WATER SOLUBLE CAMPTOTHECIN DERIVATIVES The invention relates to water soluble, camptothecin derivatives of formula (1), (I) wherein: n represents the integer 1 or 2; and i) R1 and R2 represent independently, hydrogen, lower alkyl, (C3 7)cycloalkyl;(C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R1 represents hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R2 represents -COR3 wherein R3 represents hydrogen, lower alkyl, perhalo-lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or iii) R1 and R2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) wherein: Y represents O, S, CH2, 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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