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    12.
    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.

    14.
    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.

    20.
    发明专利
    未知

    公开(公告)号：FI104373B

    公开(公告)日：2000-01-14

    申请号：FI924878

    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 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/47 ,  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.

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