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    WATER-SOLUBLE CAMPTOTHECIN DERIVATIVE
    1.
    发明专利
    WATER-SOLUBLE CAMPTOTHECIN DERIVATIVE 失效

    公开(公告)号：JP2000109475A

    公开(公告)日：2000-04-18

    申请号：JP31294099

    申请日：1999-11-02

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL J ,  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: PROBLEM TO BE SOLVED: To obtain a new compound useful as an intermediate for producing a water-soluble camptothecin derivative used for treating tumors. SOLUTION: A compound of formula I [(n) is 1 or 2; R1, R2 are each H, a 1-6C alkyl or the like, or R1 is H, a 1-6C alkyl or the like and R2 is a group of the formula; COR3, or R1 and R2 are bonded to each other together with a nitrogen atom bonded thereto to form a saturated three to seven-membered heterogeneous group; R3 is H, a 1-6C alkyl or the like; Y is O, S or the like], for example, 2'-amino-4',5'-methylenedioxy-2-trifluoroacetamidoacetophenone. The compound of formula I is obtained by reacting a compound of formula III (X is a halogen) (for example, 2'-amino-4',5'-methylenedioxy-2- chloroacetophenone) with a compound of the formula: HNR1R2 (for example, trifluoroacetamine) in the presence of a base in an aprotic polar solvent such as acetonitrile.

    DERIVATIVES OF CAMPTOTHECIN, PROCESS OF THEIR PREPARATION INTERMEDIATES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE COMPRISED
    3.
    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.

    5.
    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
    7.
    发明专利
    WATER SOLUBLE CAMPTOTHECIN DERIVATIVES 未知

    公开(公告)号：MY141374A

    公开(公告)日：2010-04-16

    申请号：MYPI9401039

    申请日：1994-04-27

    Applicant: GLAXO INC

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

    IPC: C07D491/22 ,  A61K20060101 ,  A61K31/47 ,  A61P35/00 ,  C07D20060101 ,  C07D317/66 ,  C07D319/18

    Abstract: THE PRESENT INVENTION RELATES TO WATER SOLUBLE, CAMPTOTHECIN DERIVATIVES OF FORMULA (I) WHEREIN N REPRESENTS THE INTEGER 1 OR 2; AND I) R1 REPRESENTS HYDROGEN, LOWER ALKYL, (C3-7)CYCLOALKYL, (C3-7)CYCLOALKYL LOWER ALKYL, LOWER ALKENYL, HYDROXY LOWER ALKYL, AMINO LOWER ALKYL, LOWER ALKYLAMINO LOWER ALKYL, AMINO LOWER ALKYL, LOWER ALKOXY LOWER ALKYL OR (CH2)TAR WHEREIN: T IS 0 TO 5 AND AR REPRESENTS PHENYL, FURYL, PYRIDYL, N-METHYLPYRROLYL, IMIDAZOLYL; OR PHENYL, FURYL, PYRIDYL, N-METHYLPYRROLYL, IMIDAZOLYL, WITH ONE OR MORE SUBSTITUENTS INDEPENDENTLY SELECTED FROM HYDROXY, METHOXY, HALOGEN AND AMINO; AND R2 REPRESENTS DIPHENYLMETHYL OR (CH2)TAR; OR II) R1 AND R2 TAKEN TOGETHER WITH THE LINKING NITROGEN REPRESENT N-TETRAHYDROQUINOLYL OR N-TETRAHYDROISOQUINOLYL; AND PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVATES THEREOF; THEIR USE AS TOPOISOMERASE INHIBITORS; THEIR PREPARATION; AND THEIR USE IN THE TREATMENT OF CANCER.

    Water soluble derivatives of camptothecin.
    8.
    发明专利
    Water soluble derivatives of camptothecin. 未知

    公开(公告)号：AP9400638A0

    公开(公告)日：1995-10-28

    申请号：AP9400638

    申请日：1994-04-28

    Applicant: GLAXO INC

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

    IPC: A61K20060101 ,  A61K31/47 ,  A61P35/00 ,  C07D20060101 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22

    Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (1)wherein n represents the integer 1 or 2; and r1 represents hydrogen, lower alkyl, (c3-7)cycloalkyl, (c3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, amino lower alkul, lower alkoxy lower alkyl or (ch2)tar wherein: t is 0 to 5 and ar represents phenyl, furyl, pyridyl, n-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, n-methylpyrrolyl, imidazolyl, with one or more substituents independtly selected from hydroxy, methoxy, halogen and amino; and r2 represents diphenylmenthyl or (ch2)tar; or r1 and r2 taken together with the linking nitrogen represents n-tetrahydroquinolyl or n-tetrahydroisoquinolyl; and pharmaceutically acceptable salts and solvents thereof; their use as topoisomerase inhibitors; their preparations; and their use in the treatment of cancer.

    Water soluble camptothecin derivatives
    10.
    发明专利
    Water soluble camptothecin derivatives 未知

    公开(公告)号：OA09767A

    公开(公告)日：1993-11-30

    申请号：OA60295

    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

    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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