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    77.
    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.

    1,5 Benzodiaze pine derivatives
    79.
    发明专利
    1,5 Benzodiaze pine derivatives 未知

    公开(公告)号：AP9400635A0

    公开(公告)日：1994-04-30

    申请号：AP9400635

    申请日：1994-04-13

    Applicant: GLAXO INC

    IPC: A61K38/00 ,  A61K31/551 ,  A61K38/02 ,  A61P3/00 ,  A61P5/00 ,  A61P43/00 ,  C07D243/12 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/097

    Abstract: PCT No. PCT/EP94/01130 Sec. 371 Date Oct. 30, 1995 Sec. 102(e) Date Oct. 30, 1995 PCT Filed Apr. 13, 1994 PCT Pub. No. WO94/24151 PCT Pub. Date Oct. 27, 1994The present invention relates to compounds of general formula (I) (I) and physiologically acceptable salts thereof wherein the group NR1R2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R3 is C1-6alkyl, C3-6cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R4 is phenyl or phenyl substituted by one or two groups selected from the group consisting of halogen, C1-4alkyl, trifluoromethyl, trifluoromethoxy or (CH2)nR5 wherein n is zero or 1 and R5 represents C1-4alkoxy, hydroxy, nitro, cyano, CO2R6, S(O)pCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4)alkyl, tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R6 is hydrogen, C1-4alkyl or benzyl; R7 is hydrogen or C1-4alkyl, R8 is hydrogen, C1-4alkyl, SO2CH3 or SO2CF3, X represent hydrogen, C1-4alkyl or halogen; m is zero, 1 or 2, and p is zero, 1 or 2. The invention also relates to processes for preparation of these compounds and to their use in medicine as antagonists of gastrin and CCK.

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