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    PHARMACEUTICAL PREPARATIONS
    5.
    发明专利
    PHARMACEUTICAL PREPARATIONS 未知

    公开(公告)号：CA1037026A

    公开(公告)日：1978-08-22

    申请号：CA217940

    申请日：1975-01-15

    Applicant: GLAXO LAB LTD

    Inventor： DAVIS BENJAMIN ,  PEARCE DEREK R ,  COOK MARTIN C ,  WEIR NIALL G ,  NEWALL CHRISTOPHER E ,  GREGORY GORDON I ,  PHILLIPS GORDON H

    IPC: C07J5/00

    Abstract: This invention is concerned with improvements in or relating to pharmaceutical preparations having anaesthetic activity, and more particularly aqueous preparations suitable for intravenous injection. The preparations comprise solutions of the known anaesthetic steroid 3.alpha.-hydroxy-5.alpha.-pregnane-11,20-dione in aqueous solutions of parenterally acceptable non-ionic surface active agents. The preparations also contain certain new 21-acyloxy-3.alpha.-hydroxy-5.alpha.-pregnane-11,20-diones which act as solubility promoters and constitute a further feature of the invention. Preferred classes of surface active agent are described and the useful materials fall within the class having an HLB value of at least 9, preferably from 9 to 18. Processes for preparing the preparations are described and claimed. A process for the preparation of the 21-acyloxy-3.alpha.-hydroxy-5.alpha.-pregnane-11,20-diones is described.

    ANTIBIOTICS
    6.
    发明专利
    ANTIBIOTICS 未知

    公开(公告)号：CA1048016A

    公开(公告)日：1979-02-06

    申请号：CA293802

    申请日：1977-12-23

    Applicant: GLAXO LAB LTD

    Inventor： COOK MARTIN C ,  GREGORY GORDON I ,  BRADSHAW JANICE

    IPC: C07D501/26

    Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure where R1 is a furyl, thienyl or phenyl group and R2 is a C1-C4 alkyl, C3 -C7 cycloalkyl or phenylgroup except that R2 may not represent a methyl group when R1 represents a furyl group, and in which the 3-position substituent is a carbamoyloxymethyl group possess a particularly valuable combination of properties, exhibiting high antibacterial activity against a broad range of gram positive and gram negative organisms, particularly high stability to .beta.-lactamases produced by various organisms, and stability in vivo. Such compounds include the nontoxic salts, biologically acceptable esters, 1-oxides and solvates of the parent 4-carboxylic acids. The compounds are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer. The above compounds may be prepared by (a) acylation of the corresponding 7-amino compound or (b) carbamoylation of the corresponding 3-hydroxymethyl compound.

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