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    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS
    2.
    发明授权
    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS 失效

    公开(公告)号：KR830001521B1

    公开(公告)日：1983-08-08

    申请号：KR770000334

    申请日：1977-02-15

    Applicant: GLAXO LAB LTD

    Inventor： GREGSON MICHAEL ,  SYKES RICHARD BROOK

    IPC: C07D501/32

    Abstract: Cefuroxime alkanoyloxymethyl esters I (R = C1-4 alkyl) were prepd. for use as antibiotics. Thus, cefuroxime was stirred with K2CO3 and DMF, followed by the addn. of acetoxy methyl bromide to give I (R = CH3). I are more easily absorbed through the gastrointestinal tract than the parent cefuroxime and thus are suitable for oral administraction.

    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS
    3.
    发明授权
    PROCESS FOR PREPARING CEPHALOSPORIN ANTIBIOTICS 失效

    公开(公告)号：KR830001543B1

    公开(公告)日：1983-08-10

    申请号：KR770000335

    申请日：1977-02-15

    Applicant: GLAXO LAB LTD

    Inventor： GREGSON MICHAEL ,  SYKES RICHARD BROOK

    IPC: C07D501/34

    Abstract: Cefuroxim esters I(R1 = C1-4 primary or secondary alkyl; R2 = C1-6 primary of secondary alkyl) were prepd. by the reaction of cefuroxim K salf with R2CHBrO2CR1 and the acylation of III with (Z)-2-(fur-2-y1)-2-methoxyimino-acetic acid. Thus, 4.57g cefuroxim was stirred with 760mg K2CO3 and 25ml N,N-dimethylformamide followed by the addn. of AcOCH2Br to give (R and S)-1-acetoxyethyl(6R,7R)-3-carbamoyloxymethyl-7-≮(Z)-2-(fur-2-y1)-2-methoxyiminoacetamido≉ceph-3-em-4-carboxylated. I are useful as antibiotics and are more easily absorbed after oral administration than cefuroxim.

    Penicillin antibiotics
    4.
    发明授权
    Penicillin antibiotics 失效

    公开(公告)号：US3926957A

    公开(公告)日：1975-12-16

    申请号：US46678074

    申请日：1974-05-03

    Applicant: GLAXO LAB LTD

    Inventor： GREGSON MICHAEL ,  COOK MARTIN CHRISTOPHER ,  GREGORY GORDON IAN

    IPC: C07C259/02 ,  C07D307/54 ,  C07D333/24 ,  C07D499/70 ,  C07D499/44

    CPC classification number: C07D307/54 ,  C07C259/02 ,  C07D333/24

    Abstract: WHERE R is a hydrogen atom or an organic group and Ra is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to Beta -lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

    The invention provides novel antibiotic compounds which are 6 Beta -acylamidopenam-3-carboxylic acids and non-toxic derivatives thereof, characterized in that the acylamido group has the structure

    6.
    发明专利
    未知

    公开(公告)号：DK147513B

    公开(公告)日：1984-09-10

    申请号：DK168778

    申请日：1978-04-18

    Applicant: GLAXO LAB LTD

    Inventor： GREGSON MICHAEL

    IPC: C07D501/26 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C68/02 ,  C07C68/06 ,  C07D20060101 ,  C07D501/00 ,  C07D501/20 ,  C07D501/34 ,  C07D501/60

    Abstract: Cephalosporin derivatives of the formula: in which R denotes lower alkyl and R denotes hydrogen or lower alkyl. In contrast to the free carboxylic acids, these novel esters are very well absorbed by the gastrointestinal tract and then hydrolyse rapidly to give corresponding carboxylic acids having a broad spectrum antibiotic action. They are prepared by esterification of the carboxyl group in the 4-position, by N-acylation of the 7-aminocephemcarboxylic acid ester or by carbamoylation of the hydroxymethyl group in the 3-position.

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