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    NEW CEPHEM COMPOUND
    51.
    发明专利
    NEW CEPHEM COMPOUND 失效

    公开(公告)号：JPH04288085A

    公开(公告)日：1992-10-13

    申请号：JP34383891

    申请日：1991-10-25

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： KAWABATA KOJI ,  TERASAWA TAKESHI ,  OKI HIDENORI ,  SAKANE KAZUO

    IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/18 ,  C07D501/46

    Abstract: PURPOSE:To obtain a new cephem compound, having high antimicrobial activity and useful in the medical field. CONSTITUTION:A compound expressed by formula I [R is (protected) amino; R is H or organic group; R is (protected) carboxy or COO ; R is (protected) hydroxy-lower alkyl; Z is N or CH; Y is N or N -R (R is lower alkyl), provided that R is (protected) carboxy when Y is N; R is COO when Y us N -R ] and its salt, e.g. 7beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(1-carboxy-1- methylethoxyimino)acetamido]-3-[1-(2-hydroxyethyl)-2-methyl-5- pyrazolio]aminomethyl-3-cephem-4-carboxylate (syn isomer). The compound expressed by formula I is obtained by, e.g. reacting a compound expressed by formula II or its reactive derivative at the amino or its salt with a compound expressed by formula III or its reactive derivative at the carboxy or its salt.

    56.
    发明专利
    失效

    公开(公告)号：JPH0357105B2

    公开(公告)日：1991-08-30

    申请号：JP1381981

    申请日：1981-02-03

    IPC: C07D501/16 ,  C07D501/18

    PHENACYLATED PYRIDINIOTHIOCEPHALOSPORIN
    59.
    发明专利
    PHENACYLATED PYRIDINIOTHIOCEPHALOSPORIN 失效

    公开(公告)号：JPH03128383A

    公开(公告)日：1991-05-31

    申请号：JP18885690

    申请日：1990-07-16

    Applicant: SHIONOGI & CO

    Inventor： ONOE HIROSHI ,  MINAMI KYOJI ,  ISHIKURA KOJI

    IPC: C07D501/18 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/36 ,  C07D501/57 ,  C07D505/00

    Abstract: NEW MATERIAL:A compound expressed by formula I (R is amino or acylamino; R is H or methoxy; R is H; R is vicinal dihydroxylated aryl; R is lower alkylene; R is H, carboxy-protecting group or linked to Y to form negative charge; X is O, S or sulfinyl; Y is counter ion of pyridinio group). EXAMPLE:3-(1-(3,4-Dihydroxyphenacyl)pyridinio-4-yl)thiomethyl-7beta-(2 -(2- aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxy)iminoacetamide)-3-cephe m-4- carboxylate 1-oxide. USE:An antimicrobial agent for preventing and treating susceptible infectious diseases. PREPARATION:For example, an amine expressed by formula II is used as a raw material, amidated and then subjected to heterocyclic group thiation, pyridinio formation, deprotection, esterification, sulfoxidation, sulfoxide cyclization or salt formation.

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