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    4-AMINO-2-UREIDOPYRIMIDINE-5 CARBOXAMAIDE, ITS PRODUCTION, MEDICINE CONTAINING THE SAME AND THEIR USE
    1.
    发明专利
    4-AMINO-2-UREIDOPYRIMIDINE-5 CARBOXAMAIDE, ITS PRODUCTION, MEDICINE CONTAINING THE SAME AND THEIR USE 失效

    公开(公告)号：JPH1072463A

    公开(公告)日：1998-03-17

    申请号：JP16581597

    申请日：1997-06-23

    Applicant: HOECHST AG

    Inventor： BOGER HANS GEORG ,  HOFFMANN AXEL ,  JAHNE GERHARD ,  SCHAFER HANS-LUDWIG ,  KRASS NORBERT

    IPC: A61K31/505 ,  A61P3/06 ,  C07D403/04

    Abstract: PROBLEM TO BE SOLVED: To obtain a novel compound which can manifest sufficient antihyperlipemic action with (almost) no cytotoxicity and is useful for treatment of liposis and disorder of lipid metabolism. SOLUTION: This novel compound is represented by formula I [R is H, an (F-substituted) 1-8C alkyl; R is an -O-F-substituted 1-8C alkyl, an -S-F- substituted 1-8C alkyl; R is H, F, Cl, Br, R and R may be incorporated to form an -O-F-substituted 1-5C alkylene-O-] or its acid adduct, typically 4- amino-2-(4,4-dimethylimidazolidin-2-one-1-yl)-5-[N-methly-N-(2-trifluo romethoxy) phenyl]pyrimidine-carboxamide. The compound of formula I is prepared by converting 4-amino-2-(4,4-dimethylimidazolidin-2-one-1-yl)-5-carboxylic acid to its acid chloride followed by reaction of the acid chloride with a compound of formula II.

    DIASTEREOMERS OF 1-(ISOPROPOXYCARBONYLOXY)ETHYLESTER 3-CEPHEM-4-CARBOXYLIC ACID AND PROCESS FOR THEIR PRODUCTION
    2.
    发明专利
    DIASTEREOMERS OF 1-(ISOPROPOXYCARBONYLOXY)ETHYLESTER 3-CEPHEM-4-CARBOXYLIC ACID AND PROCESS FOR THEIR PRODUCTION 未知

    公开(公告)号：SI9200204B

    公开(公告)日：2001-12-31

    申请号：SI9200204

    申请日：1992-09-07

    Applicant: HOECHST AG

    Inventor： FISCHER GERD ,  DEFOSSA ELISABETH ,  GERLACH UWE ,  HOERLEIN ROLF ,  KRASS NORBERT ,  LATTRELL RUDOLF ,  STACHE ULRICH ,  WOLLMANN THEODOR ,  ISERT DIETER

    IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/34 ,  C07D501/56 ,  C07D501/18

    Abstract: Enterally absorbable diastereomers of (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(m ethoxymethyl)-3-cephem-4-carboxylic acid 1-(isopropoxycarbonyloxy)ethyl ester of the formula I and its physiologically acceptable salts and also diastereomerically pure salts of the compounds of the general formula II where HX represents a mono- or polybasic acid and where X represents an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II are described, which is characterised in that on mixing together one equivalent of a solution of the diastereomer mixture of the formula III with 0.2 - 2 equivalents of a solution of the acid component HY the more poorly soluble diastereomer of the general formula IV is first precipitated and separated off by filtration, then the more readily soluble diastereomer of the general formula IV is precipitated from the filtration solution, it being possible in the subsequent subsidiary steps for the acid components HY to be identical or different and any desired sequence of the addition of different acid components HY to be used, and the salts obtained are optionally further purified by crystallisation.

    PROCESS FOR THE PREPARATION OF CEPHEM PRODRUG ESTERS
    5.
    发明专利
    PROCESS FOR THE PREPARATION OF CEPHEM PRODRUG ESTERS 未知

    公开(公告)号：CA2089441A1

    公开(公告)日：1993-08-15

    申请号：CA2089441

    申请日：1993-02-12

    Applicant: HOECHST AG

    Inventor： DEFOSSA ELISABETH ,  FISCHER GERD ,  GERLACH UWE ,  HORLEIN ROLF ,  KRASS NORBERT ,  LATTRELL RUDOLF ,  STACHE ULRICH ,  WOLLMANN THEODOR

    IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D277/40 ,  C07D417/12 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/34

    Abstract: Process for the preparation of cephem prodrug esters The invention relates to a process for the preparation of cephem prodrug esters of the formula (see formula I) in which R1 is C1-C5-alkanoyloxy-C1-C3-alkyl or C1-C5-alkoxycarbonyloxy-C1-C3-alkyl and X is an inorganic or organic anion, and in which the hydroxyimino group is present in the syn-form, which comprises allowing a compound of the formula II (see formula II) in which R2 is a protective group which can be removed by acid hydrolysis, to react with a bis(benzothiazol-2-yl) disulfide of the formula VI (see formula III) in which R3 is hydrogen, C1-C5-alkyl, C2-C6-alkenyl, C3-C6-alkynyl, C1-C6-alkyloxy, C2-C6-alkenyloxy, C3-C6-alkynyloxy, hydroxyl, acetoxy, halogen, nitro, amino, carboxyl or the sulfo group, and triphenylphosphine in an inert solvent, in the presence of a tertiary amine, to give a compound of the formula V (see formula IV) in which R2 and R3 have the abovementioned meanings, then reacting this compound with a 7-aminoceph-3-em-4-carboxylic acid ester of the formula III (see formula V) in which R1 has the abovementioned meaning, in inert organic or dipolar aprotic solvents at temperatures between 0.degree. and +80.degree.C and treating the resulting oxime-protected compound of the formula IV (see formula VI) in which R1 and R2 have the abovementioned meanings and in which the protected oxime group is present in the syn-form, with inorganic acids or with aliphatic or aromatic sulfonic acids in organic solvents at temperatures between +20.degree. and +110.degree.C to form the compound of the formula I.

    7.
    发明专利
    未知

    公开(公告)号：NO923452L

    公开(公告)日：1993-03-08

    申请号：NO923452

    申请日：1992-09-04

    Applicant: HOECHST AG

    Inventor： FISCHER GERD ,  DEFFOSSA ELISABETH ,  GERLACH UWE ,  HOERLEIN ROLF ,  KRASS NORBERT ,  LATTRELL RUDOLF ,  STACHE ULRICH ,  WOLLMANN THEODOR ,  ISERT DIETER

    IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/34 ,  C07D501/56

    Abstract: Enterally absorbable diastereomers of (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(m ethoxymethyl)-3-cephem-4-carboxylic acid 1-(isopropoxycarbonyloxy)ethyl ester of the formula I and its physiologically acceptable salts and also diastereomerically pure salts of the compounds of the general formula II where HX represents a mono- or polybasic acid and where X represents an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II are described, which is characterised in that on mixing together one equivalent of a solution of the diastereomer mixture of the formula III with 0.2 - 2 equivalents of a solution of the acid component HY the more poorly soluble diastereomer of the general formula IV is first precipitated and separated off by filtration, then the more readily soluble diastereomer of the general formula IV is precipitated from the filtration solution, it being possible in the subsequent subsidiary steps for the acid components HY to be identical or different and any desired sequence of the addition of different acid components HY to be used, and the salts obtained are optionally further purified by crystallisation.

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