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    61.
    发明专利
    未知

    公开(公告)号：CH566310A5

    公开(公告)日：1975-09-15

    申请号：CH1422270

    申请日：1970-09-25

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUTZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48

    Abstract: 1285790 Acylaminopenicillins FARBWERKE HOECHST AG 28 Sept 1970 [27 Sept 1969 (2)] 46107/70 Headings C2A andC2C Novel acylaminopenicillanic acids of Formula I wherein R 1 and R 2 are the same or different and are hydrogen or C 1 to C 5 alkyl or together form an optionally substituted alkylene group linking the nitrogen atoms, R 3 is hydrogen or C 1 to C 5 alkyl, A is an optionally substituted phenylene or thienylene group and B is oxygen or a chemical bond, and salts thereof, are prepared by reacting 6-aminopenicillanic acid or a salt thereof with a carboxylic acid of Formula II wherein R 1 , R 2 , R 3 , A and B are as defined above or an N-acylating derivative or salt thereof. The groups R1, R 2 and R 3 preferably contain a total of not more than 6 carbon atoms. When R 1 and R 2 form an alkylene group, this may be substituted, e.g. by C 1 to C 5 alkyl groups which may be closed into a ring and this ring may include a hetero atom. A is preferably 1,4-phenylene or 2,5-thienylene and may be substituted, e.g. by alkyl, alkoxy and/or halogen. The reaction may be carried out in water, preferably together with a water-miscible solvent, at pH 6-9 and at ambient temperature or below; an acid-acceptor, e.g. NaHC0 3 or triethylamine, is preferably present in the medium. The product may be isolated by simply lyophilizing the reaction mixture to give the penicillin in the form of a crude mixture with salts (e.g. NaCl) formed as by-products, which may be used therapeutically without purification providing the salts are non-toxic. It is purified by re-crystallization from concentrated aqueous solution. The acid chlorides of 4-amidinophenylacetic acid, 4-amidmophenoxyacetic acid and 4-(2- imidazolinyl)-phenoxyacetic acid as their hydrochloride salts are prepared by reacting the acid with thionyl chloride. Pharmaceutical compositions having antibacterial activity against gram-positive and gramnegative bacteria comprise an acylaminopenicillanic acid of Formula I as defined above or a physiologically tolerable salt thereof together with a pharmaceutical carrier.

    66.
    发明专利
    未知

    公开(公告)号：DK127432B

    公开(公告)日：1973-11-05

    申请号：DK481370

    申请日：1970-09-18

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUETZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D99/14

    Abstract: 1285790 Acylaminopenicillins FARBWERKE HOECHST AG 28 Sept 1970 [27 Sept 1969 (2)] 46107/70 Headings C2A andC2C Novel acylaminopenicillanic acids of Formula I wherein R 1 and R 2 are the same or different and are hydrogen or C 1 to C 5 alkyl or together form an optionally substituted alkylene group linking the nitrogen atoms, R 3 is hydrogen or C 1 to C 5 alkyl, A is an optionally substituted phenylene or thienylene group and B is oxygen or a chemical bond, and salts thereof, are prepared by reacting 6-aminopenicillanic acid or a salt thereof with a carboxylic acid of Formula II wherein R 1 , R 2 , R 3 , A and B are as defined above or an N-acylating derivative or salt thereof. The groups R1, R 2 and R 3 preferably contain a total of not more than 6 carbon atoms. When R 1 and R 2 form an alkylene group, this may be substituted, e.g. by C 1 to C 5 alkyl groups which may be closed into a ring and this ring may include a hetero atom. A is preferably 1,4-phenylene or 2,5-thienylene and may be substituted, e.g. by alkyl, alkoxy and/or halogen. The reaction may be carried out in water, preferably together with a water-miscible solvent, at pH 6-9 and at ambient temperature or below; an acid-acceptor, e.g. NaHC0 3 or triethylamine, is preferably present in the medium. The product may be isolated by simply lyophilizing the reaction mixture to give the penicillin in the form of a crude mixture with salts (e.g. NaCl) formed as by-products, which may be used therapeutically without purification providing the salts are non-toxic. It is purified by re-crystallization from concentrated aqueous solution. The acid chlorides of 4-amidinophenylacetic acid, 4-amidmophenoxyacetic acid and 4-(2- imidazolinyl)-phenoxyacetic acid as their hydrochloride salts are prepared by reacting the acid with thionyl chloride. Pharmaceutical compositions having antibacterial activity against gram-positive and gramnegative bacteria comprise an acylaminopenicillanic acid of Formula I as defined above or a physiologically tolerable salt thereof together with a pharmaceutical carrier.

    67.
    发明专利
    未知

    公开(公告)号：SE350758B

    公开(公告)日：1972-11-06

    申请号：SE1029469

    申请日：1969-07-22

    Applicant: HOECHST AG

    Inventor： DUERCKHEIMER W ,  SCHRINNER E

    IPC: C07D241/52 ,  C07D51/78

    Abstract: 1,248,848. Quinoxaline-1,4-dioxide derivatives. FARBWERKE HOECHST A.G. 25 July, 1969 [25 July, 1968], No. 37465/69. Heading C2C. Novel quinoxaline-1,4-dioxide derivatives of the Formula I wherein R 1 is C 1-4 alkyl and R 2 and R 3 , which may be the same or different, are H, C 1-4 alkyl or C 1-4 alkoxy are prepared by reacting the corresponding 2 - alkoxycarbonyl - 3 - R 1 - 6- R 2 - 7 - R 3 - quinoxaline - 1,4 - dioxide with hydrazine hydrate at a temperature of from 0‹ to 60‹ C. Therapeutic compositions, having anti-bacterial activity and suitable for oral or parenteral administration contain the above novel compounds and pharmaceutically suitable carriers.

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