中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

88 records (took 0.023 seconds)

    ACYLAMINOPENICILLANIC ACIDS AND PROCESS FOR PREPARING THEM
    13.
    发明专利
    ACYLAMINOPENICILLANIC ACIDS AND PROCESS FOR PREPARING THEM 未知

    公开(公告)号：IE34536B1

    公开(公告)日：1975-06-11

    申请号：IE121270

    申请日：1970-09-18

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUTZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D99/14 ,  C07D99/22 ,  A61K21/00

    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.

    14.
    发明专利
    未知

    公开(公告)号：NL7013978A

    公开(公告)日：1971-03-30

    申请号：NL7013978

    申请日：1970-09-22

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUTZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D99/16 ,  A61K27/00

    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.

    15.
    发明专利
    未知

    公开(公告)号：BE756747A

    公开(公告)日：1971-03-29

    申请号：BE756747D

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUTZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D

    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.

Patent Agency Ranking