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    12.
    发明专利
    未知

    公开(公告)号：DK125250B

    公开(公告)日：1973-01-22

    申请号：DK579768

    申请日：1968-11-27

    Applicant: HOFFMANN LA ROCHE

    Inventor： VOGLER K ,  QUITT P

    IPC: C07D277/06 ,  C07D91/16

    Abstract: 1,201,977. Penicilloic acid derivatives. F. HOFFMANN-LA ROCHE & CO. A.G. 20 Dec., 1968 [4 Jan., 1968], No. 60560/68. Heading C2C. Novel penicilloic acid derivatives of the formula wherein n is 1 to 4, R 1 is hydrogen or C 1 to C 6 acyl, and R is 2-pentenyl; n-pentyl; n heptyl; allylthiomethyl; 5-amino-5-carboxypentyl; benzyl; carboxybenzyl; α-aminobenzyl; phenoxybenzyl; phenbxymethyl; α-phenoxyethyl; α- phenoxypropyl; 2,6-dirnethoxyphenyl; 2-ethoxy-1-naphthyl; 3-carboxy-2-quinoxyalinyl; 5- methyl - 3 - phenyl - 4 - isoxazolyl; 3 - (2 - chlorophenyl) - 5 - methyl - 4 - isoxazolyl; or 3 - (2,6 - dichlorophenyl) - 5 - methyl - 4 - isoxazolyl, and salts thereof, are prepared by reacting a penicillin of formula with a diaminocarboxylic acid derivative of formula R and n being as above and R 2 being C 1 to C 6 acyl or an amino-protecting group, (e.g. tert.-butyloxycarbonyl or benzyloxycarbonyl), splitting off the protecting group if present, and optionally converting the reaction product to a salt. The reaction is performed in aqueous alkaline medium. Pharmaceutical compositions comprise the novel penicilloic acids or their pharmaceutically acceptable salts together with a pharmaceutical carrier. The compositions may be in forms for enteral or parenteral administration and are for counteracting allergic reactions produced by administering penicillins.

    17.
    发明专利
    未知

    公开(公告)号：SE362433B

    公开(公告)日：1973-12-10

    申请号：SE269368

    申请日：1968-03-01

    Applicant: HOFFMANN LA ROCHE

    Inventor： VOGLER K ,  ZANETTI G

    IPC: C07D499/00 ,  C07D499/46 ,  C07D499/48 ,  C07D99/16

    Abstract: Acyl derivatives of 6-amino penicillanic acid of general formula (I) and their addition salts. (I) R1, R2, R3 and R4 = H-, hal-, C1-7 alkyl-, C1-7 alkenyl-, cycloalkyl-, cycloalkenyl-, aralkyl-, opt. substd. aryl-, cyano-, carboxyl-, carbalkoxy-, hydroxy-, C1-7 alkoxy-, C1-7 alkylthio-, C1-7 alkyl-sulphonyl-, nitro-, nitroso-, azido-, amino-, C1-7 alkylamino-, di-C1-7 alkylamino-, carbamino-, formyl-, hal-C1-7 alkyl-, C1-7 alkoxy-C1-7 alkyl-, hydroxy-C1-7 alkyl-, amino-C1-7alkyl-, C1-7 alkylamino-C1-7alkyl-, di-C1-7alkylamino-C1-7 alkyl-, acyl-, opt. substd. sulphamido- or a heterocyclic group. R5 = H-, C1-7 alkyl-, hal-C1-7alkyl-, cyano-C1-7 alkyl-, amino-C1-7alkyl-, hydroxy-C1-7 alkyl, carboxy-C1-7 alkyl-, C1-7 alkylamino-C1-7 alkyl-, carbalkoxy -C1-7 alkyl-, C1-7 alkenyl-, cycloalkyl-, cycloalkenyl-, aralkyl, opt. substd. aryl-, aryl-sulphonylamino-C1-7 alkyl-, C1-7 alkylsulphonylamino-C1-7 alkyl-, carbalkoxy- particularly (2-nitropyrrol-1-yl-methyl) penicillin. Antibiotics.

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