中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

183 records (took 0.041 seconds)

    CEPHALOSPORIN PYRIDINIM COMPLEX
    1.
    发明专利
    CEPHALOSPORIN PYRIDINIM COMPLEX 失效

    公开(公告)号：JPH10120687A

    公开(公告)日：1998-05-12

    申请号：JP28523397

    申请日：1997-10-17

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANGEHRN PETER ,  HEINZE-KRAUSS INGRID ,  PAGE MALCOLM ,  WEISS URS

    IPC: C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/16 ,  C07D501/24 ,  C07D501/56

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject derivative, which is an antibiotic substance, comprising a specific cephalosporin pyridinium derivative, having a strong and a wide range of antimicrobial activities and especially effective against methicillin-resistant Staphylococcus aureus(MRSA), enterococci, pneumococci, etc. SOLUTION: This compound is a new cephalosporin pyridinium derivative represented by formula I [R is H, a lower alkyl, a cycloalkyl or acetyl; X is CH or N; (n) is 0, 1 or 2; (m) is 0 or 1; R is H, a lower alkyl, an ω- hydroxyalkyl, benzyl, a lower alkyl-(substituted)heterocyclic group or a group represented by the formula CH2 CONR R (R and R are each H, an ω- hydroxyalkyl, phenyl, benzyl, naphthyl, heterocylic group, etc.)] and is useful as an antimicrobial agent, etc., effective against methicillin-resistant Staphylococcus aureus(MRSA), enterococci, pneumococci, etc. The compound is obtained by reacting a compound represented by formula II with a heterocyclic carboxylic acid compound represented by formula III (R is H or an amino-protecting group).

    1-CARBA-(DETHIA)-CEPHALOSPORLN DERIVATIVE
    2.
    发明专利
    1-CARBA-(DETHIA)-CEPHALOSPORLN DERIVATIVE 失效

    公开(公告)号：JPH10101670A

    公开(公告)日：1998-04-21

    申请号：JP25459697

    申请日：1997-09-19

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANGEHRN PETER ,  HEBEISEN PAUL ,  HEINZE-KRAUSS INGRID ,  PAGE MALCOLM

    IPC: C07D463/14 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/445 ,  A61K31/4545 ,  A61P31/04 ,  C07D463/00

    Abstract: PROBLEM TO BE SOLVED: To obtain a new compound, an antibiotic having potent and wide antibacterial activity, useful as an antibacterial agent against MRSA and Pseudomonas aeruginosa. SOLUTION: This new compound is shown by formula I R is H, a (Fsubstituted) lower alkyl, cycloalkyl, etc.; R is H, OH, a lower alkyl-(Q)m [Q is CHR (R is H or a lower alkyl), etc.; (m) is 0 or 1], aryl-(Q)m , etc.; X is CH or N; (n) is 0-2}, e.g. (6R,7S)-7-[(Z)-2-acetoxyimino-2(2-amino-thiazol-4-yl)- acetylamino]-3-[(E)-1(1-carbamoylmethyl-pyridin-l-ium-3-yl)-2-oxo-pyrr olidin-3 ylidenemethyl]-8-oxo-1-aza-bicyclo[4.2.0]octa-2-ene-2-carboxylate. The compound of formula I is obtained by treating a compound of formula II with a carboxylic acid of formula m.

    ANTIMICROBIAL COMPOSITION
    4.
    发明专利
    ANTIMICROBIAL COMPOSITION 失效

    公开(公告)号：JPH11140087A

    公开(公告)日：1999-05-25

    申请号：JP26120598

    申请日：1998-09-16

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANGEHRN PETER ,  HEINZE-KRAUSS INGRID ,  PAGE MALCOLM ,  RICHTER G F HANS

    IPC: C07D501/48 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61K31/79 ,  A61P31/00 ,  A61P31/04 ,  C07D501/54 ,  C07D501/56

    Abstract: PROBLEM TO BE SOLVED: To obtain an antimicrobial composition capable of manifesting high effectiveness against methicillin-resistant Staphylococcus aureus(MRSA) and uniquely having a wide antimicrobially active spectrum for Gram-positive pathogenic bacteria and Gram-negative pathogenic bacteria or the like. SOLUTION: This antimicrobial composition contains a combination of (1) the first ingredient selected from a vinylpyrrolidinonecephalosporin derivative represented by the formula [R is a lower alkyl or the like; R and R are each hydrogen or the like; X is S, O, NH or CH2 ; (n) is 0, 1 or 2; (m) is 0 or 1; (s) is 0 or 1; R is hydrogen or the like; R is hydroxy or the like] or the like and (2) the second ingredient selected from a carbapenem-based antibiotic and a β-lactamase inhibitor.

    VINYLPYRROLIDINONE CEPHALOSPORIN DERIVATIVES
    6.
    发明专利
    VINYLPYRROLIDINONE CEPHALOSPORIN DERIVATIVES 失效

    公开(公告)号：JPH10139783A

    公开(公告)日：1998-05-26

    申请号：JP30411597

    申请日：1997-11-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANGEHRN PETER ,  HEINZE-KRAUSS INGRID ,  RICHTER HANS G F

    IPC: C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/14 ,  C07D501/18 ,  C07D501/24 ,  C07D501/48 ,  C07D501/50 ,  C07D501/54 ,  C07D501/56

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject new derivatives comprising specific vinylpyrrolidinone cephalosporin derivatives and useful for treatment and prevention, etc., of diseases due to gram-positive bacteria, especially sensitive and resistant staphylococcus, Pneumococcus and enteric coccus. SOLUTION: The new vinylpyrrolidinone cephalosporin derivatives are represented by formula I [R is a halogen, a (substituted)lower alkyl, a (substituted)phenyl, a (substituted)benzyl, a (substituted)heterocyclic group, etc.; R is H, OH, a lower alkyl-Qr (Q is an alkylene, CO or SO2 ; (r) is 0 or 1), an aryl-Qr, etc.; R is OH, a lower alkoxy, OM (M is an alkali metal), etc.; R and R are each H, a lower alkyl or phenyl; X is S, O, NH or CH2 ; (n) is 0, 1 or 2; (m) and (s) are each 0 or 1] and useful as a medicine, etc., for treatment and prevention of infectious diseases. The compound is obtained by treating a compound having formula II (R is H or trimethylsilyl; R is H, benzhydryl, etc.) with a carboxylic acid of formula III (Y is OH or its reactive derivative).

    CEPHALOSPORIN DERIVATIVES
    9.
    发明专利
    CEPHALOSPORIN DERIVATIVES 未知

    公开(公告)号：CA2121324C

    公开(公告)日：2007-07-10

    申请号：CA2121324

    申请日：1994-04-14

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANGEHRN PETER ,  WEI CHUNG-CHEN

    IPC: A61K31/545 ,  C07D501/16 ,  A61K31/546 ,  A61K31/695 ,  A61P31/04 ,  C07D501/00 ,  C07D501/18 ,  C07D501/24 ,  C07D501/48 ,  C07D501/56 ,  C07F7/10

    Abstract: Cephalosporin derivatives of the general formula wherein R1 is an acyl group derived from a carboxylic acid; R2 is hydrogen, hydroxy, lower alkyl-Q m, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q m, aryl-Q m, aryloxy, aralkoxy or a heterocyclic ring, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, -CONR4R5, -N(R5)COOR9, R5CO-, R5OCO- or R5COO- where R4 is hydrogen, lower alkyl, or cycloalkyl; R5 is hydrogen or lower alkyl; R9 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; Q is -CO- or -SO2-; m is 0 or 1; n is 0, 1 or 2; as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts. The products are antibacterially active.

Patent Agency Ranking