发明名称 New beta-lactamase stable piperacillin and azlocillin amide(s) - for treating Gram positive and Gram negative bacterial infection in humans and animals
摘要 Penicillin derivs. of formula (I) are new, where R1 = H,or an acyl gp. conventional in penicillin chemistry; R2 = H or OH; R3 = H or lower alkyl; R4 = Yn(CONH)m2pX; or R3 and R4 together with the N atom to which they are attached form an opt. substd. heterocyclic ring; m, n and p = each 0 or 1; Y and Z = each opt. branched 1-6C alkyl; X = opt. substd. aryl or an opt. substd. 5-6 membered heterocycle. USE/ADVANTAGE - (I) are semisynthetic penicillin derivs. which can be used in the therapy of bacterial diseases. (I) have high antibacterial activity against gram positive and gram negative bacteria and are of high stability towards beta-lactamase producing bacteria. The minimum inhibiting concn. of some typical cpds. (I) towards Staphylococcus aureus is 0.00312-0.00020 mmol/ml and towards Proteus vulgaris 0.00039-0.00002 mmol/ml.
申请公布号 DE4101787(A1) 申请公布日期 1992.07.23
申请号 DE19914101787 申请日期 1991.01.18
申请人 INSTITUT FUER WIRKSTOFFORSCHUNG, O-1136 BERLIN, DE;ARZNEIMITTELWERK DRESDEN GMBH, O-8122 RADEBEUL, DE 发明人 BOETTCHER, MATTHIAS, DIPL.-CHEM., O-1054 BERLIN, DE;JAEHRLING, RENATE, DIPL.-PHARM., O-1012 BERLIN, DE;WALTHER, KLAUS, DIPL.-CHEM. DR.RER.NAT., O-1040 BERLIN, DE;HABER, HANKA, DR.RER.NAT., O-1141 BERLIN, DE;RACKWITZ, CHRISTINA, DIPL.-CHEM., O-1040 BERLIN, DE;MOHS, BARBARA, O-1141 BERLIN, DE;FRANKE, RAINER, PROF. DIPL.-CHEM. DR.SC.NAT., O-1293 BASDORF, DE;KUEHNE, RONALD, DIPL.-BIO-CHEM. DR.RER.NAT., O-1141 BERLIN, DE;KOCH, ANDREAS, DIPL.-CHEM., O-1136 BERLIN, DE;TEUBNER, HERBERT, DIPL.-CHEM. DR.RER.NAT.;STEIMECKE, GUENTER, DIPL.-CHEM. DR.RER.NAT., O-3700 WERNIGERODE, DE;TITZE, HELMUT, DIPL.-CHEM. DR.RER.NAT., O-3701 SILSTEDT, DE;QUITTSCHORR, GISELA, DIPL.-CHEM., O-3700 WERNIGERODE, DE;WICHMANN, GEORG, DR.MED., O-8051 DRESDEN, DE
分类号 C07D499/00;C07D499/68 主分类号 C07D499/00
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