Cephalosporin derivatives and process for their preparation

• Main Authors: DURCKHEIMER, WALTER, LATTRELL, RUDOLF, SEEGER, KARL
• Format: Patent
• Language: English; French; German
• Published: 27.06.1984
• Subjects: AGRICULTURE; ANIMAL HUSBANDRY; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES; CHEMISTRY; FISHING; FORESTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HUNTING; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TRAPPING

Cephalosporinderivate der allgemeinen Formel gegen bakterielle Infektionen wirksame pharmazeutische Präparate, die solche Cephemderivate enthalten, Verfahren zur Herstellung der Cephemderivate und der pharmazeutischen Präparate und Verwendung der Cephemderivate zur Bekämpfung bakterieller Infektionen. 1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LU, LI, NL, SE) A cephem derivative of the formula I see diagramm : EP0111934,P10,F3 and physiologically acceptable acid addition salts thereof in which R**1 denotes C1 -C2 -alkyl, R**2 denotes a pyridinium radical see diagramm : EP0111934,P10,F4 which is substituted by 2 alkyl groups in the ortho-position which are linked to form a trimethylene to pentamethylene ring in which one carbon atom can be replaced by an oxygen atom, or denotes a 1-quinolinium radical or a 2-isoquinolinium radical and in which the R**1 O group is in the syn-position. 1. Claims (for the Contracting State AT) A process for the preparation of a cephem derivative of the formula I see diagramm : EP0111934,P11,F4 and physiologically acceptable acid addition salts thereof in which R**1 denotes C1 -C2 -alkyl, R**2 denotes a pyridinium radical see diagramm : EP0111934,P12,F1 which is substituted by 2 alkyl groups in the ortho-position which are linked to form a trimethylene to pentamethylene ring in which one carbon atom can be replaced by an oxygen atom, or denotes a 1-quinolinium radical or a 2-isoquinolinium radical in which the R**1 O group is in the syn-position which comprises a) reacting a compound of the general formula II see diagramm : EP0111934,P12,F2 or salts thereof or a reactive derivative of the compound II in which R**1 has the meaning mentioned above and R**7 denotes an amino group or a protected amino group and R**8 denotes a group which can be replaced by the pyridine, quinoline or isoquinoline derivatives corresponding to the radicals R**2 of the formula I, with these pyridine, quinoline or isoquinoline derivatives, and alpha) splitting off a protective group which may be present and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt, or b) reacting a 7-aminocephem compound of the general formula III see diagramm : EP0111934,P12,F3 or acid addition salts thereof in which R**2 has the abovementioned meaning and in which the amino group can also be present in the form of a reactive derivative, with a 2-(5-amino-1,2,4-thiadiazol-3-yl)-2-synoximinoacetic acid of the general formula IV see diagramm : EP0111934,P12,F4 in which R**1 and R**7 have the meaning mentioned above, or with an activated derivative of this compound, and alpha) splitting off a protective group which may be present, and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt.