CEPHALOSPORIN DERIVATIVE FOR ORAL ADMINISTRATION

• Main Authors: KODAMA EIJI, SHIBUYA KAZUYUKI, NISHIKIDO JIYOUJI
• Format: Patent
• Language: English
• Published: 05.03.1985
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

NEW MATERIAL:The compound of formula I [R1 is (protected) amino; A is 5- or 6-membered heterocyclic group ontaining 1-4 N, O or S atoms; R2 is 1-6C straight-chain alkyl, 3-6C branched-chain alkyl, etc.; R3 is organic group containing amino group and carboxyl group; X is S or O; R4 is H, carboxy-protecting group, etc.] or its salt. EXAMPLE:7beta-[( Z )-2-( 2-Amino-4-thiazolyl )-2-( methoxyimino acetamido )]-3-[5-(2- amino-2-ethoxycarbonyl )ethyl-1,3,4-thiadiazol-2-ylthio-methyl]-3-cephem-4-carboxylic acid. USE:Antibacterial agent effective to Gram-positive and Gram-negative bacteria. PREPARATION:For example, the compound of formula IV which is one of the compounds of formula I can be prepared by esterifying the 2-mercapto-containing amino acid of formula II, and reacting with the cephalosporanic acid of formula III.