Cephalosporin-derivater

• Main Authors: D'ANDREA, STANLEY V, SPRINGER, DANE M, KIM, OAK K, LUH, BING Y, HUDYMA, THOMAS W
• Format: Patent
• Language: Norwegian
• Published: 26.05.1999
• Edition: 6
• Subjects: CHEMISTRY; 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

Det beskrives cephem-derivater med den generelle formel V/? CH2-S-Q COOR1 hvor Q er en eventuelt substituert pyridiniumgruppe forbundet med svovelatomet via et ringkarbonatom; X er halogen; Y er hydrogen eller halogen; L1 er en furangruppe, en tiofengruppe, en C2-Ci0-alkylgruppe, eller en C2-Cio-alkylgruppe avbrutt av en eller flere grupper uavhengig valgt fra vinyl, S, SO, S02, S02NH, H eller xNxri/' H o n er O eller 1; A er C02H, P03H2, S03H eller tetrazol; og R1 er hydrogen eller en karboksyl-beskyttende gruppe; og farmasøytisk akseptable salter og/eller prodrugs derav. Derivatene er grampositive antibakterielle midler spesielt egnet til behandlingen av sykdommer forårsaket av methicillin-resistent Staphylococcus aureus (MRSA). Provided are cephem derivatives represented by general formula (I) wherein Q is an optionally substituted pyridinium group connected to the sulfur atom via a ring carbon atom; X is halogen; Y is hydrogen or halogen; L is a furan group, a thiophene group, a C2-C10 alkyl group, or a C2-C10 alkyl group interrupted by one or more groups independently selected from vinyl, S, SO, SO2, SO2NH, (IIa), (IIb); n is 0 or 1; A is CO2H, PO3H2, SO3H or tetrazole; and R is hydrogen or a carboxyl-protecting group; and pharmaceutically acceptable salts and/or prodrugs thereof. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicilin-resistant Staphylococcus aureus (MRSA).