7-bromo- and 7,7-dibromo-cepham and cephem derivatives

Details 7-bromo- and 7,7-dibromo-cepham and cephem derivatives 7-bromo- and 7,7-dibromo-cepham and cephem derivatives

C - Chemistry, Metallurgy

07

D

C07D 501/00 (2006.01) A61K 31/545 (2006.01)

Patent

CA 2256002

The present invention relates to novel 7-bromo- and 7,7-dibromo-cepham and 7-bromo- and 7,7-dibromo-cephem derivatives, to a process for the preparation thereof and to pharmaceutical and veterinary formulations containing them. These compounds are prepared by reaction of esters or amides of 6,6- dibromopenicillanic acid sulfoxides in organic solvents with or without an addition of tetrabutylammonium bromide at an elevated temperature and subsequently some of them are oxidized. According to the present invention novel compounds are potentially active as inhibitors of proteases, especially human leukocyte elastases (HLE).

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