Syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid...

C - Chemistry – Metallurgy – 07 – D

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260/101, 260/104

C07D 501/24 (2006.01) C07D 277/20 (2006.01) C07D 277/38 (2006.01) C07D 277/48 (2006.01) C07D 333/16 (2006.01)

Patent

CA 1337522

Novel syn-isomer of 3,7-disubstituted-3-cephem-4- carboxylic acid compounds are provided of the formula: Image in which R1 is a group of the formula: Image wherein R5 is hydrogen, halogen, nitro, hydroxy, lower alkoxy or acyloxy and R6 is hydroxy, lower alkoxy, acyloxy, acylamino or di(lower)alkyl- amino; a group of the formula: Image wherein R7 is amino, pro- tected amino, hydroxy or lower alkyl; or a group of the formula: Image wherein R8 is lower alkyl and R9 is imino, protected imino or oxo; R2 is an aliphatic hydrocarbon group which may have suitable substituent (s); R3 is carboxy or protected carboxy; and R4 is acyloxymethyl, hydroxymethyl, formyl or a heterocyclic- thiomethyl group which may have suitable substituent (s); or R3 and R4 are linked together to form -COOCH2-, and pharmaceutical- ly acceptable salts and tautomers thereof; the novel compounds are highly active against a number of pathogenic bacteria.

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