Cephalosporin derivatives

C - Chemistry – Metallurgy – 07 – D

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167/187, 260/104

C07D 501/56 (2006.01) A61K 31/545 (2006.01) C07D 213/64 (2006.01) C07D 213/68 (2006.01) C07D 221/04 (2006.01)

Patent

CA 1276013

ABSTRACT OF THE DISCLOSURE: The invention relates to a cephalosporin derivative of the formula: Image wherein Y is straight or branched C1-C5 alkyl or alkenyl chain, C3-C6 cycloalkanomethyl , each group being optionally substituted by halogen, or a group Image wherein n is 0 or an integer of 1 - 3, A is a group -COR3 wherein R3 is hydroxy, a group Image wherein R4 and R5, which may be the same or different, are hydrogen or C1-C5 alkyl, a group Image or a 5- or 6- membered heterocyclic group containing nitrogen and/or sulfur, and R1 and R2, which may be the same or different, are hydrogen, C1-C5 alkyl, or R1 and R2 may be combined together to form a C1-C5 cycloalky- lidene and Z is a group of the formula: Image wherein m is an integer of 3 - 5, R6 is hydrogen or alkyl of 1 - 3 carbon atoms, and R7 is alkyl or alkenyl of 1 - 5 carbon atoms, cyclo- propyl, a group -(CH2)pB wherein p is 0 or an integer of 1 - 3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or a pharmacologically acceptable salt thereof. These compounds have a strong antibacterial activity against Gram positive organisms as well as Gram negative organisms.

474936

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