Compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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260/101, 167/187

C07D 463/00 (2006.01) A61K 31/44 (2006.01) A61K 31/535 (2006.01) A61K 31/545 (2006.01) C07D 498/04 (2006.01) C07D 501/16 (2006.01) C07D 505/00 (2006.01)

Patent

CA 2013391

B2708 Abstract .beta.-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: Image (Ia) wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group, in particular that of an antibacterially active cephalosporin; CO2R6 is a carboxy group or a carboxylate anion; R3 is a y-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO2, O or CH2.

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