6-(substituted) methylenepenicillanic and 6- (substituted)...

C - Chemistry – Metallurgy – 07 – D

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C07D 499/00 (2006.01) A61K 31/43 (2006.01) A61K 31/435 (2006.01) C07D 213/26 (2006.01) C07D 213/30 (2006.01) C07D 213/61 (2006.01) C07D 213/65 (2006.01) C07D 213/89 (2006.01) C07D 233/54 (2006.01) C07D 239/26 (2006.01) C07D 241/12 (2006.01) C07D 249/06 (2006.01) C07D 249/08 (2006.01) C07D 261/08 (2006.01) C07D 277/24 (2006.01) C07D 277/64 (2006.01) C07F 9/58 (2006.01) C07F 9/62 (2006.01) C07F 9/6509 (2006.01) C07F 9/6512 (2006.01)

Patent

CA 1273008

6-(SUBSTITUTED)METHYLENEPENCILLANIC AND 6-(SUBSTITUTED)HYDROXYMETHYLPENICILLANIC ACIDS AND DERIVATIVES THEREOF Abstract Beta-lactamase inhibiting compounds of the formula Image or Image (I) (II) or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X3 is H or Br, R1 is H, the residue of certain carboxy- protecting groups or the residue of an ester group readily hydrolyzable in vivo; one of R12 and R13 is H and the other is vinyl, certain aryl, arythio, alkyl- thio, alkylsulfonyl or certain heterocyclyl, amino- methyl, thiocarboxamido or amidino groups; one of R2 and R3 is H and the other is as disclosed for the other of R12 and R13, or is Cl or CH2OH, and R18 is H or certain acyl groups; intermediates useful in their production, methods for their preparation and use, and pharmaceutical compositions containing them.

472963

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