3,6-disubstituted penam sulfone derivatives as antibacterials

Details 3,6-disubstituted penam sulfone derivatives as antibacterials 3,6-disubstituted penam sulfone derivatives as antibacterials

C - Chemistry, Metallurgy

07

D

C07D 499/87 (2006.01) A61K 31/43 (2006.01) A61P 31/04 (2006.01) C07D 499/00 (2006.01)

Patent

CA 2355738

Compounds are provided having formulae (I) and (II) wherein n is 0 or 1 and when n=1, R is a 5 or 6 membered heterocyclic ring, hydroxy, halogen, oxo, carbamoyl, alkoxy, or disubstituted amino, when n=0, R is an ester, cyano or amide group; X is CH or NH; R3 is cyano, methoxy, or acetamido; R1 is hydrogen, alkyl, a negative charge, a cation selected from the group consisting of sodium, potassium and tetraalkylammonium and acyloxyalkyl, or alkoxycarbonyloxyalkyl; and R2 is hydrogen, acyl, trisubstituted silyl carbamoyl or an amino acid residue; or pharmaceutically acceptable salts thereof.

L'invention concerne des composés représentés par les formules (I) et (II), dans lesquelles n vaut 0 ou 1, et si n=1, R est un noyau hétérocyclique à 5 ou 6 chaînons, hydroxy, halogène, oxo, carbamoyle, alcoxy, ou amino disubstitué ; si n=0, R est ester, cyano ou un groupe amide; X est CH ou NH; R¿3? est cyano, méthoxy, ou acétamido; R¿1? est hydrogène, alkyle, une charge négative, un cation sélectionné dans le groupe constitué par du sodium, du potassium, un tétraalkylammonium et un acyloxyalkyle, ou un alcoxycarbonyloxyalkyle; and R¿2? est hydrogène, acyle, un carbamoyle de silyle trisubstitué ou un résidu d'acide aminé; ou des sels pharmaceutiquement acceptables de ces composés.

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