[[(3-acylamino-2-oxo-1-azetidinyl)oxy] methyl]phosphinic acids

C - Chemistry – Metallurgy – 07 – F

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167/234, 167/241

C07F 9/568 (2006.01) A61K 31/675 (2006.01)

Patent

CA 1244035

ABSTRACT [[(3-ACYLAMINO-2-OXO-1-AZETIDINYL)OXY] METHYL]PHOSPHINIC ACIDS Antibacterial activity is exhibited by .beta.-lactams having a 3-acylamino substituent and in the 1-position a substituent having the formula Image wherein R5 and R6 are the same or different and each is hydrogen, alkyl, alkenyl, alkynyl, phenyl, substituted phenyl, cycloalkyl or a 4,5,6 or 7-membered heterocycle, or R5 and R6 together with the carbon atom to which they are attached are cycloalkyl or a 4,5,6, or 7-membered heterocycle, or one of R5 and R6 is hydrogen and the other is axido, halomethyl, dihalomethyl, trihalomethyl, alkoxycarbonyl, alkenyl, alkynyl, 2-phenylethenyl, 2-phenylethynyl, carboxyl, -CH2X1, -S-X2, -O-X2, or Image : R7 is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, 1-(ethoxycarbonyl- oxy)ethyl, 1,3-dihydro-3-oxo-1-isobenzofuranyl, Image wherein R' is hydrogen or alkyl, R" is alkyl or phenyl, R"' is hydrogen, methyl or phenyl, and Riv is hydrogen or together with R"' is -(CH2)3- or -(CH2)5-; and R8 is hydroxy, alkoxy, (substituted alkyl)- oxy, phenyloxy, (substituted phenyl)oxy, alkyl, substituted alkyl, phenyl, substituted phenyl, heteroaryl, amino, substituted amino, alkylthio, (substituted alkyl)thio, phenylthio, (substituted phenyl)thio, or Image .

454035

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