7-substituted bicyclic pyrazolidinones

Details 7-substituted bicyclic pyrazolidinones 7-substituted bicyclic pyrazolidinones

C - Chemistry, Metallurgy

07

D

167/233, 260/299

C07D 487/04 (2006.01) A61K 31/415 (2006.01)

Patent

CA 1274832

ABSTRACT OF THE DISCLOSURE The invention disclosed herein provides 7-substituted bicyclic pyrazolidinone compounds of the formula: Image I one of R1 and R2 is hydrogen, halo, C1 to C6 alkyl, C1 to C6 substituted alkyl, perfluoro C2 to C4 alkyl, C7 to C12 arylalkyl, C7 to C12 substituted aryl- alkyl, phenyl, substituted phenyl, a heterocyclic ring, nitro or cyano; a group of the formula -CX3 wherein X is fluoro, chloro, bromo or iodo; a group of the formula Image wherein z is 0, 1 or 2 and R7 is C1 to C6 alkyl, C1 to C6 substituted alkyl, phenyl, substituted phenyl, C7 to C12 arylalkyl, C7 to C12 substituted aryl- alkyl or a heterocyclic ring; a group of the formula -COR8 wherein R8 is hydrogen, C1 to C6 alkyl, C1 to C6 substituted alkyl, perfluoro C2 to C4 alkyl, trihalomethyl, C7 to C12 arylalkyl, C7 to C12 substituted aryl- alkyl, phenyl, substituted phenyl, amino, (monosubstituted)amino or (disubstituted)- amino; a group of the formula -COOR9 wherein R9 is hydrogen, an organic or inorganic cation, C1 to C6 alkyl, C1 to C6 substituted alkyl, C7 to C12 aryl- alkyl, C7 to C12 substituted arylalkyl, phenyl, substituted phenyl, a carboxy- protecting group or a non-toxic, metabolically-labile ester-forming group; a group of the formula PO3(R10)2 wherein R10 is hydrogen, an organic or inorganic cation, C1 to C6 alkyl, C1 to C6 substituted alkyl, C7 to C12 aryl- alkyl, C7 to C12 substituted arylalkyl, phenyl, or substituted phenyl; a group of the formula -CH2-??Q wherein -??Q is a quaternary ammonium group; or or a group of the formula -CH2-S-Heterocyclic ring; a group of the formula -OR11 wherein R11 is hydrogen, C1 to C6 alkyl, C1 to C6 substituted alkyl, C7 to C12 arylalkyl, C7 to C12 substituted arylalkyl, phenyl, sub- stituted phenyl or C1 to C7 acyl; or a group of the formula -NR12R13 wherein R12 and R13 are the same or different and are hydrogen, C1 to C6 alkyl, C1 to C6 substituted alkyl, C7 to C12 arylalkyl, C7 to C12 substituted arylalkyl, phenyl, substituted phenyl, C1 to C7 acyl, or a group of the formula; Image wherein Rq is C1 to C6 alkyl, C7 to C12 arylalkyl or phenyl; and the other of R1 and R2 is a group of the formula -COOR14 wherein R14 is hydrogen, an organic or inorganic cation, a carboxy-projecting group, or a non-toxic, metabolically-labile ester forming group; R3 and R4 are the same or different and are hydxogen, C1 to C6 alkyl, C1 to C6 substituted alkyl, C7 to C12 arylalkyl, C7 to C12 substituted arylalkyl, phenyl, substituted phenyl or a group of the formula -COOR15 wherein R15 has the same definition as R9; R5 and R6 are 1) each hydrogen, an amino protecting group or an acyl group derived from a C1 to C30 carboxylic acid; provided that at least one of R5 and R6 must be hydrogen; or 2) taken together to form a phthalimido group; or a pharmaceutically acceptable salt thereof. These compounds are antimicrobials, and are useful for treating bacterial infections.

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