Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

##STR00001##

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

##STR00001##

Antibacterial compounds of formula (I) are provided: ##STR00001##
as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

Antibacterial compounds of formula (I) are provided: ##STR00001##
as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

Antibacterial compounds of formula (I) are provided:

##STR00001##

as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

Disclosed are compounds of Formula I, including all stereoisomers, (N-oxides), and salts thereof, wherein A and R are as defined in the disclosure.

##STR00001##

Also disclosed is a method for preparing a compound of Formula I, comprising reacting a compound of Formula II with an aroyl enolate salt of Formula III in the presence of an acid in an aqueous solvent mixture, wherein A, R and M are as defined in the disclosure.

Also disclosed is a method for preparing a compound of Formula IV, comprising reacting a compound of Formula I with an aldehyde of Formula V in the presence of a secondary amine salt, wherein A, B and R are as defined in the disclosure.

##STR00002##

Compounds of formula (I) have antibacterial activity:

##STR00001##

wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is C(R.sub.1) or N; R.sub.1 is hydrogen or an optional substituent and R.sub.2 is hydrogen, methyl, or fluorine; or R.sub.1 and R.sub.2 taken together are CH.sub.2, CH.sub.2CH.sub.2, O, or, in either orientation, OCH.sub.2 or OCH.sub.2CH.sub.2; R.sub.3 is a radical of formula -(Alk.sup.1).sub.m-(Z).sub.p-(Alk.sup.2).sub.n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is O, S, S(O), S(O.sub.2), NH, N(CH.sub.3), N(CH.sub.2CH.sub.3), C(O), O(CO), C(O)O, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk.sup.1 and Alk.sup.2 are optionally substituted C.sub.1-C.sub.6 alkylene, C.sub.2-C.sub.6 alkenylene, or C.sub.2-C.sub.6 alkynylene radicals, which may optionally terminate with or be interrupted by O, S, S(O), S(O.sub.2), NH, N(CH.sub.3), or N(CH.sub.2CH.sub.3); and Q is hydrogen, halogen, nitrile, or hydroxyl or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms.

Compounds of formula (I) have antibacterial activity:

##STR00001##

wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is C(R.sub.1) or N; R.sub.1 is hydrogen or an optional substituent and R.sub.2 is hydrogen, methyl, or fluorine; or R.sub.1 and R.sub.2 taken together are CH.sub.2, CH.sub.2CH.sub.2, O, or, in either orientation, OCH.sub.2 or OCH.sub.2CH.sub.2; R.sub.3 is a radical of formula -(Alk.sup.1).sub.m-(Z).sub.p-(Alk.sup.2).sub.n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is O, S, S(O), S(O.sub.2), NH, N(CH.sub.3), N(CH.sub.2CH.sub.3), C(O), O(CO), C(O)O, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk.sup.1 and Alk.sup.2 are optionally substituted C.sub.1-C.sub.6 alkylene, C.sub.2-C.sub.6 alkenylene, or C.sub.2-C.sub.6 alkynylene radicals, which may optionally terminate with or be interrupted by O, S, S(O), S(O.sub.2), NH, N(CH.sub.3), or N(CH.sub.2CH.sub.3); and Q is hydrogen, halogen, nitrile, or hydroxyl or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms.