The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

A compound of formula (I) ##STR00001##
wherein X is 0, C=0 or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

A compound of formula (I) ##STR00001##
wherein X is 0, C=0 or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein W, X, Y, Z, x, R.sup.1, R.sup.2, R.sup.3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein W, X, Y, Z, x, R.sup.1, R.sup.2, R.sup.3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

A compound of formula (I)

##STR00001##

wherein X is O, C═O or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10 aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof

A compound of formula (I)

##STR00001##

wherein X is O, C═O or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10 aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof

Provided herein are novel amide prodrug forms of pharmaceutically active agents useful for central nervous system disorders.