Provided herein is a compound of Formula (I):

##STR00001##

wherein: R.sub.1 is selected from the group of —F, —Cl, —Br, —I, C.sub.1-C.sub.6 haloalkyl, C.sub.1-C.sub.6 haloalkoxy, —NO.sub.2, —C(H)═O, ═O, —CN, and COOR.sub.3; R.sub.2 is selected from the group of H and C.sub.1-C.sub.3 alkyl; and R.sub.3 is selected from the group of H, C.sub.1-C.sub.6 alkyl, and benzyl;
or a pharmaceutically acceptable salt, co-crystal, ester, solvate, hydrate, isomer (including optical isomers, racemates, or other mixtures thereof), tautomer, isotope, polymorph, or pharmaceutically acceptable prodrug thereof, along with pharmaceutical compositions and methods of using the compound in the treatment of malaria, particularly including drug-resistant malaria.

Provided herein is a compound of Formula (I):

##STR00001##

wherein: R.sub.1 is selected from the group of —F, —Cl, —Br, —I, C.sub.1-C.sub.6 haloalkyl, C.sub.1-C.sub.6 haloalkoxy, —NO.sub.2, —C(H)═O, ═O, —CN, and COOR.sub.3; R.sub.2 is selected from the group of H and C.sub.1-C.sub.3 alkyl; and R.sub.3 is selected from the group of H, C.sub.1-C.sub.6 alkyl, and benzyl;
or a pharmaceutically acceptable salt, co-crystal, ester, solvate, hydrate, isomer (including optical isomers, racemates, or other mixtures thereof), tautomer, isotope, polymorph, or pharmaceutically acceptable prodrug thereof, along with pharmaceutical compositions and methods of using the compound in the treatment of malaria, particularly including drug-resistant malaria.

The present invention discloses a method to discover selective inhibitors of phosphatases. Thus the invention provides a method for screening a test compound to determine whether the compound binds a holophosphatase selectively or non-selectively comprising: i) providing a first holophosphatase wherein said holophosphatase is captured/immobilised; ii) testing a test compound for its ability to bind to the first holophosphatase; iii) providing a second holophosphatase wherein said second holophosphatase is captured/immobilised; iv) testing the same test compound for its ability to bind to the second holophosphatase; v) comparing the binding of the test compound to said first holophosphatase with the binding to said second phosphatase wherein a compound that binds a holophosphatase selectively will bind to said first holophosphatase but not said second holophosphatase; or will bind to said second holophosphatase but not said first; or wherein a compound that binds a holophosphatase non-selectively will bind to both said first holophosphatase and said second holophosphatase.

The present invention discloses a method to discover selective inhibitors of phosphatases. Thus the invention provides a method for screening a test compound to determine whether the compound binds a holophosphatase selectively or non-selectively comprising: i) providing a first holophosphatase wherein said holophosphatase is captured/immobilised; ii) testing a test compound for its ability to bind to the first holophosphatase; iii) providing a second holophosphatase wherein said second holophosphatase is captured/immobilised; iv) testing the same test compound for its ability to bind to the second holophosphatase; v) comparing the binding of the test compound to said first holophosphatase with the binding to said second phosphatase wherein a compound that binds a holophosphatase selectively will bind to said first holophosphatase but not said second holophosphatase; or will bind to said second holophosphatase but not said first; or wherein a compound that binds a holophosphatase non-selectively will bind to both said first holophosphatase and said second holophosphatase.

The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.3a, R.sup.5a, X.sup.a and Y.sup.a are as defined herein. ##STR00001##

The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.3a, R.sup.5a, X.sup.a and Y.sup.a are as defined herein. ##STR00001##

Disclosed are compositions containing a UV-inhibitor, optionally a carrier, and optionally anions; wherein the UV-inhibitor is at least one compound of formula (I)

##STR00001##

wherein R1 is an aryl derivative, N-acyl, guanidine or aminoguanidine group, and R2 and R3 are independently an aryl group substituted with a straight or branched chain alkyl or an electron donating or withdrawing group. Also disclosed are methods for protecting a product from UV light, involving applying to said product, in an amount sufficient to protect said product from UV light, the composition. Furthermore, there is disclosed methods for providing a reversible dye to a product, involving applying to said product, in an amount sufficient to provide a visible color to said product, the composition.

Disclosed are compositions containing a UV-inhibitor, optionally a carrier, and optionally anions; wherein the UV-inhibitor is at least one compound of formula (I)

##STR00001##

wherein R1 is an aryl derivative, N-acyl, guanidine or aminoguanidine group, and R2 and R3 are independently an aryl group substituted with a straight or branched chain alkyl or an electron donating or withdrawing group. Also disclosed are methods for protecting a product from UV light, involving applying to said product, in an amount sufficient to protect said product from UV light, the composition. Furthermore, there is disclosed methods for providing a reversible dye to a product, involving applying to said product, in an amount sufficient to provide a visible color to said product, the composition.

The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.3a, R.sup.5a, X.sup.a and Y.sup.a are as defined herein. ##STR00001##

The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.3a, R.sup.5a, X.sup.a and Y.sup.a are as defined herein. ##STR00001##