Compounds and compositions comprising compounds that activate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that activate PKM2 in the treatment of cancer.

The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process:

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6 and R.sup.10 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which MLH1 and/or PMS2 activity is implicated.

The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process:

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6 and R.sup.10 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which MLH1 and/or PMS2 activity is implicated.

The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula I: ##STR00001##
wherein the variables are as defined herein.

The present invention provides a heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I): ##STR00001##
wherein
Ar is a the partial structure (1) to the partial structure (5),
Q is a bivalent group selected from the group consisting of (Ia)-(If), and
B is a ring optionally having substituent(s),
or a salt thereof.

The present invention provides a heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I): ##STR00001##
wherein
Ar is a the partial structure (1) to the partial structure (5),
Q is a bivalent group selected from the group consisting of (Ia)-(If), and
B is a ring optionally having substituent(s),
or a salt thereof.

The invention relates to novel cationic benzoxazine-based compounds of formula (I) below, in which •R represents a hydrogen atom or a C.sub.1-C.sub.4 alkyl or C.sub.1-C.sub.4 hydroxyalkyl radical, •—R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently represent: —a hydrogen atom, —a linear C.sub.1-C.sub.4 or branched C.sub.3-C.sub.4 alkyl radical, optionally substituted with a hydroxyl radical, •L represents a linear or branched, saturated C.sub.1-C.sub.30 hydrocarbon-based chain, •CAT+ represents a cationic radical chosen from: —a cationic heterocyclic radical comprising 5 to 8 ring members containing at least one heteroatom chosen from O, N and S, —a tri(hydroxy)(C.sub.1-C.sub.4)alkylammonium radical, —a non-cationic heterocycle comprising 5 or 6 ring members containing at least one heteroatom chosen from O and N, such as pyrrolidine, substituted with a cationic radical, An− represents an anion or a mixture of anions which are organic or inorganic and are cosmetically acceptable.

##STR00001##

The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.

The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.

Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.