The present invention relates to 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.

The present invention provides compounds pounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both.

The present invention relates to oximes, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.

Presented herein inter alia are novel compounds and methods of using the same for the treatment of cancers.

Presented herein inter alia are novel compounds and methods of using the same for the treatment of cancers.

Through use of this water-/oil-repellent agent including a modified heterocyclic compound having a heterocycle and a C1-40 hydrocarbon group, adequate oil-resistance can be imparted to a substrate. The heterocycle is preferably a nitrogen-containing heterocycle. The hydrocarbon group is preferably an octyl group, a decyl group, an undecyl group, a lauryl group, a tridecyl group, a myristyl group, a palmityl group, a cetyl group, an isopalmityl group, a stearyl group, or a behenyl group. The heterocycle is preferably pyrimidine, pyridazine, pyridine, diazine, triazine, oxazole, or oxadiazole.

Through use of this water-/oil-repellent agent including a modified heterocyclic compound having a heterocycle and a C1-40 hydrocarbon group, adequate oil-resistance can be imparted to a substrate. The heterocycle is preferably a nitrogen-containing heterocycle. The hydrocarbon group is preferably an octyl group, a decyl group, an undecyl group, a lauryl group, a tridecyl group, a myristyl group, a palmityl group, a cetyl group, an isopalmityl group, a stearyl group, or a behenyl group. The heterocycle is preferably pyrimidine, pyridazine, pyridine, diazine, triazine, oxazole, or oxadiazole.

The present invention relates to a compound of formula (I), or one of its pharmaceutically acceptable salts: (I) wherein R1, R2 and XY have specific definitions. It also relates to the use of such a compound in therapy; and to a process for preparing it. ##STR00001##

A 3-(alkylsulfonyl)pyridine-2-carboxylic acid or a salt thereof can be manufactured by comprising: allowing a compound represented by formula (1-N): ##STR00001## wherein X represents a halogen atom, to react with a compound represented by formula (2):
R.sup.2SM.sup.2(2) wherein R.sup.2 represents a C.sub.1-8 straight-chain alkyl group, and M.sup.2 represents a hydrogen atom or an alkali metal, to give a compound represented by formula (3-N): ##STR00002## wherein R.sup.2 and X are as defined above; allowing the compound (3-N) to react with hydrogen peroxide in the presence of a tungsten catalyst and an acid; reducing the product in the presence of a base and a heterogeneous transition metal catalyst; and hydrolyzing the product in the presence of a base.

A compound represented by formula (7): ##STR00001## or a salt thereof can be manufactured by the following steps: a step of allowing a compound represented by formula (1-S): ##STR00002## to react with a compound represented by formula (2):
R.sup.2SM.sup.2(2) to give a compound represented by formula (3-S): ##STR00003## a step of allowing the compound represented by formula (3-S) to react with hydrogen peroxide in the presence of a tungsten catalyst and an acid to give a compound represented by formula (6-S) or a salt thereof: ##STR00004##
and a step of reducing the compound represented by formula (6-S) or salt thereof in the presence of a base and a heterogeneous transition metal catalyst to give a compound represented by formula (7) or a salt thereof, wherein X, R.sup.1, R.sup.2, and M.sup.2 are defined in the specification.