Abstract: The invention relates to novel heteroarylamide derivatives having formula (I) and N-oxides, stereoisomers and pharmaceutically acceptable salts thereof, where RA, RB, R1 1, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.

Abstract: The present invention in general relates to the field of taste. In particular it relates to the reduction of astringency. One embodiment of the present invention relates to the use of at least one phospholipid for the preparation of a phenol containing composition to reduce the astringency of the composition.

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

Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.

Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

Abstract: The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.

Abstract: The present application relates to a process based on the oxidative ring opening of a compound with oxindole structure for preparation of substituted 2-(triazinylcarbonyl)sulfonanilides of the formula (1-1) proceeding from N-sulfonyl-substituted 3-triazinyloxindole of the formula (2-1), and to the 2-(triazinylcarbonyl)sulfonanilides of the formula (1-1) thus prepared, and to the use thereof as intermediates for the synthesis of fine chemicals and of active ingredients in the agricultural sector. The invention also relates to a multistage process for preparation of N-alkyl-N-[2-(1,3,5-triazin-2-ylcarbonyl)phenyl]alkanesulfonamides of the formula (4-1), proceeding from a 3-(alkylsulfanyl)-1,3-dihydro-2H-indol-2-one of the formula (7-1), wherein the multistage process also comprises, as a component step, the oxidative ring opening mentioned, and to the 2-(triazinylcarbonyl)sulfonanilides of the formula (1-1) which are obtained by the oxidative ring opening and are used as intermediates in the multistage process.

Abstract: The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.

Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.

Abstract: A method of treating an individual having Down syndrome or Alzheimer's disease, which entails the step of administering an amount of one or more compounds to the individual which improve cognitive functioning in the individual by increasing hippocampal NE levels.

Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: Embodiments of the invention relates to pharmaceutical compositions for use in the treatment of pain and inflammation in mammals, including humans, by administering compositions comprising i) an effective amount of an analgesic having an optional anti-inflammatory effect; (ii) an amount of caffeine effective in enhancement of pain relief; and, (iii) an amount of B vitamins effective in enhancement of pain relief.

Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.

Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.

Abstract: As a novel substance having a novel skeleton, provided is a novel phosphorescent organometallic iridium complex that can emit phosphorescence in a blue green to red wavelength region and has high emission efficiency. The phosphorescent organometallic iridium complex has a ligand having a pyridyl pyrimidine skeleton, i.e., the phosphorescent organometallic iridium complex has a ligand having a structure represented by the following general formula (G0). Note that in the formula, R1 and R4 to R6 separately represent hydrogen or an alkyl group having 1 to 6 carbon atoms; and R2 and R3 separately represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, a phenyl group that may have a substituent, and a pyridyl group that may have a substituent.

Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

Abstract: A composition for controlling plant diseases, containing a pyridazine compound represented by Formula (I) and fipronil, exhibits an excellent control effect against plant diseases. The present invention provides a composition for controlling plant diseases, containing the pyridazine compound represented by Formula (I) and fipronil, and a method for controlling plant diseases, including a step of applying an effective amount of the pyridazine compound represented by Formula (I) and fipronil to a plant or soil for cultivating a plant. [In the formula, R1 represents a chlorine atom, a bromine atom, a cyano group, or a methyl group, and R2 represents a hydrogen atom or a fluorine atom.