Abstract: A pyrimidine compound of the formula (1): wherein: R1 represents hydrogen, and the like; R2 represents hydrogen, and the like; R3 represents a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like; R4 and R5 are represent a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like; X represents nitrogen, and the like; Y represents nitrogen, and the like; and Z represents oxygen or —NR8— wherein R8 represents a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like. The compound has a superior activity of controlling pests.

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.

Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.

Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.

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: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.

Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway.

Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.

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: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.

Abstract: The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.

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: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.

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: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: The present invention provides a solid form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibit desirable characteristics for the same.

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.