Abstract: Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute triazoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.

Abstract: A N?-(2-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-ylthio)acetoxy)-1-naphthimidamide compound, its synthesis, and its use as an antimicrobial agent.

Abstract: A N?-(2-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-ylthio)acetoxy)-1-naphthimidamide compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Electro-optic (EO) devices having an EO polymer core comprising a first host polymer and a first nonlinear optical chromophore (NLOC); and a cladding comprising a second host polymer and a second NLOC, and methods of preparing the same; wherein the first NLOC has a first bridge covalently bonded to an electron-accepting group and an electron-donating group; wherein the second NLOC has a second bridge covalently bonded to an electron-accepting group and an electron-donating group; and wherein the second bridge is less conjugated than the first bridge such that the cladding has an index of refraction that is less than that of the EO polymer core, and wherein the second NLOC is present in the second host polymer in a concentration such that the cladding has a conductivity equal to or greater than at least 10% of the conductivity of the EO polymer core at a poling temperature.

Abstract: Compounds of Formula (I), racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions containing the compounds, racemates, enantiomers, diastereomers thereof are disclosed. These compounds have GPR40 agonist activity and are capable of modulating blood glucose levels and glucose-dependent insulin secretion mechanism, and, thus, exhibit excellent glucose lowering efficacy without the risk of hypoglycemia. These compounds could be used in preventing and/or treating type 2 diabetes through adequate control of blood glucose.

Abstract: The present invention provides novel inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-methyl-3-difluoromethyl-1H-pyrazole-4-carbaldehyde, a useful intermediate in the manufacture of fungicides.

Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.

Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.

Abstract: Provided are improved processes for the preparation of 1-aryl pyrazole compounds of formula (I) and (IB): which are substituted at the 5-position of the pyrazole ring with a carbon-linked functional group. The process described are efficient and scalable and do not utilize hazardous sulfenyl halide reagents.

Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with a pyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.

Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, fungicides: wherein Q1, R1, R1a, R2, R3 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.

Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.

Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.

Abstract: The present invention relates to a novel liquid formulation for crop protection which comprises a) pyraclostrobin; b) at least one organic solvent S1 with a water solubility of less than 2 g/l at 20° C.; c) at least one organic solvent S2 with a water solubility of at least 2 g/l at 20° C., where S2 comprises at least one solvent S2.1 with a water solubility of more than 200 g/l at 20° C. and optionally at least one solvent S2.2 with a water solubility of 2 to 200 g/l at 20° C.; d) at least one anionic surface-active substance SA1; e) at least one nonionic surface-active substance SA2; and f) water. The invention also relates to the use of the crop protection formulation for treatment of plants and seed, and to corresponding methods.

Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.

Abstract: Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.

Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.

Abstract: A glycoprotein and/or a glycopeptide which are a test substance is heated in the presence of a pyrazolone derivative, an isoxazolone derivative, a hydantoin derivative, a rhodanine derivative, a maleimide derivative, or the like under a basic condition to cleave and label a post-translational modification group for analysis, thereby enabling analysis of a post-translational modification of a serine residue and/or a threonine residue.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.

Abstract: Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6, R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.

Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.

Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoro-1-alkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.

Abstract: The present invention relates to a process for preparing 1-alkyl-3-difluoromethyl-5-hydroxypyrazoles, which are valuable intermediates for the production of fungicides.

Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I 5 in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with a pyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.

Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.

Abstract: The present invention provides: dinitropyrazole derivatives of formula (I) in which: R?NO2, NH2, NF2, NHOH, OH or NHNH2 and R??H when R?NH2, NF2, NHOH, OH or NHNH2 or R??H, NH2 or a linear or branched C1-C4 alkyl group, optionally substituted by at least one hydroxy and/or one fluoro group, when R?NO2; other than 4-amino-3,5-dinitropyrazole; and also the salts of said derivatives of formula (I) in which R??H; the preparation of said derivatives and of their salts; and energetic compositions comprising at least one of said derivatives and/or at least one salt of such a derivative.

Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.

Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.

Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

Abstract: A process for preparing pyrazole-glycoside derivatives of the general Formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C1-C8)-alkyl, where one, more than one or all hydrogen(s) may be replaced by fluorine; X (C1-C3)-alkylene, (C2-C3)-alkenylene.

Abstract: The present invention provides: dinitropyrazole derivatives of formula (I) in which: R?NO2, NH2, NF2, NHOH, OH or NHNH2 and R??H when R?NH2, NF2, NHOH, OH or NHNH2 or R??H, NH2 or a linear or branched C1-C4 alkyl group, optionally substituted by at least one hydroxy and/or one fluoro group, when R?NO2; other than 4-amino-3,5-dinitropyrazole; and also the salts of said derivatives of formula (I) in which R??H; the preparation of said derivatives and of their salts; and energetic compositions comprising at least one of said derivatives and/or at least one salt of such a derivative.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.

Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with apyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.

Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, a pharmaceutical composition of formula (I), and related methods for treating or preventing metabolic diseases or conditions.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O)m, NR4, CR15R16, C(?O) or C(?S); and R1, R1a, R2, R4, R15, R16 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: The present invention relates to a process for preparing 1-alkyl-3-difluoromethyl-5-hydroxypyrazoles, which are valuable intermediates for the production of fungicides.

Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.

Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).

Abstract: A benzoylpyrazole compound represented by the formula (I) or its salt, useful as herbicides and intermediates thereof.

Abstract: Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives and pyrazole intermediates of the same. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes and intermediates for preparing the same.

Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.

Abstract: The invention relates to colorant compositions for the oxidative dyeing of keratin fibers comprising radical scavengers in the dyeing composition. The invention also relates to methods for reducing color formation outside of the keratin fiber during oxidative dyeing comprising using such compositions.

Abstract: The invention relates to colorant compositions for the oxidative dyeing of keratin fibers comprising an inhibiting system of radical scavengers and chelants in the dyeing composition. The invention also relates to methods for reducing color formation outside of the keratin fiber during oxidative dyeing comprising using such colorant compositions.

Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is Q2 or R1; X is N, CR2 or CQ3; Y is N or CR3; Z is N or CR4; and Q1, Q2, Q3, R1 R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: The invention relates to 1-(2,4,6-trisubstituted-phenyl)-5-amino-4-substituted-pyrazole derivatives of formula (I) or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).