Abstract: A method for producing a nitroso compound of the following formula (3), comprising reacting a compound of the following formula (1) with a compound of the following formula (2) by using a tertiary alcohol and a base. wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each independently a hydrogen atom, a halogen atom, a (C1-C4) alkyl, or a (C1-C4) alkoxy.

Abstract: A regioselective one-step process for the synthesis of 2-hydroxyquinoxaline of Formula (1) or tautomers thereof: comprising reacting 1,2-phenylenediamine of Formula (2): with an excess amount of glyoxylic acid, glyoxylic acid monohydrate, or a 2,2-dialkoxyacetic acid of Formula (3): at a low temperature; wherein R1 and R2 are as defined in the specification.

Abstract: Cyhalofop is prepared by coupling 2-(4-hydroxyphenoxy)propionic acid and 3,4-difluorobenzonitrile with base in a polar aprotic solvent in the presence of a phase-transfer catalyst.

Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.

Abstract: The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.

Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.

Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.

Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein A1, A2, A3, A4, A5, X, R1, R2 and R6 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.

Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.

Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.

Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

Abstract: The disclosure relates to Azetidine-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the R1, R2, R3, Q, Y1, Z, A, B, a, and b are as defined herein, compositions comprising an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound.

Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.

Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract: The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein R1, R2, R3, and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.

Abstract: An agent for oxidative coloring of keratin-containing fibers, in particular human hair, includes as oxidation dye precursor of the developer type at least one compound of formula (I).

Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.

Abstract: A nitrogen-containing heterocyclic compound represented by formula (I-A): (wherein R1A represents lower alkyl which may be substituted with lower alkoxy, R3A represents lower alkyl substituted with fluorine atom(s), and R4A represents an optionally substituted aromatic heterocyclic group) or the like, or a pharmaceutically acceptable salt thereof; and the like, are provided.

Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.

Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.

Abstract: The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.

Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity.

Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.

Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.

Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.

Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.

Abstract: The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.

Abstract: Pigment compositions containing organic pigments with an outstanding migration-free property and an excellent rheology at high concentration, and derivatives thereof containing heterocyclic substituents. The pigment compositions contains (a) carbon black or an organic pigment containing a chromophore Q1 of the following formula, wherein Z1 and Z2 are O or N—, C· is a carbon atom with an electron in a p orbital, and n is an integer from 1 to 4; and (b) a compound containing a chromophore of the following formula (II), wherein Q2 is an m-valent residue of carbon black or of the chromophore Q1; G1 is preferably and R1, R2, R3, R4, R5, R6, and R8 are preferably all H; m is an integer from 1 to 4. The pigment compositions can be used as rheology modifiers, preferably for pigmented coating compositions.

Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.

Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract: The present invention relates to agents that find use in the treatment, management, and/or study of cancer. In particular, the present invention relates to agents (e.g., small molecules, nucleic acids) that affect MMSET expression or activity.

Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.

Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.

Abstract: The present invention relates to compounds of formula (I) wherein X, Y, Z, R1, R2, R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.

Abstract: An agricultural or horticultural fungicide contains as an active ingredient thereof at least one compound selected from the group consisting of nitrogenated heterocyclic compounds represented by formula (I) (wherein, R represents a group represented by CR1R2R3 or a cyano group, R1 to R3 represent hydrogen atoms, alkyl groups or hydroxyl groups, or the like, X1 represents a halogeno group or the like, m represents an integer of 0 to 5, X2 represents a halogeno group or the like, n represents an integer of 0 to 3, B represents a carbon atom or a nitrogen atom, D represents a 5- to 7-membered hydrocarbon ring, and A1 to A4 represent carbon atoms or nitrogen atoms, provided that A1 to A4 do not all represent carbon atoms when B represents a carbon atom) and salts thereof.

Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.

Abstract: The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye).

Abstract: The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R1, R2, Qa, Y1, Z, A, B, Qx, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.

Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG, and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.

Abstract: A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), R1 represents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; R2 represents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; R3 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; R4 and R5 independently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; R6 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; R8 and R9 independently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.