Abstract: The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-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 Bridged-Piperidine Compound.

Abstract: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-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 Bridged-Piperidine Compound.

Abstract: An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method.

Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention relates to the compound of formula (I), in which R1 represents Sn(R)3, B(OH)2, B(OR)2, a halogen atom, NO2, a radionuclide or a —N+(R)3 group, where R is a (C1-C6) alkyl group, R2 represents a hydrogen atom or a (C1-C6)alkyl group, R3 represents: a —(CH2CH2O)n2—(CH2)n3—X group, or a —(CH2CH2O)n4—(CH2)n5—Y group with Y representing a —C?C—H, a —N3 or a —Ar—(CH2)n6—(OCH2CH2)n7—X group, and X represents a halogen atom, a radionuclide or a —OSO2R? group, where R? is a CF3, CH3, t-Bu, Ph, p-NO2Ph, p-BrPh or p-CH3Ph group, and their addition salts with pharmaceutically acceptable acids, The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT or PET imaging and in therapy of melanoma, via targeted radionuclide therapy.

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

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: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

Abstract: The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract: The present invention relates to methods for the treatment of a pathology associated with hyperglycaemia, particularly diabetes, by administering quinoxalinone compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The compounds have activity as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone compounds for modulating insulin secretion in insulin-1 cells by contacting the cells with the compounds.

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.

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 compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, G1, G2, G3, Y1, Y2, n, and p are as defined in the claims. The invention also relates to methods of using the compounds of formula (I) to control or prevent infestation of plants, propagation material thereof, harvested crops or non-living materials by phytopathogenic spoilage microorganisms or organisms potentially harmful to man.

Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

Abstract: The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4)alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or a group of formula (?): —Y—Z—W—R11??(?) wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a —N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.

Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.

Abstract: The present invention relates to compounds of formula (I) that have CYP450 inhibiting properties and are useful as boosting agents when used with HIV treatments. These compounds are represented by formula including the salts and stereoisomeric forms thereof, wherein R1 is 5-thiazolyl or 3-pyridinyl; R2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C1-6-alkyl or C1-6-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C3-7cycloalkyl optionally substituted with one or more halogens; C1-6alkyl optionally substituted with heteroaryl; —O—CH2— (heteroaryl). As boosting agents they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered, or improve the bioavailability of certain drugs.

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 present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.

Abstract: The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.

Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The invention relates to compounds of formula (I) wherein the substituens are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.

Abstract: The invention relates to compounds of formula (I), where A, Ar1, Ar2, R1a, R1b, R1c, R2a, R2b, R2c, R3, R4 and R8 are as described herein, and pharmaceutical compositions thereof, methods of preparation thereof, and methods of use thereof.

Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful in modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are useful for treating pathologies in which such modulation is beneficial, as in the case of metabolic syndrome or of noninsulin-dependent type 2 diabetes. The invention also relates to pharmaceutical preparations containing such a compound, processes for preparing and intermediates useful in the preparation of a such a compound.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated 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.

Abstract: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-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 Bridged-Piperidine Compound.

Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.

Abstract: Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays.

Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

Abstract: The present invention relates to quinoxalinone derivatives of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein, as insulin secretion stimulators. Specific such quinoxaline compounds are also an aspect of the invention. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. The present invention relates to an oxopyrazine derivative represented by formula [I]: wherein X1 represents an oxygen atom or a sulfur atom; X2 represents CH or N(O)m; m represents an integer of 0 or 1; R1 represents a hydrogen atom, a C1-C12 alkyl group and the like; R2 represents a halogen atom, a cyano group and the like; R3 is a hydroxyl group, a halogen atom and the like; A1 represents C(R4R5); A2 represents C(R6R7) or C?O; A3 represents C(R8R9); R4 to R9 represent a hydrogen atom or an alkyl group, or a salt thereof, and a herbicide containing these compounds.

Abstract: The present subject matter relates to perhydroquinoxaline derivates, processes for their preparation, their use for the preparation of a medicament and medicaments containing perhydroquinoxaline derivates.

Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.

Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives of Formula (I): as disclosed herein, to their preparation and to their therapeutic application.

Abstract: The compounds represented in general formula (1) or a salt thereof are useful for glucocorticoid receptor modulators. In the formula, R1 represents a lower alkyl group, a lower cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, a lower alkyl group and the like; R3 represents a hydrogen atom, a lower alkyl group and the like; R4 and R5 represent a hydrogen atom, a lower alkyl group and the like; R6 represents a hydrogen atom, a lower alkyl group and the like; R7 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group and the like; W represents an oxygen atom, a sulfur atom, NR8 and the like; R8 represents a hydrogen atom, a lower alkyl group and the like; X represents an oxygen atom or a sulfur atom; Y represents a lower alkylene group and the like; Z represents an oxygen atom, a sulfur atom, NR9, OCO or OSO2; R9 represents a hydrogen atom, a lower alkyl group and the like respectively.

Abstract: The invention relates to compounds of formula (I), where: A is a bond, an oxygen, or an —CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are hydrogen or halogen, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally, substituted by one or more halogen atoms, or a —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, and to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano, —OR5, hydroxyalkyl, —COOR5, —NR6R7, ONR6R7, —

Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.

Abstract: Compounds, compositions and methods for treating GHS-R mediated disorders are described herein.

Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.