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 invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.

Abstract: Ternary pesticidal mixtures comprising, as active components, an anthranilamid compound of the formula I wherein the variables are defined according to the description, and two fungicidal compounds II and III selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates, guanidines, antibiotics, nitrophenyl derivates, sulfur-containing heterocyclyl compounds, organometal compounds and other active compounds according to the description, in a synergistically effective amount, methods for controlling pests, and harmful fungi, methods of protecting plants from attack or infestation by insects, acarids or nematodes, methods for treating, controlling, preventing or protecting an animal against infestation or infection by parasites, compositions containing these mixtures, and methods for their preparation.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.

Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.

Abstract: The present invention provides formulations which may comprise macrocyclic lactones and at least one spirodioxepinoindole derivative or a spirooxepinoindole derivative for combating parasites in birds and mammals. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

Abstract: A process of preparation of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 represent H; or either R1 represents ethyl and R2 represents n-hexyloxycarbonyl that applies to industrial scale, novel intermediates useful for the preparation thereof, and processes of preparing said intermediates.

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: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.

Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.

Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: The present invention provides for methods of using tert-butyl alcohol (TBA) co-solvent systems in the formulation and production of a pharmaceutical agent with low solubility. The present invention also provides for pharmaceutical compositions made using the novel co-solvent system. In one embodiment, the invention provides for a method of making dantrolene sodium (DS) formulation for intravenous use (DS-IV). This instantaneous reconstitution of the DS-IV product constitutes a significant improvement in the pharmacotherapy of patients undergoing malignant hyperthermia during surgery.

Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.

Abstract: The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them.

Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.

Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.

Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-fosetylate, an insecticide active substance and optionally a further fungicide active substance.

Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Abstract: Pesticidal mixtures comprising, as active components, 1) an anthranilamid compound of the formula I wherein the variables are defined according to the description, and 2) at least one fungicidal compound II selected from the following groups: strobilurins, carboxamides, heterocylic compounds and other active compounds according to the description, in a synergistically effective amount, methods for controlling pests, and harmful fungi, methods of protecting plants from attack or infestation by insects, acarids or nematodes, methods for treating, controlling, preventing or protecting an animal against infestation or infection by parasites, compositions containing these mixtures, and methods for their preparation.

Abstract: Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.

Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.

Abstract: Subjects that have a 16p11.2 microdeletion syndrome are treated by administering compositions that include mGluR inhibitors, including mGluR antagonists that include mGluR negative allosteric modulators. Administration of compositions employed in the methods of the invention can treat psychiatric, including neuropsychiatric disorders, cognitive impairments, attention, obesity, intellectual disability and seizure disorders.

Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.

Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.

Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.

Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.

Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: In accordance with the present invention, there are provided formulations of gamma secretase modulators (GSMs) which are suitable for oral delivery and have improved transport properties relative to prior art formulations thereof. Also provided are methods for the preparation of such improved formulations and uses thereof for the delivery of GSMs to subjects in need thereof.

Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.

Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.

Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.

Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).

Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.

Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.

Abstract: A therapeutic agent or a prophylactic agent for neuropathic pain provides a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent for neuropathic pain includes as effective ingredients a cyclohexane derivative, represented by the following formula, or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.

Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Abstract: A pest controlling composition comprising tolclofos-methyl and a neonicotinoid compound represented by the formula (1) as active ingredients.