Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.

Abstract: The invention relates to new polymorphs of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate, the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.

Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.

Abstract: The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract: The present invention provides a process for preparing the amorphous rabeprazole sodium. The process comprises the following steps: (a) Contacting rabeprazole sodium compound with a solvent system to thereby obtain a clear solution under a first temperature, wherein said solvent system is a mixture of at least two categories of organic solvents; (b) Stirring said clear solution of step (a) under a second temperature for a certain time period to obtain a solution containing resultant separated solid, wherein said second temperature is equal to or lower than said first temperature; (c) Filtering said solution containing resultant separated solid obtained from step (b) to obtain a wet solid; and (d) Drying said wet solid to obtain an amorphous rabeprazole sodium compound.

Abstract: A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1H-benzimidazole.

Abstract: The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds.

Abstract: The invention relates to a process for preparing the compound of formula 1, a valuable intermediate product in the synthesis of the pharmaceutical active substance dabigatran etexilate.

Abstract: The invention relates to inhibitors of enzymes that disrupt the assembly and function of the mitotic spindle, compositions comprising the inhibitors of Formula (I), kits and articles of manufacture comprising the inhibitors and inhibitor compositions, and methods of using the inhibitors and inhibitor compositions. The inhibitors and inhibitor compositions are useful for treating, preventing or modulating diseases in which mitotic kinesins, including kinesin-like spindle protein (KSP), may be involved; symptoms of such diseases; or the effect of other physiological events mediated by mitotic kinesins, including KSP.

Abstract: Inhibitors of RSV replication of formula (I) the addition salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydro-thiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar2 or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydro-furanyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzth

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: The invention relates to new salt forms of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate.

Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.

Abstract: The present invention relates to benzimidazole derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical compositions and methods of treatment, comprising administering said pharmaceutical compositions to patients.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: The present invention relates to benzimidazole carboxamides of formula I, the use of the compounds of formula I of as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of pharmaceutical compositions and methods of treatment, comprising administering said pharmaceutical compositions to a patients.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.

Abstract: The invention is concerned with novel benzimidazole derivatives of formula (I) wherein A, n and R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.

Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.

Abstract: The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ?CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.

Abstract: Formulations are provided, comprising: a compound of Formula I, a pharmaceutically acceptable salt thereof, or a mixture of any two or more thereof; and an ingredient selected from a hydrophilic solvent, a lipophilic solvent, an emulsifier, or a mixture of any two or more thereof; wherein the compound of Formula I is: In some embodiments, the formulations are liquids. In other embodiments, the formulations are solids. Also provided are methods of preparing such formulations.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.

Abstract: The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.

Abstract: Novel compounds of the formula I (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R, Q, W, X and Z have the meanings indicated in Patent Claim 1, are suitable as antidiabetics.

Abstract: The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n?H2O (wherein n? is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-benzimidazole.nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.

Abstract: The present invention is directed to novel substituted pyrazole compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.

Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.

Abstract: The invention relates to compounds of formula (I): Wherein X1, X2, X3, X4, Y and W are as described herein. The invention also relates to a preparation method and to a therapeutic application.

Abstract: A ligand contains: a benzimidazole skeleton; and functional groups at the 5-position and the 6-position of the benzimidazole skeleton. The functional group is capable of forming a coordinate bond with a metal, and contains a nitrogen atom.

Abstract: The present invention provides compounds represented by the formula (Ia): the formula (Ib): the formula (Ic): and the formula (Id): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.

Abstract: A subject of the present Application is novel derivatives of benzimidazole and imidazopyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products.

Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.

Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-

Abstract: The present invention relates to a process for the preparation of quartenary ammoniumsalts of esomeprazole. Further, the present invention also relates to the use quartenary ammoniumsalts of esomeprazole for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the quartenary ammoniumsalts of esomeprazole, as such.

Abstract: The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n?H2O (wherein n? is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-benzimidazole.nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.

Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.

Abstract: Novel compounds of the formula I in which D, X, X?, W, Y, T and R1 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.

Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.

Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.

Abstract: This invention relates to novel carboxyl- or hydroxyl-substituted benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.

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, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.

Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

Abstract: Substituted benzimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections are also provided.