Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract: The present invention provides gas-induced method for phase-transforming organic solids, such as pharmaceutical crystals. The inventive method subjects the polymorphs of pharmaceutical agents to various pressures of gases (such as CO2, N2O, and CH4) to induce phase transform with ease.

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 provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.

Abstract: Disclosed herein are novel compounds which are useful as intermediates for producing substituted sulfoxide compounds and a process for producing the same. Further disclosed is a process for producing the substituted sulfoxide compounds used as pharmacologically active agents, employing the novel intermediates of the present invention.

Abstract: Small, low molecular weight compounds of the formula I and/or the formula II, as defined herein, which inhibit Cu-ATPases, ATP7A and ATP7B. Compositions and methods therefore, are provided.

Abstract: Disclosed are a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.

Abstract: Disclosed herein are novel compounds which are useful as intermediates for producing substituted sulfoxide compounds and a process for producing the same. Further disclosed is a process for producing the substituted sulfoxide compounds used as pharmacologically active agents, employing the novel intermediates of the present invention.

Abstract: The present invention relates to a process for the preparation of crystalline dexlansoprazole.

Abstract: The present invention relates to the salts of dexlansoprazole in amorphous form. The present invention further relates to processes for the preparation of salts of dexlansoprazole.

Abstract: The present invention relates to crystalline forms of dexlansoprazole designated as forms A and B, and their preparation. The present invention further relates to processes for the preparation of anhydrous dexlansoprazole and dexlansoprazole sesquihydrate using crystalline Forms A and B of dexlansoprazole.

Abstract: An improved process for the preparation of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole of Formula I, (I) with high enantiomeric excess from racemic mixture.

Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Abstract: The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation.

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 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 present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.

Abstract: The present invention is directed to a process for the catalytic oxidation of the thioether 5-methoxy-2-((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)methylthio)-1H-benzimidazole to its sulfoxide: 5-methoxy-2-((4-methoxy-3,5-dimethyl-2-pyridinyl) methyl) methylsulfinyl)-1H-benzimidazole comprising: reacting the thioether with: 1) a transition metal catalyst; and, 2) an oxygen source; wherein the thioether is oxidized to the sulfoxide commonly known as omeprazole and wherein one of either the R and S enantiomers is formed to an enantiomeric excess.

Abstract: The present invention relates to process for preparation of optical resolution of substituted 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles either as a single enantiomer or in an enantiomerically enriched form. Thus, for example, R-1,1?-binaphtyl-2-2?-diyl hydrogen phosphate was reacted with 2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (Lansoprazole) in a mixture of benzene and cyclohexane to obtain diasteremeric complexes. The diasteremeric complexes were subjected to fractional crystallization to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole.R-1,1?-binaphthyl-2-2?-diyl hydrogen phosphate. The separated isomer was treated with sodium bicarbonate in a mixture of ethyl acetate and water to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (dexlansoprazole).

Abstract: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.

Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.

Abstract: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.

Abstract: A process for preparation of optically pure or optically enriched enantiomers of sulphoxide compounds of formula (I), such as omeprazole and structurally related compounds, as well as their salts and hydrates.

Abstract: Provided is dexlansoprazole propylene glycolate hydrate. Polymorphic forms thereof are also provided. The dexlansoprazole propylene glycolate hydrate maybe such that the propylene glycol component is present in approximately equal proportions of (R) absolute configuration and (S) absolute configuration, or present in predominantly (R) absolute configuration, or predominantly (S) absolute configuration. Salts of dexlansoprazole are also provided. In particular, crystalline dexlansoprazole isopropylammonium salt and crystalline MTBE solvate of dexlansoprazole t-butylammonium salt are provided. Pharmaceutical formulations comprising dexlansoprazole propylene glycolate hydrate are also provided. Furthermore, processes for preparation of dexlansoprazole propylene glycolate hydrate are provided.

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: A process for the enantioselective synthesis of a sulphoxide of a compound of Formula I or a pharmaceutically acceptable salt thereof in the form of a single enantiomer or in an enantiomerically enriched form wherein R1 to R4 are same or different and selected from the group consisting of hydrogen, C1 to C4 linear or branched alkyl, C1 to C4 linear or branched alkoxy, aryl, aryloxy alkoxy substituted by halogen or alkoxyalkoxy; X is either CH or N, said process comprising oxidizing the prochiral sulphide, compound of Formula II in an organic solvent with an oxidizing agent in presence of titanium (IV)alkoxide, (?)-Diethyl-D-tartrate, C1-C4 alcohol, and water; and optionally converting the compound of formula I into a pharmaceutically acceptable salt.

Abstract: A stable R-(+)-lansoprazole alkylamine salt and a process for preparing the salt.

Abstract: There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.

Abstract: The present invention relates to novel crystalline forms of Dexlansoprazole and a process for the preparation of amorphous Dexlansoprazole.

Abstract: Disclosed herein is a method for the production of disulfide compounds of the formula (I) PAC-SA—SB—R* (I) wherein PAC-SA is a residue of a pharmaceutically active drug a metabolite thereof or a pharmaceutically acceptable salt thereof that is covalently bonded via the sulfur atom, SA of a reduced sulfhydryl, sulfinyl, sulfonyl or sulfonamide group to the sulfur atom SB of an oxidized sulfhydryl group of a pharmacologically acceptable sulfhydryl compound in the absence of an acid. Preferably the pharmaceutically active drug is a proton pump inhibitor and the sulfhydryl compound is N-acetyl cysteine. The disulfide compounds according to the invention can be prepared either in vitro or in vivo and are stable in the acidic conditions of the stomach. Pharmaceutical compositions containing compounds of the formula (I) and a method for the treatment or prophylaxis of gastrointestinal disorders using compounds of the formula (I) are also described.

Abstract: The present invention is directed to a process for the catalytic oxidation of the thioether 5-methoxy-2-((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)methylthio)-1H-benzimidazole to its sulfoxide: 5-methoxy-2-((4-methoxy-3,5-dimethyl-2-pyridinyl) methyl)methylsulfinyl)-1H-benzimidazole comprising: reacting the thioether with: 1) a transition metal catalyst; and, 2) an oxygen source; wherein the thioether is oxidized to a sulfoxide and wherein one of either the R and S enantiomers is formed to an enantiomeric excess.

Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The present invention relates to process for optical purification of esomeprazole or a salt thereof. Thus, esomeprazole sodium having 20 to 1% R-omeprazole by weight of the sum of the contents of esomeprazole and R-omeprazole is precipitated from a solvent selected from an alcohol or a mixture of alcohols and the precipitated solid is collected to obtain optically pure esomeprazole sodium.

Abstract: The present invention provides novel solvate of dexlansoprazole (or R-lansoprazole), particularly diol solvate and its hydrate form of dexlansoprazole (or R-lansoprazole) which is chemically known as (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole compound of the formula (I), as well as processes for the preparation thereof. The said solvates are useful in the preparation of dexlansoprazole with enhanced chiral purity and better HPLC purity with less sulphone impurity content.

Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: Methods of treating one or more growth deregulated cells are disclosed. An effective amount of a pharmaceutical composition including a proton pump inhibitor is administered thereby treating a growth deregulated cell outside of the gastric lumen of a subject.

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: A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract: A crystal of dexlansoprazole and sorbitol. The crystal is a co-crystal or a salt thereof of dexlansoprazole and sorbitol. There is also a method for making the co-crystal or salt thereof.

Abstract: Process for the preparation of crystalline anhydrous (R)-2-[[[3-methyl-4-(2,2,2-trifluoroetoxy)-2-piridyl]methyl]sulphinyl]benzimidazole (dexlansoprazole).

Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof.

Abstract: The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.

Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.

Abstract: The present invention relates to a process for the preparation of pure Rabeprazole sulfoxide using the solvent mixture for the extraction steps and this invention further relates to the process for the preparation of amorphous Rabeprazole sodium using pure rabeprazole base in presence of aqueous NaOH and water miscible solvent and adding an anti-solvent.