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: Compounds represented by formula (Ia) are disclosed by the invention, along with compositions and complexes thereof, optionally in combination with compounds of formula (Ib). Pharmaceutical formulations and methods of making and using such compounds are also disclosed.

Abstract: The present invention provides processes for purifying 6-methoxy omeprazole, products using such processes, pharmaceutical formulations using such products, and methods of using such products for gastric acid inhibition.

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: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract: Improved processes for preparing substituted 2-(2-pyridylmethyl)sulfinyl-1H-benzimidazoles are disclosed.

Abstract: The method for obtaining derivatives of [[(pyridil substituted)methyl]thio]benzomidazol (I), where each of R1, R3 and R4, independently of each other, is hydrogen, an alkyl, alkoxy or fluorinated alkoxy of 1 to 6 carbon atoms, and R2 is nitro, halogen, alkoxy or halogenated alkoxy of 1 to 6 carbon atoms, or a group —OR—(CH2)n—OR8, where n is an integer between 1 and 6 and R8 represents hydrogen or an alkyl group with 1 to 6 carbon atoms, which involves (a) reacting an N-oxide of a methylpyridine with an anhydride of activated carboxylic acid or of sulfonic acid, and (b) reacting the intermediate formed in stage (a) with a corresponding mercaptobenzomidazol. The compounds (I) are useful in the synthesis of derivatives of [[(pyridil substituted)methyl]sulfinyl]benzomidazol, such as omeprazol, lansoprazol, rabeprazol or pantoprazol.

Abstract: The present invention relates to a novel form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, known under the generic name omeprazole. More specifically, it relates to a novel crystalline form of the potassium salt of the (S)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole. The present invention also relates to processes for preparing such a form of the potassium salt of (S)-omeprazole and pharmaceutical compositions containing it.

Abstract: The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.

Abstract: Nitrate salt compositions with anti-ulcer medicines having formula (A) and (B) wherein the (A) class compounds: R=H, OCH3, OCHF2; R1=CH3, OCH3; R2=H, CH3; R3=CH3, CH2—CF3, (CH2)3—OCH3; wherein the (B) class compounds: RI3, RI4 equal to or different from each other, are respectively free valence hydrogen, (1), —CH2—N(CH3)2; Y=S, N—RI6, CRI7RI8; X=O, S, N—RI1; RI2=H, CH3; n=0, 1; Z=N—CN, N—SO2NH2, CH—NO2 or formula (VIIA) RI5=H, —NH—CH3, NH2; RI6, RI7, RI8, RI1, equal to or different from each other, are hydrogen, free valence. The invention also comprises the methods for the preparation of above salts.

Abstract: The present invention relates to a novel process for the preparation of the magnesium salt of the (−)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole trihydrate, ie. S-omeprazole magnesium salt trihydrate. The present invention also relates to the S-omeprazole magnesium salt trihydrate prepared in accordance with the new process and pharmaceutical compositions containing it. Furthermore, the present invention also relates to new intermediates used in the process.

Abstract: There is provided a solid pharmaceutical composition in a dosage form that is not enteric-coated, having active ingredients including a non-enteric coated proton pump inhibitor and at least one buffering agent. The proton pump inhibitor is omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, derivative, free base, or salt thereof, in an amount of approximately 5 mg to approximately 300 mg; and the buffering agent is in an amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor. The dosage form includes a suspension tablet, a chewable tablet, an effervescent powder, or an effervescent tablet. Also provided is a method for treating an acid-related gastrointestinal disorder in a subject in need thereof by administering to the subject a solid pharmaceutical composition.

Abstract: The present invention provides processes for purifying 6-methoxy omeprazole, products using such processes, pharmaceutical formulations using such products, and methods of using such products for gastric acid inhibition.

Abstract: The present invention relates to a novel crystalline form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, known under the generic name omeprazole. Further, the present invention also relates to the use of the novel crystalline form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole for the treatment of gastrointestinal disorders, pharmaceutical compositions containing it as well as processes for the preparation of the novel crystalline form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole.

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 present invention relates to novel compounds of Formula I, and pharmaceutically acceptable salts thereof, as antibacterial agents. The compounds of the present invention are nitric oxide releasing derivatives of proton pump inhibitors (NO-releasing PPIs). In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above. The invention also relates to new intermediates for use in the preparation of the novel compounds. Additionally the present invention relates to co-administration of NO-releasing PPIs with other known medicaments.

Abstract: Compounds represented by formula (Ia) are disclosed by the invention, along with compositions and complexes thereof, optionally in combination with compounds of formula (Ib). Pharmaceutical formulations and methods of making and using such compounds are also disclosed.

Abstract: Lansoprazole of formula (I) can be produced economically in a high yield using a simple, two-step method comprising reacting hydroxymethylpyridine and benzimidazole starting materials in the presence of a phosphine compound and a dialkyl azodicaboxlate and oxidizing the product of the first step in the presence of an organic radical catalyst:

Abstract: The invention relates to the dihydrate of the magnesium salt of pantoprazole.

Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.

Abstract: Process for the manufacturing of slightly soluble or less soluble alkaline salts of substituted sulphinyl heterocycles containing an imidazole moiety with formula I preferably alkaline salts of a proton pump inhibitor compound, wherein the process comprises the step of reacting the substituted sulphinyl heterocycle of Formula I with a source of the cation in the presence of a base, characterized by a washing step in which the prepared alkaline salt of the substituted sulphinyl compound is washed with a basic aqueous solvent mixture. The obtained bulk drug substance resulting in a bulk product that in an aqueous suspension of the substituted sulphinyl heterocycle having a pH not significantly lower than that of a saturated water solution of the pure compound prepared. Alternatively, the process for manufacturing a pharmaceutical dosage form comprising the active substance could be adjusted.

Abstract: The present invention relates to a novel crystalline form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl-1H-benzimidazole, known under the generic name omeprazole. Further, the present invention also relates to the use of the novel crystalline form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole for the treatment of gastrointestinal disorders, pharmaceutical compositions containing it as well as processes for the preparation of the novel crystalline form of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole.

Abstract: The present invention relates to a novel form of the (−)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, i.e. S-omeprazole. More specifically, it relates to a novel form of the magnesium salt of the S-enantiomer of omeprazole trihydrate. The present invention also relates to processes for preparing such a form of the magnesium salt of S-omeprazole and pharmaceutical compositions containing it. Furthermore, the present invention also relates to new intermediates used in the process.

Abstract: 2-Sulfonylpyridine derivatives can be industrially produced efficiently by reacting a sulfonyl cyanide derivative with an &agr;,&bgr;-unsaturated carbonyl compound and a 2-{[(2-pyridyl)methyl]thio}-1H-benzimidazole skeleton can be formed in one step in a good yield by reacting this type of the 2-sulfonylpyridine derivative with a 2-methylthio-1H-benzimidazole derivative in the presence of an organolithium compound.

Abstract: Disclosed are novel compounds of formula (I): 1

Abstract: An improved process of synthesis of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl-1H-benzimidazole (omeprazole) by oxidation of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole with 3-chloroperoxybenzoic acid in ethyl acetate wherein omeprazole is poorly soluble, at a temperature between −10° C. and 5° C. is disclosed. The second step is a purification of the crude product by dissolution and reprecipitation of the final product.

Abstract: In view of the situation of the prior art, the present invention specifies the structure of a late-stage product of Mailard reaction in vivo having a close relation with various tissue disorders, and provides a diagnostic reagent for complications associated with diabetes or renal failure, containing the above compound as a main component.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: The present invention relates to a novel process for the synthesis of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, known under the generic name omeprazole. Moreover, the present invention also relates to manufacture of a pharmaceutical preparation thereof and its use in medicine. The novel process for the preparation of omeprazole, comprises the step of oxidizing 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]thio]-1H-benzimidazole in an organic solvent with an oxidizing agent in the presence of a titanium complex and optionally in the presence of a base.

Abstract: Methods and compositions are disclosed utilizing optically pure (−) lansoprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of lansoprazole. The optically pure (−) isomer is also useful for the treatment of gastroesophageal reflux. (−) Lansoprazole is an inhibitor of H+ release and is therefore useful in the treatment of other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.

Abstract: Novel compounds of the formula 1

Abstract: An improved process of synthesis of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl-1H-benzimidazole (omeprazole) by oxidation of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole with 3-chloroperoxy-benzoic acid in ethyl acetate wherein omeprazole is poorly soluble, at a temperature between −10° C. and 5° C. is disclosed. The second step is a purification of the crude product by dissolution and reprecipitation of the final product.

Abstract: The present invention relates to pyridone derivatives and herbicidal compositions containing the pyridone derivatives as active ingredients.

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective &bgr;3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.

Abstract: A pharmaceutical formulation comprising a benzimidazole derivative as active ingredient, and as excipients, at least one cyclodextrin and at least one amino acid.

Abstract: The present invention relates to an efficient process for the preparation of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylthio]-1-H-benzimidazole hydrochloride starting from 3,5-Lutidine and its conversion to Omeprazole (5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylsulfinyl]-1H-benzimidazole) by selective oxidation with hydrogen peroxide.

Abstract: 2-Sulfonylpyridine derivatives can be industrially produced efficiently by reacting a sulfonyl cyanide derivative with an &agr;, &bgr;-unsaturated carbonyl compound and a 2-{[(2-pyridyl)methyl]thio}-1H-benzimidazole skeleton can be formed in one step in a good yield by reacting this type of the 2-sulfonylpyridine derivative with a 2-methylthio-1H-benzimidazole derivative in the presence of an organolithium compound.

Abstract: The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in a chlorinated aliphatic hydrocarbon or aromatic hydrocarbon solvent, such as methylene chloride or toluene; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate or formic acid solution and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Omeprazole and compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent and diminished levels of alcoholic solvent are also described.

Abstract: The present invention provides acetone complexes of sulfoxide compounds, useful as medicines such as inhibitors of gastric acid secretion and anti-ulcer agents or as intermediates for production of medicines, a process for producing the same and a purification method of using the same. Namely, it is the acetone complexes of sulfoxide compounds or of pharmaceutically acceptable salts thereof represented by the following formula: (wherein R1 represents a hydrogen atom, a methoxy group or a difluoromethoxy group, R2 represents a methyl group or a methoxy group, R3 represents a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group, R4 represents a hydrogen atom or a methyl group, n and m independently represent an integer of 1 to 4, and B represents a hydrogen atom, an alkali metal atom or ½ alkaline earth metal atom), which are obtained by treating the sulfoxide compounds or pharmaceutically acceptable salts thereof with acetone.