Abstract: The antihypertensive agent of the present invention contains a soluble silicon compound. The soluble silicon compound is preferably metasilicic acid or a salt thereof. In one embodiment, the antihypertensive agent of the present invention contains deep sea water containing the soluble silicon compound, or a dried product of such deep sea water. It is preferred that in such embodiment, the antihypertensive agent further contains metasilicic acid or a salt thereof. The amount of silicon present in the deep sea water in the form of silicic acid (SiO2—Si) is 25 ?M or more. The deep sea water is typically collected at a depth of 300 m or deeper, and preferably at a depth of 600 m or deeper.

Abstract: New 1,2,3- or 1,2,3,4- or 1,2,3,4,5- substituted imidazolium salts and their uses as solvent in catalyzed organic reactions, as well as compositions containing them and a transition metal compound. They can be used in the following reactions: the telomerisation of conjugated dienes, dimerisation of olefins, the oligomerisation of olefins, polymerization of olefins, alkylation of olefins, hydrogenation of olefins, olefin metathesis, hydroformylation of olefins, ring-closing metathesis of olefins, ring-opening metathesis polymerisation of olefins, symetric or asymetric epoxidation of olefins (including heteroatom substituted olefins) and the cyclopropanation of olefins, condensation reaction, hydrogenation reaction, isomerization reaction, Suzuki cross-coupling reactions, amination reaction, partial oxidation of alkancs, kinetic resolution of racemic mixtures, hydrogenation of imines, hydrogenation of ketones, transfer hydrogenation and hydroxylation of aromatic organic compounds.

Abstract: Disclosed is a commercially suitable method for producing a 1-substituted-5-acylimidazole compound. A 1-substituted-5-acylimidazole compound is produced with a high position selectivity by reacting an N-substituted amidine compound or a salt thereof with a ketone compound in the presence of a base.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Abstract: The reaction of N-alkylimidazol with alkyl sulfonates, at room temperature, favors the production of 1,3-dialkylimidazolium alkane-sulfonates as crystalline solids at high yields. The alkane-sulfonate anions may be easily substituted by a series of other anions [BF4, PF6, PF3(CF2CF3)3, CF3SO3 and (CF3SO2)2N] through simple anion, salt, or acid reactions in water at room temperature. The extraction with dichloromethane, filtration, and evaporation of the solvent, allows the production of the desired ionic liquids at a yield of 80-95%. The purity of these ionic liquids (in some cases >99.4%) is performed using the intensity of 13C satellite signals from the magnetic resonance spectrums of the N-methyl imidazolium group as an internal standard.

Abstract: Methods of preparing imidazole-based compounds are disclosed.

Abstract: The present invention relates to compounds of formula wherein R1, R2, X, Y and Ar are as defined herein and to their pharmaceutically active salts, with the exclusion of the racemic compound 4-benzyl-4,5-dihydro-1H-imidazole or its tautomer (CAS 131548-83-9).

Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Provided are: a process for production of a benzyloxypyrrolidine derivative in high yield and safety, and a process for production of a hydrochloride powder of a benzyloxypyrrolidine derivative in high yield and safety; the process for production of a benzyloxypyrrolidine derivative expressed by the general formula (2) [Chemical formula 2], in reacting a pyrrolidinol derivative represented by the general formula (1) [Chemical formula 1] with a benzyl halide derivative in the presence of an alkali metal hydroxide, wherein the reaction is carried out in either of the following conditions A or B; condition A: an aprotic polar solvent, and condition B: an aliphatic ether solvent containing a phase transfer catalyst:

Abstract: This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.

Abstract: The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same.

Abstract: Alpha crystalline form of strontium ranelate of formula (I): characterised by its powder X-ray diffraction diagram and by a water content of from 22 to 24%. Medicinal products containing the same which are useful in the treatment of osteoporosis and arthrosis.

Abstract: An adjuvant suitable for use with a lipophilic agrochemical has the formula (I), R1—(CO)m—O—[—R2O—]n—R3, wherein R1 is a C16 to C20 straight or branched chain alkyl or alkenyl group, R2 is ethyl or isopropyl, n is from 8 to 30 and m is 0 or 1 and when R2 is ethyl, R3 is a C1 to C7 alkyl group and when R2 is isopropyl, R3 is hydrogen or a C1 to C7 alkyl group, provided that when R1 is oleyl, R2 is isopropyl and R3 is hydrogen, n is not 10. An adjuvant composition comprising an agrochemical and an adjuvant of formula (I) is also claimed. Adjuvants of the invention show effective bioperformance enhancement despite having little or no surfactant properties.

Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X and n are defined herein.

Abstract: This invention provides metal complexes being useful as catalyst components in metathesis reactions and in reactions involving the transfer of an atom or group to an ethylenically or acetylenically unsaturated compound or another reactive substrate and, with respect to a sub-class thereof, for the polymerisation of ?-olefins and optionally conjugated dienes, with high activity at moderate tempera-tures. It also provides methods for obtaining polymers with very narrow molecular weight distribution by means of a living reaction. It also provides methods for making said metal complexes and novel intermediates involved in such methods. It further provides derivatives of said metal complexes which are suitable for covalent bonding to a carrier, the product of such covalent bonding being useful as a supported catalyst for heterogeneous catalytic reactions. It also provides a direct one-step synthesis of pyrrole, furan and thiophene compounds from diallyl compounds.

Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.

Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis, Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

Abstract: The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.

Abstract: This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homo-substitution.