Abstract: This invention is directed to alkyl cobalt (III) dioximates and methods for making these dioximates.

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: Disclosed are novel pyrrole derivatives, a process for their manufacture, pharmaceutical compositions containing such compounds and the use of such compounds in the treatment of HIV mediated diseases.

Abstract: In the present invention relates to a novel series of antimalarial 1,2,4-trioxanes analogues of general formula 7, wherein R represents cycloalkyl groups selected from the groups consisting of cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl or aryl groups selected from phenyl, 4-bromophenyl and 4-chlorophenyl, R1 and R2 represent hydrogen, alkyl group selected from methyl, ethyl, propyl and decyl, aryl selected from phenyl or parts of a cyclic systems such as cyclopentane, cyclohexane, substituted cyclohexane, cycloheptane bicyclo(2.2.1)heptane, adamantane and its preparation thereof; several of these novel compounds show promising antimalarial activity against multidrug resistant malaria in mice.

Abstract: The invention provides a pharmaceutical composition for the treatment of dementia or Alzheimer's disease in which the active therapeutical agent is donepezil hydrochloride in an amorphous state.

Abstract: The present invention relates to a &bgr;3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof, which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type II diabetes and/or obesity. The compound can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compound can be used to reduced neurogenic inflammation or as an antidepressant agent. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.

Abstract: Process for preparing 1,10-phenanthroline ligands represented by the formula which comprises coupling a 1,10-phenanthroline of the formula with a ketone e.g. a dialkyl, cycloalkyl or bicycloalkyl ketone with a metal coupling reagent, preferably a lanthanide II e.g. samarium II, wherein R is hydrogen, alkyl, cycloalkyl, bicycloalkyl or aryl e.g. phenyl. The hydroxy group of the product may be converted to derivatives e.g. esters and ethers to form additional ligands. The hydroxy group of the product also may be converted to a reducible group e.g. the methoxy ether and the ether replaced by hydrogen in the reduction. The reduction product wherein R of the starting material is hydrogen can be coupled with a ketone in the process to provide 2,9-disubstituted 1,10-phenanthroline ligands. The ligands provided are preferably in chiral form and complex with metals, e.g. transition metals, which serve as catalysts in many processes such as addition and substitution reactions.

Abstract: The invention is polymerizable composition comprising a) an organoborane/amine complex wherein the organoborane is a trialkyl borane or an alkyl cycloalkyl borane and the amine is selected from the group of amines having an amidine structural component; aliphatic heterocycles having at least one nitrogen in the heterocyclic ring; an alicyclic compound having bound to the ring a substituent having an amine moiety; primary amines which in addition to a primary amine have one or more hydrogen bond accepting groups of an ether, polyether, thioether or halogen wherein there is an alkylene chain of at least two carbon atoms between the primary amine and the hydrogen bond accepting group, and conjugated imines; and, b) one or more of monomers, oligomers or polymers having olefinic unsaturation; and optionally c) an effective amount of a compound which causes the complex to disassociate wherein the compound which causes disassociation of the complex is kept separate from the complex until initiation of polymerizat

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHCH2—Ar—, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or C1-4alkoxy groups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di[C1-4alkyl]amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzy

Abstract: The present invention refers to a process for the preparation of (1H)-benzo[c]quinolizin-3-ones derivatives of general formula (I) which involves only three steps and the use, as starting products, of commercially available, or easily preparable, compounds. The compounds of formula (I) are useful as inhibitors of 5&agr;-reductases.

Abstract: To provide low odor polyoxyalkylene polyol, a process for producing the same, and a low odor urethane prepolymer and a low odor urethane composition using the same as a raw material. The low odor polyoxyalkylene polyol comprising polyoxyalkylene polyol with amine added thereto, the amine having at least one amino group represented by the following formula (1): is provided, wherein R1, R2 and R3 independently represent hydrogen atom or an organic group which may contain a hetero atom in which an atom bonded to nitrogen atom is carbon atom.

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: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: Acid fluorides, for example carboxylic acid fluorides and sulfuryl fluoride are produced by reacting the corresponding acid chlorides with hydrogen fluoride adducts of ammonium fluoride or amine hydrofluorides (which act as a catalyst or as a fluorination agent). Consumed HF adducts may be regenerated with HF.

Abstract: The present invention provides: a process in which, when a hydroxyalkyl ester is produced by carrying out a reaction between a carboxylic acid and an alkylene oxide in the presence of a catalyst, the contamination of the hydroxyalkyl ester with water can be inhibited to the maximum limit without washing the inside of a production apparatus together with the raw carboxylic acid or the hydroxyalkyl ester as an aimed product, or without carrying out azeotropic distillation with water and an azeotropic solvent. The process comprises a washing step and thereafter a drying step in the interval of from the stop of a production of the hydroxyalkyl ester till the restart of this production, wherein the washing step is a step of washing the inside of a production apparatus with water and/or an aqueous basic solution, and wherein the drying step is a step of drying under reduced pressure and/or hot-air-drying the inside of the production apparatus.

Abstract: An apparatus and method is disclosed for producing alcohols, particularly methanol, according to an alcohol synthesis process. The apparatus comprises a catalytic distillation reactor where reactants are fed into the catalytic distillation reactor to undergo catalytic reaction to form methanol. Methanol production beyond the thermodynamic limit is achieved in the apparatus through use of multiple distillation stages, preferably at least three.

Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2 , which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.

Abstract: Disclosed are compounds of the formula: wherein: A, B, C, E, F, and G are substituents as defined herein, which compounds bind to the benzodiazepine site of GABAA receptors and are therefore useful in treatment of central nervous system (CNS) diseases.

Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.