Abstract: The present invention provides a method of purifying diphtheria toxin comprising (1) fermenting a microorganism strain capable of producing diphtheria toxin using glucose as a carbon source, said method comprising adding glucose to a growing culture whereby the addition of glucose maintains microorganism growth effective to support diphtheria toxin production; and (2) purifying the diphtheria toxin from the culture by contacting a toxin containing preparation derived therefrom with an ion exchange matrix, eluting a fraction containing the toxin, applying the eluate to a hydrophobic matrix, and eluting a fraction containing the toxin.

Abstract: Methods are provided for purification of Factor VIII polypeptides by immunoaffinity chromatography and ion exchange chromatography, in which the eluate from the immunoaffinity column is diluted with a solution comprising higher salt concentration, or lower non-polar agent concentration than that of the elution solution, prior to passing the diluted solution through the ion exchange column. The methods result in improved purification without significant yield loss.

Abstract: The invention provides improved agents and methods for treatment of diseases associated with amyloid deposits of A&bgr; in the brain of a patient. Preferred agents include humanized antibodies.

Abstract: The present invention concerns fusion of Fc domains with biologically active peptides and a process for preparing pharmaceutical agents using biologically active peptides.

Abstract: Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.

Abstract: A monoazo reactive red dyestuff of the formula (I), 1

Abstract: Novel improved mixed crystals of monoazo dyes of formula (I), wherein R1 is methyl or chlorine, and R2, R3 and R4 are each independently of the others hydrogen, methyl or chlorine, which dyes have been laked with alkaline earth metal cations and ammonium cations in a molar ratio of about 1:2. The mixed crystals are single-phase. The products according to the invention, while having a fine particle size, exhibit substantially better fasteness properties than similar known products and are therefore excellently suitable as tinctorially strong pigments. In addition, the part played by after-treatment is less critical.

Abstract: An oligonucleotide, capable of specific cleavage and amplification of a pab gene which codes for pab, an antigenic protein of Mycobacterium tuberculosis, or an RNA derived therefrom, as well as being useful in high sensitive detection and identification thereof, is provided. Further, a combination of oligonucleotides, useful in specific amplification, high sensitive detection and identification of an RNA derived from Mycobacterium tuberculosis pab gene as well as a process for detecting Mycobacterium tuberculosis by using said combination, are provided.

Abstract: The present invention relates to SAD polypeptides, nucleic acids encoding such polypeptides, cells, tissues and animals containing such nucleic acids, antibodies to such polypeptides, assays utilizing such polypeptides, and methods relating to all of the foregoing. Methods for treatment, diagnosis, and screening are provided for SAD related diseases or conditions characterized by an abnormal interaction between a SAD polypeptide and a SAD binding partner.

Abstract: The present invention relates to a gene and the coded protein thereof that is involved in the development of sequelae of local ischaemia. The new protein is a serine threonine protein kinase and provides a new therapeutic approach to the prophylaxis and therapy of apoplexy.

Abstract: A novel process for making estra-4,9(10)-diene-3,17-dione steroids from readily available 19-nor-androst-4-ene-3-one steroids by a straightforward three-step process. Products of this process are important intermediates in the preparation of biologically active substances.

Abstract: The present invention relates to an improved process for the preparation of 3-propenyl cephalosporin DMF solvate, more particularly, the present invention relates to an improved process for the preparation of cefprozil DMF solvate of the formula (I), which is useful for the preparation of cefprozil of the formula (XIV).

Abstract: The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I), also, the invention provides a method for preparation of the thioester derivatives and reaction of the thioester derivatives with cephem carboxylic acids to produce cephalosporin antibiotic compounds having general formula (II).

Abstract: A description follows of ligands having general formula (I) wherein R1, R2, R3, R4, R5, and R6, the same or different, are selected form hydrogen, halogen, C1-C10 alkyl, C6-C15 aryl optionally halogenated, or adjacent pairs of Ri groups (with i ranging from 1 to 6) are bound to each other to give cyclic hydrocarbon structures condensed with the thiophene or pyridine ring: R7 is selected from H, C1-C10 alkyl, C6-C15 aryl: R8 is selected from C1-C10 alkyl and C6-C15 aryl. The complexes of the above ligands with transition metals are also described.

Abstract: The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems, including age related cognitive disorders such as senility and Alzheimer's disease, nerve injuries, peripheral neuropathies, and seizure disorders such as epilepsy.

Abstract: A process of preparing a compound of Formula I 1

Abstract: Compounds of the formula I, in which M, A1, A2, K1 and K2 have the meanings given in the description are novel effective tryptase inhibitors.

Abstract: Compounds of the formula I, wherein M, A1, A2, K1 and K2 have the meanings as indicated in the description are novel effective tryptase inhibitors.

Abstract: Crystalline monohydrate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: A process for preparing a compound of formula (II) 1

Abstract: A process for preparing compound (E) from compound (A), with or without isolation of intermediate products, characterised by one or more of the following steps:

Abstract: Carbazoles of formula (I) with R2=hydroxyfunctional amide (hydroxamic or esters) are disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: This invention relates to dihydro-furan-2-one derivatives, their intermediates and methods of manufacture.

Abstract: A compound of the formula (I):

Abstract: The present invention relates to an improved eco-friendly process for the preparation of vinylpyridine from corresponding picoline over modified zeolite catalyst in vapour phase which comprises reacting picoline with formaldehyde with a molar ratio of formaldehyde to picoline in the range of 1:1 to 4:1, at a temperature ranging between 200° C. to 450° C., at a weight hourly space velocity in the range of 0.25 hr−1-1.00 hr−1 over a modified commercial zeolite catalyst to obtain a high yield and selectivity of the desired product.

Abstract: The present invention relates to certain spirooxindole derivatives of the formula I, and pharmaceutically acceptable salts thereof, which exhibit good analgesic properties and are particularly effective in the treatment of chronic pain.

Abstract: Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: A process for preparing glycidylphtalimide or it optically active compound by reacting a phthalimide alkalimetal salt with an epihalohydrin or an optically active epihalohydrin in an alcohol solvent; or

Abstract: This invention relates to the reversible protection of hydroxy-silane functional groups by acid cleavable protecting groups. The development of reversible protecting groups greatly enhances the current utility of silanes while introducing further novel applications. For instance, reversibly protected silanes are of particular value in applications where room temperature cure and/or adhesion is of value, such as coatings, high resolution imaging, caulks, adhesives, sealents, gaskets, and silicones. Reversibly protected silanes can also be beneficially used in reticulating agents, and in sizing agents, tires, and release coatings. The incorporation of reversibly protected silanes into coating resins is of particular value. The reversibly protected silane can be incorporated into the coating resin by polymerizing a monomer containing the reversibly protected silane into the resin or by post-addition into the coating formulation.

Abstract: A process produces &egr;-caprolactone by the oxidation of cyclohexanone by feeding a crude reaction mixture to a first distillation column; distilling off a first distillate containing low boiling components including unreacted cyclohexanone from the top of the first distillation column; recovering a first side-cut fraction containing unreacted cyclohexanone in a higher concentration than in the first distillate from an intermediate tray; recovering a first bottom liquid containing high boiling components including &egr;-caprolactone from the bottom; introducing the first side-cut fraction to a second distillation column; recovering a second bottom liquid containing unreacted cyclohexanone from the bottom of the second distillation column; recycling the second bottom liquid into the raw material cyclohexanone; introducing the first bottom liquid to a third distillation column to thereby yield a third distillate containing &egr;-caprolactone from the third distillation column.

Abstract: The invention provides a process for producing glycolide by depolymerization by heating of a glycolic acid oligomer in the presence or absence of a solvent, which process ensures stable depolymerization. The depolymerization reaction is carried out while the content of alkaline metal ions in a glycolic acid oligomer-containing depolymerization reaction system is controlled to 0.001% by mass or lower; a sulfate or an organic acid salt, each in the form of di- or poly-valent cations, or a mixture thereof is allowed to be present as a stabilizer in the depolymerization reaction system; or the content of alkaline metal ions in the depolymerization reaction system is controlled to 0.001% by mass or lower, and a sulfate or an organic acid salt, each in the form of di- or poly-valent cations, or a mixture thereof is allowed to be present as a stabilizer in the depolymerization reaction system.

Abstract: Disclosed are novel processes for preparing 1,3-dioxolane nucleosides of general formula I and II: 1

Abstract: This invention relates to attachment chemistries for binding macromolecules to a substrate surface or to other conjugation targets. More particularly, this invention relates to attachment chemistries involving branched or linear structures having one or more hydrazide attachment moieties for binding the macromolecules to a substrate surface, or for other conjugation reactions. Novel modifying reagents are provided for the introduction of protected hydrazide attachment moieties or precursor forms of such hydrazides to the macromolecule, either as a single hydrazide or as multiple hydrazides.

Abstract: A process for obtaining substantially fat free products from whole stillage produced during ethanol production from agricultural products, such as cereal grains. More particularly, at least a portion of the fat is removed from both the thin stillage stream and the wet distillers grains that result from whole stillage.

Abstract: The present invention relates to a process for preparing an alkyl ester of a fatty acid wherein a transesterification reaction is carried out between a fat or oil and an alcohol in the presence of a catalyst comprising a composite metal oxide having a perovskite structure; and a process for preparing an alkyl ester of a fatty acid wherein a transesterification reaction is carried out between a fat or oil and an alcohol in the presence of a catalyst comprising at least one member selected from the group consisting of oxides, hydroxides and carbonates of alkaline earth metals is used as the catalyst, with the alcohol made into a supercritical state or subcritical state. According to the present invention, the alkyl ester of a fatty acid which can be effectively utilized as a diesel fuel oil or the like can be prepared at high efficiency and on an industrial scale mainly from triglyceride contained in a fat or oil, especially a waste oil.

Abstract: In one embodiment, this invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are androgen receptor antagonists which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents.

Abstract: By means of a new process for the resolution of racemic 3-aminopentanenitrile, enantiomerically enriched 3-aminopentanenitrile or its salts can be obtained. For this, racemic 3-aminopentanenitrile is reacted with an enantiomerically enriched organic acid and one of the two diastereomeric salts formed is separated off and then converted into the enantiomerically enriched 3-aminopentanenitrile or its salts.

Abstract: The invention concerns the use as catalyst for transforming carbamates of compounds corresponding to the general formula (I): —Sn (X) (X′) wherein: X′ is selected among chloride, bromide, iodide, thiocyanate radicals, sulphonate radicals, advantageously perfluorinated on the carbon bearing the sulphonate function; X is selected among the values of X′ and among radicals of formula Y-Z; Y is selected among the chalcogen groups, advantageously light (that is oxygen and sulphur); Z is selected in the group consisting of trisubstituted tin, monosubstituted zinc, and the oxygenated acid radicals after ignoring the OH function. The invention is applicable to the coating industry.

Abstract: This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-[4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl]-L-glutamic acid: wherein: X2 is a halo group, and is —F, —Cl, —Br, or —I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic esterification (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).

Abstract: The present invention relates to a process for producing aromatic dicarboxylic acids by the oxidation of dimethylbenzenes wherein the dimethylbenzenes are mixed with an oxygen containing gas, solvent and catalyst in a reactor, the improvement comprising agitating the reaction mixture with one or more asymmetric radial impellers in combination with at least one axial impeller.

Abstract: A copper oxide based catalyst for dehydrogenation of cyclohexanol, which is a copper oxide-zinc oxide based catalyst or a copper oxide-silicon oxide based catalyst further comprising one of palladium, platinum and ruthenium in a very small amount; and a method for preparing the copper oxide based catalyst which comprises combining the co-precipitation method or the kneading method and the spray method. The copper oxide based catalyst for dehydrogenation of cyclohexanol exhibits high activity and high selectivity, and thus may be used for producing cyclohexanone at a reduced reaction temperature and/or with an enhanced yield, as compared to a conventional catalyst.

Abstract: A process for preparing 1,3-di-halo-substituted benzene derivatives (II) from 2,6-di-halo-substituted benzaldehydes (I) (where X1, X2 are each independently F, Cl, Br, and R1, R2, R3 are each independently H, halogen, OH, C1-C12-alkyl, CF3, CHO, C6-C14-aryl, Oalkyl, Oaryl, NO2) by reacting with an alkaline medium, which comprises initially charging the alkaline medium and metering in the 2,6-di-halo-substituted benzaldehyde (I) or initially charging the 2,6-di-halo-substituted benzaldehyde (I) and metering in the alkaline medium.

Abstract: A method for the preparation of sevoflurane which comprises (a) providing a liquid mixture of (CF3)2CHOCH2Cl, hydrogen fluoride, and an amine and (b) reacting the mixture, to form (CF3)2CHOCH2F.

Abstract: The present invention is an improvement upon the process for the production of 1,3-propanediol (PDO) wherein an aqueous solution of 3-hydroxypropanal (HPA) is formed, and the HPA is subjected to hydrogenation to produce a crude PDO mixture comprising PDO, water, MW176 acetal, and high and low volatility materials, wherein the crude PDO mixture is dried to produce a first overhead stream comprising water and some high volatility materials and a dried crude PDO mixture as a first distillate bottoms stream comprising PDO, MW176 acetal, and low volatility materials, and wherein the dried crude PDO mixture is distilled to produce a second overhead stream comprising some high volatility materials, a middle stream comprising PDO and MW176 acetal, and a second distillate bottoms stream comprising PDO and low volatility materials.

Abstract: A process for producing 1,3-propanediol comprising the steps of: a) forming an aqueous solution of 3-hydroxypropanal, b) hydrogenating the 3-hydroxypropanal to form a first crude 1,3-propanediol mixture comprising 1,3-propanediol, water, and MW 132 cyclic acetal, c) distilling the first crude 1,3-propanediol mixture to remove water and low boiling impurities and form a second crude 1,3-propanediol mixture, d) contacting the second crude 1,3-propanediol mixture with a solid acid purifier at a temperature of from about 50 to about 250° C. to convert the MW 132 cyclic acetal to more volatile cyclic acetals, and e) separating the more volatile cyclic acetals from the 1,3-propanediol by distillation or gas stripping.

Abstract: The invention provides a catalytic, chemospecific and stereospecific method of oxidizing a wide variety of substrates without unwanted side reactions. Essentially, the method of the instant invention, under relatively mild reaction conditions, catalytically, stereospecifically and chemospecifically inserts oxygen into a hydrocarbon C—H bond. Oxidation (oxygen insertion) at a tertiary C—H bond to form an alcohol (and in some cases a hemiacetal) at the tertiary carbon is favored. The stereochemistry of an oxidized tertiary carbon is preserved. Ketones are formed by oxidizing a secondary C—H bond and ring-cleaved diones are formed by oxidizing cis tertiary CH bonds.

Abstract: A process for recovering cumene, characterized by subjecting 2,3-dimethyl-2,3-diphenylbutane produced in a process in which cumene is used, to hydrogenolysis in the presence of a catalyst thereby to convert it into cumene, and recovering the cumene.

Abstract: There is provided a process for aromatics conversion by contacting a feed suitable for aromatics conversion under conversion condition and in the presence of a catalyst comprising ITQ-13. Examples of such conversion processes include isomerization of aromatic (xylenes) feedstock, disproportionation of toluene to benzene and xylenes, alkylation and transalkylation of aromatics, conversion of light paraffins and light olefins to aromatics, conversion of naphtha to aromatics, and conversion of alcohol to aromatics.

Abstract: A process for isomerizing xylenes in a feed containing xylenes is disclosed which process comprises: contacting the feed with a first isomerization catalyst in a first reactor under a first set of conditions effective to isomerize xylenes in the feed; and contacting the xylenes with a second isomerization catalyst in a second reactor under a second set of conditions effective to isomerize xylenes in the feed. The second reactor is typically a clay treater and contains a further catalyst effective under the second set of conditions to remove olefins in the feed. Any ethylbenzene in the feed is removed, either by dealkylation or isomerization, in the first reactor or in a third reactor upstream of the first and second reactors.

Abstract: The present invention is directed to a process for upgrading Fischer-Tropsch products comprising oxygenates, C6+ olefins, and optionally heteroatom impurities such as nitrogen compounds, by contacting the product stream with acidic olefin cracking catalyst. This acidic olefin cracking catalyst converts the oxygenates and C6+ olefins in the Fischer-Tropsch product to form valuable light olefins such as propylene, butenes, and some pentenes, while leaving paraffins in the Fischer-Tropsch product largely unreacted. The light olefins formed can easily be separated and used for a variety of purposes.