Abstract: Compounds of the general formula and to the use thereof for controlling microorganisms are provided.

Abstract: A clayish subterranean formation, such as may be encountered in rock surrounding a well bore during hydrocarbon recovery operations may be stabilized with relatively high molecular weight acid ammonium salts of an imide of polymaleic anhydride. The salts may be unneutralized or partially neutralized. The invention is particularly relevant to hydraulic fracturing fluids used in enhanced oil recovery. The compositions herein are made in the presence of a reactive solvent, such as a polyalkylene glycol, e.g. polyethylene glycol. The compositions of this invention are more environmentally friendly than some current technology.

Abstract: A process for preparing optically active amines, a process for preparing racemic amines which can be resolved using optically active carboxylic acids or enzymes, and racemic and optically active amines and optically active amides are described.

Abstract: ?-Ketol unsaturated fatty acid derivatives represented by the following formula (1), ?-ketol unsaturated fatty acid amide derivatives represented by the following formula (6), and plant growth regulators containing, as the active ingredient, at least one of these derivatives: wherein R1 represents linear C1-5 alkyl; R represents hydrogen, etc.; R3 represents hydrogen, etc.; R4 represents hydrogen, etc.; R5 represents hydrogen, etc.; n is an integer from 3 to 15; and the carbon atoms at the A- and B-positions may be in either (R)- or (S)-configuration; and wherein R7 represents C1-17 alkyl, etc; R8 represents hydrogen, etc.; R9 represents ?-ketolalkylene; and R10 represents specific divalent linear hydrocarbyl.

Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.

Abstract: This present invention provides materials for use as solid or concentrated chemical precursors for the production of organic peroxy acids (peracids). Organic peroxy acids are formed using a precursor according to the invention when they are combined with hydrogen peroxide or a hydrogen peroxide precursor such as a percarbonate or a perborate in aqueous medium. Organic peroxy acids, such as peroxyacetic acid, are used currently to disinfect medical equipment such as endoscopes and related items.

Abstract: Novel retro-anandamides are presented which have high affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy, as well as suppression of the immune system, enhancement of appetite and in treatment of certain mental disorders.

Abstract: The invention is concerned with novel hexafluoroisopropanol substituted cyclohexane derivatives of formula (I) wherein R1 to R4, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.

Abstract: The present invention provides novel heterobifunctional and monobifunctional polyethylene glycol derivatives for the pegylation of therapeutically active proteins. The heterobifunctional PEGs which bear two different functional groups as well as the monobifunctional PEGs which contain two similar functional groups, may be used for cross-linking purposes. The cross-linking may be intramolecular between two areas within the same molecule or intermolecular between two separate molecules. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which the conjugate is derived. New syntheses for preparing such bifunctional derivatives are described.

Abstract: The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: Ion-detecting sensors for detecting a target ion in a sample are provided. The sensor comprises a plasticizer-free copolymer comprised of polymerized units of methacrylate monomers having pendent alkyl groups of different length and a functionalized ionophore of said ion, wherein at least a portion of the functionalized ionophore is grafted into the copolymer through covalent linkages. Sensors may comprise ionophores such as hydrophilic crown ethers or functionalized derivative of 3-oxapentandiaminde-type ionophores. This invention further provides sensors for detecting target ions in a sample, comprising plasticizer-free molecularly imprinted polymers, wherein the polymers comprise polymerized units of methacrylate monomers having pendent alkyl groups of different length and a functionalized ionophore of said ion. In particular, a magnesium ion sensor comprising a functionalized derivative of a 3-oxapentandiaminde-type calcium ion-selective ionophore is provided.

Abstract: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.

Abstract: Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.

Abstract: The invention relates to compounds of formula (I): wherein: B represents a hydrogen atom, a COOR group, a CONRR? group, or a (C1–C6)alkyl group substituted by a COOR, CONRR? or OR group, G1 represents a —X?—(CH2)n—X—(CH2)m—X?— chain wherein X, X?, X?, n and m are as defined in the description, Cy represents a grouping of formula (II) or (III): G2 represents an alkylene chain as defined in the description, and A represents a NRCOR?, NRCSR?, CONRR?, CSNRR?, NRCONR?R? or NRCSNR?R? group.

Abstract: A refined product of a polyoxypropylene fatty acid isopropanolamide surfactant, having a high stability in storage and a very small change in smell thereof, is obtained by heat-treating an addition-reaction mixture prepared from a compound of the formula (III) and propylene oxide in a molar amount of 0.5 to 10 times that of the compound of the formula (III), and containing the target compound of the formula (I) and an oxazoline compound of the formula (II) produced as a by-product with water or an alkaline aqueous solution at 50 to 100° C., to hydrolyze the oxyazoline compound and to control the content of the oxyazoline compound to 0.1% by mass or less; and a detergent composition containing the refined product in a content of 1 to 50% by mass, exhibits enhanced thickening, foaming, emulsifying, dispersing and dissolving properties. [R1?C1–C19alkyl or alkenyl group, X=oxypropylene group, n=average number of addition-reacted X groups of 0.

Abstract: The present invention provides novel monofunctional polyethylene glycol aldehydes for the pegylation of therapeutically active proteins. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which the conjugate is derived. New syntheses for preparing such aldehydes are described.

Abstract: Prodrug compounds capable of permeating a desired biological compartment and releasing a biologically active molecule in active form to effect a therapeutic functional change in the compartment to which it is introduced.

Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.

Abstract: This disclosure describes unique chemical structures for use as solid or concentrated chemical precursors to the production of peroxy acids when combined with hydrogen peroxide or a hydrogen peroxide precursor such as percarbonates or perborates. Peroxy acids (peracids) such as peroxyacetic acid are used currently to disinfect medical equipment such as endoscopes and related items. It has been discovered that these structures are not currently listed in Chemical Abstracts and do not appear to be the subject of any prior art related to this or any other similar application. The specification for this claim includes chemical structures for each claimed precursor as well as means of synthesis that could be carried our by any skilled synthetic organic chemist. Practical uses for this invention include several antimicrobial applications of which at least one example is included.

Abstract: Alkylpolypropyleneoxide amidotriamines having antimicrobial activity are described. The compounds are useful as antimicrobial preservatives in various types of pharmaceutical compositions. Ophthalmic compositions containing these compounds as disinfecting agents or preservatives are also described.

Abstract: A thickener which is superior in handling characteristics and blending stability and has a high thickening action is provided, comprising a fatty acid alkanolamide represented by the general formula (1) and a surfactant composition comprising the thickener and at least one surfactant: wherein R1 represents a straight-chain or branched alkyl or alkenyl group having 5 to 21 carbon atoms which may be substituted with at least one hydroxy group, R2 and R3 independently represent an alkyl group having 1 to 2 carbon atoms, AO represents an oxyalkylene group having 2 to 4 carbon atoms and n denotes a number of 0 to 10 in average.

Abstract: A method for repeatedly converting a solvent from a state of solvent to a state of antisolvent with relatively little loss of solvent. The method is used to allow for processing of large amounts of solute material with minimum amounts of solvent.

Abstract: Fluorinated compounds and emulsions including the compounds. The compositions are useful as oxygen carriers and surfactants. In one embodiment, the fluorinated compound is pH sensitive. In one embodiment, the fluorinated compound is a vitamin E derivative. In one embodiment, the fluorinated compound is a vitamin K derivative.

Abstract: A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a &bgr;-galactosidase inhibitor or a glycolipid metabolic disorder treating agent.

Abstract: Universal supports for oligonucleotide synthesis include a support material represented by the following formula: In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl, or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.

Abstract: A sprayable analgesic composition containing an analgesic which is absorbed into the bloodstream through the buccal mucosa and a pharmacologically acceptable liquid carrier.

Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.

Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus.

Abstract: Acylated &agr;-hydroxyarylbutanamines and related sulfonamides, ureas and carbamates that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds.

Abstract: The invention provides processes for preparing N-protected &bgr;-amino aldehyde compounds which are useful as synthetic intermediates for preparing glycopeptide antibiotic derivatives. The processes include cleaving a carbon-carbon double bond to form the N-protected &bgr;-amino aldehyde compound.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)

Abstract: The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.

Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, which compounds have utility in treating clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Process for the preparation of a Schiff base of an &agr;-alkyl-&agr;-amino acid amide and an aldehyde, wherein the corresponding &agr;-aminonitrile is contacted with a base and the aldehyde and wherein it is ensured that the reagents are in good contact. The Schiff base obtained may be further hydrolysed to form the &agr;-alkyl-&agr;-amino acid amide and the aldehyde. Preferably a substituted or unsubstituted benzaldehyde is used as the aldehyde. The reaction is preferably carried out in a practically homogeneously mixed phase obtained by using a solvent, for example methanol or ethanol. Preferably NaOH or KOH is used as the base.

Abstract: Methods for producing amide derivatives of the formula [XV] are described. These derivatives are useful as HIV protease inhibitors. wherein R4 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl or an optionally substituted heteroarylalkyl, R6 and R7 are the same or different and each is a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl or an optionally substituted aralkyl, or R6 and R7 combinedly form, together with the adjacent nitrogen atom, a hetero ring, said hetero ring being optionally substituted by halogen atom, alkyl, alkenyl, alkoxy, amino, alkoxycarbonyl, carboxamide or alkyl-substituted carbamoyl, and R8 is a hydrogen atom, an alkyl, an optionally substituted aryl or an optionally substituted aralkyl, or an enantiomer thereof.

Abstract: The present invention relates to blocked polyisocyanate cross-linking agents and their use in one-component stoving lacquers, in particular in solvent-containing or predominantly water-based plastics coatings having a soft-feel effect.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)

Abstract: A process for preparing an &agr;-haloketone of the formula (1) 1

Abstract: The present invention relates to compounds and pharmaceutical compositions useful for treating pain. The invention also relates to methods of treating or alleviating pain in mammals, comprising administering to a mammal suffering from pain, a pain-alleviating amount of a compound of the general formula (I) or (II).

Abstract: The present invention reveals a novel structure of guaiacoxypropanolamines shown in formula I: The composition comprising formula I acts as active intergant and pharmaceutical acceptable vehicle. The composition by perfect administration routes in the mammal when given potential &agr;/&bgr;-adrenergic blocking, is selective for emergency hypertension.

Abstract: A method for stimulation of transcription factor AP (activator protein)-1 by administering a compound of the formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, c-propyl, n-butyl, sec.-butyl, iso-butyl, tert.-butyl, c-butyl, n-pentyl, sec.-pentyl, iso-pentyl, tert.-pentyl, neo-pentyl, c-pentyl, c-hexyl and c-heptyl; RNa and RNb are the same or different and selected from hydrogen, methyl and ethyl; R2, R3, R5 and R6 are independently selected from hydrogen, methyl, methoxy, thiomethyl, hydroxy, fluoro, chloro, bromo, trifluoromethyl, phenyl and benzyl; n is 1, 2 or 3; R′ and R″ are the same or different and selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec.-butyl, and iso-butyl or R′ and R″ together form a saturated heterocyclic ring of 5-7 atoms; and pharmaceutically acceptable salts, hydrates and solvates thereof, to a mammal in need thereof.

Abstract: N-Substituted glucamine compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agents selected from among nucleosides, nucleotides, immunomodulators, immunostimulants or various combinations of such other agents.

Abstract: A more practical synthesis for preparing discodermolide and structurally related analogues, novel compounds useful in the process and novel compounds prepared by the process.

Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.

Abstract: Described are cyclohexylamine derivatives of Formula I 1

Abstract: The invention concerns a composition, in particular a cosmetic composition, comprising at least a powder substance and a branched amide used as dispersion agent. The invention also concerns novel branched amides of formula (I′).

Abstract: The present invention provides novel methods for ligand discovery. The inventive methods rely on a process termed “tethering” where potential ligands are covalently bonded or “tethered” to a target and subsequently identified.

Abstract: An impurity-free biologically active mixture of 2-methyl-4-isothiazolin-3-one and 5-chloro-2-methyl-4-isothiazolin-3-one, which is useful as a biocide in various products, can be prepared by reacting N-methyl-3-mercaptopropionamide or N,N′-dimethyl-3,3′-dithiodipropionamide or a mixture thereof dissolved in a first organic solvent with sulfuryl chloride dissolved in a second organic solvent, which is different from the first organic solvent, at a temperature ranging from 5 to 20° C. and, optionally, centrifuging the resulting product mixture to obtain the desired mixture substantially free of 4,5-dichloro-2-methyl-4-isothiazolin-3-one impurity.

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.