Abstract: The invention relates to an aqueous pharmaceutical composition for parenteral administration comprising Tapentadol or a physiologically acceptable salt thereof, wherein the concentration of Tapentadol is within the range of from 0.10 to 8.00 mg/mL, based on the weight of Tapentadol free base and based on the total volume of the composition; and wherein the pH value of the composition is buffered and within the range of from 4.0 to 6.0. The invention also relates to a container comprising the pharmaceutical composition and a process for the preparation thereof. The invention also relates to a kit comprising the contained according to the invention in a packaging. The pharmaceutical composition according to the invention is particularly useful for treating pain, especially acute pain, preferably in pediatric patients.

Abstract: Disclosed is a method to make N-acetyl-p-aminophenol. The method includes steps for converting biomass-derived p-hydroxybenzoates to p-hydroxybenzamide, then to p-aminophenol; and then N-acetylating the p-aminophenol.

Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.

Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like

Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolized to a biologically active agent; and X is R, or up to three R moieties attached to a linker, Y1, Y2 or Y3. Self-assembly of the amphiphilic prodrugs into reverse lyotropic phases, particularly hexagonal, cubic and sponge, is disclosed.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.

Abstract: This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.

Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.

Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.

Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.

Abstract: The present invention relates to a composition comprising phenacetin, in particular a Phenacetinum 4CH homeopathic medicament for use in the treatment of cancer.

Abstract: The present invention concerns a liquid formulation that is stable to oxidation and that is based on paracetamol in an aqueous solvent obtainable by the following steps: (i) dissolving in a reaction vessel paracetamol in an aqueous solvent having a temperature between 65° C. and 95° C., and having pH between 5.0 and 6.0; (ii) cooling the solution so formed to a temperature equal to or above 35° C. and below 40° C. under an atmosphere of nitrogen; (iii) adding cysteine hydrochloride and sodium hydroxide simultaneously to the solution without stirring; (iv) closing the reaction vessel, and stirring the solution of step iii) in a nitrogen atmosphere. It further relates to a method for preparing the formulation.

Abstract: The present invention refers to ready-to-use highly stable paracetamol injectable solutions, prepared by mixing paracetamol, water, propylene glycol, and a citrate buffer. (pH 4.5 to 6.5), and by heating said solution under preset conditions. The resulting solution may be stored for an extended period of time within a wide range of temperatures, with no paracetamol precipitation and/or its chemical modification.

Abstract: The present invention relates to continuous processes for the preparation of primary and secondary N-acetylated aromatic amines of formula I or O-acetylated product of o-hydroxy benzoic acid of Formula II using acetic acid as an acetylating agent. wherein R1 has a definition of hydrogen atom, C1-C4 alkyl group or C1-C4 alkoxy group.

Abstract: This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.

Abstract: This invention discloses drug-delivery compositions, methods of making prodrugs, and methods of drug delivery using a self-assembled gelator. The backbone of the gelator can contain a drug or prodrug, such as acetaminophen or salicin. Additional drugs or agents can be encapsulated in the gelator. Enzymatic or hydrolytic cleavage can be used to release the drugs.

Abstract: There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression. More particularly, there is described an abuse resistant pharmaceutical composition for the treatment of inter alia, depression and controlled release pharmaceutical compositions of related thereto.

Abstract: This invention pertains to chemometric methods for the analysis of chemical, biochemical, and biological data, for example, spectral data, for example, nuclear magnetic resonance (NMR) spectra, and their applications, including, e.g., classification, diagnosis, prognosis, etc., especially in the context of bone disorders, e.g., conditions associated with low bone mineral density, e.g., osteoporosis.

Abstract: Disclosed is a process for modifying the morphology and/or polymorphism of an organic substance, which process comprises treating the solid substance, or a solution or dispersion thereof, with one or more amphiphilic proteins.

Abstract: A new use for paracetamol in a method of treating glaucoma, which method comprises administering to a patient in need of such treatment 500 mg to 1000 mg of paracetamol in oral format 4 to 6 hourly. An ophthalmic solution is also provided containing between 0.1 to 5% of paracetamol which is administered as one to two drops in each eye 4 to 6 hourly. The ophthalmic solution further includes one or more of the following excipients: hydroxypropylmethylcellulose, benzalconium chloride, polyacrylic acid such as Teargel®.

Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.

Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.

Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.

Abstract: Compounds selected from: where DRUG-OH, DRUG-COOH and DRUG-NH2 are biologically active compounds; each X is independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone moiety), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO—, where y is 2-4 or 6-24 and —(CH2CH2O)zCH2COO—, where z is 2-24; each Y is independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester moiety), —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety), —CO(CH2)mO—, where m is 2-4 or 6-24 and —COCH2O(CH2CH2O)n— where n is between 2-24; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.

Abstract: The invention relates to a novel ultra-thin hydrophobic and oleophobic layer, formed by self-assembly on a solid substrate surface, of compounds of the general formula A-B in which A represents a group of the formula in which Z represents C or N+, X represents C—H or C-L, L being an electron-attracting group selected from F, Cl, Br, I, CF3, NO2 and N(CH3)3+, Y represents H or CH3, or Y forms a 5- or 6-atom heterocycle with X, T represents NH, CO, CONH or NH2+U?, U? being a soluble anion such as e.g. F?, Cl?, Br?, I, OH?, NO3?, HSO4?, SO42?, CO32?, HCO3? or SCN?, and B represents a C1-C20 linear aliphatic alkyl group partially or completely substituted with F, and a method of preparing this layer and its use as an epilame.

Abstract: The present invention relates to a novel process for the preparation of compounds of formula (V) wherein X, Q, R1, R1a and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents.

Abstract: The present invention concerns a method for the controlled precipitation of organic compounds giving crystals with a very small average size and a very narrow size distribution.

Abstract: The present invention relates to a method for the preparation of Florfenicol from Fluoroamine compound, namely (1R,2S)-1-[4-(methylsulfonyl)phenyl]-2-amino-3-fluoro-1-propanol (II), by reaction with dihaloacetic acid ester in an organic solvent in presence of an inorganic base.

Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.

Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.

Abstract: Disclosed herein are novel binaphthol derivatives and methods for the optical resolution of amino acids or amino alcohols and for the optical transformation of D, L-forms of amino acids using the same.

Abstract: The present invention provides a method for the reductive acetamidation of an aryl nitro compound by reacting a substituted acid with an aryl nitro compound and adding a catalytic amount of a base with the substituted acid and the aryl nitro compound to form an acetamidation aryl nitro compound. The acetamidation aryl nitro compound is then purified.

Abstract: Novel compounds having the structure (I) where R=methyl, ethyl or propyl, R1=methyl or H, R2=methyl, ethyl or propyl, R3=methyl or H, R4=methyl or ethyl, R5?H or methyl, and where R3 and R5 are not both H, excluding N-ethyl-2-methyl-N-(3-methylphenyl) propanamide, can have desirable odour properties, typically of a tropical fruit, cassis character and find use in perfumes and perfumed products

Abstract: A method for obtaining aqueous formulations with easily oxidizable active principles, notably phenols, stable over a prolonged period, comprising subjecting them to extreme deoxygenation by bubbling with an inert gas and/or placing wider vaccum, protecting them against possible resorption of oxygen by keeping them under an inert gas atmosphere, by filling, under inert gas, into bottles previously cleared of air by insufflation with inert gas, then subjecting them, while stoppering, to low pressure as obtained in the bottle, of 65,000 Pa maximum, to obtain aqueous solutions having a residual oxygen concentration in the solution below 2 ppm, and preferably of the order of 1 ppm and even 0.5 ppm useful as injectable preparations having an oxygen concentration in the solution below 2 ppm.

Abstract: A process of producing organic compounds, such as acetaminophen, nitroalcohols and indoles, employs a catalyst system of an oxyethylene ether and a metal containing inorganic or organic reagent. The oxyethylene ether at least partially complexes the metal of the inorganic or organic reagent. As such, the reactions may be conducted neat. The processes are environmentally friendly and operationally simple.

Abstract: The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl group is cleaved off, and further describes 4-acetamino-1-naphthol ethers obtained thereby.

Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Disclosed is a 2-amino-5-acylamino-4-substituted-phenol compound having the structural formula I: wherein Y is a substituent group, and R′ is a ballast group. Also disclosed is a simplified method for preparing a photographic coupler using this compound.

Abstract: Disclosed is a 4-acylamino-2-hydroxy-5-substituted-acylanilide compound having the structural formula I: wherein R is hydrogen or an alkyl group, Y is a group linked to the rest of the compound by a —O—, —S—, or —N— atom; and R′ is a substituent group. Also disclosed is a method of using the compound in making a cyan dye-forming photographic coupler.

Abstract: The present invention relates to systems and methods for generating polymorphs of compounds. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline polymorphs that find use as improved drugs, pigments, explosives, nonlinear optical crystals, solid-state reactive compounds, and other polymorphic materials.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: A benzene compound of the formula wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient.

Abstract: The present invention relates to a compound having the formula: 1

Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.

Abstract: The present invention relates to a process for preparing 2,4-dichloro-5-hydroxyacetanilide by reacting 3-hydroxyacetanilide with sulfuryl chloride in the presence of from 3 to 30 parts by weight of an aliphatic carboxylic acid having from 1 to 6 carbon atoms per part by weight of 3-hydroxyacetanilide with vigorous mixing at from 20 to 100° , removing gaseous components from the reaction mixture, setting a ratio of from 1.0 to 6 parts by weight of aliphatic carboxylic acid per part by weight of 3-hydroxyacetanilide employed and removing 2,4-dichloro-5-hydroxyacetanilide as a solid.