Abstract: The invention provides compositions comprising a therapeutically effective amount of a compound of general formula (I): wherein R1, R2 and R3 may be independently selected from H, OH and OMe; wherein X is C1 or C2 and wherein for C2 each carbon is linked by a single or multiple bond (preferably a double bond) and is substituted with one or more H or OH; for use as a medicament for treating or preventing the development of medical conditions characterised by inappropriate platelet aggregation.

Abstract: The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.

Abstract: The present invention relates to salts and compositions of tramadol and ibuprofen, their crystal form, processes for preparation of the same and their uses for the treatment of pain.

Abstract: There is described a process for the manufacture of a racemic 2-aryl propionic acid compound, or a pharmaceutically acceptable salt thereof, which comprises reacting the S- or R-enantiomer of the corresponding 2-aryl propionic acid compound with a base.

Abstract: Abstract Compounds of the formula (I) in the form of racemates, enantiomerically pure diastereomers or a mixture of diastereomers, where the radicals R1 are identical or different and are each C1-C4-alkyl; m is 0 or an integer from 1 to 4; n is 0 or an integer from 1 to 3; p is 0 or an integer from 1 to 5; R2 is an aromatic hydrocarbon radical or a C-bonded heterohydrocarbon radical and R3 is an aliphatic or C-bonded heteroaliphatic hydrocarbon radical; R2 and R3 are identical or different and are each an aliphatic or C-bonded heteroaliphatic hydrocarbon radical; R4 is an unsubstituted or C1-C6-alkyl-, C1-C6-alkoxy- or halogen-substituted hydrocarbon radical; and A is a secondary amino group, are ligands for metal complexes which are suitable as catalysts for homogeneous enantioselective hydrogenation.

Abstract: Compositions and methods included herein describe the treatment of atherosclerosis and other vascular diseases such as thrombosis, restenosis after angioplasty and/or stenting, and vein-graft disease after bypass surgery, by inhibition of the expression or biologic activity of the toll-like receptor 4 (TLR4) and/or myeloid differentiation factor 88 (MyD88). TLR4 cell signal transduction is at least partially responsible for the manifestation, continuation, and/or worsening of atherosclerosis and other forms of vascular disease. The present invention provides several means with which to inhibit this signal transduction pathway by affecting the biological activity of the TLR4 receptor and/or MyD88.

Abstract: The present invention belongs to a spiro phosphine-oxazoline and preparation method and application thereof, particularly, publishes a novel spiro phosphine-oxazoline and the preparation method of its iridium complex. The substituted 7-diaryl phosphino-7?-carboxy-1,1?-Lo-dihydro-indene is used as the starting raw material to synthesize the novel spiro phosphine-oxazoline of the present invention through a two-step reaction. The novel spiro phosphine-oxazoline and the iridium precursor are complexed to become a complex, and then through ion exchange, an iridium/phosphine spiro-oxazoline complex with different anions can be obtained. The present invention overcomes the shortcomings of the existing technology. The cheap readily available amino alcohol is used as the raw material to synthesize the novel spiro phosphine-oxazoline, on the fourth position of the oxazoline ring of which there is no substitutent.

Abstract: The present invention relates to salts of Memantine and COX-INHIBITORs, their crystal form, the processes for preparation of the same and their uses for the treatment of various disorders, including pain.

Abstract: A multi-step method for the continuous synthesis of ibuprofen or a synthetic precursor of ibuprofen is provided that does not require any intermediate purification or isolation steps and uses reagents compatible with downstream reactions. According to some embodiments, a method is provided wherein isobutylbenzene and a propionyl compound may be converted into a first product in a first Friedel Crafts acylation reaction. The first product may then be converted into a second product in a 1,2-aryl migration reaction. Finally, the second product may be converted into ibuprofen in a hydrolysis reaction. The present invention also provides a method wherein only the first and second reaction steps or only the second and third reaction steps are performed. An apparatus is also provided having two or more microreactors and two or more junctions in particular arrangements for the synthesis of ibuprofen or a synthetic precursor of ibuprofen.

Abstract: The present invention provides phenylalkylcarboxylic acid compounds and compositions containing such compounds which facilitate the delivery of biologically active agents.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one y-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: The present invention relates to a compound represented by formula (I): (wherein the symbols in formula were described in the description), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention binds to and is antagonistic to an LPA receptor (particularly, EDG-2), it is useful for prevention and/or treatment of urinary system disease (prostatic hypertrophy or neurogenic bladder dysfunction disease, spinal cord neoplasm, nucleous hernia, spinal canal stenosis, diseases caused by diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, and polyuria), carcinoma-associated disease, proliferative disease, inflammation system disease, immune system disease, disease by secretory dysfunction, brain-related disease and/or chronic disease.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: Methods and an apparatus for producing stable crystal polymorphs are provided. Inner surfaces of glass vials with a concave bottom topography are coated with nonstick compounds to select for nucleation of stable polymorphs.

Abstract: Sodium ibuprofen compositions and methods of manufacturing tablets and caplets comprising sodium ibuprofen are described. The formulation is advantageous because it allows for the formation of tablets having low sodium content and further provides tablets exhibiting improved physical stability, high tablet hardness and high strength, coupled with excellent dissolution and bioavailability characteristics. The formulations and processes are further advantageous because they can be produced in large quantities without an unacceptable number of defective tablets.

Abstract: The present disclosure describes the design and synthesis of a novel class of water soluble curcumin-based compounds. These water soluble curcumin-based compounds are shown to provide superior cell killing activity and exhibit increased and cell internalization solubility in aqueous solutions as compared to the free (unconjugated) curcumin. The present disclosure provides compositions for the treatment or prevention of a variety of disease states or conditions, such as but not limited to, cancer, other cell hyperproliferative disorders and chronic inflammatory conditions, said compositions comprising a water soluble curcumin-based compound.

Abstract: This disclosure provides a method of preparing a crystalline molecular sieve comprising: (a) providing a reaction mixture comprising at least one source of ions of tetravalent element Y, at least one source of alkali metal hydroxide, water, optionally at least one seed crystal, and optionally at least one source of ions of trivalent element X, the reaction mixture having the following molar composition: Y:X2=2 to infinity, preferably from about 2 to about 1000, OH?:Y=0.001 to 2, preferably from 0.1 to 1, M+:Y=0.001 to 2, preferably from 0.

Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.

Abstract: The invention relates to novel 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) in which A, B, D and G are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selectively herbicidal compositions comprising, firstly, the 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.

Abstract: The invention relates to a novel 2-ethyl-4,6-dimethylphenyl-substituted tetramic acid derivatives of the formula (I) in which A, B, D and G are as defined above, to a plurality of processes and intermediates for the preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly 2-ethyl-4,6-dimethylphenyl-substituted tetramic acid derivatives of the formula (I) or (I-a?) and secondly at least one crop plant compatibility-improving compound.

Abstract: The present invention fabricates mesocrystals of organic and organo-metallic compounds. Supersaturated solutions are made with different sums of an organic or organo-metallic compound and the organic or organo-metallic compound is added with an excipient. Through a water bath, mesocrystals are obtained from the supersaturated solutions with well-faceted nucleation and growth. Different polymorphisms are induced with different ratios of enantiomers. And the dissolution rate for fabricating the API is enhanced.

Abstract: The present invention provides protein-based biomarkers and biomarker combinations that are useful in qualifying breast cancer status in a patient. In particular, the biomarkers of this invention are useful to determine metastasis-free survival of breast cancer patients. The biomarkers can be detected by SELDI mass spectrometry in serum samples fractionated by means of anion exchange chromatography. Some of the biomarkers have been identified as: Apolipoprotein A1; Apolipoprotein A2; Haptoglobin alpha 1; Transferrin; Complement C3a; and truncated forms thereof.

Abstract: Abstract Compounds of the formula (I) in the form of racemates, enantiomerically pure diastereomers or a mixture of diastereomers, where the radicals R1 are identical or different and are each C1-C4-alkyl; m is 0 or an integer from 1 to 4; n is 0 or an integer from 1 to 3; p is 0 or an integer from 1 to 5; R2 is an aromatic hydrocarbon radical or a C-bonded heterohydrocarbon radical and R3 is an aliphatic or C-bonded heteroaliphatic hydrocarbon radical; R2 and R3 are identical or different and are each an aliphatic or C-bonded heteroaliphatic hydrocarbon radical; R4 is an unsubstituted or C1-C6-alkyl-, C1-C6-alkoxy- or halogen-substituted hydrocarbon radical; and A is a secondary amino group, are ligands for metal complexes which are suitable as catalysts for homogeneous enantioselective hydrogenation.

Abstract: Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using alkyl/aryl iodides with alcohols or water treated by photosensitizers are provided. The resultant carbon-isotope labeled esters and acids, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits and method for PET studies are also provided.

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: [Problems to be Solved] It is an object of the present invention to provide an agent and a method for maintaining and promoting the stability of a membrane protein, and in particular, a transporter (for example, an ABC transporter) on a cell membrane. [Solution] The present invention provides: a method of treating a cell with carboxylic acid including 4-phenylbutyric acid or a derivative thereof to suppress the decomposition of a protein existing on a cell membrane, so as to maintain and promote the stability of the protein on the membrane; and an agent for stabilizing a membrane protein, which comprises carboxylic acid including 4-phenylbutyric acid or a derivative thereof.

Abstract: The invention relates to a method for producing particles with a length-width ratio of less than about 1.4 from a pharmaceutical substance, which method includes the following stages, that is: (a) provision of a melt of the pharmaceutical substance; (b) production of droplets of the melt by spraying into a processing chamber; (c) repeated guiding of solid particles past sprayed droplets in the processing chamber with the aid of a process gas jet which is guided in a defined way and whose temperature is fixed, depending on the solidification point of the melt, so that at least some of the droplets come into contact with particles and solidify thereon; (d) removal of particles from the processing chamber as a function of the particle size. The invention further relates to particles of pharmaceutical substances and the use thereof.

Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.

Abstract: The invention is directed a process of preparing a compound of formula (I), wherein R1, R2, R3 and z are as defined herein.

Abstract: The use of a compound for the reduction or elimination of bitterness caused by flavan-3-ols is provided. Compositions having greater than 0.01 wt % flavan-3-ols and that comprise an effective amount of the compound are also provided.

Abstract: The present invention discloses an ibuprofen amine salt and the synthesis thereof, and more particularly an ibuprofen amine salt yielded by the neutralization reaction of a racemic mixture of ibuprofen with tris(hydroxymethyl)aminomethane in a solution system of water and an organic solvent. Compared with racemic mixtures of ibuprofen, the ibuprofen amine salt has higher solubility and a higher melting point, thereby having better bioavailability and properties than racemic mixtures of ibuprofen during pharmaceutical processing. Further, the ibuprofen amine salts of the present invention are stable between pH 4 and 9 so that they can be more widely applied to medicines.

Abstract: A free-flowing hydrated sodium salt of ibuprofen of controlled median particle size and water content is provided. It can be produced by adding aqueous NaOH to a non-boiling solution or slurry of ibuprofen in an organic solvent that can be distilled along with water at a temperature in the range of 50 to 120° C. The rate of NaOH addition is at a rate that does not cause the resultant reaction mixture to boil before the addition has been completed. After completing the addition, the water is removed with some of the organic solvent by distillation. After cooling, the hydrated sodium salt of ibuprofen is recovered from the resultant slurry. The process enables the median particle size of the sodium salt of ibuprofen formed to be controlled by selection and use of a predetermined effective concentration of NaOH in the aqueous NaOH solution used.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: A process for producing a solubilized ibuprofen, preferably in the form of a granulate, the process comprising the steps of: providing a mixture comprising solid ibuprofen and a first base selected from the group consisting of sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium glycinate, potassium glycinate and tribasic sodium and potassium phosphates and mixtures thereof, and reacting the ibuprofen and the first base in essentially dry state. The obtainable granulate and the pharmaceutical compositions and dosage forms that may be produced therefrom are distinguished by their high solubility and rapid disintegration and dissolution in aqueous media, by their good flow properties and compressibility, by rapidly achieving onset of analgesic effect.

Abstract: (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.

Abstract: Methods for preparing compound of formula (I) are described, wherein R1-R3 are defined herein, as are methods for preparing the intermediates formed therein. Also described are methods for enantioselectively preparing a chiral compound of the following structure, wherein R2 and R3 are defined herein.

Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R<1>, R<2>, R<3>, X, Y, Z, m, and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.

Abstract: The present invention relates to the use of one or more retinoid agonists and/or antagonists comprising retinoids with selective Retinoid X Receptor (RXR) agonistic or antagonistic activity alone or in combination with one or more peroxisome proliferator activated receptor (PPAR) ligands for the manufacture of a medicament for the (preferably oral or topical) treatment (this term including prevention/prophylaxis and/or therapy) of one or more manifestations of metabolic syndrome (also known as syndrome X), also called diseases hereinafter, especially from one or more manifestations thereof selected from the group consisting of diabetes type II, obesity, dyslipidemia, hypertension and polyneuropathy, each of which can also be linked with a high risk of cardiovascular diseases. Corresponding methods, the compounds and combinations for use in the treatment of the mentioned diseases and comparable invention embodiments are also described.

Abstract: The invention relates to a method for preparing 2,5-dimethylphenylacetic acid by converting p-xylene with chloroacetyl chloride into 2-chloro-1-(2,5-dimethylphenyl)ethanone, which is reacted with the compound of the formula (II) to give the compound of the formula (III), which is then rearranged to give a mixture of the compounds (IV) and (V), which is then hydrolyzed to 2,5-dimethylphenylacetic acid.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.

Abstract: Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and th

Abstract: Polyhalogenated cinnamic acids and cinnamic acid derivatives are prepared by reacting diazonium salts accessible from polyhalogenated anilines with acrylic acid or acrylic acid derivatives in the presence of a homogeneous, palladium-containing catalyst at about ?5 to about +100° C. Some of the cinnamic acids and cinnamic acid derivatives obtainable in this way are new. Cinnamic acids and cinnamic acid derivatives which can be prepared according to the invention can be used for the preparation of indanones which are precursors for agro- and pharmaceutical chemicals and for substances having liquid-crystalline properties.

Abstract: The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs.

Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient.

Abstract: The present disclosure is directed to modulators of cyclooxygenase (COX) enzymes and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of non-specific pain, tension-type pain, headache, migraine, lower back pain, sciatica, dental pain, muscular pain, pain associated with acute soft tissue injuries, bursitis, tendonitis, lumbago, periarthritis, tennis elbow, sprains, strains, muscular problems associated with sports injuries, muscular problems associated with accidents, period pain, primary dysmenorrhoea, acute sore throat pain, osteoarthritis, rheumatoid arthritis, cancer, any disorder requiring analgesic response, any disorder requiring anti-inflammatory response, any disorder requiring antipyretic response, any conditions mediated by cyclooxygenase, cystic fibrosis, dementia, Alzheimer's disease, and/or conditions mediated by levels of ?-amyloid are described.

Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.

Abstract: The present invention relates to a method for deuteration of an inert alkane using activated palladium carbon. The present invention discloses “A method for deuteration of a hydrogen atom of a methyl group or a hydrogen atom bonded to a carbon atom at benzyl position and the other carbon atoms of an alkylene group having not less than 2 carbon atoms, in a compound containing the methyl group or the-alkylene group having not less than 2 carbon atoms, directly bonded to an aromatic ring which may have a substituent, which comprises placing said compound in a deuterated solvent in the presence of activated palladium carbon, under sealed reflux condition”.

Abstract: Disclosed herein is a novel process for producing Sodium dihydrate salt of Ibuprofen of Formula (Structure I) by treating a salt of long chain carboxylic acid of Formula (Structure III) with Ibuprofen of Formula (Structure II) in the presence of an aqueous organic solvent.

Abstract: The present invention relates to a novel process for preparing 2,4,5-trimethylphenyl-acetic acid by reacting pseudocumene with dichloroacetyl chloride in a Friedel-Crafts reaction to give 2,2-dichloro-1-(2,4,5-trimethylphenyl)ethanone, converting the 2,2-dichloro-1-(2,4,5-trimethylphenyl)ethanone to 2,4,5-trimethylmandelic acid using an alkali metal hydroxide and reducing the 2,4,5-trimethylmandelic acid to 2,4,5-tri-methylphenylacetic acid.