Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: A method and a pharmaceutical composition in the form of a hydroalcoholic solution in which at least one hypoglycemia-inducing/insulinotropic active principle is dissolved in a stable and complete manner at a dosage that is reduced by 30% to 50% compared with the usual oral unit dosage, for its trans-buccal mucosal application in the spot treatment of postprandial hyperglycemia in type II diabetes in man or animals. Also, disclosed is a method of preparing said formulation and to its specific use in the spot treatment of postprandial hyperglycemia (PPHG) in the context of type II diabetes.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.

Abstract: The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimised.

Abstract: A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.

Abstract: Provided is a process for preparing 4-borono-L-phenylalanine, which has steps of: reacting N-protected (S)-4-halophenylalanine of formula (I), a boronating agent and an organolithium to obtain a reaction mixture, wherein the reaction mixture comprises N-protected (S)-4-boronophenylalanine of formula (II) and the R group represents a protecting group; isolating the N-protected (S)-4-boronophenylalanine from the reaction mixture; deprotecting the R group of the N-protected (S)-4-boronophenylalanine to obtain L-BPA.

Abstract: The invention relates to compounds, to compositions comprising the same and uses thereof for the prevention or treatment of pain, e.g neuropathic pain while having neutral or beneficial effect on metabolic parameters.

Abstract: The invention provides methods for increasing resting metabolic rate, reducing waist circumference, and weight control by administering a composition comprising dietary fiber, phenylalanine, tyrosine, tea blend, caffeine, and Lycium plants or Lycium plant extract preparations to the subject. The invention also provides a food or dietary supplement formulation which contains dietary fiber, phenylalanine, tyrosine, tea blend, caffeine, and Lycium plants or Lycium plant extract preparations.

Abstract: Peptides useful as angiotensin converting enzyme inhibitors are provided. Also provided are compositions comprising one or more of the peptides and methods for preventing, treating and/or diminishing one or more syndromes associated with angiotensin converting enzyme by using the peptides.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: Compositions based on amino acids are described, for improving the myocardial ventricular function in patients suffering from diabetes, particularly but not exclusively II type diabetes. The compositions according to the invention comprise up to 75% of the branched chain amino acids leucine, isoleucine and valine, as active ingredients. Preferably, the compositions also comprise, as further active ingredients, up to 50% of threonine and lysine. Other essential amino acids are preferably also provided, in particular methionine, phenylalanine, histidine, tryphtophan, as well as non essential amino acids, in particular tyrosine and/or cyst(e)ine (i.e., cystine and cysteine). Other amino acids can be added, provided that their sum is in a percentage being lower than 20% with respect to the other active ingredients, and less than 10% for each single amino acid.

Abstract: This invention provides a process of making optically pure melphalan of the formula by hydroxyethylation, in a regioselective manner, of the aromatic amino group rather than the glycinic amino group.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: A thin film composition for oral administration that adheres to and dissolves in a mouth of a user, wherein the thin film is a single layered water-soluble solid comprising at least one D-amino acid contained in a plurality of hydrophobic carriers dispersed throughout the thin film. The hydrophobic carriers comprise oil and the composition further comprises a phospholipid, an emulsifier, and a water soluble polymer. The preferred D-amino acids are D-leucine, D-tryptophan, D-methionine, and D-tyrosine. A method of reducing dental plaque in a subject entails placing the thin film composition contemplated herein into a mouth of the subject.

Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.

Abstract: This invention relates to radioactive tyrosine derivatives for imaging bone metastases, a method for imaging or diagnosing bone metastases, compositions and kits for imaging bone metastases.

Abstract: This invention relates to octahydro-binaphthol derivatives, which can recognize amino acids and amino alcohols enantioselectively and transform L-amino acids into D-amino acids and optically resolve amino acids or amino alcohol with high efficiency.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The invention provides compounds which are -amino acid hydrogen peroxide solvates, wherein the side chain of the -amino acid has no basic nitrogen. A process for preparing the compounds and uses thereof are also described.

Abstract: The present invention relates to a method for the enzymatic hydroamination of C—C double bonds catalyzed by enzymes structurally and/or functionally related to phenylalanine ammonia lyase (PAL) isolated from microorganisms of Petroselinum crispum, Rhodoturula glutinis and/or functional active derivatives thereof.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: This invention is related to preparation of photosensitive ruthenium based aminoacid monomers and oligomers, aminoacid monomer-protein cross-linking using photo sensitat ion and conjugation on micro and nano-structures by ruthenium-chelate based monomers. Its vast range biotechnolgy applications of multifunctional, biocompatible, stabilE and specific micro and nanobio-conjugates, which will stand-alone or simultaneously enable (i) both purification and determination, (ii) both targeting and imaging and theranostics and (iii) catalysis and determination. The construction and method of preparation is applicable to silica materials, superparamagnetic particles, QDs, CNTs, Ag/Au nanoparticles and Au surfaces and polymeric materials. The photosensitive aminoacid monomer linkers can react via chemically and biocompatible to a lot of different micro and nano-surface and then to the protein when they act as a single-step cross-linking reaction using irradiation.

Abstract: The present invention herein provides a combination of stable isotope-labeled aliphatic amino acids, which permits the structural analysis of a high molecular weight protein, in particular, a high molecular weight protein whose molecular weight exceeds 60 kDa. This is a combination of stable isotope-labeled amino acids which is characterized in that arginine (Arg), glutamine (Gln), glutamic acid (Glu), lysine (Lys), methionine (Met) and proline (Pro) satisfy the following requirements concerning the labelling pattern: (b) one of the methylene hydrogen atoms of at least one of the methylene groups is deuterated and the both of the two methylene hydrogen atoms of at least one of the methylene groups are likewise deuterated; and (d) when they each have a methyl group, the hydrogen atoms of the methyl group except for one of the same are deuterated, or the methyl group is completely deuterated.

Abstract: Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2?)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble.

Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.

Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.

Abstract: Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2?)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble.

Abstract: The invention relates to a process for preparing optically active ?-aminoacetals by resolution of a racemic mixture or of a mixture of enantiomers via the formation of diastereoisomeric salts, and also novel intermediates in the form of diastereoisomeric salts.

Abstract: A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.

Abstract: Provided are a marker for determining sensitivity to an anticancer agent capable of distinguishing a therapeutic response of an individual patient and a novel means for a cancer therapy using the marker. The marker for determining sensitivity to an anticancer agent contains a substance in a metabolic pathway in which L-phenylalanine and/or N,N-dimethyl glycine are/is involved.

Abstract: Disclosed is a method for producing precursors for L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the ?-methylated derivatives thereof, the precursor, and to a method for producing L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the ?-methylated derivatives thereof from the precursor. A compound of formula (3) is provided which enables automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine. The enantiomeric purity of the product is ?98%.

Abstract: The invention provides improved therapeutic and diagnostic fullerenes and endohedral fullerenes. The fullerenes and endohedral fullerenes of the invention are derivatized with at least two charged functional groups (and preferably more than two charged functional groups) to provide for water-solubility and improved in vivo biodistribution. Improved derivatized fullerenes and endohedral fullerenes carry a plurality of functional groups at least two of which are charged. Preferably at least about ? of the possible derivations sites on the fullerene caged carry derivatives and preferably at least about ½ of the functional groups on the fullerene cage are charged groups. The invention also provides water-soluble endohedral metallofullerene with improved biodistribution which are useful as in vivo imaging agents, including MRI contrast agents.

Abstract: A pharmaceutical or a foodstuff including as an active ingredient a peptide containing Tyr (Y), Phe (F), Trp (W), or His (H) and a hydrophobic amino acid adjacent thereto, or an analog thereof.

Abstract: There is provided a method for producing easily highly-purified acylphenylalanine that is useful as a raw material of pharmaceutical products and the like, which comprises the step of reacting an acid chloride with phenylalanine in a mixed solvent of an organic solvent and water, while keeping the solvent under the alkali condition by using potassium hydroxide.

Abstract: The present application relates to novel difluorophenol derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: This invention provides a process of making 4-(bis-(2-hydroxyethyl)amino)-L-phenylalanine of the formula by hydroxyethylation, in a regioselective manner, of the aromatic amino group rather than the glycinic amino group.

Abstract: New nateglinide crystals, i. e. nateglinide A-type crystals (main peaks in powder X-ray diffraction: 4.4°, 5.2°, 15.7°, 18.5° (2?)), M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2?)) and P-type crystals (main peaks in powder X-ray diffraction: 4.8°, 5.3°, 14.3°, 15.2° (2?)), can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble or, alternatively, by dissolving nateglinide in a mixed solvent composed of a solvent in which nateglinide is highly soluble and another solvent in which it is difficultly soluble, cooling the nateglinide solution to form crystals, filtering the mixture and drying the crystals at a specified temperature.

Abstract: A method for producing B-type crystals of nateglinide substantially free of H-type crystals is provided, which comprises drying solvated wet crystals of nateglinide at a low temperature until no solvent remains and making a crystal conversion thereof. According to this method, B-type crystals of nateglinide can be produced at an industrial scale without allowing other forms of the crystalline polymorphism to coexist.

Abstract: A tubular or spherical nanostructure composed of a plurality of peptides, wherein each of the plurality of peptides includes no more than 4 amino acids and whereas at least one of the 4 amino acids is an aromatic amino acid.

Abstract: The present invention provides the S enantiomer of a compound of formula (I) wherein n is 1 or 2 as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.

Abstract: The present invention relates to a process for the preparation of nateglinide, preferably in B-form, substantially free from the H-form, comprising three steps starting from D-phenylalanine methyl ester or a salt thereof.

Abstract: Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)s—N(R4)—B-J-T; and s. R3, R4, A, B, J and T have the meanings disclosed in the description. These compounds are PPAR? modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.

Abstract: New nateglinide crystals, i.e. nateglinide A-type crystals (main peaks in powder X-ray diffraction: 4.4°, 5.2°, 15.7°, 18.5°(2?)), M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8°(2?)) and P-type crystals (main peaks in powder X-ray diffraction: 4.8°, 5.3°, 14.3°, 15.2°(2?)), can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble or, alternatively, by dissolving nateglinide in a mixed solvent composed of a solvent in which nateglinide is highly soluble and another solvent in which it is difficultly soluble, cooling the nateglinide solution to form crystals, filtering the mixture and drying the crystals at a specified temperature.

Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.

Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically compatible salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.