Abstract: The present invention provides a novel method for the preparation of 18F-fluoride (18F) for use in radiofluorination reactions. The method of the invention finds use especially in the preparation of 18F-labelled positron emission tomography (PET) tracers. The method of the invention is particularly advantageous where bulk solutions are prepared and stored in prefilled vials rather than being freshly prepared on the day of synthesis. Also provided by the present invention is a radiofluorination reaction which comprises the method of the invention, as well as a cassette for use in carrying out the method of the invention and/or the radiofluorination method of the invention on an automated radiosynthesis apparatus.

Abstract: A process is provided for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct, which is unreactive with the base and is highly stable, and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear- or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.

Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET tracer.

Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET tracer.

Abstract: The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2].

Abstract: A solution for an alignment film of a liquid crystal display device includes a photo decomposition type polyimide acid which forms the alignment film in response to radiation of a polarized light, wherein a viscosity of the solution is not more than 35 mPa·s.

Abstract: There is provided a halogen-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein, m represents 0, 1 or 2, n represents 0, 1 or 2, A represents optionally substituted C3-C7 cycloalkyl or optionally substituted C5-C7 cycloalkenyl group, Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom, R1 and R3 independently represent optionally substituted C1-C4 chain hydrocarbon, halogen or hydrogen, R2 and R4 independently represent optionally substituted C1-C4 chain hydrocarbon, —C(?G)R5, cyano, halogen or hydrogen, G represents oxygen or sulfur, and R5 represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.

Abstract: This invention relates to novel cyclo alkyl compounds suitable for labeling by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.

Abstract: A perimidine-substituted squarylium dye is represented by the following formula (I):

Abstract: The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18F]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).

Abstract: It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.

Abstract: A process is provided for producing [18F]FACBC, which can reduce the production amount of impurities.

Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.

Abstract: The classical process for the rearrangement of substituted benzil to benzilic acid is performed in the presence of sodium or potassium hydroxide as a base using ethanol-ether as a medium. The reaction requires reflux temperature for complete conversion. However, these bases containing metallic ions and generate metallic containing effluent waste which may require additional expenditure for treatment. Moreover, because of corrosive nature of base, and use of flammable solvent, the safety measures are needed during large scale production. Another method also reported for benzilic acid rearrangement at 380° C. which is practically not feasible. The present invention describes the use of quaternary ammonium hydroxides as a base for the rearrangement of the substituted benzils to benzilc acids. It also avoids the use of solvent and reaction can be carried out at relatively lower temperatures. Because of the solvent free reaction condition it reduces the mass/volume of reaction mixture.

Abstract: It is intended to provide a bicyclic ?-amino acid derivative having excellent activity as an ?2? ligand. The present invention provides a compound represented by the general formula (I): wherein R1, R2, R2?, R4, R5, R6, R7, R8, and R8? are a hydrogen atom or the like; and R3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.

Abstract: The present invention relates to certain carbocyclic and oxacarbocyclic fumaric acid oligomers and the use thereof for preparing a pharmaceutical preparation as well of pharmaceutical preparations containing these compounds.

Abstract: Disclosed is a process for preparing 3-(amino)-3-cyclobutylmethyl-2-hydroxy-propionamide hydrochloride, an intermediate useful in the preparation of the HCV protease inhibitor (1R,5S)—N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide.

Abstract: A method for producing a (2-formyl-1-alkenyl)cyclopropane compound represented by the formula (1): wherein R1 and R2 are the same or different, and independently represent a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aryl group or an optionally substituted aralkyl group, which comprises reacting a formylcyclopropane compound represented by the formula (3): wherein R1 is the same as defined above, with an aldehyde compound represented by the formula (4): wherein R2 is the same as defined above, in the presence of a base.

Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.

Abstract: A polyamic acid comprising at least 10 mol % repeating units represented by the formula [1] or [2]; and a polyimide represented by the formula [3] or [4] which is obtained from the polyamic acid. A polyimide film having high heat resistance and satisfactory in light-transmitting properties and tensile strength is obtained from the polyamic acid. (In the formulae, R1 and R2 each independently represents hydrogen or C1-10 alkyl; R3 and R4 each independently represents hydrogen, halogeno, C1-10alkyl, or phenyl or the R3 and R4 on adjoining carbon atoms are bonded to each other to form C3-8 cycloalkyl or phenyl; R5 represents a divalent organic group; and n is an integer of 2 or larger.

Abstract: A process is provided for producing [18F]FACBC, which can reduce the production amount of impurities.

Abstract: The invention relates to the field of pharmaceutics and more specifically to cycloalkylamidoacid compositions useful in the preparation of cycloalkyaminoacids and oxazolidinediones, and processes for making cycloamidoacids X and R are defined herein.

Abstract: Methods of treating blood disorders are described.

Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, I, m and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.

Abstract: It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.

Abstract: A method for producing a (1-alkenyl)cyclopropane compound represented by the formula (2): wherein R1 and R2 are the same or different, and independently represent a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aryl group or an optionally substituted aralkyl group, which comprises bringing a (2-formyl-1-alkenyl)cyclopropane compound represented by the formula (1): wherein R1 and R2 are the same as defined above, into contact with a palladium catalyst.

Abstract: A process which comprises reacting a 1,2,3,4-cyclobutanetetracarboxylic-1,2:3,4-dianhydride [1] with an alcohol [2] in the presence of an acid catalyst to obtain a compound [3], isomerizing the compound [3] with a base catalyst into a compound [4], reacting the compound [4] with an organic acid to obtain a compound [5], and reacting the compound [5] with a dehydrating agent to obtain a 1,2,3,4-cyclobutanetetracarboxylic-1,3:2,4-dianhydride: wherein R1 and R2 are each independently hydrogen, halogeno, alkyl of 1 to 10 carbon atoms, halogenated alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, phenyl, or cyano; and R3 is alkyl of 1 to 10 carbon atoms.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The invention relates to arylcycloalkyl-substituted derivatives and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.

Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.

Abstract: The invention relates to the preparation of ultra-high purity 1,2-diaminocyclohexanetetraacetic acid being essentially free of unwanted metal and metal ion contaminants and its use as a stabilizer for ultra-high purity hydroxylamine compounds used extensively in the production of high premium electronic components.

Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.

Abstract: Phenylalanine enamide derivatives of formula (1) are described: 1

Abstract: This invention employs camphorsultam as a chiral recoverable auxiliary to provide a new method for manufacturing valproic acid and valproic acid amides that facilitates the enantioselective or diasteroselective production of valproic acid analogs on a larger scale.

Abstract: This invention relates to a novel advantageous process for the stereoselective preparation of 2-hydroxy-4-phenylbutyrates (HPB esters) and of their precursors. This is done by starting from readily accessible &agr;-unsaturated &agr;-hydroxy-&ggr;-keto esters which can be prepared by Claisen condensation.

Abstract: The present invention relates to novel amidino compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof; wherein R1 is selected from C1-4 alkyl, C3-4 cycloalkyl, C1-4 hydroxyalkyl, and C1-4 haloalkyl; to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.

Abstract: GABA analogs such as gabapentin and pregabalin are useful to prevent and treat inflammatory diseases.

Abstract: Squaric acid derivatives of formula (1) are described: 1

Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: A shell and tube heat exchanger reactor with forced circulation is used to improve heat and mass transfer for exothermic liquid--liquid, gas-liquid and gas-liquid-solid reactions. Enhanced productivity and selectivity are obtained.

Abstract: A pharmaceutical compound of the formula: ##STR1## in which n is 1 or 2, R.sup.1 is --CO.sub.2 H, R.sup.2 is hydrogen or C.sub.1-4 alkyl andR.sup.3 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, optionally substituted phenyl C.sub.2-10 alkenyl,(optionally substituted phenyl).sub.2 -C.sub.1-4 alkyl, optionally substituted C.sub.3-7 cycloalkyl, optionally substituted C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl or optionally substituted C.sub.3-7 cycloalkyl-C.sub.2-10 alkenyl, orR.sup.2 and R.sup.3, together with the carbon atom to which they are attached, form an optionally substituted C.sub.4-7 cycloalkyl group;or a salt or ester thereof other than the compounds .gamma.-propylidene-L-glutamic acid, .gamma.-ethylidene-L-glutamic acid and .gamma.-methylidene-L-glutamic acid.

Abstract: The invention is directed to optically active 1-amino-hydroxycycloalkanecarboxylic acid compounds represented by the formula: ##STR1## wherein n is 0, 1, 2, 3, or 4; methods of their synthesis; and their use as compounds to fix the confirmation of a peptide or protein molecule when introduced into the peptide or protein in the place of a normal amino acid.

Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.