Abstract: A pharmaceutical composition for treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for treatment and/or prevention of diseases associated with decrease in bone mass.

Abstract: The invention relates to an improved process for preparing 3-acyloxy-2-methylbenzoic acids by heating substituted naphthalenes in the presence of alkali metal hydroxides and subsequently acylating.

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

Abstract: The present invention provides compounds of the formula: wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor useful in the treatment of pain, Alzheimer's disease, memory loss or dementia or loss of motor function.

Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Abstract: The present invention provides a neurodegenerative disease therapeutic agent containing as its active ingredient a (15R)-isocarbacycline derivative indicated by the following formula [I] or a 15-deoxy-isocarbacycline derivative indicated by the following formula [III]: (wherein, R1 represents a C1-C6 alkylene group, and R2 represents a hydrogen atom, a C1-C7, alkyl group or protective group); or, (wherein, R1 and R2 are the same as those defined in formula [I]).

Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

Abstract: The invention relates to a novel process for synthesizing organic compounds of general formula (I): said process may be carried out on an industrial scale and makes it possible to obtain from a mixture of racemic alcohols of formula (II), the corresponding chiral alcohols of R configuration, in a high chemical yield.

Abstract: The instant invention provides reagents and methods for diagnosis, detection and treatment of cancers (for example, prostate cancers). In particular, the invention provides methods to generate various functionalized PSMA ligands, and their uses in diagnosis, detection, imaging, and treatment of prostate cancers, especially those overexpressing PSMA.

Abstract: The production process of the present invention comprises a step of allowing a carboxylic acid derivative represented by the formula (1): wherein ring Z is a monocyclic or polycyclic non-aromatic or aromatic ring, and R1 is a halogen atom or a group represented by the formula (2): —OR??(2) wherein R is a hydrogen atom or a hydrocarbon group, to react with an organometallic compound represented by the formula (3): R2-M??(3) wherein R2 is a hydrocarbon group, and M is a metallic atom which may have a ligand, or the formula (4): -MgY??(4) wherein Y is a halogen atom, and a carboxylic acid halide represented by the formula (5): wherein R3 is a hydrocarbon group or a heterocyclic group, and X is a halogen atom, to yield the tertiary alcohol ester represented by the formula (6): wherein Z, R2 and R3 have the same meanings as defined above.

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: A compound represented by the formula (I) or a salt thereof: wherein n represents an integer of 1 to 3, R represents an alkyl group having 3 to 8 carbon atoms, a group represented by the following formula: R1(CH2)k— (wherein k represents 0 or an integer of 1 to 3; R1 represents a saturated cyclic alkyl group having 3 to 7 carbon atoms or a saturated condensed cyclic alkyl group having 6 to 8 carbon atoms, and the group R1 may be substituted with a lower alkyl group having 1 to 4 carbon atoms) and the like, and Ar represents a condensed bicyclic group such as naphthalen-1-yl group, which has suppressing action on prostaglandin and leukotriene production and is useful for prophylactic and/or therapeutic treatment of various inflammatory diseases and the like caused by these lipid mediators.

Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Alcohol and water solvates of 6-(5-carboxy-5-methyl-hexyloxy)-2,2-dimethylhexanoic acid monocalcium salt are crystalline and have the formula (I), wherein R1 is H or lower alkyl, and x is a number from 0 to 10, and are useful for treating dyslipidemia.

Abstract: Microorganisms capable of producing novel polyalkanoates having 3-hydroxybenzoylalkanoic acids as monomer units by utilizing benzoylalkanoic acids as starting materials are cultured in media containing benzoylalkanoic acids and saccharides, and the polyhydroxyalkanoates produced in the culture cells are extracted and recovered.

Abstract: Disclosed are a process of subjecting a diester of a long-chain dicarboxylic acid having 18 to 21 carbon atoms to intramolecular condensation in the presence of titanium tetrachloride or zirconium tetrachloride and a trialkylamine to form an ?-alkoxycarbonylated macrocyclic ketone, and a process for producing a macrocyclic ketone by hydrolyzing an ?-alkoxycarbonylated macrocyclic ketone obtained by the process and then subjecting the hydrolyzate to decarboxylation. The invention provides a process for producing a macrocyclic ketone efficiently, which permits high concentration synthesis.

Abstract: An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the condensation of an aldehyde and an acetoacetate in the presence of a novel catalyst system that includes a pyridyl carboxylic acid and a secondary amine. It has been found that through the use of the present invention the purity and yield of the desired isomer of the benzylidene intermediate can be maximized, thus avoiding the requirement of additional purification steps. The use of these intermediates can then be further reacted to form the required dihydropyridines, again having a very high purity and yield compared with the prior art.

Abstract: A method for the production of aliphatic fluoroformates, wherein carbonyl fluoride is made to react with aliphatic alcohol in the presence of sodium fluoride in ether at a temperature of ?20° to 50° C. The method is carried out using carbonyl fluoride obtained by reacting phosgene with surplus powdered sodium fluoride, whereby the grains thereof have a specific surface of 0.1 m2/g or more and/or an average diameter of 20 ?m or less, at a temperature ranging from 25° to 120° C. The method enables unstable fluoroformates such as tertiobutyl to be obtained with excellent yields.

Abstract: A method for preparing bromofluorenes includes a step of dispersing a compound selected from the group consisting of fluorene, fluorenone, and derivatives of fluorene and fluorenone in water to prepare a disperse system. Bromination is initiated by adding bromine Br2 into the disperse system. Thus, bromofluorenes can be efficiently and economically prepared without using any environmentally harmful organic solvent requiring a high cost to dispose of.