Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.

Abstract: A laminate adhesive that can suppress elution of a low molecular weight compounds of a composite film into the content, so as to prevent the inherent properties or performances of the content from being spoiled by the low molecular weight compounds. In the laminate adhesive, the polyester polyol contains naphthalenedicarboxylic acid and/or alkyl ester thereof as an acid component, and concentration of cyclic ester compounds in extracted water, which are extracted from a composite film bonded by the laminate adhesive by water of 0.5 mL/cm2 per unit area of the composite film, is 0.5 ppb or less in terms of dibutyl phthalate concentration measured by a gas chromatograph-flame ionization detector.

Abstract: The present invention provides a novel protein and its use. The protein or its salt, the partial protein, its amide or ester, or salts, and DNA encoding the same can be employed for obtaining antibodies and antisera, constructing the expression system of the protein of the present invention, for constructing the assay system for the GABA transporter activity and screen medicament candidate compounds using the expression system, for making drug design based on the steric structure of GABA transporters, as agents for producing probes or PCR primers in gene diagnosis, for preparing transgenic animals or as pharmaceuticals for the prevention/treatment of genetic disorders.

Abstract: A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.

Abstract: Novel glucose transporter proteins, novel vesicular glutamate transporter proteins and a novel potential-dependent K+ channel protein, are useful as, for example, diagnostic markers, hyperlipemia, arteriosclerosis, etc. These proteins, compounds promoting or inhibiting the activities thereof, etc., which are obtained by a screening method with the use of these proteins, and so on, are usable as safe drugs for the prevention/treatment of the diseases above.

Abstract: The present invention aims at providing a method of determining a ligand to an orphan receptor. Specifically, the present invention provides a method of determining a ligand to a receptor protein, to which no ligand has been determined, which comprises using a fusion protein of the receptor protein and a fluorescent protein.

Abstract: The present invention provides an androgen receptor antagonistic agent and a superior prophylactic or therapeutic agent for hormone-sensitive cancer, which contain a compound of the formula: wherein, R1 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R2 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R3 is a hydrogen atom, a hydrocarbon group which may have substituent(s), an acyl group or a heterocyclic group which may have substituent(s), R4 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, and R5 is a cyclic group which may have substituent(s); or a salt thereof, or its prodrug.

Abstract: Polyurethane resin water dispersion being good in storage stability and excellent in initial adhesion and resistance to moist heat, and aqueous polyurethane adhesive employing the polyurethane resin water dispersion. The polyurethane resin water dispersion is produced in the manner that polyisocyanate is allowed to react with polycaprolactone polyol comprising polycaprolactone polyol having a number average molecular weight of not less than 3,000 and active-hydrogen-group-containing compound having anionic group, to synthesize isocyanate terminated prepolymer, first, and, then, the isocyanate terminated prepolymer thus produced is allowed to react with polyamine in water. The use of the polyurethane resin water dispersion can produce the aqueous polyurethane adhesive having improved storage stability, initial adhesion and resistance to moist heat.

Abstract: A process for easily and industrially advantageously producing both a tricyclic fused heterocyclic derivative having acetylcholinesterase inhibitory activity and an intermediate for the derivative. The process for producing the target compounds comprises the following reaction.

Abstract: The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervious system function modulators, and pancreatic function modulators, and (2) development of receptor binding assay systems using the expression of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.

Abstract: A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Abstract: A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is further substituted, Ring C is a dihydrofuran-ring which may be further substituted and R is hydrogen atom or an acyl group or a salt thereof has an excellent lipid peroxidation inhibitory activity and is useful as a lipid peroxidation inhibitor.

Abstract: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2—Z is not —X1—X2—CH2—Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

Abstract: The present invention provides a process for producing an intermediate for thienopyrimidine derivatives having the GnRH antagonistic activity at an industrial large scale. The process for production of the present invention relates to a process for producing a compound represented by the formula (III): wherein respective symbols have the same meanings as those described below, or a salt thereof, which comprises subjecting a compound represented by the formula (I): wherein R1 denotes hydrogen, nitro, halogen, phthalimido, mono- or di-(alkylcarbonyl)amino or alkoxy, or a salt thereof, to an acid halogenating reaction, which is successively reacted with malonic acid ester and magnesium alkoxide, treated with an acid, and reacted with sulfur and a compound represented by the formula: NCCH2COOR2 [wherein R2 denotes alkyl or aryl], or a salt thereof, in the presence of primary amine.

Abstract: To provide a laminate adhesive that can keep on having adequate adhesiveness and also can prevent the odor and taste of the inherent properties of the content packed by the packing product from being spoiled even after high temperature sterilization treatment, such as the hot-water spray sterilization treatment, the hot-water rotary sterilization treatment or the steam sterilization treatment, to provide a usage of the laminate adhesive, the laminate adhesive comprises a curing component containing polyisocyanate and a base component containing polyol, wherein a silane coupling agent is contained in at least the curing component. Preferably, the silane coupling agent is mixed with both of the curing component and the base component. Further preferably, epoxysilane is mixed with the curing component and also aminosilane and oxyacid of phosphorus or derivative thereof are mixed with the base component.

Abstract: The protein of the present invention and a DNA encoding the same can be used as therapeutic/prophylactic agents for diseases such as infectious diseases. The protein of the present invention is also useful as a reagent for screening a compound or its salt capable of promoting or inhibiting the activity of the protein of the present invention. Furthermore, a compound or its salt inhibiting the activity of the protein of the present invention and a neutralization antibody inhibiting the activity of the protein of the present invention can also be used as therapeutic/prophylactic agents for diseases such as bronchial asthma, chronic obstructive pulmonary disease, etc.

Abstract: A KiSS-1 peptide or a salt thereof can be produced in a large scale by subjecting a fusion protein or peptide in which a KiSS-1 peptide is ligated to the N-terminal of a protein or peptide having cysteine at the N-terminal, to the reaction of cleaving the peptide bond on the amino acid side of the cysteine residue.

Abstract: According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.

Abstract: The solvent-free two-component adhesive composition of the present invention is prepared by a polyol component (A) and a polyisocyanate component (B), wherein the composition comprises at least one polyol component having crystallinity and selected from the group consisting of a polyester polyol, a polyether polyol, a polycarbonate polyol and a polyurethane polyol in an amount of 3 to 50% by weight relative to the total weight of the components (A) and (B). The adhesive composition has the initial viscosity of about 100 to 1,500 mPa·s (in particular, 100 to 1,000 mPa·s) at 70° C. immediately after the components (A) and (B) are mixed together, and the increasing ratio of viscosity after the composition is stood at 70° C. for 10 minutes to the initial viscosity of 120% or less. According to the present invention, a composite laminated film having the good external appearance can be produced simply and effectively.

Abstract: TNF-&agr; inhibitors containing a heterocyclic compound having angiotensin II antagonistic activity which are useful as preventives/remedies for inflammatory diseases, etc.