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

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: A wood preservative that comprises as an active ingredient a Piper methysticum, plant or a processed product thereof or a compound represented by Formula (I): wherein R1, R2, R3, R4 and R16 are same or different and each denotes a hydrogen atom, hydroxy or a C1-4 alkoxy, or R1 and R2 are taken together to form a group represented by —O—(CH2)n—O— wherein n is an integer of 1 to 3, R5 is a C1-4 alkoxy and X is —CH═CH—, —CH2—CH2— or epoxyethylene, and the bond: denotes a single bond or a double bond can prevent the attacking wood by an insect harmful to the wood and also prevents the appearance and the growth of a wood-rotting fungus or a wood- staining fungus while being highly safe to humans and animals without exerting no adverse effect on the environment.

Abstract: The betacellulin mutein or its salt of the present invention is useful for better therapeutic drug for diabetes. Since they have intact BTC activity and reduced EGF activity, and no antigenicity-related problems.

Abstract: Genes encoding novel proteins named AID (Activation-Induced cytidine Deaminase), that are structurally related to APOBEC-1, an RNA editing enzyme, and have a cytidine deaminase activity similar to APOBEC-1, have been found by preparing cDNA libraries from mouse B cell clone CH12F3-2 (which undergoes class switch recombination from IgM to IgA at an extremely high rate after activation of the cells by stimulation with cytokines), with and without stimulation with cytokines, and performing subtraction cloning using the libraries.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula 1

Abstract: The invention relates to metastin derivatives represented by the formula: X-AA1-AA2-AA3-AA4-Z (I), or a salt thereof, or a pro-drug thereof, which have cancer metastatis suppressing activity and cancer proliferation suppressing activity. The invention also relates to the use of these derivatives as drugs for preventing or treating cancers.

Abstract: The present invention provides a method of producing an optically active form of a compound represented by the formula (I) having a steroid C17,20-lyase inhibitory activity and is useful as an agent for the prophylaxis or treatment of prostatism, tumor such as breast cancer, and the like or a salt thereof, which method includes reacting a mixture of optically active compounds of a naphthalene derivative represented by the formula: wherein R is a nitrogen-containing heterocyclic group, R1 is a hydrogen atom, a hydrocarbon group or an aromatic heteromonocyclic group, R2 is a hydrogen atom or a lower alkyl group, * shows the position of an asymmetric carbon, R3, R4, R5, R6, R7, R8 and R9 are each independently a hydrogen atom, a hydrocarbon group, a hydroxy group, a thiol group, an amino group, a carbamoyl group, an acyl group or a halogen atom, and R7 is bonded with R6 or R8 to form, together with a carbon atom on a naphthalene ring, a 5 or 6-membered ring containing an oxygen atom, with an op

Abstract: The present invention relates to novel secretory polypeptides and precursor proteins thereof, which show a high homology to MIA (melanoma inhibitor activity)/CD-RAP (bovine cartilage-derived retinoic acid-sensitive protein); are specifically expressed in the cartilage tissue; and have an effect on the cartilage differentiation. The polypeptides and the DNAs encoding the same can be used for the diagnosis, treatment, or prevention of bone and joint diseases or pathological angiogenesis. As well, the polypeptides are useful as a reagent for screening a compound that promotes or inhibits the activity of the polypeptides. The antibody to the polypeptides can be used for the detection, quantification, or neutralization of the polypeptide in a test sample fluid. Further by using the promoter of the present invention, a therapeutic protein can be expressed predominantly in the cartilage tissue for a gene therapy.

Abstract: The present invention is intended to provide excellent preventives and/or remedies for heart diseases. Specifically, the present invention provides heart muscle cell apoptosis inhibitors, preventives and/or remedies for heart diseases, comprising a compound represented by the following formula: wherein R represents an optionally substituted hydrocarbon group, an optionally substituted aromatic heterocyclic group, or an optionally substituted amino group; or a salt thereof.

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: The punch coated with Cr-Dopé-N is advantageous as a punch for preparing tablets containing an acidic substance or an adhesive substance and is excellent in corrosion resistance and releasing property.

Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

Abstract: This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein. In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein can be obtained in high yield.

Abstract: Crystals of (E)-4-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino]-4-phenylbutyric acid (provided that crystals having a melting point of 126° C. to 127° C. are excluded), which have an excellent anti-diabetic action.

Abstract: A method for removing from a peptide the diketone of the methionine residue, and a method for manufacturing a peptide or salt thereof which does not possess an N-terminal methionine residue, characterized by having a peptide or salt thereof which possesses a diketone of the optionally oxidized N-terminal methionine residue react with 3,4-diaminobenzoic acid or a salt thereof in the presence of acetic acid and sodium formate, formic acid and sodium formate, or formic acid and sodium acetate.

Abstract: This invention relates to cell lines that are obtained using cultured cell lines derived from human liver as a host and that stably express a number of human cytochromes P450. The human liver-derived cultured cell lines of the present invention are useful in, for example, analyzing an enzyme participating in the metabolism of xenobiotics or endogenous substrates, because of their stable expression of human cytochromes P450 CYP1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C9, 2D6, and 3A4.