Abstract: A process for preparing a compound represented by the following formula: wherein each symbol is as defined below, or a salt thereof, characterized by subjecting a compound represented by the following formula: wherein R1 is an electron-attracting group; R2, R3, R4, R5, R6 and R7 are each a hydrogen atom, a halogen atom, an optionally substituted amino group, an optionally substituted hydroxyl group, an optionally substituted thiol group, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group, provided that R6 and R7 may be united to form a ring; and R8 is a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, to a ring-closing reaction.

Abstract: This invention relates to a novel metalloprotease having a proteolytic activity, its partial peptide or a salt either of them, a DNA coding for the protein, a recombinant vector comprising the DNA, a transformant carrying the recombinant vector, a process for producing the protein, a pharmaceutical composition comprising the DNA, an antibody against the protein, a method for screening for a compound which activates or inhibits a proteolytic activity of the protein, a kit for screening for the compound, and a compound which activates or inhibits a proteolytic activity of the protein which is identified by the screening method or the kit. The DNA coding for the protein of the present invention can be used as a therapeutic and prophylactic composition for a variety of diseases including diabetic nephropathy, glomerulonephritis, pulmonary fibrosis, hepatolienal fibrosis, hepatocirrhosis, osteopetrosis and herniated disk.

Abstract: This invention relates to a novel polypeptide involving in the modulation of central nervous system function, circulatory function, immune function, gastrointestinal function, metabolic function, reproductive function, etc., it can be used as a drug for treating or preventing a variety of diseases, e.g. HIV infection or AIDS (acquired immune deficiency syndrome) or the like.

Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.

Abstract: An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.

Abstract: The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone derivatives for bone diseases and chondropathy: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 is a hydrogen atom or hydrocarbon group; R3 is a hydrogen atom, hydrocarbon group or halogen; n is an integer of 0-3; or a salt thereof.

Abstract: Novel 2,4-oxazolidinedione compounds of the formula: wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is —CO—, —CH(OH)— or —NR3— (wherein R3 is an alkyl group which may be substituted); m is 0 or 1; n is 0, 1 or 2; X is CH or N; A is bivalent straight or branched hydrocarbon chain residue having 1 to 7 carbon atoms; R1 and R2 each are hydrogen or an alkyl group, or R1 and R2 are combined with each other to form a 5- to 6-membered heterocyclic group optionally containing nitrogen; L and M each are hydrogen, or L and M are combined with each other to form a bond, or pharmaceutically acceptable salts thereof, having excellent hypoglycemic and hypolipidemic activities and are useful as anti-diabetics or hypolipidemic agents.

Abstract: 1,3-Azole derivatives, pharmaceutical compositions thereof and methods for regulating the function of retinoid-related receptors with 1,3-azole derivatives are disclosed. Such regulation may be useful for preventing or treating diabetes, preventing or treating hyperlipidemia, preventing or treating impaired glucose tolerance (IGT) or for preventing transition from impaired glucose tolerance to diabetes.

Abstract: DNA primers effective in screening G protein coupled receptor protein-encoding DNA fragments are provided. The primers which are complementary to nucleotide sequences that are in community with (homologous to) the nucleotide sequences encoding amino acid sequences corresponding to or near the first membrane-spanning domain or the sixth membrane-spanning domain each of known various G protein coupled receptor proteins were designed and synthesized. Methods of amplifying G protein coupled receptor protein-encoding DNAs using the above DNA primers, and novel target G protein coupled receptor protein-encoding DNAs are also provided. Screening of DNA libraries can be efficiently carried out. Human pituitary gland or amygdala-derived and mouse pancreas-derived G protein coupled receptor proteins, etc.

Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula: wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula: wherein R3′ is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5′ wherein n is 2 or 3, and R5′ is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6′ wherein n is 2 or 3, and R6′ is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyanot carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonyl-methyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract: The present invention provides, as an industrially advantageous production method, a method of producing a compound represented by the formula (III)

Abstract: To provide a composition having a steroid C17,20-lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the pophylaxis or treatment of prostatism and tumors such as beast cancer and the like.

Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, pplycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.

Abstract: A bromine-impregnated activated carbon wherein the contents of any alkali metal, any alkali earth metal and iron are not higher than 0.3 wt % and the content of bromine is not lower than 3 wt %, with respect to the weight of a material activated carbon. The bromine-impregnated activated carbon has improved adsorption characteristics to the alkyl sulfides, which have not been sufficiently removed by activated carbons prepared by the conventional techniques. Further, variations in the absorption characteristics can be reduced and the activated carbon can exhibit a stable performance in removing the alkyl sulfides.

Abstract: Galanin receptor proteins, production and use thereof including screening of galanin receptor agonists and antagonists are provided. Galanin receptor proteins, etc. or salts thereof, partial peptides thereof, DNAs coding for the above galanin receptor protein, processes for producing the above receptor protein, methods of screening for a galanin receptor agonist and/or antagonist or screening kits therefor, agonist and/or antagonist compounds or salts thereof obtained by the above screening method or the screening kit, pharmaceutical compositions containing the above compound or its salt, and antibodies against the above receptor protein are provided. It is allowable to efficiently screen a galanin receptor agonist or antagonist by using the galanin receptor protein, the partial peptide thereof, the galanin receptor protein-encoding DNA, the receptor protein-containing cell or its membrane fraction.

Abstract: D-mannitol having a specific surface area of not less than about 1 m2/g is disclosed. The D-mannitol shows improved compressibility and is useful as an excipient.

Abstract: The present invention provides a composition for neurotrophic action which comprises a compound of the formula: wherein Ar is an optionally condensed phenyl group which may be substituted; n is an integer of 1 to 10; R is a hydrogen atom or a hydrocarbon group which may be substituted; and Y is an amino group which may be substituted or a nitrogen-containing saturated heterocyclic group which may be substituted; or a salt thereof, which compounds are useful for preventing and/or treating (1) neurodegenerative diseases (e.g. senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, Creutzfelt-Jakob disease, amyotrophic lateral sclerosis, diabetic neuropathy, etc.), (2) neuropathy in cerebrovascular diseases (e.g. impairment of cerebral blood flow based on cerebral infarction, cerebral hemorrhage, cerebral sclerosis, etc.), brain trauma, spinal cord injury, cerebritis sequela and cerebral palsy, (4) mental diseases (e.g.

Abstract: A novel compound of the formula: wherein R1 is a halogen atom, an optionally substituted heterocyclic, hydroxy, thiol or amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, or an optionally esterified or amidated carboxy group; B is an optionally substituted aromatic group; Y is a divalent aliphatic hydrocarbon group, or a salt thereof, which have an excellent insulin secertion-promoting and blood sugar-depressing effect, and useful in agents for diabetes.