Abstract: A process for producing a biodegradable polymer having free carboxyl at the &ohgr;-end charcterized by polymerizing a cyclic ester compound in the presence of a hydroxymonocarboxylic acid derivative having protected carboxyl or a hydroxydicarboxylic acid derivative having protected carboxyl, and then deprotecting the thus obtained polymer having protected carboxyl at the &ohgr;-end. Use of the above process makes it easy to control the molecular weight of the target biodegradable polymer and the content of free carboxyl therein, thereby enabling the efficient production of a polymer having a high purity and being contaminated with littel catalyst remaining therein.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, 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, alkylcarbonylmethyl, 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: A method for producing a compound of the formula: (1) in a secondary or tertiary alcohol in the presence of a base, or (2) in the absence of a base is provided.

Abstract: A sustained-release composition containing a hydroxynaphthoic acid salt of a biologically active substance and a biodegradable polymer, a method of its production, and a pharmaceutical composition containing said sustained-release composition.

Abstract: A bypass type prefilled syringe has a tubular body formed with a bypass for establishing communication between front and rear compartments for preliminarily storing medicament and pharmaceutical liquid, respectively. A gasket for dividing interior space of the tubular body into the front and rear compartments includes a plurality of circumferential ribs . A plurality of annular recesses are each formed between neighboring ones of the circumferential ribs. First and second axial slots are formed on the circumferential ribs so as to define a bent outflow path for the pharmaceutical liquid at the time of communication between the front and rear compartments via the bypass.

Abstract: Quickly disintegrating solid preparations which contain: a) an active ingredient; b) D-mannitol having an average particle size of 30 &mgr;m to 300 &mgr;m; c) a disintegrating agent; and d) celluloses.

Abstract: This invention relates to prophylactic or therapeutic drug for diabetic nephropathy or glomerulonephritis, comprising, as an active ingredient, a compound or salt thereof represented by general formula (I) 1

Abstract: A process for conveniently producing a stable protein powder retaining the higher-order structure at a high level which comprises freezing a protein-containing solution at a cooling rate of about −300 to −10° C./min. and then drying.

Abstract: The present invention relates to a protein having a Na+—HCO3− cotransporter activity and a DNA encoding it. The present protein and the present DNA can be used as or for [1] obtaining an antibody and antiserum, [2] constructing an expression system for the present protein, [3] development of a system for measuring the activity of a Na+—HCO3− cotransporter and screening of a drug candidate compound using the same expression system, [4] performing drug design based on the steric structure of a Na+—HCO3− cotransporter protein, [5] a reagent for making a probe or a PCR primer in gene diagnosis, [6] making a transgenic animal, or [7] a composition for gene prevention and/or treatment.

Abstract: Novel acylhydrazine derivatives exhibiting an inhibitory activity against activated blood coagulation factor X, which are compounds of general formula (I) or salts thereof, wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; R1 and R2 are each hydrogen or optionally substituted hydrocarbyl, or alternatively R1 and R2 or the substituent of X1 and R2 may be united to form an optionally substituted ring; X1 and X2 are each free valency, optionally substituted alkylene, or optionally substituted imino; D is oxygen or sulfur; A is —N(R3)—Y— or —N═Y—, R3 is hydrogen, optionally substituted hydrocarbyl, or acyl; Y is an optionally substituted chain hydrocarbon group or an optionally substituted cyclic group; and Z is (1) optionally substituted amino, (2) optionally substituted imidoyl, or (3) an optionally substituted nitrogenous heterocycle group.

Abstract: This invention provides new benzoxazepine compounds represented by the formula: 1

Abstract: A compound represented by the formula: wherein m is 1 or 2, R1 is a halogen or an optionally halogenated C1-2 alkyl; one of R2 and R3 is a hydrogen atom and the other is a group represented by the formula: wherein n is 3 or 4; R4 is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.

Abstract: A method for producing a compound of the formula: wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group and ring A is an imidazole ring which is optionally substituted further, or a salt thereof, which method comprises reacting a compound of the formula: wherein ring A is as defined above, or a salt thereof, and a compound of the formula: R—M1  (II) wherein M1 is an alkali metal atom or a group of the formula: —Mg—Y1 where Y1 is a halogen atom, and R is as defined above, or a salt thereof, and bringing the resulting product into contact with an acid.

Abstract: A nasal preparation comprising a compound represented by the formula: wherein Ring A is an optionally substituted 5- or 6-membered aromatic heterocyclic ring, Ring B is an optionally substituted 5- or 6-membered aromatic homocyclic or heterocyclic ring, R1 is a hydrogen atom, a hydroxyl group or a lower alkyl group, and n is 0 or 1, which has an Na—H exchange inhibiting activity, or a salt thereof exhibits excellent bioabsorbability and an Na—H exchange inhibiting activity superior to that of an oral preparation, thus being useful as a prophylactic and/or therapeutic agent for ischemic heart diseases such as myocardial infarct and arrhythmia.

Abstract: A method for producing a compound represented by the formula: 1

Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.

Abstract: G Protein-coupled receptor proteins originating in the vicinity of rat brain stem and human brain or salts thereof, or peptide fragments thereof or amides, esters or salts of the same; ligands thereto; a method/kit for screening compounds capable of altering the binding properties of the ligands to the G protein-coupled receptor proteins; the compounds or salts thereof obtained by the above screening; antibodies against the G protein-coupled receptor proteins, etc.

Abstract: Disclosed is a sustained-release preparation comprising 1) a polymer of lactic acid having a weight-average molecular weight of about 25,000 to about 60,000 and 2) a physiologically active substance, and which releases the physiologically active substance over a period of at least about 5 months; the sustained-release preparation shows an almost continuous zero order release of the physiologically active substance over a period of as long as about 5 months.

Abstract: A production method of a compound represented by the formula wherein R1 and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R3 is an electron-withdrawing group, and R4, R5 and R6 are each a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, is provided as an industrially advantageous production. method for forming a carbon-carbon bond at the 5-position of oxazole, which method includes reacting a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, with a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, in the presence of an acid or a base.

Abstract: A sustained-release preparation comprising a bioactive substance having an acidic group and a biodegradable polymer having an optionally protected basic group which improves the rate of incorporation of the bioactive substance, suppresses its leakage early after adminstration, and exhibits constantly suppressed release for an extended period of time.