Abstract: The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase. 4-Substituted aryl-5-hydroxyisoquinolinone derivatives, represented by a general formula (1) and their pharmacologically acceptable addition salts.

Abstract: A process for the industrial production of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (Compound I), an effective immunosuppressant. The process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride or a hydrate thereof includes the steps of reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to form ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate; reducing the resulting ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, followed by mesylation, iodination and nitration, to form 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene; forming 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol using a formaldehyde solution; and reducing the resulting 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol to form the desired product.

Abstract: There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid ? antagonistic activity and are useful for the treatment or prevention of side effects which are caused by ? receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

Abstract: The invention provides novel (2S)-2-ethylphenylpropanoic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor (PPAR) ? to activate and exhibit lipid-lowering effect, inhibitory effect on the arteriosclerosis, antiobesity effect, blood glucose-lowering effect, etc., their addition salts, and their medicinal compositions. (2S)-2-Ethylphenylpropanoic acid derivatives represented by a general formula (1) [wherein R1 denotes a halogen atom or trifluoromethyl group, R2 denotes a hydrogen atom, halogen atom or trifluoromethyl group, and, when R2 denotes a hydrogen atom, R3 denotes a halogen atom or trifluoromethyl group and, when R2 denotes a halogen atom or trifluoromethyl group, R3 denotes a hydrogen atom, halogen atom or trifluoromethyl group], and their addition salts.

Abstract: The invention is to provide an oral solid pharmaceutical that is uniform in the content of KRP-197, having bladder-selective anticholinergic activity, being a therapeutic drug for pollakiuria and urinary incontinence, and being active with a very low dosage, that can be taken quantitatively, and that is easy in the handling. Since KRP-197 becomes unstable to light under the influence of additives, the invention is to select the additives to be used and to obtain a pharmaceutical with high stability. By formulating KRP-197 with drug-making carriers, a pharmaceutical that is uniform in the content, capable of taking quantitatively and easy in the handling has been provided. Furthermore, by using polyvinyl pyrrolidone for binder and by making into tablet coated with a coating base containing titanium dioxide and ferric oxide, a pharmaceutical capable of taking quantitatively and excellent in the light stability has been provided.

Abstract: Novel bicycloamide derivatives (general formula (1)) and pharmaceutically acceptable salts thereof effectively inhibit DPP-IV. The bicycloamide derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(4-carbamoylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Abstract: Preparation of (S)-2-[[3-[N-[4-[(4-fluorophenoxy)phenyl]methyl]carbamoyl]-4-methoxyphenyl]methyl]butanoic acid (referred to as compound (I)) on an industrial scale lies in the finding of crystals homogeneous and excellent in the stability and the establishment of a preparative process thereof. Novel crystals of compound (I) homogeneous and excellent in the stability characterized by exhibiting the diffraction angles (2?) at at least 17.7°, 19.0° and 24.1° in the X-ray powder diffraction are provided by recrystallizing from an alcoholic solvent and purifying by acid-base treatment.

Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

Abstract: Upon performing the clinical study of (S)-2-[3-[N-[4-(4-fluorophenoxy)benzyl]carbamoyl]-4-methoxybenz yl]butanoic acid (hereinafter abbreviated as KRP-101), of which improvement in the lipidmetabolism is expected in a microdose, no oral solid dosage form that allows KRP-101 to be administered quantitatively has been embodied. After mixing KRP-101 with additives (excipient, disintegrator and lubricant), the mixture is granulated, pressed into tablets and coated with coating agent, thereby film-coated tablets uniformly containing a small amount of KRP-101 are obtained, making it possible to administer amicrodose of KRP-101 quantitatively on clinical study.

Abstract: A compound as represented by the general formula (I) shown below exhibits high antibacterial activity against gram-positive bacteria, in particular, such drug-resistant bacteria as mRNA, PRSP and VRE: wherein R1 is a methyl group, a fluoromethyl group, a methoxymethyl group, an acetoxymethyl group, a hydroxymethyl group or a methylene; R2 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable cation and an ester of a prodrug; R3 is a hydrogen atom or a halogen atom; R4 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, a fluoromethyl group, a trifluoromethyl group or a fluorine atom; and R5 is a hydrogen atom or a fluorine atom, with exceptions where R1 is a methyl group, R4 and R5 are at the same time a hydrogen atom, and R3 is a fluorine atom.

Abstract: OBJECT To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. SOLVING MEANS There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe.

Abstract: A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; R is a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylcarbonyl group, or a C1 to C6 alkylsulfonyl group; m is 1 or 2; and n is 2 or 3.

Abstract: The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor ? (PPAR?) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.

Abstract: A method of treating multiple sclerosis including administering Interferon-? and a phosphodiesterase inhibitor in combination in a therapeutically effective amount.

Abstract: A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): wherein the rings A and B are each a benzene ring which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring having a hydrogen atom substituted with a nitrogen atom; R1 and R2 are each independently a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylsulfonyl group, a C1 to C6 alkylcarbonyl group, or a C1 to C6 alkoxycarbonyl group, or R1 and R2 are bound to one another to form the ring D; m is 1 or 2; n is 2 or 3; and q is an integer from 1 to 4.

Abstract: A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof: wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring) that are each independently selected from the group consisting of a halogen atom, a substituted or unsubstituted C1 to C6 alkyl group, and a substituted or unsubstituted C1 to C6 alkoxyl group; R is a C1 to C6 alkylsulfonyl group, a C1 to C6 alkylcarbonyl group, a C1 to C6 alkoxycarbonyl group, or a formyl group; m is 1 or 2; n is 2 or 3; and q is 1 or 2.

Abstract: This invention relates to a medicament containing as an active ingredient, a novel propanolamine having a 1,4-benzodioxane ring or a pharmaceutically acceptable salt thereof: The present compound is represented by the above formula wherein R1-3 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1–C6)alkyl group, a (C1–C6)alkoxy group, a (C1–C6)alkylsulfonamido group, or a phenyl group; R4-5 each represents a hydrogen atom or a (C1–C6)alkyl group; and A represents any of a benzene ring, a pyridine ring and a pyrimidine ring. This compound is useful as a prophylactic or therapeutic agent for diabetes, obesity, hyperlipemia, depression, a respiratory disease, or a gastrointestinal disease.

Abstract: A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; m is 1 or 2; and n is 2 or 3.

Abstract: The present invention provides diaryl ether derivatives that exhibit significant immunosuppressive effects with less side effects. The diaryl derivatives of the present invention are represented by the following general formula (1): one example is 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propanediol.

Abstract: Phenoxyalkylcarboxylic acid derivative represented by the following formula, wherein R1 indicates hydrogen atom, methyl group or ethyl group, m is an integer from 2 to 5, and n is an integer from 3 to 8, X1 and X2 each independently represent sulfur atom, oxygen atom, sulfinyl group or sulfonyl group, proviso X1 and X2 are not simultaneously oxygen atom; their alkali salts and hydrates thereof are useful as antiallergic agents.