Abstract: The present invention provides diaryl sulfide 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-benzyloxyphenylthio)-2-chlorophenyl]propyl-1,3-propanediol.

Abstract: Solid preparations for oral use for facilitating the administration in a small dose of KRP-297, which is a ligand common to peroxisome proliferator-activated receptors PPAR ? and PPAR ? (i.e., nuclear receptors) and has an effect of ameliorating insulin resistance, which contain the drug ingredient in a uniform content and can be easily and quantitatively taken. By preparing solid preparations for oral use composed of a trace amount of the drug ingredient together with pharmaceutical carriers, it is possible to provide tablets which contain the drug component in a uniform content and can be easily and quantitatively taken.

Abstract: Oxazolidinones having a bicyclic[3.1.0]hexane containing 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, and wherein the variables R1, R2, R3, R4, R4a, A, Ar, HAr, n, r, and s are as defined herein.

Abstract: With compounds for drugs, agricultural chemicals, etc., the invention provides a novel method for superposing molecular structures of those compounds.

Abstract: Oxazolidinones having a bicyclic[3.1.0]hexane containing 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, and wherein the variables R1, R2, R3, R4, R4a, A, Ar, HAr, n, r, and s are as defined herein.

Abstract: The invention provides novel substituted carboxylic acid derivatives that bind to receptor as ligands of human peroxisome proliferator-activated receptor (PPAR) to activate it and exhibit potent triglyceride-lowering action, cholesterol-lowering action and blood glucose-lowering action, and processes for preparing them. The invention relates to substituted carboxylic acid derivatives represented by a general formula (1), their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

Abstract: The invention provides alkali metal salt of 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide and its hydrate. A method has been found, wherein, upon preparing KRP-297, the alkali metal salt of KRP-297 and its hydrate are formed in the reaction system and, after separation and purification, they are freed again from salt, thereby KRP-297 can be advantageously purified industrially for preparation.

Abstract: The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by a general formula (1) wherein R1 denotes a chlorine atom, bromine atom, nitro group, trifluoromethoxy group, ethoxy group, propoxy group or isopropoxy group, and R2 denotes a hydrogen atom or chlorine atom, their medicinally acceptable salts, their hydrates and a process for preparing them.

Abstract: A homogeneous crystal having excellent stability which is suitable for the industrial-scale production of 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide (KRP-297). The novel crystal of KRP-297 is produced through recrystallization from an alcohol solvent. It is characterized by having diffraction angles (2&thgr;) at at least 9.7°, 15.0°, and 22.5° in X-ray powder diffractometry.

Abstract: The invention creates a very high-novelty medicinal drug for the carbohydrate and lipid metabolism-related diseases by finding out an inhibitory substance or antagonist against PPAR &agr; and PPAR &ggr;, and relates to an application of fatty acid CoA thioester that was found out as an active inhibitory substance against peroxisome proliferator-activated receptor &agr; and &ggr; (hereinafter referred to as PPARs) to the assay of medicinal drug, and a use of fatty acid CoA thioester for medicinal drug.

Abstract: The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation action of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them. The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein A denotes a phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and a process for preparing them.

Abstract: The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives that bind to receptor to activate as ligands of human peroxisome proliferator-activated receptor (PPAR) and exhibit blood glucose-decreasing action and lipid-decreasing action, and processes for preparing them. It relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein the bond mode of A denotes —CH2CONH—, —NHCONH—, —CH2CH2CO— or —NHCOCH2—, and B denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, halogen atom, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and processes for preparing them.

Abstract: O-anisamide compounds and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them, wherein the o-anisamide compounds are represented by a general formula (1) [wherein R denotes a carboxyl group, carboxymethyl group or CH2CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, and their hydrates.

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: The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes for the preparation of both. The compounds are 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives represented by the formula (1) where A denotes a single bond or methylene (CH2), Y denotes a nitrogen atom or ═CH—, V denotes a single bond or methylene (CH2), T denotes a hydroxyl group, amino group, lower alkoxycarbonyl group, carboxyl group, aldehyde group or the like, Q denotes a halogen atom, lower alkyl group or lower alkoxy group, and R1 denotes a hydroxyl group, lower alkoxy group or the like, and addition salts thereof.

Abstract: Oxazolidinones having a bicyclic[3.1.0] hexane containing 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.

Abstract: A method of treating an industrial waste liquor containing 1-cyclopropyl-7-(3-methyl-1-piperazinyl)-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (gatifloxacin), comprising adding aqueous sulfuric acid to said liquor to form a sulfate of said gatifloxacin, and/or a hydrate of said sulfate; and the sulfate, and/or hydrate of said sulfate, made by said method.

Abstract: The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted heteroquinolinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes for the preparation of both. These compounds relate to 6-substituted heteroquinolinecarboxylic acid derivatives represented by a general formula (1) (wherein A denotes a single bond or methylene (CH2), Y denotes a nitrogen atom or ═CH—, V denotes a single bond or methylene (CH2), T denotes a hydroxyl group, amino group, lower alkoxycarbonyl group, carboxyl group, aldehyde group or the like, R denotes a nitro group, trifluoromethyl group or halogen atom, and R1 denotes a hydroxyl group or lower alkoxy group), and addition salts thereof.

Abstract: The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them. The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein A denotes a pyridyl group or cyclohexyl group], their medicinally acceptable salts, their hydrates and a process for preparing them.

Abstract: The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor &agr; (PPAR&agr;), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride). It relates to a substituted phenylpropanoic acid derivatives represented by a general formula (1), their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.