Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1

Abstract: (S)-(−)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperi-dine represented by the formula (IV): 1

Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Abstract: The present invention provides a method for screening or identifying therapeutic or prophylactic agents for renal diseases, which comprises assaying a test substance for the activity of up-regulating the expression of fatty acid-binding protein (FABP), and novel mouse proximal renal tubular epithelial cell lines useful therein. The present invention also provides therapeutic or prophylactic agents for renal diseases comprising, as an active ingredient, an agent having activity of up-regulating FABP expression; agents for up-regulating the expression of FABP, and for treating or preventing renal diseases, which comprise a compound having activity of peroxisome proliferator-activated receptor (PPAR) agonist or carnitine palmitoyltransferase (CPT) inhibitor or the like.

Abstract: The present invention provides a method for screening or identifying therapeutic or prophylactic agents for renal diseases, which comprises assaying a test substance for the activity of up-regulating the expression of fatty acid-binding protein (FABP), and novel mouse proximal renal tubular epithelial cell lines useful therein. The present invention also provides therapeutic or prophylactic agents for renal diseases comprising, as an active ingredient, an agent having activity of up-regulating FABP expression; agents for up-regulating the expression of FABP, and for treating or preventing renal diseases, which comprise a compound having activity of peroxisome proliferator-activated receptor (PPAR) agonist or carnitine palmitoyltransferase (CPT) inhibitor or the like.

Abstract: The present invention provides a novel agent for prophylaxis or treatment of inflammatory bowel diseases for oral administration or intra-intestinal infusion, which comprises as an active ingredient a compound of the formula (I): 1

Abstract: The present invention is to provide a benzenesulfonic acid salt and a benzoic acid salt of (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid represented by the formula (I): wherein * represents an asymmetric carbon, which are excellent in antihistaminic activity and anti-allergic activity, and a process for producing the same.

Abstract: The present invention provides a novel agent for prophylaxis or treatment of inflammatory bowel diseases for oral administration or intra-intestinal infusion, which comprises as an active ingredient a compound of the formula (I): or a pharmaceutically acceptable salt thereof; a use of said active ingredient in preparation of an agent for prophylaxis or treatment of inflammatory bowel diseases; and a method for prophylaxis or treatment of inflammatory bowel diseases.

Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: wherein Ro is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R” (in which the nitrogen atom is protected), R1 and R2 are lower alkyl groups, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.

Abstract: The present invention relates to small molecules according to formula (I) that are potent inhibitors of &agr;L&bgr;2 mediated cell adhesion and which could be useful for the treatment of inflammatory diseases:

Abstract: The present invention discloses an efficient preparation method of spherical fine particles containing a drug for an easily-swallowed, controlled-release preparation comprising the production of drug-containing spherical fine particles (mean particle size: 60-200 &mgr;m) by adding a binder solution to a mixture containing an excipient powder having the property of retaining solvent (and preferably having a mean length of the long axis of 40 &mgr;m or less) and a drug powder (preferably having a mean length of the long axis of 50 &mgr;m or less), followed by high-speed mixing granulation.

Abstract: The present invention discloses sustained release particles having a mean particle size of 300 &mgr;m, or less, comprising a drug-containing core substance coated with a mixed coating of a hydrophobic organic compound-water-insoluble polymer, which prevents sticking during compression molding when producing oral sustained release tablets, a preparation method of those sustained release particles, and a preparation method of tablets using those sustained release particles.

Abstract: The present invention relates to compound of formula (I), that are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.

Abstract: The present invention relates to a method for screening and identifying therapeutic agents or preventive agents for central nervous system diseases which comprises assaying a suppressing effect of a test substance on an expression of a splicing variant transcribed from presenilin-2 gene and to a method for examining central nervous system diseases which comprises detecting an expression of a splicing variant transcribed from presenilin-2 gene in a test sample originated from an animal individual.

Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): 1

Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Abstract: A preparation capable of releasing a medicinal substance at a targeted site in the intestine, wherein the preparation dose not releases medicinal substance in endogastri at all, but can quickly release a medicinal substance when it reaches the desired site in the intestine after a certain period of time from discharge of the preparation from the stomach, and wherein a core material containing a medicinal substance is coated with a mixed film of a hydrophobic organic compound—an enteric polymer.

Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.

Abstract: A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.