Abstract: A system for releasing a drug specifically in the colon of the gastrointestinal tract, which comprises a drug (b) coated with an organic acid-soluble polymer material (a), and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract; a colon-specific drug release oral preparation, which comprises a composition comprising a drug (b) coated with an organic acid-soluble polymer material (a) and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract, said composition being coated with an enteric coating polymer material (d). The invention provides a drug release system and a preparation which utilize enterobacteria, which do not form harmful substances due to the release-starting mechanism, show rapid degradation, and have higher colon specificity.

Abstract: The present invention relates to a pharmaceutical composition useful for rapid disintegration, which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution. Since rapid disintegration of the pharmaceutical composition of the present invention and rapid dissolution of the medicament contained in the preparation can be made in the digestive tracts pH-independently, good bioavailability can be attained.

Abstract: The present invention relates to a novel potassium channel protein expressed exclusively in the brain, a gene encoding this protein, a vector containing this gene, a host cell containing this vector, and so on.

Abstract: The invention provides for novel compressed tablets capable of rapidly disintegrating in aqueous solutions, comprising at least one non-saccharide water soluble polymer, which are free of organic solvent residues, and methods of making such pharmaceuticals.

Abstract: The invention provides a hydrogel-type sustained-release preparation comprising (1) at least one drug, (2) an additive which insures a penetration of water into the core of the preparation and (3) a hydrogel-forming polymer, wherein said preparation is capable of undergoing substantially complete gelation during its stay in the upper digestive tract such as stomach and small intestine and is capable of releasing the drug in the lower digestive tract including colon. By the preparation of the invention, the drug is efficiently released and absorbed even in the colon so that a steady and sustained release effect can be achieved.

Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].

Abstract: The invention provides a tablet and methods for making the tablet comprising a gel-forming material and at least one particle comprising an active agent in contact with a coating material to modify release of the active agent.

Abstract: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.

Abstract: The present invention relates to a pharmaceutical composition useful for rapid disintegration, which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution. Since rapid disintegration of the pharmaceutical composition of the present invention and rapid dissolution of the medicament contained in the preparation can be made in the digestive tracts pH-independently, good bioavailability can be attained.

Abstract: The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containiing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.

Abstract: Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—.

Abstract: 4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine compounds or salts thereof and pharmaceutical compositions containing 4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine compounds, or salts thereof, and a pharmaceutically acceptable carrier. The chemical structure of these compounds is characterized by a difluoro group on a ring carbon atom adjacent to an azepine ring carbon atom substituted with a methylidene group. Pharmaceutical compositions containing these compounds are particularly useful as oxytocin antagonists and are effective in inhibiting threatened premature birth or abortion and precesarean birth, and are effective as a remedy for dysmenorrhea and other such conditions.

Abstract: The present invention relates to sustained-release pharmaceutical compositions for ionic pharmaceutically active substances (excluding ionic prostanoic acid derivatives) containing ionic compounds having opposite charges to those of the active substances and increasing hydrophobicity of the active substances. More specifically, the invention relates to sustained-release pharmaceutical compositions comprising the ionic pharmaceutically active substances and the ionic compounds having opposite charges to those of the active substances and increasing hydrophobicity of the active substances that contain hydrophobic groups in the molecule thereof. The pharmaceutical composition of the invention can exhibit excellent sustained release effect of the active substance, irrespective of water solubility possessed by the ionic pharmaceutically active substances.

Abstract: Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)&dgr; activating effect or a PPAR&dgr;- and PPAR&ggr;-activating effect or a pharmaceutically acceptable salt thereof; pharmaceutical compositions wherein the cholesterol-lowering effect is an LDL-cholesterol-lowering effect; and a method for identifying a compound having a cholesterol-lowering effect characterized by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect thereof. Means for Solution: It is found out that a compound exerting an excellent cholesterol-lowering effect on higher animals such as humans and ape has an effect of activating PPAR&dgr; or PPAR&dgr; and PPAR&ggr;.

Abstract: A pharmaceutical composition for preventing or treating visual function disorders caused by ocular circulatory disorders (for example, ocular hypertension and glaucoma) and visual function disorders based on ciliary tension (for example, myopia) whose active component is a vasopressin antagonist.

Abstract: A tricyclic pyrrole or pyrazole derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof, which shows strong affinity and selectivity for the 5-HT2C receptor and is useful for the treatment of central nervous system diseases such as sexual disorders, eating disorders, anxiety, depression and sleeping disorders. (In the above formula, each symbol means as follows; Y ring: an unsaturated five-membered ring which may have 1 to 3 of one or more types of hetero atom(s) each selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom or an unsaturated six-membered ring having 1 or 2 nitrogen atom(s), X: a bond or a carbon atom, a double bond or a single bond, V: a nitrogen atom or a group represented by a formula CH, and A: a straight or branched lower alkylene group which may be substituted with a halogen atom or a cycloalkyl group).

Abstract: Composition and methods for treating ocular allergic reactions are disclosed. In particular, the invention is directed to compounds which inhibit human conjunctival mast cell degranulation.

Abstract: An anti-Helicobacter pylori pharmaceutical composition containing a 1-hydroxy-3-methyl-quinolone derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. Since it shows antibacterial action upon Helicobacter pylori, this invention is effective for the treatment or prevention of infection with Helicobacter pylori in human and infection with related bacteria belonging to the genus Helicobacter in animals. Also, the anti-Helicobacter pylori pharmaceutical composition of the present invention is useful for the prevention (including prevention of relapse) or treatment of diseases of the upper digestive organs, such as peptic ulcers (e.g., gastric and duodenal ulcers), inflammations (e.g., acute or chronic gastritis or duodenitis) and gastric cancer, as well as MALT (mucosa-associated lymphoid tissue) lymphoma or chronic heart diseases.

Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.

Abstract: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. The compound has an antagonistic effect on muscarinic M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.