Abstract: A novel benzamide derivative represented by the following general formula: wherein R represents an alkyl group having 3 to 6 carbon atoms or a salt thereof, and a medicament comprising said derivative as an active ingredient. The medicament has excellent enhancing action on gastrointestinal tract motility, and is orally available with reduced side effects. Therefore, the medicament is extremely useful as an agent for therapeutic treatment of digestive diseases, an agent for improving function of gastrointestinal tract motility and the like.

Abstract: 1H-Imidazopyridine derivatives represented by the following general formula or salts thereof: wherein R1 represents hydrogen atom, hydroxyl group, an alkyl group, a cycloalkyl group, styryl group, or an aryl group; R2 represents hydrogen atom, an alkyl group, a halogen atom, hydroxyl group, amino group, a cyclic amino group, or phenoxy group; ring A represents a homocyclic or heterocyclic ring which may be substituted; R3 represents a saturated nitrogen-containing heterocyclic group; and m represents an integer of from 0 to 3. The derivatives have excellent inhibitory actions against production of TNF or IL-1 and are extremely useful as preventive or therapeutic agents for diseases in which a cytokine is mediated.

Abstract: Aqueous solution, including at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol represented by the following formula: ##STR1## and pharmacologically acceptable salt thereof. The aqueous solution also includes at least one photostabilizer selected from the group consisting of saccharide, sugar alcohol, and polyalcohol. A content of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof is 0.01 to 10% (w/v) based on a volume of the aqueous solution. A content of the at least one photostabilizer is 1 to 50% (w/v) based on the volume of the aqueous solution. The content of the at least one photostabilizer is at least 10% (w/w) based on a total weight of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof. Method of making a stabilized aqueous solution.

Abstract: A percutaneous absorption type preparation comprising a support and a plaster layer laminated thereon, which composes tulobuterol in a proportion of not less than 5 wt % in a dissolution state and an adhesive. The preparation of the present invention retains the active ingredient, tulobuterol, at a high concentration in a complete dissolution state in the plaster layer. Therefore, it is free of time-course changes in drug releasing property and adhesive property caused by precipitation of drug crystals with the lapse of time. The inventive preparation is superior in percutaneous absorption of the drug, particularly percutaneous absorption rate at the initial stage of the administration; shows superior duration of efficacy by maintaining effective blood concentration for a long time; and is associated with less changes with the lapse of time in adhesive property such as adhesion to the skin.

Abstract: Dihydrate crystal of 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperid ino]propionic acid providing high-intensity diffraction peaks at diffraction angles (2.theta.) of about 4.2.degree., 17.0.degree., and 21.3.degree. in a powder X-ray diffraction profile; a medicament comprising the dihydrate crystal; and a process for preparing the dihydrate crystal which comprises the steps of treating a crystalline substance containing an anhydride crystal of the above compound with hydrous acetone, and subjecting the product to drying treatment and moistening treatment.

Abstract: Aqueous solution, including at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol represented by the following formula: ##STR1## and pharmacologically acceptable salt thereof. The aqueous solution also includes at least one photostabilizer selected from the group consisting of saccharide, sugar alcohol, and polyalcohol. A content of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof is 0.01 to 10% (w/v) based on a volume of the aqueous solution. A content of the at least one photostabilizer is 1 to 50% (w/v) based on the volume of the aqueous solution. The content of the at least one photostabilizer is at least 10% (w/w) based on a total weight of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof. Method of making a stabilized aqueous solution.

Abstract: 5-Amino-7-((3S,4S)-3-amino-4-methyl (or ethyl)-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoqu inoline-3-carboxylic acid or a pharmacologically acceptable salt thereof represented by the following formula wherein asymmetric carbon atoms marked with asterisks are in the S-configurations and R.sup.1 represents methyl group or ethyl group; and an antibacterial agent comprising said compound as an active ingredient.

Abstract: A percutaneous absorption preparation comprising a support and, formed on one side thereof, a plaster layer comprising a pressure-sensitive adhesive and tulobuterol in an amount not lower than its saturation solubility in the pressure-sensitive adhesive, the tulobuterol contained in the plaster layer consisting of dissolved tulobuterol and crystalline tulobuterol with the ratio of the content of the crystalline tulobuterol to that of the dissolved tulobuterol being from 0.1 to 10.

Abstract: A benzenesulfonamide derivative represented by the following general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom; R.sup.2 represents a C.sub.1 -C.sub.10 straight- or branched-chain alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group which may be substituted with one or more C.sub.1 -C.sub.6 alkyl groups on its ring, a C.sub.1 -C.sub.6 alkyl group substituted with one or more C.sub.3 -C.sub.8 cycloalkyl groups, 1-adamantylmethyl group, 2-norbornylmethyl group, or a C.sub.1 -C.sub.6 alkyl group substituted with one or more phenyl groups whose benzene ring may have one or more substituents; R.sup.3 represents a hydrogen atom or a lower alkyl group; and n is an integer of from 2 to 4, and a pharmacologically acceptable salt thereof. The present compounds have thromboxane A.sub.

Abstract: A percutaneous preparation of tulobuterol is disclosed, comprising a support having thereon a base layer comprising a pressure-sensitive adhesive containing tulobuterol, the pressure-sensitive adhesive comprising polyisobutylene. The preparation achieves persistent and effective administration of tulobuterol through the skin into the body.

Abstract: A benzamide derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkanoyl group; R.sup.2 represents a hydrogen atom or a halogen atom; R.sup.3 represents a lower alkoxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; A represents C.sub.1 -C.sub.7 alkylene group which may optionally be substituted with a lower alkyl group; X represents a methylene group, an oxygen atom, or a sulfur atom; m represents an integer of from 0 to 3; n represents an integer of from 0 to 3; and p represents an integer of from 0 to 2 and a pharmacologically acceptable salt thereof is provided. These compounds are useful since they have gastrointestinal stimulating activity, and a pharmaceutical composition comprising said compound is useful for the treatment of gastrointestinal diseases.

Abstract: Tricyclic compounds represented by the following formula: ##STR1## wherein X represents --CH.dbd.CH--, --CH.sub.2 O--, or --O--;R.sup.1 represents a lower alkyl group,R.sup.2 represents a hydrogen atom or a lower alkyl group; andn represents an integer of from 1 to 5, pharmacologically acceptable salts thereof, and a method for preparing the same. The present compounds have anti-allergic and anti-histaminic activities and reduced side effects, and are useful as anti-allergic agents and anti-histaminic agents.

Abstract: A benzamide derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkanoyl group; R.sup.2 represents a hydrogen atom or a halogen atom; R.sup.3 represents a lower alkoxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; A represents C.sub.1 -C.sub.7 alkylene group which may optionally be substituted with a lower alkyl group; X represents a methylene group, an oxygen atom, or a sulfur atom; m represents an integer of from 0 to 3; n represents an integer of from 0 to 3; and p represents an integer of from 0 to 2 and a pharmacologically acceptable salt thereof is provided. These compounds are useful since they have gastrointestinal stimulating activity, and a pharmaceutical composition comprising said compound is useful for the treatment of gastrointestinal diseases.

Abstract: A percutaneous preparation of tulobuterol is disclosed, comprising a support having thereon a base layer comprising a pressure-sensitive adhesive containing tulobuterol, the pressure-sensitive adhesive comprising polyisobutylene. .Iadd.In a preferred embodiment, the base layer further contains a thermoplastic resin. .Iaddend.The preparation achieves persistent and effective administration of tulobuterol through the skin into the body.