Abstract: Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

Abstract: Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

Abstract: A sustained-release pranoprofen preparation is disclosed. The preparation comprises an effective amount of pranoprofen and one or more sustained-release components selected from the group consisting of oily components, water-soluble components, water-insoluble components, and intestinally soluble components. It controls release of pranoprofen and lowers the maximum pranoprofen concentration in blood, maintaining its concentration in blood at a certain level for a long period of time. It reduces risks of side effects and can effectively treat diseases with dosing once or twice a day.

Abstract: A diclofenac sodium plaster has a backing material and a paste spread on the backing material. The paste is composed of diclofenac sodium, a penetration enhancer composed of 1-menthol and propylene glycol, and a hydrophilic base composed principally of a water-soluble polymer.

Abstract: A composition for foaming preparation comprising (a) an organic acid of which the crystal surface is coated with a sugar and (b) a carbonate is disclosed. In the composition, an organic acid is completely shut off from a carbonate by a sugar coating so that the acid does not react with the carbonate over a prolonged storage time. When the composition is put into mouth, the sugar which covers the acid is readily dissolved, allowing the acid and the carbonate to react and to generate carbon oxide gas. An excellent foaming calcium preparation can be produced by using calcium carbonate as the carbonate or by adding other salt of calcium to the composition. Such a calcium preparation gives a good taste and favorable feeling upon administration. It is especially suitable for regular administration of calcium over an extended period of time.

Abstract: Quinoline derivatives of the formula, ##STR1## wherein > A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

Abstract: Compressed-molded preparations are disclosed. In the preparation coated granules of a pharmaceutical composition are compressed and molded together with non-coated component(s) containing 10% or more by weight of non-swelling polymers. According to the preparation there is little breakdown of the coating of coated granules at the time of compressing and molding, and the rate of disintegration, and in turn, the release rate of the pharmaceutical component, can be freely controlled or modulated.

Abstract: Described herein are antidirarrheal compositions containing loperamide hydrochloride as an effective ingredient and a saccharide, for example, a monosaccharide, oligosaccharide or sugar alcohol in an amount as much as at least 3,000 times the weight of loperamide hydrochloride.

Abstract: A sustained-release tablet is disclosed. The tablet is a combination of powder (A) comprising an oil component, water insoluble polymer, or both, and a pharmaceutically active component and powder (B) comprising a water soluble polymer and a pharmaceutically active component. An ideal release rate for individual pharmaceutically active component can easily be ensured by controlling its release rate by changing the ratio of powders (A) and (B).

Abstract: Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus is useful as a antimicrobial agent.

Abstract: A process for preparing 21-desoxyprednisolone 17-esters of formula (IV) is disclosed. ##STR1## The process comprises reacting a prednisolone 17.alpha.,21-cyclic orthoester with an acid in a 40-60% lower alcohol solution to produce a prednisolone 17-ester, sulfonylating the prednisolone 17-ester into a prednisolone 17-ester 21-sulfonate, and reacting the sulfonate with an alkali metal iodide in methyl ethyl ketone in the presence of a lower fatty acid to produce the compound of formula (IV). The process ensures economical industrial production of high purity 21-desoxyprednisolone 17-esters, an excellent local anti-inflammatory medicine, in a high yield by simple procedures.

Abstract: A triazole derivative is disclosed. The compound have a general formula, ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together form a lower alkylene group, R.sup.3 represents a lower alkyl group, and n denotes an integer of 0 to 2, provided that not both R.sup.1 and R.sup.2 are a hydrogen atom at the same time. The triazole derivatives and their salts are effective for curing or preventing deep-seated mycoses, e.g. mycotic meningitis, mycotic infectious diseases of respiratory organs, fungemia, and urinary tract mycosis.

Abstract: Ointments are disclosed, which contain (a) 0.05-1 wt. % of deprodone propionate and (b) 89-99.95 wt. % of a base formed of white petroleum and a liquid hydrocarbon. The ointments may additional contain (c) 1-10 wt. % of a polyhydric alcohol.

Abstract: Antimycotic external imidazole preparations are disclosed. They contain the following ingredients:(a) 0.1-5 wt. % of (E)-1-[2-methylthio-1-[2-(pentyloxy)phenyl]ethenyl]-1H-imidazole hydrochloride;(b) 0.01-3 wt. % of a basic substance; and(c) an external preparation base.

Abstract: Water-containing external preparations are disclosed, which contain, as essential ingredients, (a) 0.05-1 wt. % of deprodone propionate and (b) 1-20 wt. % of a polyhdric alcohol.

Abstract: Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus is useful as an antimicrobial agent.

Abstract: An external adhesive preparation comprising a steroid for treatment of skin diseases in admixture with an adhesive gel base comprising as essential components a water-soluble high molecular weight compound, water and a water-retaining agent. The external adhesive preparation is useful for treatment of skin diseases by applying the preparation spread on a soft support directly to diseased parts on the skin, thereby administering the contained steroid to the skin.

Abstract: Steroid derivatives represented by formula (I) are disclosed. ##STR1## wherein R is a hydrogen atom, a halogen atom, a hydroxy group, or a group --OCOR.sub.1, wherein R.sub.1 is a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group, a cycloalkyl group, or an aryl group. The compounds are useful for curing or alleviating inflammation or rheumatism.

Abstract: An expectorant comprising a hydroxyalkylcysteine derivative of the following formula (I) is disclosed. ##STR1## wherein n represents an integer of 1 to 4. The expectorant is stabile, has little side effects and toxicity, and exhibits an excellent expectorant effect.

Abstract: A platinum complex having the following formula (I) is disclosed, ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each independently represents a methyl group or an ethyl group, and the configuration of 1,2-diaminocyclohexane is either cis-, trans-l-, trans-d-, or trans-dl-.The compound possess excellent antitumor activity with a high therapeutic index and abundant water solubility, and thus are effective as an antitumor agent.