Abstract: Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula ##STR1## wherein R.sup.1 is hydrogen, R.sup.2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R.sup.1 and R.sup.2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R.sup.3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R.sup.4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R.sup.5 is hydrogen or methyl, m is 1-2, and n is 0-2.

Abstract: A method of producing diphenyl sulfone compounds of the formula (I) ##STR1## wherein R is an alkyl having 1 to 8 carbon atoms, a cycloalkyl having 3 to 8 carbon atoms, an alkenyl having 2 to 8 carbon atoms or an arylalkyl which may have substituent(s) on the aromatic ring, comprising reacting 4,4'-dihydroxydiphenyl sulfone with a compound of the formulaR--Xwherein R is as defined above and X is halogen, characterized by conducting the reaction in 0.3-1.5 weight parts of an aqueous solvent per weight part of 4,4'-dihydroxydiphenyl sulfone in the presence of 1.5-3 moles of an alkali per mole of 4,4'-dihydroxydiphenyl sulfone. Since the method of the invention permits production of 4-substituted hydroxy-4'-hydroxydiphenyl sulfones, specifically 4-n-propoxy-4'-hydroxydiphenyl sulfone or 4-isopropoxy-4'-hydroxydiphenyl sulfone using an inexpensive solvent, with good selectivity and economical feasibility, they are industrially advantageous.

Abstract: The present invention provides an industrially valuable method for preparing an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound which is useful as a starting material for an optically active benzopyran compound with antihypertensive, coronary blood flow-increasing activities and the like, provides a diastereomeric ester compound which is useful as an intermediate for said epoxy compound and also provides a use of said diastereomeric ester compound in making of said epoxy compound, and further an optically active benzopyran compound which is useful as medicine.

Abstract: The present invention relates to an immunosuppressive agent which comprises at least one compound selected from the compounds of formula ##STR1## wherein R represents a hydrogen atom or an acyl, Y represents carbonyl or hydroxymethylene and represents a single bond or a double bond and their lactones, in an effective amount and a pharmaceutically acceptable carrier; a method of prophylaxis and therapy for suppressing rejection or autoimmune diseases which comprises administering the above-mentioned compound or its lactone in an effective amount; and a novel compound of formula ##STR2## or its lactone.

Abstract: A styryl compound of the formula(I): ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt or an ester thereof is disclosed.Since the compounds of the present invention possess potent and long-lasting leukotriene-antagonistic actions and inhibitory actions against leukotriene, and exhibit better absorption by the oral administration.Further, the compounds of the present invention possess 5-lipoxygenase-inhibitory actions and/or cyclooxygenase-inhibitory actions, inhibitory actions to biosynthesis of LTB4, chemotactic actions against human leucoccyte, chymase-inhibitory actions, inhibitory actions to release of histamine or antihistamine actions.

Abstract: A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.

Abstract: Novel stable, non-hygroscopic 2'-deoxy-2'-methylidenecytidine dihydrate and its methods for production, and compositions with improved solubility containing same and saccharide(s).

Abstract: Novel .beta.-form crystals of 6-(3,6-dihydro-2-oxo-2H-1,3,4-thiadiazin-5-yl)-3,4-dihydro-2(1H)-quinolino ne useful as cardiotonics.

Abstract: The present invention provides a new diastereomer ester compound which is useful as an intermediate in the making of an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound.

Abstract: Phosphite compounds of the formula ##STR1## wherein R.sup.1 is an alkyl having 1 to 22 carbon atoms, and use thereof. The phosphite compounds of the present invention show stabilizing action on organic materials and are useful as antioxidants. A combined use of the compounds of the present invention with hindered phenol compounds, light stabilizers or thioalkanoate compounds further improves stabilizing effect.

Abstract: The present invention provides an industrially valuable method for preparing an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound which is useful as a starting material for an optically active benzopyran compound with antihypertensive, coronary blood flow-increasing activities and the like, and also provides a diastereometric ester compound with a 3-halo-4-hydroxy-2H-1-benzopyran compound which is useful as an intermediate for said epoxy compound.

Abstract: A thienocycloheptapyridazine compound of the formula ##STR1## wherein R stands for hydrogen, a halogen or a C.sub.1-4 alkyl, Ar stands for an aryl, a heteroaryl, or an aryl or a heteroaryl having as a substituent at least a halogen, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy, nitro, amino, hydroxy, trifluoromethyl and/or a C.sub.2-5 alkanoylamino; and the bond between 4-position and 42-position represents a single bond or a double bond, which is useful as an antianxiety agent, amnesia-treating drug, a brain function-activating drug or an antidementiac drug.

Abstract: A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 (wherein R.sup.1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R.sup.2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl); R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.

Abstract: A fused thiophene compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof. In the above formula, one of E.sup.1, E.sup.2 and E.sup.3 is sulfur atom and other two of them are C--R.sup.1 and C--R.sup.2 respectively. R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, nitro, amino, cyano, hydroxyl, formyl, alkyl, alkoxy, haloalkyl, arylalkyl, acyl, alkoxyalkyl, acyloxyalkyl, hydroxyalkyl, acyloxyalkanoyl, alkoxyalkanoyl, hydroxyalkanoyl, aryloxyalkanoyl, haloalkanoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylthio, arylsulfinyl, arylsulfonyl, hydroxysulfonyl, halosulfonyl, sulfamoyl, substituted sulfamoyl, carboxyl, acylamino, alkoxycharbonyl, carbamoyl, substituted carbamoyl or substituted amino. D is --CH.sub.2 -- or --S(O).sub.m -- (m is 0, 1 or 2). Q is straight or branched chain alkylene. T is primary amino, secondary amino or tertiary amino.

Abstract: An industrial microbicidal/microbistatic composition which comprises (1) 4,5-dichloro-1,2-dithiol-3-one and (2) N-dodecylguanidine hydrochloride or N-dodecylguanidine acetate and a method of killing or inhibiting the growth of microbe or controlling slime formation using said composition.

Abstract: A process for the commercial-scale crystallization and purification of tetrakis[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionyloxymethyl]methane which comprises melt-blending the reaction mixture resulting from the transesterification between pentaerythritol and a lower alkyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionate and containing tetrakis[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionyloxymethyl]methane with a water-soluble solvent under reflux, then blending the resulting melt-blend with a cooled, mixed solvent composed of 0.2-1.5 parts by weight, per part by weight of the above-mentioned reaction mixture, of a water-soluble solvent and 0.06-0.09 part by weight, per part by weight of the water-soluble solvent, of water to thereby cause crystallization, and further adding water for stabilizing the resulting beta crystal structure.

Abstract: 3,4-Dihydrothieno[2,3-d]pyrimidine compounds having immunoregulating and carcinostatic actions of the general formula ##STR1## wherein A represents a C.sub.1-4 alkylene; R.sup.1 represents hydrogen, an alkyl, an aryl which may be substituted or --N(R.sup.7)(R.sup.8); R.sup.2, R.sup.3 and R.sup.4 represent hydrogen, a halogen, hydroxy, an alkyl which may be substituted by a halogen, an alkoxy, nitro, cyano or --N(R.sup.9)(R.sup.10); R.sup.5 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl or an alkoxycarbonyl; R.sup.6 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl, an alkoxycarbonyl, a halogenosulfonyl or --SO.sub.2 N(R.sup.12)(R.sup.13); or R.sup.5 and R.sup.6 may, taken together, form a C.sub.3-6 alkylene chain, and their pharmaceutical use.

Abstract: Amino acid derivatives of the formula ##STR1## wherein: Q is W--(CH.sub.2).sub.m --(A).sub.n --CO--B-- whereinA is oxygen atom or --NH--;B is ##STR2## or --(CH.sub.2).sub.l -- wherein X is sulfur atom or --CH.sub.2 --, and l is an integer from 1 to 3;W is ##STR3## wherein Hal is halogen atom; n is an integer of 0 or 1; andm is an integer from 0 to 3;Y is sulfur atom or --CH.sub.2 --; andR is hydrogen atom, formyl group, C.sub.1-5 alkoxycarbonyl group, --C.tbd.N or ##STR4## wherein R.sup.1 is hydrogen atom, andR.sup.2 is hydroxyl group, C.sub.1-5 alkylcarboxy group, phenylcarboxy group, C.sub.1-5 alkoxy group or phenyl C.sub.1-5 alkoxy group;with the proviso that when R is hydrogen atom, formyl group or C.sub.1-5 alkoxycarbonyl group, W is ##STR5## The compounds mentioned above specifically inhibit prolyl endopeptidase activity and are useful as agents for the treatment and prevention of dementia and amnesia.

Abstract: The invention provides alpha crystals of tetrakis[3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionyloxymethyl]methane that occur as round granular crystals with high purity, uniform grain size, narrow grain size distribution and good flowability.

Abstract: Bis(cyclohexylphenol) compounds of the formula ##STR1## wherein R is an alkyl having 1 to 6 carbon atoms, Y is --S--, --SO-- or --SO.sub.2 -- with the proviso that when R is methyl in the ortho position to the hydroxy, Y is --SO-- or --SO.sub.2 --and their use. The above-mentioned compounds are useful as antioxidants and biocides for industrial use.