Abstract: In accordance with the present invention, there is provided an intraorally rapidly disintegrable preparation which comprises a spray-dried powder comprising a sugar alcohol, of which unit particle is a primary particle, and an active ingredient, which has hardness having no problem in practical use and shows good disintegrability in the oral cavity. The above preparation can be produced by a common compression molding method, preferably by a direct tableting method.

Abstract: There are provided granules having a good taking property wherein an active ingredient, at least one kind of soluble additive having an average particle size of smaller than 50 &mgr;m and at least one kind of disintegrator are contained.

Abstract: Provided is a process for efficiently producing N-glycyltyrosine of high purity represented by the following formula: a salt thereof, or a solvate thereof, which comprises adding dropwise to an aqueous suspension of tyrosine or a salt thereof 2 equivalents or more of a haloacetyl halide and an aqueous solution of an inorganic base simultaneously in the presence or absence of an organic solvent, and subjecting the resulting N-haloacetyltyrosine to a reaction with an ammonium ion. Also provided are N-glycyl-L-tyrosine dehydrate having the crystal structures showing specific diffraction patterns in X-ray powder diffraction and processes for producing the same which are characterized by comprising crystallizing the dihydrate from an ethanol-water mixed solvent or water.

Abstract: The present invention relates to glutathione monoester sulfonate represented by formula (I): ##STR1## (wherein R.sup.1 represent lower alkyl, and R.sup.2 represents lower alkyl, or substituted or unsubstituted aryl) which readily crystallizes and has high stability, and a simple process for producing the same. According to the process, the product having high purity can be obtained in high yields.

Abstract: In the formulae, R.sup.1, R.sup.2, and R.sup.3 independently represent lower alkyl or aryl, and R.sup.4 represents lower alkyl.The present invention relates to a process for producing an indolocarbazole derivative represented by Formula (II), comprising the acidic treatment of a silylated indolocarbazole derivative represented by Formula (VI).

Abstract: An indole derivative represented by formula (I): ##STR1## wherein R.sup.1 is a lower alkoxymethyl group or a formyl group, R.sup.2 is a lower alkyl group, R.sup.3 is a hydrogen atom or a lower alkyl group and R.sup.4 is a hydrogen atom or a lower alkyl group, which is useful as an intermediate for the synthesis of a compound, 5-aziridino-3-hydroxymethyl-l-methyl-2- (1H-indole-4,7-dione)prop-.beta.-ene-.alpha.-ol, which has antitumor activity.

Abstract: Carbacephem and cephem compounds represented by the formula: ##STR1## [Wherein X is S or CH.sub.2 ; n is an integer of 1 to 5; R.sub.1 is an unsubstituted or substituted heterocyclic group (where the heterocyclic group is a 5- or 6-membered heterocyclic group having 1 to 4 of O, S and N); R.sub.2 is a group represented by the formula: ##STR2## (where R.sub.4 is an unsubstituted or substituted phenyl or 2-aminothiazolyl) or a group represented by the formula: ##STR3## (where R.sub.5 is an unsubstituted or substituted lower alkyl); R.sub.3 is hydrogen, an alkali metal, an alkaline earth metal, an organic ammonium group or an ester residue, and R.sub.1 may be a quaternary ammonium group, where --CO.sub.2 R.sub.3 represents --CO.sub.2.sup.- ] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for treating various infections.

Abstract: Disclosed are optically active acylated cephalosporin analogs which are useful as antibacterial agents and methods for preparing such compounds.

Abstract: Optically active cephalosporin analogs of the formula ##STR1## wherein R.sub.2 represents a hydrogen or a group represented by the formula ##STR2## wherein R.sub.3 is a straight or branched lower alkyl group having 1 to 6 carbon atoms, a straight or branched lower alkoxy group having 1 to 6 carbon atoms or a phenyl group and R.sub.4 is a hydrogen or a straight or branched lower alkyl group having 1 to 6 carbon atoms; and A.sub.2 represents a straight or branched lower alkyl group having 1 to 6 carbon atoms or a straight or branched lower alkyl group having 1 to 6 carbon atoms which is substituted with one or two carboxyl groups, are useful as antibacterial agents.

Abstract: Carbacephem compounds represented by the formula: ##STR1## [wherein R.sub.1 is a lower alkylsulfonyloxy, unsubstituted or substituted arylsulfonyloxy, azido, cyano, carbamoyloxy, unsubstituted or substituted heterocyclic thio ("heterocyclic" means a 5- or 6-membered heterocyclic group having 1 to 4 O, S or N atoms), unsubstituted or substituted lower alkylthio, or unsubstituted or substituted arylthio group; R.sub.2 and R.sub.3 are groups frequently used in the cephalosporin chemistry] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for curing various infections.

Abstract: Optically active cephalosporin analogs are produced by an optically selective acylation reaction. The reaction is carried out in the presence of a microbial enzyme which catalyzes the selective optical acylation. The products thus obtained are useful as antibacterial agents.

Abstract: Optically active cephalosporin analogs are produced by optically selective deacylation of an optically inactive acylated analog. The compounds are useful as intermediates in the preparation of optically active acylated antimicrobial agents.

Abstract: Disclosed are optically active cephalosporin analogs which are produced by optically selective deacylation of an optically inactive acylated analog. The compounds are useful as intermediates in the preparation of optically active acylated antimicrobial agents.

Abstract: Novel cephalosporin analogs are disclosed which are useful as intermediates in the production of other compounds having antibacterial activity. Methods for producing the compounds are also disclosed.