Abstract: A pharmaceutical preparation for rectal or vaginal administration, comprising a prostaglandin compound and an alkali metal salt of a fatty acid having 8 to 12 carbon atoms, and a method for administering a prostaglandin compound, comprising rectally or vaginally administering same in the presence of an alkali metal salt of a fatty acid.According to the present invention, absorption of prostaglandin from rectum or vagina can be enhanced.The prostaglandin can be stabilized in the preparation.

Abstract: Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.

Abstract: Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.

Abstract: 1,4-Dihydropyridine derivatives of the general formula: ##STR1## wherein X.sup.1 and X.sup.2 independently represent hydrogen, fluoromethyl, fluoromethoxy, halogen, cyano, or nitro; R.sup.1 represents a lower alkyl; R.sup.2 represents acyl, alkoxycarbonyl, acylalkyl, an N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, heterocycle-alkyl, haloalkyl, alkenyl, or alkynyl; A represents an alkylene comprising a carbon atom to which 2 alkyls are bonded and having in total at least 5 carbon atoms; m represents the integer 1, 2 or 3; acid addition salts thereof; a method of production thereof; and pharmaceutical compositions containing such compound(s).Such compounds have pharmacological activities, in particular potent and long lasting hypotensive activity, coronary vasodilatation, cerebral vasodilatation, peripheral vasodilatation, renal vasodilatation and platelet aggregation inhibitory activity.

Abstract: 1. A cephalosporin derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (bonded by the ester linkage), which may optionally be substituted by one or two lower alkyl groups at the amino group thereof, R.sup.2 is an 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl or 5-methyl-1,3-dioxolen-2-on-4-ylmethyl group, R.sup.3 is a carbamoyloxymethyl group, which may optionally be substituted by one or two lower alkyl groups, or a heterocyclothiomethyl group, which may optionally be substituted by one or more appropriate substituents, and R.sup.4 is a hydrogen atom or a hydroxy group, or its non-toxic salt are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.

Abstract: Compounds satisfying four specific requirements, namely: (1) a log P value in the range of from 2.5 to 6, (2) a molecular structure with at least one carboxyl group, (3) a pKa value for the carboxyl group of not less than 2.5 and (4) absence of halo substitution, and nontoxic salts thereof promote absorption of pharmacologically-active substance through the rectum into the bloodstream and are effective to raise the concentration of such active substance in the bloodstream even when the active substance is usually unabsorbable or absorbable through the rectum only with considerable difficulty. The compounds are combined with pharmacologically-active ingredients, with pharmaceutical bases suitable for rectal administration of drugs and with appropriate combinations of both.

Abstract: A cephalosporin derivative of the formula: ##STR1## wherein R represents ##STR2## or its pharmaceutically acceptable acid addition salt is found to be useful as orally administrable antibiotics having broad anti-microbial activities against both Gram-positive and Gram-negative bacteria.

Abstract: Novel cephalosporin derivatives, namely pivaloyloxymethyl 7.beta.-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1 H-tetrazol-5-yl]thio]methyl]-ceph-3-em-4-carboxylate and its pharmaceutically acceptable acid addition salts are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.

Abstract: Novel penicillins of the formula ##STR1## wherein R is a branched chain alkyl group of from 3 to 14 carbon atoms, and their pharmaceutically acceptable salts, are easily absorbed in the blood and tissues through oral administration and show excellent antimicrobial activity against Gram-positive and Gram-negative bacteria, particularly against microorganisms of the genus Pseudomonas, such as Pseudomonas aeruginosa.

Abstract: Novel d-.alpha.-isobutylsulfobenzylpenicillin hemi-solvate crystals of the formula: ##STR1## (wherein A is a solvent selected from the class consisting of alcohols, ketones, ethers and esters) have excellent antibacterial activities and improved stability in terms of shelf-life.

Abstract: .alpha.-Sulfophenylacetic acid derivatives of the general formula: ##STR1## (wherein R is a substituted or unsubstituted primary alcohol, cyclic alcohol or phenol compound residue), which are of value as intermediates of antibacterial agents, are selectively produced in a high yield by bringing a diester compound of the general formula: ##STR2## (wherein R has the same meaning as defined above) into contact with a strong acid.

Abstract: .alpha.-Sulfophenylacetic acid derivatives of the general formula: ##EQU1## (wherein R is a substituted or unsubsituted primary alcohol, cyclic alcohol or phenol compound residue), which are of value as intermediates of antibacterial agents, are selectively produced in a high yield by bringing a diester compound of the general formula: ##EQU2## (wherein R has the same meaning as defined above) into contact with a strong acid.