Abstract: A naphthothiopyranone derivative represented by the formula: ##STR1## (wherein R.sup.1 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms) and an acid addition salt thereof have more excellent antagonist effect at serotonin 3 receptors than the prior art compounds and the effects based thereon, e.g. anti-vomiting effect, gastrointestinal movement regulating effect and anti-anxiety effect.

Abstract: Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.

Abstract: A fused benzenoxyacetic acid derivative of the formula (I): ##STR1## and salts thereof possess an agonistic on PGI.sub.2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertention.

Abstract: A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof.The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.

Abstract: Disclosed are fluorobenzene derivatives, which are important intermediates for producing herbicidal oxazolidinedione derivatives, and methods of producing them. The fluorobenzene derivatives include compounds of a formula (11): ##STR1## where X is a halogen atom, R.sup.3 is a nitro, amino or isocyanato group or R.sup.1 OCONH, and R.sup.1 is an alkyl or phenyl group. Via the intermediates of the invention, oxazolidinedione derivatives can be produced with high yield.

Abstract: Interleukin-1.beta. (IL-1.beta.) and derivatives, and their pharmaceutical compositions for use in treating arthritis or inflammation.

Abstract: Interleukin-1.alpha. (IL-1-.alpha.) and derivatives, and their pharmaceutical compositions for use in treating arthritis or inflammation.

Abstract: The present invention provides novel thiazolidine-2,4-dione derivatives possessing blood sugar-lowering action and aldose reductase-inhibitory action, their salts, their preparative processes and drugs containing them, and relates to thiazolidine-2,4-dione derivatives represented by a general formula (1) ##STR1## [wherein R.sup.1 and R.sup.2 denote identically or differently hydrogen atoms or lower alkyl groups, R.sup.3 denotes a phenyl group, naphthyl group, benzoyl group or 5-membered or 6-membered heteroring and its benzene-condensed ring, which may have one or more substituents, A denotes a carbonyl group, sulfonyl group or bonding hand, and B denotes a lower alkylene, lower alkenylene or bonding hand], or their salts, or thiazolidine-2,4-dione derivatives represented by a general formula (2) ##STR2## [wherein R.sup.4 denotes a hydrogen atom or lower alkyl group, and R.sup.1 and R.sup.3 are same as above ], or their salts.

Abstract: Two-cistronic Met-IGF-I expression vector, in which the first cistron encodes a protective peptide with a molecular weight of about 500-50,000 and the second cistron encodes IGF-I, was provided. Also provided is a process for preparing Met-IGF-I, which comprises transforming E. coli with said vector and growing the resultant transformant, followed by the lysis of the cell culture and isolation of Met-IGF-I.

Abstract: A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.

Abstract: A solid dispersion and a method of producing a solid dispersion of a sparingly water-soluble drug characterized by mixing the sparingly water-soluble drug and a water-soluble polymer at a temperature where neither the water-soluble drug nor water-soluble polymer is melted.

Abstract: The present invention provides novel pyridinium derivatives which are effective, for example, in diagnosis of diabetes, diabetic complications, aging, diseases accompanied by aging, etc. and also provides an antibody prepared from said derivative as a hapten.The pyridinium derivatives of the present invention are novel compounds represented by the following general formulae: ##STR1## wherein R and R' may be the same or different and are optionally substituted alkyl groups, and their pharmaceutically acceptable salts.It is possible to conduct the diagnosis of diabetes, diabetic complications, aging, diseases accompanied by aging, etc. using a compound of the present invention as an indicator. Moreover, it is possible to utilize a compound of the present invention for the evaluation of the pharmaceutical effect of pharmaceuticals effective for diabetes-related diseases, aging and diseases accompanied by aging.

Abstract: The present method for the treatment of pancreatitis, which comprises administering an effective amount of a pyrazolopyridine compound of the following formula: ##STR1## wherein R.sup.1 is lower alkyl, (substituted) aryl, or a heterocyclic group,R.sup.2 is a group of the formula ##STR2## wherein R.sup.4 is protected amino or hydroxy and R.sup.5 is hydrogen or lower alkyl; cyano; a group of the formula --A--R.sup.6, wherein R.sup.6 is an acyl group, and A is (halogenated) lower aliphatic hydrocarbon group; amidated carboxy; an unsaturated heterocyclic group; or (protected) amino; andR.sup.3 is hydrogen, lower alkyl, lower alkoxy or halogen; or a pharmaceutically acceptable salt thereof, to a human being having pancreatitis or an animal having pancreatitis in need thereof.

Abstract: A pharmaceutical composition for treating a peptic ulcer, which comprises a myosin light chain kinase inhibitor as an active ingredient and a pharmaceutical additive. The myosin light chain inhibitor reduced the gastric acid secretion and is considered an excellent anti-ulcer agent.

Abstract: A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 -- or ##STR2## (i) R.sup.1 and R.sup.2, which may the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X--A-- (R.sup.4)n wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR3## --A-- is a pyridyl or pyrrolyl ring, n is 1.about.5, R.sup.4 is 1 --H or C1-8 alkyl, 2 C1-14 alkoxy, 3 C1-6 alkylthio, 4 --OH, halogen, --NO.sub.2 or trihalomethyl, 5 the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, 6 tetrazole, 7 --SO.sub.3 H or --CH.sub.2 OH, 8 the formula: --SO.sub.2 NR.sup.41 R.sup.42 9 the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R.sup.

Abstract: The present invention concerns a mutant cephalosporin C acylase derived from a precursor of the formula:A.sup.1-268 --X.sup.1 --Tyr--X.sup.2 --A.sup.272-304 --X.sup.3 --A.sup.306-773(SEQ ID NO:1), wherein:A.sup.1-268 is the same amino acid sequence as that from Thr.sup.1 to Gly.sup.268 of native CC acylase,A.sup.272-304 is the same amino acid sequence as that from Gln.sup.272 to Tyr.sup.304 of native CC acylase,A.sup.306-773 is the same amino acid sequence as that from Val.sup.306 to Ala.sup.773 of native CC acylase,X.sup.1 is Met or other amino acid,X.sup.2 is Ala or Tyr, andX.sup.3 is Cys or Ser,provided that when X.sup.1 is Met and X.sup.2 is Ala, X.sup.3 is Ser; and that the mutant cephalosporin C acylase has a property selected from the group consisting of higher enzymatic potency and higher processing efficiency, as compared to native CC acylase.

Abstract: Tetrahydroimidazopyridine derivatives which are useful for the treatment of irritable bowel syndrome are provided and can be represented by the following formula, ##STR1## wherein either one of X and Y is nitrogen and the other one is a radical represented by the formula .dbd.C(R.sup.1)--; and R is a radical of the formula ##STR2## a radical of the formula ##STR3## or a radical of the formula ##STR4## in which R.sup.1, R.sup.2 and R.sup.3 are same or different and represent hydrogen or a C.sub.1 -C.sub.6 alkyl group, and salts thereof. Pharmaceutical compositions are also provided.

Abstract: The present invention relates to novel cephalosporins of the formula (I); ##STR1## wherein, R.sub.1 represents a C.sub.1 .about.C.sub.4 alkyl group or ##STR2## wherein, R.sub.2 and R.sub.3, independently, represent hydrogen or a C.sub.1 .about.C.sub.3 alkyl group and R.sub.4 represents hydrogen or a C.sub.1 .about.C.sub.4 alkyl group;R.sub.1a represents hydrogen or an amino-protecting group;Q represents CH or N; andthe formula ##STR3## represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient.

Abstract: Disclosed are carbostyril derivatives and their salts of the formulas ##STR1## The compounds have anti-peptic ulcer effects, and are useful as a treating agent for curing peptic ulcers in the digestive system, such as ulcers in the stomach and in the duodenum. The compounds particularly have prophylaxis and curing effects for treating chronic ulcers, for example experimental acetic acid-induced ulcers and cautery ulcers, with both low toxicity and few side-effects. Also disclosed are processes for preparing the compounds and for preparing pharmaceutical compositions containing them.