Abstract: A rapid-releasing oral particle pharmaceutical preparation with its unpleasant taste masked comprising a core and a film layer coating the core, the core at least containing a drug having an unpleasant taste and a water-swelling agent, and the film layer at least containing ethylcellulose and a water-soluble substance, the amount of the drug in the core being at most 40% (based on the final particle preparation and so on), the amount of the water-swelling agent being about 35% to about 70%, the amount of ethylcellulose in the film layer being about 3 to about 11%, and the amount of the water-soluble substance being about 0.1 to about 0.8 times the weight of the ethylcellulose.

Abstract: A method of preventing or eliminating mycoplasma contamination of animal or plant cell cultures, which comprises adding an anti-mycoplasmally effective amount of 5-amino-7-(2-aminomethylmorpholino)-1-cyclopropyl-6, 8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or its salt to a culture medium in which animal or plant cells are cultivated; and an agent or a preparation for preventing or eliminating mycoplasma contamination of animal or plant cell cultures, comprising 5-amino-7-(2-aminomethylmorpholino)-1-cyclopropyl-6, 8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or its salt.

Abstract: A novel cloned DNA encoding a rabbit Tumor Necrosis Factor (TNF) or a principal portion thereof, a vector having said DNA inserted thereinto, a host transformed with said vector, a novel polypeptide having or containing the rabbit TNF or a principal portion thereof, and a process for producing said polypeptide comprising cultivating said transformed host.

Abstract: Medicament for the treatment of cerebral insufficiency diseases comprising as an active ingredient a compound of the formula: ##STR1## wherein n is 3, 4, 5 or 6; R.sup.1 is hydrogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, hydroxy-(C.sub.2 -C.sub.6) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C.sub.1 -C.sub.6) alkyl, unsubstituted or substituted arylcarbonyl-(C.sub.1 -C.sub.6) alkyl, or acyl; R.sup.2 is hydrogen atom, halogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or trifluoromethyl; and R.sup.3 is hydrogen atom or C.sub.1 -C.sub.6 alkyl, or an acid addition salt thereof, novel 2-(1-piperazinyl)-4-phenyl-cycloalkanopyrimidine derivatives having excellent cerebral function improving activity, processes for the preparation thereof.

Abstract: Novel 2-(1-piperazinyl)-4-phenyl-cycloalkanopyridine derivatives of the formula (I): ##STR1## wherein n is 3, 4, 5, 6 or 7; R.sup.1 is a hydrogen atom, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.6 cycloalkyl-(C.sub.1 -C.sub.4) alkyl, hydroxy-(C.sub.2 -C.sub.6) alkyl, C.sub.1 -C.sub.3 alkoxy-(C.sub.2 -C.sub.6) alkyl, acyloxy-(C.sub.2 -C.sub.6), alkyl, unsubstituted or substituted aroyl-(C.sub.1 -C.sub.6) alkyl, unsubstituted or substituted aryl, heteroaryl, or acyl; R.sup.2 and R.sup.3 are the same or different and are each a hydrogen atom, a halogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, or hydroxy; R.sup.4, R.sup.5 and R.sup.6 are the same or different and are each a hydrogen atom, C.sub.1 -C.sub.6 alkyl, or phenyl, or two of R.sup.4, R.sup.5 and R.sup.6 combine to form a single bond or C.sub.1 -C.sub.3 alkylene; R.sup.7 and R.sup.8 are the same or different and are each a hydrogen atom or C.sub.

Abstract: An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, ##STR1## wherein Y represents --NH-- or --O--; R.sub.1 and R.sub.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R.sub.1 and R.sub.2, taken together, form a lower alkylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R.sub.

Abstract: A quinoline derivative of the formula ##STR1## wherein Z is an amino group or a halogen atom, and R.sub.1, R.sub.2 and R.sub.3 are the same or different and each represents a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms,and an ester thereof and a salt of the derivative or the ester and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful as antibacterial agents.

Abstract: A human TNF polypeptide mutant having an amino acid sequence of modified human TNF polypeptide, a DNA having a base sequence encoding the above human TNF polypeptide mutant and a method of producing the above human TNF polypeptide mutant by culturing a host transformed with a vector having inserted therein the above DNA. The above human TNF polypeptide mutant is soluble and has antitumor activity.

Abstract: Heteroarylcarboxamide derivatives of the formula I: ##STR1## wherein A means an alkylene group, X means <NCHPh.sub.2 or <C.dbd.CPh.sub.2 in which Ph means phenyl and .circle.Het means a group of the formulas: ##STR2## in which Y means nitrogen atom or .dbd.CH--, R.sub.1 means hydroxy, a lower alkoxy or mercapto, R.sub.2 means hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, nitro or cyano, R.sub.3 means a lower alkyl group, provided that R.sub.2 is attached at the 7-position when Y means nitrogen atom, or physiologically acceptable salts thereof, a process for preparing the same and a pharmaceutical composition containing the same as an active ingredient. The compounds of the present invention and salts thereof show an excellent antiallergic activity and thus are useful for the prophylaxis and treatment of allergic diseases.

Abstract: A 6-fluoroprostaglandin having the formula: ##STR1## wherein A is a carbonyl group or a hydroxymethylene group, R.sup.1 is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl group or a substituted or unsubstituted 5- or 6-membered cycloalkyl group, R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group, each of R.sup.3 and R.sup.4 which may be the same or different is a hydrogen atom or a protecting group, R.sup.5 is a hydrogen atom or a hydroxyl group, and is a single bond or a double bond, and its salt when R.sup.2 is a hydrogen atom.

Abstract: The present invention relates to compounds represented by the general formula (I): ##STR1## wherein R.sub.1 is H or methoxy, R.sub.2 is H, methoxy, OH or F, R.sub.3 is H or F, R.sub.4 is H or F at 7-, 8- or 9-position, and .circle.Ar is a benzene, thiophene or pyridine ring, provided that (i) at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, (ii) R.sub.2 or R.sub.3 is F when R.sub.4 is F, (iii) R.sub.1, R.sub.3 and R.sub.4 are H when R.sub.2 is methoxy or OH, (iv) R.sub.2 and R.sub.3 are not simultaneously F, and (v) R.sub.2 and R.sub.3 are H or F, and both R.sub.1 and R.sub.4 are H when .circle.Ar is a thiophene or pyridine ring, or a physiologically acceptable acid addition salt thereof.

Abstract: The present invention relates to quinoline derivatives of the formula ##STR1## wherein Z is an amino group or a halogen atom, R is ##STR2## in which R.sub.1 is a hydrogen atom, a lower alkyl or haloalkyl group, R.sub.2 is a hydrogen atom or a lower alkyl group, R.sub.3 is a lower alkyl or haloalkyl group, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 and R.sub.6 are the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocyclic ring, and n is 0 or 1, with the proviso that when Z is an amino group, R is (B);and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.

Abstract: Agent for the removal of nucleic acids and/or endotoxin from a liquid containing the nucleic acids and/or endotoxin and further useful substances (e.g. proteins, hormones, etc.), which comprises as an active ingredient a chitosan having a low molecular weight, particularly that having an intrinsic viscosity of 0.01 to 5 (dl/g) and further a colloid equivalent of not less than 2 meq/g of evaporated residue.

Abstract: Compounds of the formula: ##STR1## wherein R is hydrogen, alkoxycarbonyl, benzyloxycarbonyl, heteroarylalkyl, phenylalkenyl, or --T--(Y).sub.p --R.sub.6 (wherein T is single bond or alkylene, Y is oxygen, sulfur or carbonyl, R.sub.6 is phenyl, substituted phenyl, naphthyl, or diphenylmethyl, and p is 0 or 1, provided that when T is single bond, p is 0); R.sub.1 is halogen, hydroxy, alkoxy, cycloalkyloxy, alkenyloxy, alkynyloxy, alkoxy interrupted by oxygen or carbonyl, alkylthio, amino, monosubstituted amino, or a substituted alkoxy; R.sub.2 is hydrogen; R.sub.3 is hydrogen, halogen, amino, alkylamino, dialkylamino, alkanoylamino, or nitro; R.sub.4 is hydrogen, halogen, nitro, sulfamoyl, alkylsulfamoyl, or dialkylsulfamoyl; or any two adjacent groups of the R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may combine to form alkylenedioxy, and the remaining two groups are each hydrogen; R.sub.5 is hydrogen or alkyl; X is alkylene; m and n are each 1 or 2; provided that at least one of the groups R.sub.2, R.sub.3 and R.

Abstract: There are provided tripeptide compounds represented by the following formula ##STR1## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a C.sub.4-7 cycloalkyl or C.sub.

Abstract: The present invention relates to a quinoline derivative of the formula ##STR1## wherein Z is an amino group or a halogen atom, R.sub.1 is a hydrogen atom or a methyl or ethyl group, R.sub.2 is a hydrogen atom or a methyl or fluoromethyl group, R.sub.3 and R.sub.4 are the same or different and each represents a hydrogen atom or a methyl group, and n is 1 or 2;and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.

Abstract: Compounds of the formula: ##STR1## wherein X is alkylene or --(CR.sub.6 .dbd.CR.sub.7).sub.r -- wherein R.sub.6 is H, alkyl or phenyl, R.sub.7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond; R.sub.1 is H, halogen, alkyl, alkoxy, alkylthio, cycloalkyloxy, cycloalkylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R.sub.2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R.sub.1 and R.sub.2 may combine to form tetramethylene or --CH.sub.2 OCR.sub.8 R.sub.9 O-- (R.sub.8 and R.sub.9 are alkyl); R.sub.3 is H, alkyl or hydroxyalkyl; R.sub.4 is H or alkyl; R.sub.5 is phenyl, heteroaryl or --(CH.sub.2).sub.m --CHR.sub.10 R.sub.11 (R.sub.10 is H or phenyl, R.sub.11 is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and a salt thereof, process for the preparation thereof, and pharmaceutical composition containing the same.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 represents fluorine atom at the para position, chlorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para or meta position; and R.sub.2 represents hydrogen atom, methyl group, ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group, provided that R.sub.2 represents ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group when R.sub.1 represents fluorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para position, and a pharmaceutically acceptable salt therof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and pharmaceutically acceptable salts thereof show excellent cytoprotective effect and useful for prophylaxis and treatment of peptic ulcer and inflammatory gastrointestinal diseases.

Abstract: Compounds of the formula: ##STR1## wherein A means an alkylene; Y--Z means ##STR2## --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or ##STR3## R.sub.1 and R.sub.2 are each a substituent; R.sub.3 is hydrogen atom, alkyl, or alkoxy; R.sub.4 is phenyl, phenylalkyl, phenylalkenyl, diphenylmethyl, naphthyl, thiazolyl, optionally substituted pyridyl, optionally substituted pyrimidinyl, quinolyl, benzoylalkyl, benzoyl, furoyl, thenoyl, phenyloxycarbonyl, phenyloxysulfonyl, or phenylsulfonyl; a is 2 or 3, b and c are each 1 or 2, and d is an integer of 0 to 2, provided that the phenyl, phenyl moiety and naphthyl may optionally be substituted, and a pharmaceutically acceptable salt thereof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and salt thereof show potent calcium antagonistic activity and are useful for prophylaxis and treatment of hypertension and/or ischemic heart disease.

Abstract: The present invention relates to a 1,8-naphthyridine derivative of the formula ##STR1## wherein X is a fluorine or chlorine atom, and R is a hydrogen atom, or a methyl or ethyl group;and esters thereof and salts thereof are processes for preparation thereof. These compounds show excellent anti-bacterial activity and are useful antibacterial agents.