Abstract: A microorganism having a capability of introducing a 7.beta.-hydroxyl group into a 7-unsubstituted bile acid, and a process for preparing a bile acid having a 7.beta.-hydroxyl group characterized by bringing the above microorganism into contact with a 7-unsubstituted bile acid to convert the acid to a bile acid having a 7.beta.-hydroxyl group. The process permits ursodeoxycholic acid useful as a cholagogue and intermediates therefor to be efficiently prepared.

Abstract: This invention concerns a method for the production of a 3-arylindoline compound represented by the general formula ##STR1##

Abstract: The present invention is a therapeutic or prophylactic agent for viral diseases whose active ingredient is antileukoprotease (ALP). Formulations containing ALP as an active ingredient have particularly effective application against viral diseases, particularly viral diseases caused by viruses which are activated by tryptase Clara, i.e. viruses with envelope glycoproteins, which replicate by infection of the respiratory-tract, such as influenza virus, parainfluenza virus, RS virus, measles virus and mumps virus.

Abstract: Bacillus sp. TTUR 302 which belongs to the genus Bacillus and is capable of converting bile acids having a 7.alpha.-hydroxyl group or a 7-keto group into bile acids having a 7.beta.-hydroxyl group; and a process for producing bile acids having a 7.beta.-hydroxyl group which comprises incubating this microorganism in an enriched medium containing bile acids having a 7.alpha.-hydroxyl group or a 7-keto group and collecting the formed bile acids having a 7.beta.-hydroxyl group (ursodeoxycholic acids, etc.). The process is easy to operate and safe as compared with the conventional chemical synthesis method. It is also superior to the conventional microbial methods particularly in the case of industrial production, since the microorganism of the invention is a facultative anaerobe and thus capable of effecting the conversion of the bile acids under aerobic conditions at a high substrate concentration.

Abstract: Disclosed is a cholestasis ameliorant containing tauroursodeoxycholic acid, which is more excellent in solubility than ursodeoxycholic acid, as the active ingredient. The ameliorant is useful for the treatment of intrahepatic cholestasis due to drug-induced hepatopathy, viral hepatitis or the like and the treatment of cholestasis occurring after surgical operation for the treatment of obstructive jaundice.

Abstract: 4-amino-5-oxy-2,6,6-tri methyl-2-cycloheptene compounds represented by the following general formula: ##STR1## (wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom, an alkyl group which may have a substituent, or a phenyl group which may have a hydroxyl group, lower alkoxy group, amino group, nitro group, carboxyl group, lower alkoxycarbonyl group or halogen atom, or R.sup.1, R.sup.2 and the nitrogen atom together represent a saturated nitrogen heterocyclic group; R.sup.3 represents a hydrogen atom, a lower alkyl group or a lower aliphatic acyl group); and W represents an oxo group, oxime group or oxime ether group; and their pharmacologically acceptable salts and solvates.The 4-amino-5-oxy-2,6,6-trimethyl-2-cycloheptene compounds exhibit an effect against rat peripheral arterial occlusion models, spontaneous hypertensive rats and histamine-induced airway contraction models, and are thus useful as remedy for hypertension, peripheral arterial occlusion and bronchial asthma.

Abstract: A hepatitis C virus proliferation inhibitor comprising a bile acid or a physiologically acceptable salt thereof is disclosed, as well as a method for treating a mammal infected with hepatitis C and a pharmaceutical composition for treating hepatitis C. As the bile acid to be used in the present invention, free bile acids, such as ursodeoxycholic acid and chenodeoxycholic acid, and conjugated bile acids such as tauroursodeoxycholic acid are exemplified. Also, as the physiologically acceptable salt, alkali metal salts such as the sodium salt of the bile acid is exemplified.

Abstract: 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido?1, 2-a!pyrimidin-4-one represented by the following formula; ##STR1## and the physiologically-acceptable salts thereof showed to have excellent inhibitory effect on the proliferation of vascular smooth muscle cells and are effective to prevent the occurrence of restenosis after the operation of PTCA, and hence the compounds can be useful for the therapeutic and preventive treatment for arteriosclerosis and other diseases whereto the proliferation of vascular smooth muscle cells is directly concerned.

Abstract: The present invention relates to enteric granule-containing tablets which are prepared by tabletting a mixture of enteric granules containing an active agent, with one or a combination of 2 or more compounds selected from synthetic hydrotalcite, dried aluminum hydroxide gel, aluminum hydroxide/sodium hydrogen carbonate coprecipitate, alumina hydroxide/magnesium, synthetic aluminum silicate and dihydroxyaluminumamino acetate. The invention provides high-strength tablets which are formulated with specific excipients which allow a higher enteric granule content, faster dispersion in the enteric granules, no loss of drug elution properties or acid resistance of the enteric granules upon tabletting, with less damage in the coating and low weight variation of the tablets during tabletting, as compared to tablets containing coated granules according to the prior art.

Abstract: A method for the production of granules by the use of a high speed agitated granulating machine provided with agitating means for rolling and agitating a substance for granulation, spray means for spraying a binding liquid on the substance, disintegrating means for disintegrating particles arising from granulation, and drying means for drying the particles, characterized by effecting the production by causing the means to act on the substance for granulation simultaneously thereby performing the agitating, granulating, disintegrating, and drying operations simultaneously. An apparatus for automatically implementing the method is also disclosed. The method for high speed agitating sterilization according to this invention is capable of producing granules which are extremely homogeneous in contents of components and excellent in flowability and compression moldability. The granules in process of formation do not easily form coarse lumps as by cohesion and the produced granules possess stable quality.

Abstract: Indoline compounds represented by the general formula: ##STR1## wherein R.sup.1 represents the group ##STR2## R.sup.2 represents a phenyl group which may be substituted or an aromatic heterocyclic group, and R.sup.3 represents hydrogen, a halogen, or a lower alkyl group, hydroxyl group, lower alkoxy group, carbamoyl group or lower alkoxycarbonyl group, and physiologically acceptable salts thereof, and their solvates, as well as 5-HT.sub.3 receptor antagonists containing them as effective components. The indoline compounds of the invention have stronger antagonism against intestinal 5-HT.sub.3 receptors than known 5-HT.sub.3 receptor antagonists and also have excellent sustained action, making them useful as prophylactic or therapeutic agents against vomiting or irritancy induced by chemotherapy or radiation, irritable bowel syndrome, diarrhea, and the like.

Abstract: The present invention is directed to a purification method for hydrophobic polypeptides by using high performance liquid chromatography, characterized by using a mixed solvent as a moving phase, in which the portion of trifluoroacetic acid is from 3 to 10% by volume, and polyvinyl alcohol-based column filler in the said high performance liquid chromatography. The method according to the present invention is useful as a purification method for hydrophobic polypeptides in view of the fact that the pulmonary surfactant, which is prepared from the hydrophobic polypeptide purified according to the method of the present invention, shows better surface active property than the hydrophobic polypeptides purified by customary methods for the purification.

Abstract: The present invention relates to a granulating and coating technique, and more particularly to a technique wherein powder and granules are contained in a drum rotating about a substantially horizontal axis and the rotary drum is rotated for granulation of the granules and (or) coating. There is provided a rotary drum (1) for containing the powder and granules (M) and rotating about the substantially horizontal axis, and also provided a buffle member (12) continuously or intermittently rotating or swinging at the inside of the powder and granules (M) layer in the rotary drum (1). The buffle is turned in the granules, so that the raw materials for the powder and granules can be prevented from adhering to the buffle member and the rotary drum or from peeling off therefrom, thus obtaining products of uniform coating.

Abstract: The present invention relates to a granulating and coating technique, and more particularly to a technique wherein powder and granules are contained in a drum rotating about a substantially horizontal axis and the rotary drum is rotated for granulation of the granules and (or) coating. There is provided a rotary drum (1) for containing the powder and granules (M) and rotating about the substantially horizontal axis, and also provided a baffle member (12) continuously or intermittently rotating or swinging at the inside of the powder and granules (M) layer in the rotary drum (1). The baffle is turned in the granules, so that the raw materials for the powder and granules can be prevented from adhering to the baffle member and the rotary drum or from peeling off therefrom, thus obtaining products of uniform coating.

Abstract: A remedy for inflammatory intestinal diseases which contains as the active ingredient 9-(4-acetyl-3-hydroxy-2-n-propylphenoxymethyl)-3-(1H-tetrazol-5-yl)-4H-pyr ido[1,2-a]pyrimidine-4-one represented by the formula: ##STR1## or a physiologically acceptable salt thereof. The compound specified in the present invention can remedy not only inflammatory responses caused in inflammatory intestinal diseases in a short time but also remove the symptoms deriving from digestive organs, which are caused together with the inflammatory response of the intestine.

Abstract: Microorganisms from the genus Bacillus are used to convert chenodeoxycholic acid to 3-alpha-hydroxy-7-keto-5-beta-cholanic acid under aerobic conditions and alkaline pH. Preferred strains are Bacillus FERM BP-4390, Bacillus FERM BP-4391, Bacillus FERM BP-3651, Bacillus FERM BP-3393, Bacillus FERM BP-3398, Bacillus FERM BP-3395 and Bacillus FERM BP-3396. Microorganisms from the genus Bacillus are used to convert cholic acid to 3-alpha-hydroxy-7,12-diketo-5-beta-cholanic acid under aerobic conditions and alkaline pH. Preferred strains are Bacillus FERM BP-3393 and Bacillus FERM BP-3398. Microorganisms from the genus Bacillus are used to convert cholic acid to 3-alpha, 12-alpha-dihydroxy-7-keto-5-cholanic acid under aerobic conditions and alkaline PH. Preferred strains are Bacillus FERM BP-3395 and Bacillus FERM BP-4390.

Abstract: 3-.alpha., 7-.alpha.-dihydroxy-12-keto-5-.beta.-cholanic acid is microbially produced from cholic acid by alkalophilic Bacillus strains. The preferred strains are Bacillus sp. FERM BP-3394 and Bacillus sp. FERM BP-3397.

Abstract: A growth promoter for Bifidobacterium species comprising gourd food, from yugao gourd, as active ingredient is provided. The growth promoter has a more selective and more marked growth-promoting effect than conventional bifidus factors.

Abstract: A suspension type aerosol inhalations containing (a) 0.015 to 5.00% (w/w) of a pyrido[1,2-a]pyrimidine compound of the formula: ##STR1## where R is a n-propyl or allyl group, A is a tetrazolyl or carboxyl group, and n is a whole number of 0 to 2, and (b) 0.015 to 5.00% (w/w) of a fatty acid ester.

Abstract: There are provided 4,5-Dihydroxy-2,6,6-trimethyl-2-cyclohepten-1-one, a method for preparing the same and an antiulcer agent containing the same as an effective ingredient.