Abstract: Disclosed are indane compounds represented by the formula: ##STR1## wherein R.sup.1 is aryl, lower alkyl, cycloalkyl, halogeno-lower alkyl, lower alkenyl, phenyl-substituted lower alkenyl, monocyclic or bicyclic aromatic heterocyclic having N, O or S as a hetero atom, lower alkoxy, phenoxy, lower alkylamino, lower alkenylamino, phenylamino, lower alkyl substituted by monocyclic or bicyclic aromatic heterocyclic having N, O or S as a hetero atom, or lower alkenyloxy; R.sup.2 is H or lower alkyl; X is carbonyl or thiocarbonyl; Alk is single bonding arm or lower alkylene; and the dotted line is presence or absence of a double bond, for treating endotoxin shock and/or nephritis.

Abstract: There is disclosed an indole-containing peptide represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group or formyl group; and X represents oxygen atom or sulfur atom,an ester thereof or pharmaceutically acceptable salts thereof.

Abstract: Novel succinimide derivatives of formula I!: ##STR1## wherein Ring A is tri-lower alkoxyphenyl, R.sup.1 and R.sup.2 combine each other to form a group of the formula:>N--R.sup.3or one of R.sup.1 and R.sup.2 is lower alkoxy, and the other is group of the formula: --NHR.sup.3, in which R.sup.3 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof, these compounds have excellent antithrombotic activity and are useful as antithrombotic drug, or synthetic intermediate for preparing other antithrombotic drug.

Abstract: An imidazopyridine derivative of formula I! is disclosed ##STR1## wherein R.sup.1 is lower alkyl, R.sup.2 is a group of the formula ##STR2## Z is oxygen, R.sup.0 is a pyridyl, furyl or thienyl group, R.sup.3 is carboxyl or lower alkoxycarbonyl, Ring A is tetrazoyl-substituted phenyl and pharmaceutically acceptable salts thereof, for use in the prophylaxis and treatment of hypertension.

Abstract: Thiazine derivatives of the formula [I]: ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each hydrogen atom; R.sup.3 is hydrogen atom or a halogen atom; X is sulfur atom; R.sup.6 is naphthyl, a sulfur-containing monoheterocyclic group or a substituted phenyl; Z.sup.1 is two hydrogen atoms; Z.sup.2 is oxygen atom; A is a lower alkylene; R.sup.7 and R.sup.8 are the same or different and are each i) hydrogen atom, ii) a lower alkyl, iii) a lower alkenyl, iv) a lower alkynyl, or v) a lower alkyl which is substituted by a substituted phenyl, or both form together with the adjacent nitrogen atom a nitrogen-containing monoheterocyclic group; except for the compound [I] wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen atom, X is sulfur atom, R.sup.6 is a halogenophenyl, Z.sup.1 is two hydrogen atoms, Z.sup.2 is oxygen atom, A is a lower alkylene, R.sup.7 and R.sup.

Abstract: A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula [I]: ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group and R.sup.2 is a hydrogen atom or a protecting group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.

Abstract: A gene encoding an esterase originated from a microorganism of the genus Serratia, a mutant strain having high esterase productivity containing said gene, a recombinant plasmid comprising said gene inserted into a vector plasmid, a novel microorganism transformed with said recombinant plasmid, and a method for the production of an esterase which comprises cultivating the mutant strain or the novel microorganism as set forth above in a medium and collecting the produced esterase outside and inside the cells. Said mutant strain having high esterase productivity and new transformed microorganism have excellent esterase productivity and can produce the desired esterase in high purity on a large scale.

Abstract: There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.

Abstract: There is disclosed a process for preparing D-mandelic acid comprising the steps of:(1) treating racemic mandelic acid with a culture broth, cells or treated cells of a microorganism having ability of converting L-mandelic acid into benzoylformic acid.(2) treating the reaction mixture of the step (1) with a culture broth, cells or treated cells of a microorganism having ability of stereoselectively reducing benzoylformic acid into D-mandelic acid, and(3) isolating and collecting the D-mandelic acid from the reaction mixture.

Abstract: Disclosed are .beta.-carboline derivatives represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen atom, a lower alkyl group, a lower alkoxy group or hydroxy group; R.sup.5 represents hydrogen atom, or R.sup.1 and R.sup.5 are bonded to represent a lower alkylenedioxy group; R.sup.2 represents hydrogen atom, a halogen atom, a lower alkoxy group or hydroxy group; R.sup.3 represents hydrogen atom, a carbamoyl lower alkyl group, a lower alkyl group, a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkanoyl group, an arylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, an aralkyl group, formyl group or a di(lower alkyl)sulfamoyl group; n represents 0, 1 or 2; and the symbol * represents an asymmetric carbon atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

Abstract: A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula: ##STR1## wherein a group of the formula: --SR.sup.1 is a protected or unprotected mercapto group, and the group of the formula: .dbd.NR.sup.2 is a protected or unprotected imino group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(2,3,4-trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.

Abstract: An imidazopyridine derivative is disclosed of the formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, R.sup.2 is hydrogen, lower alkylsulfonyl or a group of the formula ##STR2## where Z is oxygen or two hydrogen atoms, R.sup.0 is lower alkyl, lower alkoxy, phenyl, hydrogen, di(lower alkyl) amino or lower alkenyl, R.sup.3 is carboxyl or lower alkoxycarbonyl and Ring A is substituted phenyl, and pharmaceutically acceptable salts thereof that are useful in prophylaxis and treatment of hypertension.

Abstract: A method for treatment of diabetes, which comprises administering to a patient with diabetes an effective amount of a dihydrochalcone derivative of the formula: ##STR1## wherein Ar is an aryl group, R.sup.1 is a hydrogen atom or an acyl group, R.sup.2 is a hydrogen atom, an acyl group or .alpha.-D-glucopyranosyl group, or R.sup.1 and R.sup.2 may combine together to form a substituted methylene group, R.sup.3 and R.sup.4 are each a hydrogen atom or an acyl group, OR.sup.5 is a protected or unprotected hydroxy group or a lower alkoxy group; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed is a process for preparing a .beta.-lactam compound represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy-substituted lower alkyl group or an amino group each of which may be protected; R.sup.2 represents hydrogen atom or an ester residue; X represents a methylene group which may be substituted by a lower alkyl group, sulfur atom or a group represented by the formula: --A--CH.sub.2 -- where A represents sulfur atom, oxygen atom or methylene group; and W represents an active ester residue of hydroxyl group, or a salt thereof, which comprises the steps of treating a 1-aza-3-thia-bicycloalkane compound represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 and X have the same meanings as defined above, or a salt thereof with a base in the presence of a desulfurizing agent and then reacting the resulting compound with an active esterifying agent of hydroxyl group.

Abstract: An imidazopyridine derivative is disclosed of the formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, R.sup.2 is a group of the formula ##STR2## where Z is oxygen atom, R.sup.0 is lower alkyl, R.sup.3 is carboxyl or lower alkoxycarbonyl and Ring A is tetrazolyl-substituted or unsubstituted phenyl, and pharmaceutically acceptable salt thereof, that are useful in prophylaxis and treatment of hypertension.

Abstract: A controlled release pharmaceutical preparation comprising (a) a core containing a pharmaceutically active substance and an organic acid, and (b) a coating film formed on the surface of the core by aqueous coating of a water-insoluble and water-slightly permeable acrylic polymer containing a trimethylammonium-ethyl group, which exhibits well controlled dissolution and release of the pharmaceutically active substance when administered and can maintain the desired blood level of the active substance for a long period of time, and a method for producing the preparation.

Abstract: A sustained release pharmaceutical preparation comprising a carrier, an effective ingredient layer containing a medicinal compound and a heat-meltable material as a binder which is formed around said carrier and a coating layer containing a non-heat-meltable dissolution-controlling agent and a heat-meltable material as a binder which is formed around said effective ingredient layer and the process for preparing the same. According to the present invention, the formation of the effective ingredient layer and the formation of the coating layer can be successively carried out in the same apparatus without using any solvents or drying step in short hours to give a sustained release pharmaceutical preparation which can release a medicinal compound at a suitable dissolution rate according to the physical property of the medicinal compound.

Abstract: There is disclosed a pharmaceutical composition for inhibiting the platelet aggregation comprising acetylsalicyclic acid or a pharmaceutically acceptable salt thereof and a 1,5-benzothiazepine derivative of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group or a lower alkoxy group, R.sup.2 is hydrogen atom or a lower alkanoyl group, R.sup.3 is a lower alkyl group, R.sup.4 is hydrogen atom or a lower alkyl group and R.sup.5 is a lower alkyl group or a halogen atom, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed is a polysulfate of a .beta.-cyclodextrin in which at least one of 7 D-glucose units constituting the .beta.-cyclodextrin is a unit represented by the formula (I-a): ##STR1## wherein R.sup.1 is an alkyl group having 1 to 8 carbon atoms, a lower alkyl group having a substituent(s) or a lower alkenyl group, or a salt thereof, which has excellent antiretrovirus activity and is useful as an antiretrovirus agent.

Abstract: There is disclosed a pharmaceutical composition for inhibiting platelet aggregation comprising 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof and a 1,5-benzothiazepine derivative of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group or a lower alkoxy group, R.sup.2 is a lower alkanoyl group, R.sup.3 and R.sup.4 are a lower alkyl group and R.sup.5 is hydrogen atom, a lower alkyl group or a halogen atom, or a pharmaceutically acceptable salt thereof.