Abstract: A process for preparing optically active 3-phenylglycidic acid esters comprising reacting a racemic trans-3-phenylglycidic acid with an alkanol in the presence of a hydrolase to esterify preferentially either (2S, 3R) isomer or (2R, 3S) isomer of said racemic compound and isolating and collecting the resulting optically active 3-phenylglycidic acid ester from the reaction mixture, whereby the optically active ester can be produced in a single step and in a highly pure form. The optically active 3-phenylglycidic acid esters are useful for the preparation of 1,5-benzothiazepine derivatives having pharmacological activities such as platelet aggregation inhibitory activity.

Abstract: A microorganism derived from a host microorganism capable of producing d-biotin by introducing a recombinant plasmid being incorporated with a biotin gene cloned from a microorganism of the genus Serratia capable of producing d-biotin and further integrating an exogenous biotin gene into the chromosome, and a process for preparing d-biotin which comprises cultivating the microorganism in a culture medium so that d-biotin is formed and accumulated in the culture medium and collecting the d-biotin. The microorganism of the invention has an extremely high productivity of d-biotin, and hence, d-biotin can be produced in a large amount by cultivating the microorganism of the invention.

Abstract: Process for preparing carbapenem derivative of the formula [I], which comprises subjecting azetidinone compound of the formula [II] to intramolecular cyclization reaction together with elimination reaction of the group of --SR.sup.4, followed by re-adding said group of --SR.sup.4 to the 2-position of the carbapenem skeleton of the intramolecularly cyclized compound, which is industrially useful as process for preparing carbapenem antimicrobials or synthetic intermediate therefor. ##STR1## wherein R.sup.1 is protected or unprotected hydroxy-substituted lower alkyl group, R.sup.2 is hydrogen atom or ester residue, R.sup.3 is hydrogen atom or lower alkyl group, and the group of --SR.sup.4 is group which can be used as substituent at 2-position of the carbapenem antimicrobials.

Abstract: Naphthalene derivative of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R.sup.3 is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: --OR.sup.4 and --OR.sup.5 are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.

Abstract: A method for determination of a pyrogen content which comprises bringing a specimen into contact with an adsorbent composed of a nitrogen-containing heterocyclic compound bonded to a water-insoluble carrier directly or through a spacer, and after or without eluting the pyrogen adsorbed on the adsorbent, determining the content of the adsorbed pyrogen by the Limulus method.

Abstract: A naphthyloxazolidone derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, hydroxy group, nitro group, amino group, sulfo group, aminosulfonyl group, a lower alkenyloxy group, a lower alkynyloxy group, a mono or di(lower alkyl)aminocarbonyloxy group, a lower alkanoyloxy group or a lower alkoxy group which may have a substituent selected from an aryl group, a cycloalkyl group, an oxygen-containing heteromonocyclic group, hydroxy group, a lower alkoxy group, cyano group, a di(lower alkyl)amino group, aminocarbonyl group, a lower alkoxycarbonyl group, a lower alkanoyloxy group, a lower alkylthio group, a lower alkylsulfinyl group and a lower alkylsulfonyl group; R.sup.2 is hydroxy group, a lower alkoxy group, a lower alkylsulfonyloxy group, triazo group or an amino group which may have a substituent selected from a lower alkyl group and a lower alkanoyl group, and a pharmaceutically acceptable salt thereof are disclosed.

Abstract: Disclosed are a dicarboxylic acid compound represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group, phenyl group or hydroxyl group; R.sup.1 represents a straight or branched alkyl group having 1 to 10 carbon atoms or a lower alkyl group substituted by a group selected from aryl group, a sulfur- or nitrogen-containing heterocyclic monocyclic group and a cycloalkyl group having 4 to 8 carbon atoms; R.sup.2 represents a substituted or unsubstituted aryl group, a cycloalkyl group having 4 to 8 carbon atoms or a sulfur-containing or nitrogen-containing heterocylcic group; X represents sulfur atom, oxygen atom or a substituted or unsubstituted imino group; Y.sup.1 represents imino group, oxygen atom or sulfur atom and Y.sup.2 represents nitrogen atom, or Y.sup.1 represents a vinylene group and Y.sup.2 represents a group: --CH.dbd.

Abstract: Process for preparing optically active cis-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one compounds [I] of the formula: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted benzene, R.sup.1 is hydrogen or di-lower alkylaminoalkyl, which comprises subjecting 1,5-benzothiazepin-4(5H)-one (II) of the formula [II]: ##STR2## wherein R.sup.4 is hydrogen or lower alkanoyl, and the other symbols are the same as defined above, to asymmetric reduction with a reaction product of optically active .alpha.-amino acid and metal hydride, in high optically yield, and said compounds [I] are very important as intermediate for preparing various medicines.

Abstract: There is disclosed a process for preparing 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, or a salt thereof which comprises subjecting a propionate derivatives of the formula: ##STR2## wherein R.sup.2 is an ester residue and R.sup.1 is the same as defined above, to intramolecular cyclization in the presence of a sulfonic acid compound of the formula:R.sup.3 SO.sub.3 H (III)wherein R.sup.3 is a lower alkyl group or a substituted or unsubstituted phenyl group, in a non-halogenated organic solvent and, if desired, converting the product to a salt thereof.

Abstract: Thiazine derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.

Abstract: A process for producing an esterase by cultivating an esterase-producing microorganism is disclosed. The cultivation is carried out in a medium to which has been added an ester of sorbitan or polyoxyethylene sorbitan and a substituted or unsubstituted fatty acid having 12 to 18 carbon atoms along with an amino acid which has the formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group which may be substituted with a substituent selected from the group consisting of hydroxy, carboxy, amino, guanidino, carbamoyl, mercapto, methylthio, phenyl, hydroxyphenyl, imidazolyl and indolyl, and R.sup.2 is hydrogen, or R.sup.1 and R.sup.2 are combined to form trimethylene.

Abstract: An inidazoindolizine derivative of the formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, R.sup.2 is hydrogen, cyano, lower alkyl, lower alkanoyl, lower alkoxycarbonyl, phenyl-lower alkoxycarbonyl, lower alkylsulfonyl, substituted or unsubstituted phenyl, arylcarbonyl, or 5- or 6-membered nitrogen-containing heteromonocyclic group-substituted carbonyl, Ring A is substituted or unsubstituted phenyl, and m is 0 or 1, or a pharmaceutically acceptable salt thereof, and process for preparation thereof, said imidazoindolizine derivatives and pharmaceutically acceptable salts thereof show excellent angiotensin II inhibitory activities and are useful in the prophylaxis or treatment of hypertension.

Abstract: A method for removing tri-substituted silyl group from .beta.-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.

Abstract: Guanidinyl-containing compounds, and related compounds and salts, useful as cell receptor antagonists for modulating cell adhesion via integrin receptors and/or fibronectin receptors, are disclosed. Methods for synthesizing, testing, formulating, and using the compounds as therapeutic agents are also disclosed.

Abstract: Disclosed is a controlled release pharmaceutical preparation, comprising a core containing a pharmaceutically active ingredient, and a porous film of a hydrophobic polymeric substance or a hydrophobic polymeric substance and a hydrophilic polymeric substance, the core being coated with the porous film. Disclosed is also a method for producing the same. The controlled release pharmaceutical preparation of this invention posseses a desired dissolution rate by controlling the porosity of the porous film.

Abstract: A polysulfate of a cyclodextrin in which at least one of 6 to 8 D-glucose units constituting the cyclodextrin has been replaced by a unit represented by Formula(1): ##STR1## wherein R is a group represented by the formula: ##STR2## where R.sup.1 to R.sup.7 are defined in the specification, which have an excellent antiretrovirus activity, particularly an excellent proliferation-inhibiting activity against HIV.

Abstract: A polysulfate of a cyclodextrin in which at least one of 6 to 8,D-glucose units constituting the cyclodextrin has been replaced by a unit represented by Formula (1): ##STR1## wherein R is a group represented by the formula: ##STR2## where R.sup.1 to R.sup.7 are defined in the specification, which have an excellent antiretrovirus activity, particularly an excellent proliferation-inhibiting activity against HIV.

Abstract: Thiazine (or oxazine) derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.

Abstract: There is disclosed a process for preparing optically active 3-phenylglycidic acid ester compound, which comprises permitting a culture broth, cells or treated cells of a microorganism having an ability of stereoselectively hydrolyzing a (2R, 3S)-3-phenylglycidic acid ester compound to act on a racemic 3-phenylglycidic acid ester compound which may also have a substituent on the phenyl group, thereby hydrolyzing the (2R, 3S) optically active isomer and separating and collecting the (2S, 3R) antipode from the reaction mixture.

Abstract: Novel biphenyl derivatives of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted aminocarbonyl group, aminothiocarbonyl group, a substituted or unsubstituted lower alkoxycarbonyl group, cyano group, or a group of the formula: ##STR2## one or two of R.sup.2 to R.sup.7 are hydrogen atom, and the remaining groups are the same or different and are each a lower alkoxy group, a phenyl(lower)alkoxy group or hydroxy group, or the adjacent two groups thereof combine to form a lower alkylenedioxy group, and Alk.sup.1 is a lower alkylene group, or a pharmaceutically acceptable salt thereof, which are useful for the prophylaxis and treatment of hepatic diseases, and processes for preparing the same, and intermediates therefor.