Abstract: A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

Abstract: A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

Abstract: A pharmaceutical preparation efficaciously promotes tissue wound repair. The wound repair promoter according to the present invention includes at least one active ingredient selected from the group consisting of compounds represented by Formula (1), salts of the compounds, and hydrates of the compounds or the salts. In the formula, R1 and R2 are each, identically or differently, selected from hydrogen and a hydrocarbon group optionally having one or more substituents selected from the group consisting of halogens, —COOR3, —CONR32, —COR3, —CN, —NO2, —NHCOR3, —OR3, —SR3, —OCOR3, —SO3R3, and —SO2NR32, where R3 is, identically or differently in each occurrence, selected from hydrogen and an optionally substituted aliphatic hydrocarbon group; and n represents an integer of 1 or more.

Abstract: Provided is a method for separating the four optical isomers of Nahlsgen.

Abstract: A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

Abstract: A pharmaceutical preparation efficaciously promotes tissue wound repair. The wound repair promoter according to the present invention includes at least one active ingredient selected from the group consisting of compounds represented by Formula (1), salts of the compounds, and hydrates of the compounds or the salts. In the formula, R1 and R2 are each, identically or differently, selected from hydrogen and a hydrocarbon group optionally having one or more substituents selected from the group consisting of halogens, —COOR3, —CONR32, —COR3, —CN, —NO2, —NHCOR3, —OR3, —SR3, —OCOR3, —SO3R3, and —SO2NR32, where R3 is, identically or differently in each occurrence, selected from hydrogen and an optionally substituted aliphatic hydrocarbon group; and n represents an integer of 1 or more.

Abstract: Provided is a method for separating the four optical isomers of Nahlsgen.

Abstract: The present invention provides a process for preparing a novel phenylalanine derivative of the formula (I): wherein X1 is a halogen atom, X2 is a halogen atom, Q is a group of the formula —CH2— or —(CH2)2— and Y is a lower alkyl group, or a pharmaceutically acceptable salt thereof, which has excellent inhibitory effects on ?4 integrin-mediated cell adhesion, and an intermediate useful in the process.

Abstract: The present invention provides a process for preparing a novel phenylalanine derivative of the formula (1): wherein X1 is a halogen atom, X2 is a halogen atom, Q is a group of the formula —CH2— or —(CH2)2— and Y is a lower alkyl group, or a pharmaceutically acceptable salt thereof, which has excellent inhibitory effects on ?4 integrin-mediated cell adhesion, and an intermediate useful in the process.

Abstract: The present invention is to provide a benzenesulfonic acid salt and a benzoic acid salt of (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid represented by the formula (I): 1

Abstract: The present invention is to provide a benzenesulfonic acid salt and a benzoic acid salt of (S)-4-[4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidino]butanoic acid represented by the formula (I): wherein * represents an asymmetric carbon, which are excellent in antihistaminic activity and anti-allergic activity, and a process for producing the same.

Abstract: An optically active salt of 1,5-benzothiazepine compound of the formula (I) or (II): ##STR1## wherein each of Ring A and Ring B is a substituted or unsubstituted benzene ring, and R.sup.1 and R.sup.2 are the same or different and each is a lower alkyl group, can be prepared by resolving a racemic salt of 1,5-benzothiazepine compound of the formula (I) or (II) by means of preferential crystallization.

Abstract: A novel process for preparing 1,5-benzothiazepine derivative ?II!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted benzene ring, and R.sup.3 is H, (di-lower alkylamino)-lower alkyl or substituted or unsubstituted piperazinyl-lower alkyl, or a salt thereof, in high yield and in a single step from a novel 3-(2-amino-substituted or unsubstituted phenylthio)-2-hydroxy-3-substituted or unsubstituted phenylpropionamide compound. Said 1,5-benzothiazepine derivative ?II! is useful as an intermediate for preparing medicaments such as diltiazem hydrochloride.

Abstract: An optical resolution process of the compound of the formula (1): ##STR1## wherein Ring A and Ring B are a substituted or unsubstituted benzene ring and R.sup.1 and R.sup.2 are the same or different and a lower alkyl group, by utilizing difference in solubility between the two diastereoisomeric salts prepared by treating the racemic compound (1) with an acidic resolution agent. The present process is industrially advantageous with compared to conventional processes for preparing an optically active 3-hydroxy-1,5-benzothiazepine derivative which are useful as an intermediate for preparing medicines.

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 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: .alpha.-(S)-amino acid..alpha.-phenylethanesulfonate compounds and methods of optical resolution of .alpha.-amino acids and .alpha.-phenylethanesulfonic acids are described.

Abstract: The present invention relates to the optical resolution of a p-hydroxyphenylglycine salt with simultaneous racemization of the undesired enantiomer thereof. The invention is carried out by preferential crystallizing out the desired enantiomer from a supersaturated solution of the racemic modification thereof in a lower aliphatic acid in the presence of an aliphatic or aromatic aldehyde.

Abstract: p-Hydroxyphenylglycine..alpha.-phenylethanesulfonate which is useful for the production of optically active p-hydroxyphenylglycine and optically active .alpha.-phenylethanesulfonic acid is disclosed. p-Hydroxyphenylglycine..alpha.-phenylethanesulfonate is produced by either reacting DL-p-hydroxyphenylglycine with optically active .alpha.-phenylethanesulfonic acid or reacting (.+-.)-.alpha.-phentylethanesulfonic acid with optically active p-hydroxyphenylglycine to form two diastereomers of DL-p-hydroxyphenylglycine optically active .alpha.-phenylethanesulfonate or optically active p-hydroxyphenylglycine (.+-.)-.alpha.-phenylethanesulfonate, and isolating one diastereomer according to the difference between solubilities of the diastereomers, optionally, combining selective crystallization of one diastereomer and epimerization of another diastereomer in the case of reaction of DL-p-hydroxyphenylglycine and optically active .alpha.-phenylethanesulfonic acid.

Abstract: DL-.alpha.-amino acids or a salt thereof can be obtained by racemizing an optically active .alpha.-amino acid or a salt thereof in the presence of an aliphatic acid and an aldehyde.