Abstract: The present invention describes cyclic peptide compounds which modulate integrin mediated adhesion. These compounds can inhibit both .beta..sub.1 and .beta..sub.2 mediated adhesion. The invention further relates to therapeutic uses for these compounds in the treatment of adhesion related pathologies.

Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed is a pyridazinone compound represented by the formula (I): ##STR1## wherein X represents hydrogen atom or the like; Y represents a single bonding arm, oxygen atom or sulfur atom; A represents a straight or branched alkylene group which may have a double bond;B represents carbonyl group or thiocarbonyl group; and R.sup.2 represents an alkyl group having 1 to 10 carbon atoms which may be substituted or the like; orB represents sulfonyl group; and R.sup.2 represents a lower alkenyl group or the like;R.sup.1 represents hydrogen atom or the like; R.sup.3 represents hydrogen atom or the like; R.sup.4 represents hydrogen atom or the like; and R.sup.5 represents hydrogen atom or the like,or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a process for the production of a 4-substituted azetidinone. The process comprises reacting ##STR1## wherein R represents a hydrogen atom or a protecting group for N, R.sup.1 represents an alkyl which may be a substituent having an unprotected or protected hydroxyl group; and Z represents a leaving group; with ##STR2## wherein R.sup.2 represents hydrogen or alkyl, R.sup.3 and R.sup.4 each represent hydrogen, alkyl, alkenyl, alkynyl, phenyl, cycloalkyl, or naphthyl, or R.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a ring system; X and Y each represent oxygen, sulfur or N-r.sup.1, wherein r.sup.1 represents a hydrogen atom or lower alkyl; A, B, D and E each represent nitrogen or C-r.sup.2, wherein r.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy, provided that at least two of A, B, D and E are C-r.sup.

Abstract: Disclosed is a process for preparing a D-amino acid selected from the group consisting of D-methionine, D-valine, D-leucine, D-isoleucine and D-histidine, which comprises the steps of:making a culture or treated culture of a microorganism having ability to asymmetrically degrade a L-amino acid selected from the group consisting of L-methionine, L-valine, L-leucine, L-isoleucine and L-histidine act on a corresponding racemic amino acid to the L-amino acid; andseparating and collecting the remaining D-amino acid.

Abstract: A propiophenone derivative the formula ?I!: ##STR1## wherein R' is a lower alkanoyl group and R" is a hydrogen atom, or R' is a hydrogen atom and R" is a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.

Abstract: A TPN solution to be prepared before using which comprises two separate infusions of an amino acid-infusion and a saccharide-infusion wherein both of said infusions contain no sulfite ion, either one of said infusions contains a water-soluble vitamin B, a pH of the infusion containing a water-soluble vitamin B is acidic and a pH of the TPN solution prepared by mixing both infusions is neutral. According to the TPN solution of the present invention, a water-soluble vitamin B can be stably preserved in a TPN solution for a long term though it has been recognized that the water-soluble vitamin B could not be contained in a TPN solution. The present invention enables to practically use a TPN solution previously containing a water-soluble vitamin B.

Abstract: An imidazopyridine derivative of the formula ?I!: ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a lower alkanoyl group, and R.sup.3 and R.sup.4 are each lower alkyl groups, or both combine at the end thereof to form an alkylene group having 3 to 6 carbon atoms, and a pharmaceutically acceptable salt thereof, said imidazopyridine derivatives have an excellent angiotensin II antagonistic activity and are useful for the prophylaxis or treatment of hypertension.

Abstract: Disclosed is a hair-growing (restoration) agent which comprises a carnitine compound represented by the formula (I): ##STR1## wherein R.sup.1 to R.sup.3 each represent an alkyl group having 1 to 6 carbon atoms; R.sup.4 represents an aliphatic acyl group having 3 to 31 carbon atoms which may be substituted; R.sup.5 represents an alkyl group having 3 to 31 carbon atoms which may be substituted, or an alkenyl group having 3 to 31 carbon atoms which may be substituted; and X.sup.- represents an anion of a pharmaceutically acceptable acid,as an active ingredient.

Abstract: Novel sulfonamide derivatives of the formula ?I!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted monocyclic, bicyclic or tricyclic hydrocarbon, or substituted or unsubstituted heterocyclic group, Q is single bond, --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is --0--, --S-- or --NH--, Alk is lower alkylene or alkenylene, Z is --O-- or --NH --, R is substituted or unsubstituted aromatic heterocyclic or aryl, R.sup.1 is H, substituted or unsubstituted amino, substituted or unsubstituted lower alkyl, alkenyl, alkynyl, substituted or unsubstituted lower alkylthio, or alkoxy, or substituted or unsubstituted heterocyclic or aryl, or pharmaceutically acceptable salts thereof, which are useful in the prophylaxis or treatment of disorders associated with endothelin activities such as hypertension, pulmonary hypertension, renal hypertension, Raynaud disease, bronchial asthma, gastric ulcer, chronic heart failure, etc.

Abstract: Disclosed are a pyridazinone compound represented by the formula: ##STR1## wherein (1) R.sup.1 is a substituted or unsubstituted C.sub.1-10 alkyl, a C.sub.3-6 cycloalkyl, a lower alkenyl, a heterocyclic group having N, O or S atom or camphor-10-yl; R.sup.3 is hydrogen, a substituted or unsubstituted lower alkyl or a lower alkenyl; or R.sup.1 and R.sup.3 are bonded at terminal ends thereof to form a lower alkylene; and Z is a group represented by the formula: ##STR2## where n is 1 or 2; and D is hydrogen or a halogen; or (2) R.sup.1 is a substituted or unsubstituted C.sub.1-10 alkyl, a substituted or unsubstituted phenyl, a C.sub.3-6 cycloalkyl, a lower alkenyl, a heterocyclic group having N, O or S atom or camphor-10-yl; R.sup.3 is hydrogen, a substituted or unsubstituted lower alkyl or a lower alkenyl; or R.sup.1 and R.sup.3 are bonded at terminal ends thereof to form a lower alkylene; and Z is a group represented by the formula: ##STR3## and R.sup.

Abstract: A method for prophylaxis or treatment of diabetes, which comprises administering to a patient with diabetes an effective amount of a dihydrochalcone derivative of the formula ?I!: ##STR1## wherein Ar is an aryl group, R.sup.1 is 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: A benzenesulfonamide derivative of the formula ?I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.

Abstract: A pharmaceutical preparation for oral administration which is controlled to release a medicinal active ingredient at a targeted site in the intestinal tract comprising (a) a core containing a medicinal active ingredient and (b) a press-coated layer comprising an enteric polymer, said layer being provided around the core. In the pharmaceutical preparation of the present invention, the medicinal active ingredient is not released during residence in the stomach and, after discharged from the stomach, until reaching a targeted site in the intestine, and thereafter is quickly released, so that the medicinal active ingredient is efficiently delivered to the targeted site in the intestinal tract.

Abstract: A process for preparing D-lysine using a microorganism which has the ability to asymmetrically degrade L-lysine in a reaction medium is disclosed. The process is performed by first bringing racemic lysine into contact with a culture or a treated culture of the microorganism, and then collecting and isolating the D-lysine from the reaction mixture.

Abstract: Cyclized integrin receptor antagonist compounds useful in modulating cell adhesion, including adhesion related to fibronectin, as well as leukocyte adhesion to endothelial cells, are disclosed. Methods for synthesizing, testing, formulating, and using the compounds as therapeutic agents are also disclosed.

Abstract: There are disclosed novel substituted naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives that are useful in a method of treating immuno-inflammatory diseases in a mammalian patient suffering therefrom. Pharmaceutical compositions containing the sulfonamide compounds are also provided.

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: Novel process for preparing azetidinone compound of the formula ?III!: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula ?I!: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula ?II!: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound ?Ill! being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.

Abstract: Disclosed is a pyridazinone compound represented by the formula (I): ##STR1## wherein X represents hydrogen atom or the like; Y represents a single bonding arm, oxygen atom or sulfur atom; A represents a straight or branched alkylene group which may have a double bond;B represents carbonyl group or thiocarbonyl group; and R.sup.2 represents an alkyl group having 1 to 10 carbon atoms which may be substituted or the like; orB represents sulfonyl group; and R.sup.2 represents a lower alkenyl group or the like;R.sup.1 represents hydrogen atom or the like; R.sup.3 represents hydrogen atom or the like; R.sup.4 represents hydrogen atom or the like; and R.sup.5 represents hydrogen atom or the like,or a pharmaceutically acceptable salt thereof.