Abstract: Dioxacycloalkane compounds of the formula ?1! ##STR1## wherein A is ##STR2## wherein W is ##STR3## X is --CO-- or --SO.sub.2 --; Y is --CH.sub.2 --, --O-- or --NR.sup.25 --; and R.sup.1 is an aralkyl which may be substituted by lower alkoxy;R.sup.2 is a hydrogen atom or a lower alkyl;R.sup.3 is --(CH.sub.2)d-SR.sup.26 or ##STR4## R.sup.4 and R.sup.5 are each a hydrogen atom or a lower alkyl; and E is --C(R.sup.29)(R.sup.30)-- or --CH.sub.2 CH.sub.2 --, pharmaceutically acceptable salts thereof, intermediates for producing said compounds, and methods for producing said intermediates. The compounds of the formula ?1! have a strong inhibitory activity against renin and show continuous hypotensive action by oral administration. They are useful as hypotensive agents or therapeutic agents for heart failure.

Abstract: Chroman derivatives of the formula ?I! ##STR1## wherein R.sup.1 is a cyano, a nitro, a trihalomethyl, a trihalomethoxy or a halogen atom; R.sup.2 is a lower alkoxyalkyl, an aryloxyalkyl or a dialkoxyalkyl; R.sup.3 is a lower alkoxyalkyl or an aryloxyalkyl; R.sup.4 is a hydroxy, a formyloxy or a lower alkanoyloxy; X is N--H, an N--optionally substituted lower alkyl, an oxygen atom, a sulfur atom or a single bond; and Y is an optionally substituted aromatic ring residue or an optionally substituted heterocyclic residue, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The compound of the present invention and pharmaceutically acceptable salts thereof have selective and excellent coronary vasodilating action and extremely weak hypotensive action.

Abstract: Compounds of the formula ##STR1## wherein R is a hydrogen atom or an acyl; U is --O--, --CHR.sup.1 -- or --NR.sup.2 -- wherein R.sup.1 is a hydrogen atom or a hetero ring, and R.sup.2 is a hydrogen atom or a lower alkoxycarbonyl lower alkyl; V is --O--, --S--, --CHR.sup.3 -- or --NR.sup.4 -- wherein R.sup.3 is a hydrogen atom or a lower alkoxycarbonyl, and R.sup.4 is a hydrogen atom, a lower alkyl or an acyl; W is methyl, a hetero ring or optionally substituted phenyl; X and Y are the same or different and each is --CH.sub.2 -- or --S--; m is an integer of 0 to 6; and n is an integer of 1 to 4, and pharmaceutically acceptable salts thereof.The compounds of the present invention have specifically strong inhibitory activity against prolyl endopeptidase, and suppress decomposition and inactivation of TRH, substance P, neurotensin, vasopressin and the like. Accordingly, the compounds can be used for the prophylaxis and/or treatment of dementia and amnesia including Alzheimer's disease.

Abstract: Novel proline derivatives of the following formula (I) ##STR1## wherein each symbol is as defined in the specification, which specifically inhibit prolyl endopeptidase activity and can be used for the prevention and/or treatment of dementia and amnesia as agents which act directly on the central symptoms of dementia.

Abstract: Compounds of the formula I ##STR1## are disclosed. In this formula, R is a member selected from the group consisting of --CR.sub.1 R.sub.2 R.sub.3, hydroxy, an alkoxy group having 1 to 4 carbon atoms and --NR.sub.4 R.sub.5, in which at most one of R.sub.1, R.sub.2 and R.sub.3 is hydrogen and the remainder are each independently selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, a cycloalkylalkyl having 4 to 9 carbon atoms and a 3 to 6 membered cyclic ether; R.sub.4 and R.sub.5 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; R.sub.6 and R.sub.7 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; and R.sub.8 is hydrogen, an alkyl group having 1 to 4 carbon atoms, hydroxy, an alkoxy group having 1 to 4 carbon atoms or halogen. Salts of these compounds are also disclosed.

Abstract: Disclosed is a novel oxazinone derivative represented by formula (I) given below or a pharmaceutically acceptable acid-addition salt thereof, which is useful as an anti-inflammatory agent, an agent for suppressing neutrophil infiltration and as a serine protease inhibitor: ##STR1## where A includes, for example, ##STR2## in which W is --O--, --S--, --CH.dbd.CH-- or --NR.sup.9 -- or means that (CH.sub.2).sub.n is directly bonded to (CH.sub.2).sub.n,V.sup.2 is .dbd.CR.sup.12 -- or .dbd.N--, andD is 5 to 7-membered carbon ring or hetero ring;X is --O--, --S--, --CO--, or --NR.sup.15 or means that A is directly bonded to (CH.sub.2).sub.l ;Y is --O--, --CH.dbd.CH-- or --NR.sup.16 -- or means that (CH.sub.2).sub.l is directly bonded to Z;Z is --CH.sub.2 -- or --CO--; andl is an integer of 0 to 4.Further, R and R.sup.1 to R.sup.16 are hydrogen atom, lower alkyl group, etc.

Abstract: Provided is a novel (1R, 2S)-1-acyl-2-carboxycyclohex-4-ene derivative represented by the following general formula [I], and its producing method, ##STR1## (where R.sup.1 represents a hydrogen atom, a lower alkyl group, or substituted or unsubstituted aryl group, and R.sup.2 represents a hydrogen atom, or a lower alkyl group). Also provided is a method of producing a (3S, 4R)-4-substituted-3-carboxycyclopentanone derivative represented by the following general formula [A], ##STR2## (where R.sup.1 and R.sup.2 are the same as those mentioned above).

Abstract: Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of .alpha.-amino aldehyde derivative [I] and compound [II] in the presence of BF.sub.3.OEt.sub.2, as shown in the following reaction formula, .alpha.-amino-.beta.-hydroxy-.delta.-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R.sup.1 is a protective group on the amino group, R.sup.2 is a lower alkyl group which may be branched, and R.sup.4 is a cyclohexyl group or phenyl group).

Abstract: A 1,3,2-dioxathiolane oxide derivative is represented by the following formula: ##STR1## wherein X represents --S(O)-- or --S(O).sub.2 --;R.sup.1 represents a hydrogen atom, an alkali metal atom, a benzyl group, or a lower alkyl group;R.sup.2 represents a lower alkyl group which may be substituted with a methylthio group, or a benzyl group, andR.sup.3 and R.sup.4 may be the same or different and independently represent a hydrogen atom, an alkyl group having one to ten carbon atoms, a lower alkyl group substituted with a guanidyl group, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group, or a phenethyl group, or together form an alkylene group.

Abstract: 4H-3,1-benzoxazin-4-one derivatives represented by formula (I) below: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a lower alkyl group, a lower alkylthioalkyl group, or a lower alkanesulfinylalkyl group, R.sup.3 represents a hydrogen atom a hydroxyl group, a lower alkoxy group, or a lower acyloxy group, X represents an amino acid residue selected from the group consisting of alanine, valine, and phenylalanine, n represents an integer of 0, 1, or 2, and Y means a substituent selected from the group consisting of an alkanoyl group having 2 to 6 carbon atoms which may be substituted by a phenyl group, a benzyloxycarbonyl group, a lower alkoxycarbonyl group, a cinnamoyl group, and a methoxysuccinyl group. These derivatives exhibit a strong serine protease inhibiting effect, and are useful as effective components of agents for preventing and curing diseases caused by the excessive effect of serine proteases, e.g.

Abstract: Novel peptide derivatives of the following formula ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable acid addition salts thereof and analogous copounds thereof.Since the derivatives and their pharmaceutically acceptable acid addition salts of the present invention possess stronger actions on central nervous system (e.g. antagonistic action against hypothermia, locomotor stimulant action, signal reflex stimulant action), they are of use as a therapeutic medicament for central nervous disorders such as impaired consciousness, depression, hypomnesia, the like in association association with schizophrenia, melancholia, senile dementia, sequelae of cerebrovascular disorders, head trauma, epilepsy and spinocerebellar degeneracy.

Abstract: Amino acid derivatives of the formula ##STR1## wherein: Q is W--(CH.sub.2).sub.m --(A).sub.n --CO--B-- whereinA is oxygen atom or --NH--;B is ##STR2## or --(CH.sub.2).sub.l -- wherein X is sulfur atom or --CH.sub.2 --, and l is an integer from 1 to 3;W is ##STR3## wherein Hal is halogen atom; n is an integer of 0 or 1; andm is an integer from 0 to 3;Y is sulfur atom or --CH.sub.2 --; andR is hydrogen atom, formyl group, C.sub.1-5 alkoxycarbonyl group, --C.tbd.N or ##STR4## wherein R.sup.1 is hydrogen atom, andR.sup.2 is hydroxyl group, C.sub.1-5 alkylcarboxy group, phenylcarboxy group, C.sub.1-5 alkoxy group or phenyl C.sub.1-5 alkoxy group;with the proviso that when R is hydrogen atom, formyl group or C.sub.1-5 alkoxycarbonyl group, W is ##STR5## The compounds mentioned above specifically inhibit prolyl endopeptidase activity and are useful as agents for the treatment and prevention of dementia and amnesia.

Abstract: This invention relates to new carboxylic acid derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or aryl, and pharmaceutically acceptable salt thereof which inhibit activity of DHP-I, to a process for preparing them and to an antibacterial composition comprising them and carbapenem antibiotics.

Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.

Abstract: The invention relates to a method for treatment of carcinoma or sarcoma tumor in mammals which comprises administering to said mammal an effective amount of a tetracyclo compound of the formula: ##STR1## in which R.sup.1 is formyl, protected formyl, hydroxymethyl, protected hydroxymethyl, arylaminomethyl, carboxy, protected carboxy, aryliminomethyl, hydroxyiminomethyl, alkoxyiminomethyl, acyloxyiminomethyl, semicarbazonomethyl or arylsemicarbazonomethyl,R.sup.2 is hydroxy, alkoxy, or protected hydroxy,R.sup.3 is hydrogen and R.sup.4 is methyl, hydroxymethyl or protected hydroxymethyl, orR.sup.3 and R.sup.4 are combined together to form methylene or oxo,R.sup.5 is hydroxy, alkoxy or protected hydroxy, andR.sup.6 is hydrogen, imino-protective group or alkyl,and pharmaceutically acceptable salts thereof.

Abstract: The invention relates to novel furanone derivatives, having an aldose reductase-inhibitory activity, of the formula ##STR1## wherein A is a lower alkylene group,R.sup.1 is a carboxy, hydroxy, protected hydroxy or lower alkoxycarbonyl group,R.sup.2 is a hydrogen or halogen atom or a halo (lower) alkyl group, andR.sup.3 is a hydrogen atom or a hydroxy, carboxy, lower alkoxy or lower alkoxycarbonyl group.

Abstract: The invention relates to compounds of antihypertensive and antithrombotic activity of the formula or its pharmaceutically acceptable salt: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, or lower alkoxyphenyl,R.sup.2 is hydrogen or lower alkyl,R.sup.4 is lower alkyl,R.sup.6 is hydrogen or lower alkyl,R.sup.7 is lower alkyl which is optionally substituted by hydroxy or lower alkanoyloxy, andR.sup.10 is hydrogen or lower alkyl which is optionally substituted by carboxy or esterified carboxy.

Abstract: New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.

Abstract: New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.

Abstract: A biologically pure culture of Streptomyces sandaensis which is capable of producing an antitumor and antimicrobial compound, designated FR-900482 substance, is disclosed.