Abstract: A method of treating cognitive deficiencies is described by administering a quinazoline derivative of the general formula ##STR1## wherein A represents ##STR2## in which n is 1-10, P is a bond or (CH.sub.2).sub.m in which m is 0-10, and M is .dbd.O, .dbd.S, .dbd.NR, .dbd.CRR', ##STR3## novel compounds of the above are also described as well as methods of manufacture and pharmaceutical compositions.

Abstract: An optically active compound of formula (I): ##STR1## in which R.sup.3 represents groups of formula --A--COOR.sup.4, whereinA represents alkylene groups having 3 or 5 carbon atoms andR.sup.4 represents hydrogen or an alkyl group having 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof.

Abstract: Thiazolidinecarboxylic acid amides having combined antiallergic and antiasthmatic activities with an antagonist activity against platelet Activating Factor and having the following general formula (I) ##STR1##

Abstract: The present invention is concerned with novel imidazo[2, 1-b][3]benzazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.4 represents hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, phenyl or halo; R.sup.5 represents hydrogen, C.sub.1-4 alkyl or halo; L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.

Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders. Compounds of particular interest are of Formula I ##STR1## wherein W is N or CH.sub.2 ; wherein X is N or CR.sup.2 ; wherein Y is (CH.sub.2).sub.n and n is 1 to 3; wherein Z is C.dbd.R.sup.3 or CR.sup.4 R.sup.5, or wherein Y and Z together forms --CR.sup.6 .dbd.CR.sup.7 --, --CR.sup.6 .dbd.CR.sup.7 --CH.sub.2 or --CR.sup.6 .dbd.CR.sup.7 --CH.sub.2 --CH.sup.2 --; wherein the remainder of the variables are as defined in the specification; or a pharmaceutically suitable salt or tautomer thereof.

Abstract: Compounds of formula (I): ##STR1## [wherein: A-- B is .dbd.C.dbd.CH--or a nitrogen atom; R.sup.1 is hydrogen, alkyl, aryl or aralkyl; and Z is alkylene] and pharmaceutically acceptable salts thereof are useful in the treatment and prevention of allergies and asthma.

Abstract: A tricyclic compound represented by the general formula (1) and salts thereof are disclosed. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.

Abstract: A class of 6-arylpyrimidines which is useful in the control of weeds is of the general formulae: ##STR1## wherein R.sup.2 is selected from hydrogen, halo, substituted or unsubstituted alkyl, haloalkyl, polyhaloalkyl, haloalkenyl, polyhaloalkenyl, haloalkynyl, polyhaloalkynyl, alkenyl, alkynyl, alkoxy, alkylthio, alkoxycarbonylalkyl, cyano, alkoxyalkyl, alkoxycarbonyl, cycloalkyl, aralkyl, alkylamino, dialkylamino, or dialkylaminocarbonyl group; R.sup.3 is an alkyl, alkenyl, alkynyl, or haloalkyl group; R.sup.5 is an alkyl, alkenyl, alkynyl, alkenynyl, or alkoxyalkyl, group; R.sup.6 is an aryl group (e.g. aromatic ring); and X is oxygen or sulfur. R.sup.2 and R.sup.3 may form a fused ring.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, CF.sub.3, aryl, substituted aryl, heteroaryl, -O-C.sub.1 -C.sub.7 alkyl, or -O-C.sub.3 -C.sub.7 cycloalkyl; R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, CF.sub.3, NO.sub.2, halogen, OR.sup.7, NR.sup.8 R.sup.9 or S(O).sub.m R.sup.10, wherein m is 0, 1 or 2; R.sup.4 is H, C.sub.1 -C.sub.7 alkyl, arylmethyl, or substituted arylmethyl; R.sup.5 and R.sup.6 are each independently H, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, aryl, substituted aryl, heteroaryl, arylmethyl, substituted arylmethyl, or taken together constitute a chain of (CH.sub.2).sub.k groups, wherein k is 3, 4, or 5; R.sup.7, R.sup.8 and R.sup.9 are each independently H, C.sub.1 -C.sub.7 alkyl, -C(.dbd.O)-(C.sub.1 -C.sub.7 alkyl), -C(.dbd.O)-aryl, or -(C.dbd.O)heteroaryl; R.sup.10 is C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.

Abstract: Compounds of formula (I): ##STR1## in which: Q is nitrogen or .dbd.CH--; R.sup.1 and R.sup.2 are hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl or halogen; and R.sup.3 is a substituted alkyl groups or a pharmaceutically acceptable salt thereof have valuable anti-allergic and anti-asthmatic activities. The compounds are prepared by reacting a corresponding compound where R.sup.3 is replaced by a hydrogen atom with a compound to introduce the group R.sup.3.

Abstract: Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.

Abstract: The present invention relates to a process for preparing 3-amino-9,13b-dihydro-1H-dibenz[c,f]-imidazo[1,5-a]azepine-hydrochloride, as follows:a) hydrogenating 6-phthalimidomethyl-5H-dibenz[b,e]-azepine, to produce 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine;b) reacting the 6-(phthalimidomethyl)-6,11-dihydro-5H-dibenz[b,e]azepine with hydrazine, to produce 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine;c) reacting the 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepine with bromooyanogen, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine; andd) precipitating the 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine in the presence of DMF and HCl, to produce 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine-hydrochloride.

Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.

Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: A process for formation of a base from a base precursor, which comprises decomposing the base precursor in the presence of a catalyst. The base precursor has the following formula (I) or (II):(R.sup.1 --C.tbd.C--CO.sub.2 H).sub.x .multidot.B (I)R.sup.2 (--C.tbd.C--CO.sub.2 H).sub.2 .multidot.B.sub.y (II)wherein R.sup.1 is a monovalent group selected from the group consisting of hydrogen, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aryl group, a heterocyclic group, an aralkyl group, an acyl group, an alkoxycarbonyl group, carbamoyl, --CO.sub.2 M (M is an alkali metal) and --CO.sub.2 H.B, each of which may have one or more substituent groups; R.sup.

Abstract: 3-Piperazinyl-1,2-benzazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of disorders in which serotonin and/or dopamine release is of predominant importance.

Abstract: This invention relates to an improved process for the preparation of cyanoalkyl lactams by the reaction of an unsaturated nitrile with a lactam, said cyanoalkyl lactam of the formula ##STR1## wherein R is H, or methyl, R.sub.1 is H, methyl or ethyl and n is a number ranging from 2-11 and wherein each of the methylene groups may carry a lower alkyl substituent as shown. The improvement comprises: reacting said lactam with an alpha-beta unsaturated nitrile having from 3-6 carbon atoms in the presence of a catalytic amount of a diazabicycloalkene of the formula ##STR2## wherein R, R.sub.1 and n have the above meaning. Typically, acrylonitrile is reacted with .epsilon.-caprolactam in the presence of diazabicycloundecene.

Abstract: New heterocyclic derivatives having the general formula: ##STR1## wherein X is ##STR2## or CO.sub.2 R' whereinR' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, andA-- is --(CH.sub.2).sub.n --Y--(CH.sub.2).sub.m --,wherein n and m are 0 or 1 and --Y-- is --O--, --S--, --CH.sub.2 --, or --NR''--, wherein R'' is hydrogen or C.sub.1-6 -alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics and in human and animal health as anthelmintics, etco- and endoparasiticides, insecticides and acaricides.

Abstract: A compound of formula (I): ##STR1## in which R is optionally substituted phenyl; C.sub.3-8 cycloalkyl; C.sub.5-8 cycloalkenyl; C.sub.1-8 alkyl which may be straight or branched; C.sub.2-8 alkenyl which may be straight or branched; 5- or 6-membered heterocyclyl; or optionally substituted phenyl C.sub.1-4 alkyl, each of Y and Z, which may be the same or different, is oxygen or sulphur; and X is --CH.sub.2 -- or oxygen, a process for the preparation of such compounds and their use in human and veterinary medicine.

Abstract: There are described new halocyclopropyl compounds of the general formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, independently of each other, are hydrogen or C.sub.1-4 -alkyl,X is hydrogen or halogen,Y is halogen,n is 0, 1, 2 or 3,U and V are hydrogen or halogen, andW is a heterocyclic group of formula ##STR2## in which T is halogen, C.sub.1-4 -alkyl, C.sub.1-4 -haloalkyl, CN or OR.sub.9Q is CH or N,Z is O or S,R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each a straight, branched or cyclic C.sub.1-7 -alkyl group optionally substituted by up to six halogen atoms, orR.sub.4 and R.sub.5, can also together form a 4 to 7 membered ring that is saturated or unsaturated and can contain further hetero atoms, such as O, S or N, and can optionally be substituted by one to three methyl groups or one to six halogen atoms, andR.sub.9 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-4 -haloalkyl,processes for their preparation and their use as herbicide with high selectivity.

Abstract: Novel quinolone and naphthyridine antibacterial agents are herein described having improved in vivo activity both orally and subcutaneously where the 7-side chain of such compounds contain an .alpha.-amino acid; also described are its corresponding optical isomers, methods of preparation as well as compositions and methods of treating infections diseases.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridge arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl,, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.6 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.

Abstract: Novel heterocyclicmethanols are disclosed having the formula: ##STR1## wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl; R.sup.1 is hydrogen, loweralkyl or carbethoxymethyl;R.sup.2 is hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl;R.sup.3 is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino;the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R.sup.4 loweralkyl group, or R.sup.1 may form methylene or --CH.sub.2 -C(O)-bridges with R.sup.4 ;the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: Novel cyclized N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.

Abstract: The compounds of formula I ##STR1## in which the substituents X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6, are defined hereinbelow. The compounds have advantageous herbicidal properties and are useful, for example, for combating undesired plants.

Abstract: Disclosed are compounds of formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidized etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C.sub.2 -C.sub.20 -acyl, cyano, free or functionally modified carboxy; and R.sub.2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidized etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3 or 4, and R.sub.1 and R.sub.2 are as defined above under formula I and salts thereof; e.g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e.

Abstract: The invention provides novel imidazoquinolines, processes for their preparation and pharmaceutical compositions containing them. The compounds have Formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,R.sup.1 and R.sup.2 are the same or different and are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyalkyl, C.sub.1-6 hydroxyalkyl, hydroxy, halogen, nitro, carboxy, carboxylic lower alkyl ester, carbamoyl, carbamoyloxy, cyano, loweralkanoyl, lower alkanoylamino or trifluoromethyl, Het is a heterocyclic group chosen from imidazolyl, imidazolinyl, benzimidazolyl, thiazolyl, thiazolinyl, quinolyl, piperidyl, pryidyl, benzothiazoly and pyrimidyl, any of which heterocyclic groups may be substituted, and x is 0 or 1, and pharmaceutically acceptable salts thereof.The compounds are anti-ulcer/anti-secretory agents.

Abstract: The invention relates to a novel process for the preparation of the optically pure 2S- or 2R-indolinecarboxylic acid of the formula ##STR1## and salts thereof. The process comprises forming the heterocyclic 5-membered ring in formula I from an open chain precursor by diastereoselective cyclization.

Abstract: Amidines of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl groups and the sum of the carbons in R.sub.1 and R.sub.2 is from 2 to 16 are produced by cyanoethylation of the lactam: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, followed by reduction and, finally, cyclization by dehydration. The compounds produced are useful for curing epoxy and urethane resins.

Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.

Abstract: A compound of formula (I): ##STR1## in which R is optionally substituted phenyl; C.sub.3-8 cycloalkyl; C.sub.5-8 cycloalkenyl; C.sub.1-8 alkyl which may be straight or branched; C.sub.2-8 alkenyl which may be straight or branched; 5- or 6- membered heterocyclyl; or optionally substituted phenyl C.sub.1-4 alkyl, each of Y and Z, which may be the same or different, is oxygen or sulphur; and X is --CH.sub.2 -- or oxygen, a process for the preparation of such compounds and their use in human and veterinary medicine.

Abstract: The subject invention concerns novel and useful antiviral compounds referred to as eudistomins. These compounds are obtainable from well-known and available marine organisms. Their utility is as antiviral agents as well as antibacterial and antitumor agents in some cases.

Abstract: The invention provides a compound of formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,Ar is a phenyl or naphthyl group which may be substituted or unsubstituted,R.sup.1 and R.sup.2 are the same or different and are hydrogen, alkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, hydroxy, halogen, nitro, carboxy, a carboxylic alkyl ester, carbamoyl, carbamoyloxy, cyano, acyl, acylamino or trifluoromethyl, or an acid addition salt thereof.The compounds are useful for the treatment of ulcers or hypersecretion in mammals. Pharmaceutical compositions containing the novel compounds and processes for their preparation are described.