Abstract: The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

Abstract: Novel 2-(4-piperidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds, intermediates and processes for the preparation thereof, and methods of treating psychoses employing compounds and compositions thereof are disclosed.

Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.

Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.3, --COR.sup.3, --CONR.sup.3 R.sup.4 or --SO.sub.2 R.sup.3 (wherein R.sup.3 and R.sup.4, which may be the same or different each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.3 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.3 or --SO.sub.2 R.sup.3);and R.sup.2 represents a group of formula (a), (b) or (c): ##STR2## wherein R.sup.5 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.

Abstract: A .beta.-carbolin-3-carboxylic acid derivative of the formula ##STR1## wherein: X is oxygen, sulphur or NR.sup.10, wherein R.sup.10 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl;R.sup.3 is (a) C.sub.1-10 -alkoxy, C.sub.1-10 -alkenyloxy, C.sub.6-10 -aryloxy, C.sub.7-11 -aralkoxy or C.sub.8-12 -aralkenyloxy, each optionally substituted with one or more hydroxy groups, halogen atoms, CF.sub.3 groups, C.sub.1-10 -alkoxy groups or C.sub.2-4 -alkenyloxy groups or each optionally substituted with an amino, di-C.sub.1-6 -alkylamino, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl group; or (b) NR.sup.11 R.sup.12, wherein R.sup.11 and R.sup.12 are the same or different and each is (i) hydrogen, (ii) hydroxy, (iii) C.sub.1-10 -alkyl, (iv) C.sub.2-10 -alkenyl, (v) C.sub.6-10 -aryl, (vi) C.sub.7-11 -aralkyl, (vii) C.sub.8-12 -aralkenyl, (viii) C.sub.3-7 -cycloalkyl, or (ix) C.sub.

Abstract: The invention provides potent and selective antagonists of 5-HT and 5-HT.sub.3 receptors which are tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the group represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and physiologically acceptable salts and solvates thereof.

Abstract: Compounds which are potent and selective antagonists of the effect of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, anxiety, and nausea and vomiting, of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula (a), (b) or (c): ##STR2## one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;n represents 1 or 2;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5 ; andX represents an oxygen or a sulphur atom, and, when Im represents an imidazolyl group of formula (c), X may also represent the group NR.sup.6, where R.sup.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl wherein the phenyl moiety is optionally substituted by one or more C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, halo, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl or carboxy groups; R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, chloro, fluoro, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl and carboxy, and phenyl, phenyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkoxy in which any phenyl moiety is optionally substituted by any of these groups; R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.

Abstract: Phenoxy-substituted beta-carbolines of the formula I ##STR1## X is COOR.sup.3, CONHC.sub.1-3 -alkyl or oxadiazolyl of the formula ##STR2## R.sup.2 is H, lower alkyl or cycloalkyl, R.sup.3 is lower alkyl,R.sup.4 is hydrogen, lower alkyl or lower alkoxyalkyl,R.sup.1 is hydrogen, halogen, lower alkyl, lower alkoxy, acyl, phenyl, C.sub.2-5 alkylenedioxy, trifluoromethyl, nitrilo, nitro, lower alkoxycarbonyl, azido, SO.sub.2 R.sup.6, SO.sub.2 NR.sup.7 R.sup.8, or NR.sup.9 R.sup.10,R.sup.6 is lower alkyl,R.sup.7 and R.sup.8 independently are lower alkyl or together with the nitrogen atom form a hetero ring,R.sup.9 and R.sup.10 independently are hydrogen, lower alkyl, acyl or together with the nitrogen atom form a hetero ring system,with the proviso that X is not COOEt, if ##STR3## is 5-phenoxy and R.sup.4 is methyl or ##STR4## is 6-(4-methoxyphenoxy) and R.sup.4 is methoxymethyl have valuable pharmacological properties.

Abstract: A process is disclosed for the preparation of 4-alkoxyalkyl .beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is an optionally substituted aliphatic hydrocarbon residue,R.sup.3 is lower alkyl, andR.sup.A is hydrogen, halogen, COOR.sup.4 or OR.sup.5, R.sup.4 meaning lower alkyl and R.sup.5 meaning hydrogen, lower alkyl, cycloalkyl, or optionally substituted pheny,by reaction of a compound of Formula II in the presence of AgBF.sub.4 with an alcohol of the formula R.sup.2 OH wherein R.sup.2 has the meanings given above.

Abstract: .beta.-Carbolines of general Formula I ##STR1## wherein Y represents the residue ##STR2## and R.sup.a and R.sup.b, being identical or different, mean respectively hydrogen, C.sub.1-6 -alkoxy, phenyl, C.sub.3-7 -cyclo-alkyl, optionally substituted C.sub.1-6 -alkyl or C.sub.1-6 -alkoxycarbonyl, and R.sup.c and R.sup.d, being identical or different, mean respectively hydrogen or C.sub.1-6 -alkyl or jointly a linkage, andR.sup.4 is hydrogen, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl andR.sup.5 is hydrogen, halogen, OR.sup.6, NR.sup.7 R.sup.8 or CH R.sup.9 R.sup.10 wherein R.sup.6 means C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or an optionally substituted aralkyl, aryl or hetaryl residue, R.sup.7 and R.sup.8, being identical or different, represent hydrogen, C.sub.1-6 -alkyl, C.sub.3-6 -alkenyl, or jointly with the nitrogen atom a saturated heterocyclic five- or six-membered ring which optionally contains a further hetero atom, R.sup.9 means hydrogen or C.sub.1-6 -alkyl, R.sup.10 means hydrogen, C.sub.

Abstract: .beta.-Carbolines of general Formula I ##STR1## wherein R.sup.3 is ##STR2## or --COOR", wherein R' is C.sub.1-3 alkyl or C.sub.3-6 cycloalkyl and R" is C.sub.1-4 alkyl; R.sup.4 is hydrogen, methyl, ethyl or methoxymethyl; and R.sup.A is ##STR3## wherein X is C.sub.1-12 straight-chain, branched-chain, saturated or unsaturated alkyl or a corresponding alkyl group with a CH.sub.2 -group substituted by a carbonyl group and R"" is one or more of fluorine, chlorine, bromine, or iodine, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-5 acyloxy, phenyl, C.sub.2-5 alkylenedioxy, trifluoromethyl, nitrilo, nitro or --NR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V, which can be the same or different are hydrogen, C.sub.1-3 alkyl, C.sub.1-5 acyl or phenyl, or collectively with the amido nitrogen atom form a 3- to 6-membered hetero ring, which are prepared conventionally by esterifying a corresponding compound wherein R.sup.A is H or R.sup.

Abstract: A 7-bromo-.beta.-carboline compound of the formula (I): ##STR1## wherein R.sup.1 =H or C.sub.1 -C.sub.5 alkyl and R.sup.2 =C.sub.1 -C.sub.5 alkyl or benzyl, is produced by reacting a .beta.-carboline compound of the formula (II): ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and R.sup.3 =H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or benzyloxy, with a brominating agent in an organic solvent in the presence of an alkalic and then hydrolyzing the resultant procursory 7-bromo-.beta.-carboline compound of the formula (III): ##STR3## is a solvent in the presence of a mineral acid.

Abstract: Heteroaryloxy-.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is an optionally substituted heteroaryl residue,R.sup.2 is hydrogen, lower alkyl or lower alkoxyalkyl,X is a COOR.sup.3 -group wherein R.sup.3 means H or lower alkyl, or represents a CONR.sup.4 R.sup.5 -group wherein R.sup.4 and R.sup.5 mean respectively hydrogen or lower alkyl, R.sup.4 and R.sup.5 being capable of forming, together with the nitrogen atom, a 5- to 6-membered heterocycle, or means an oxadiazolyl residue of the formula ##STR2## wherein R.sup.6 means hydrogen, lower alkyl or cycloalkyl, are valuable pharmaceuticals.

Abstract: The present invention relates to new compounds which are the 1,2-dihydro-4-methyl-1-oxo-5H-pyrido(4,3-b)indoles with the formula (I): ##STR1## in which R represents hydrogen or an alkoxy or aryl carbonyloxy group. These compounds are intermediates of synthesis in the preparation of compounds which can be used in the pharamaceutical industry. The invention is also concerned with their synthesis.

Abstract: 5,6,7,8-tetrahydro-beta-carbolines derivatives of formula I ##STR1## wherein R.sup.1 is an oxadiazolyl radical of the formula ##STR2## COOR.sup.3 or CONR.sup.4 R.sup.5, R.sup.2 is H, lower alkyl or cycloalkyl,R.sup.3 is H or lower alkyl,R.sup.4 and R.sup.5 are H or lower alkyl, whereby R.sup.4 and R.sup.5 cannot be hydrogen at the same time, or R.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 5- or 6-member ring, which additionally can contain a heteroatom, andR.sup.A is hydrogen, .dbd.O, cycloalkyl, --COOR.sup.3 with R.sup.3 having the above-mentioned meanings, or lower alkyl, which optionally can be substituted by OH, halogen, lower alkoxy, phenyl, phenyloxy, --NR.sup.4 R.sup.5, whereby R.sup.4 and R.sup.5 have the above-mentioned meanings, and R.sup.B can be hydrogen, lower alkyl or lower alkoxyalkyl,have valuable pharmacological properties.

Abstract: The present invention concerns derivatives of 5H-pyrido[4,3-b]-indole with the following general formula: ##STR1## in which n represents a whole number from 2 to 4, R.sub.1 represents hydrogen or a lower alkyl group; R.sub.2 represents hydrogen, a hydroxy group or a lower alkyloxy group; R.sub.3 and R.sub.4 represents hydrogen, a lower alkyl group or hydroxyalkyl group, R.sub.5 can be identical or different and represents hydrogen, a hydroxy group or a lower alkyl group, as well as the tautomeric forms and the addition salts with pharmaceutically acceptable mineral or organic acids.The invention also concerns their preparation process, and their use as medicaments.

Abstract: In an instant film pack of the type comprising a parallelepipedal housing having a top wall in which an exposure aperture is formed and a front end wall with a film unit exit slot through which an instant film unit is withdrawn. A supporting member is provided to prevent the film unit from being improperly withdrawn. The supporting member comprises a pair of resilient arms attached to the bottom of the film pack at the front end and extending in the direction of withdrawal of the film unit. The resilient arms are so formed as to extend close to the juncture of the front end of a guide member and an edge controller disposed in a pack holder in which the film pack is loaded for use.

Abstract: This invention provides a group of antipsychotic/anxiolytic agents of the formula. ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, alkoxy or alkyl;R.sup.2 is hydrogen, phenyl or phenyl substituted with an alkyl, alkoxy, halogen, trifluoromethyl, cyano or nitro group;R.sup.3 and R.sup.4 are hydrogen or, together, complete the benzo ring; andn is 1 to 7;or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: Histaminic H.sub.1 -receptor antagonists of the formula: ##STR1## in which R.sup.1 is ##STR2## where R.sup.2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo, nitro, cyano or trifluoromethyl; and R.sup.3 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo, nitro, cyano or trifluoromethyl;X is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halo;Z is ##STR3## where R.sup.4 is pyridinyl, quinolinyl or benzoyl, any of which may be substituted by alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo or trifluoromethyl; and m is one of the integers 2, 3 or 4; andn is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof.

Abstract: Histamine H.sub.1 receptor antagonists of the formula: ##STR1## in which R.sup.1 and R.sup.2 taken together represent an ortho-fused 1,2-indolo or 2,3-indolo moiety of the formulas: ##STR2## where R.sup.4 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or halo; andR.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, benzyl, phenyl or substituted phenyl or benzyl where the substituent is taken from the group alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo or trifluoromethyl;R.sup.3 is ##STR3## where one X is --N.dbd. and the other is --CH.dbd.;Y is --N.dbd. or --CH.dbd.;and R.sup.6 and R.sup.7 are alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or halo;n is one of the integers 0 or 1;m is one of the integers 0, 1, 2 or 3; ando is one of the integers 1 or 2;or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.

Abstract: New .beta.-carboline-3-carboxylic acid esters have the general formula I: ##STR1## wherein R.sup.4, R.sup.5 and R.sup.6 have specified meanings. The new compounds exhibit surprising psychotropic properties.

Abstract: .beta.-carbolin-3-carboxylic acid derivatives of the general formula ##STR1## wherein R.sup.1 is methyl, ethyl, n-propyl or iso-propyl, and whereinR.sup.2 is hydrogen, methyl, ethyl, n-propyl or iso-propyl, provided that R.sup.1 is not methyl, when R.sup.2 is hydrogen, are produced by different methods.The compounds are useful in psychopharmaceutical preparations, being antagoinists of benzodiazepines.

Abstract: New substituted .beta.-carbolines of formula I ##STR1## wherein R.sup.3 is hydrogen or a non-carboxyl based substituent, and R.sup.4-9 have various meanings,are valuable pharmaceutical products with long lasting action on the central nervous system.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen or a protecting group,R.sup.2 is --CH.dbd.CR.sub.2.sup.4 or --C.tbd.CR.sup.4,R.sup.4 is hydrogen or halogen,R.sup.3 is hydrogen, lower alkyl or lower alkoxyalkyl,R.sup.A is, inter alia, hydrogen, OR.sup.7, lower alkyl, which optionally is substituted with aryl, lower alkoxy or NR5R6,R.sup.5 and R.sup.6 can be the same or different and in each case is hydrogen, lower alkyl or together with the nitrogen atom a 5-6 member ring, which can contain another heteroatom,R.sup.7 is lower alkyl, optionally substituted aryl or aralkyl, andeach compound can contain one or more R.sup.A radicals which are not hydrogen, have valuable pharmacological properties.

Abstract: Indole derivatives of formula I ##STR1## R is hydrogen, one or two halogen atoms or one or two organic radicals in the 4-, 5-, 6- or 7-position(s),R.sup.1 and R.sup.4 are the same or different and each is hydrogen, alkyl of 1 to 3 carbon atoms or alkoxyalkyl of 1 to 3 carbon atoms in each of the alkoxy and alkyl portions,R.sup.3 is phenyl, --COOalkyl, --PO.sub.3 (alkyl).sub.2, --SO.sub.2 aryl, --SO.sub.2 alkyl, ##STR2## each of 1 to 3 carbon atoms in each alkyl group, and A and B each independently is alkyl of 1 to 3 carbon atoms or together with the connecting N-atom form a pyrrolidono, piperidino, morpholino or piperazino group,are valuable intermediates for preparing valuable tryptophans and .beta.-carbolines.

Abstract: .beta.-carbolines of formula I ##STR1## can be prepared by reacting an indole of formula II: ##STR2## with an azabutadiene of formula III ##STR3## in the presence of an acid at 50.degree.-200.degree. C.

Abstract: 1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4, 3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyl)]-2,3,4,5 -tetrahydro-1H-pyrido[4,3-b]indole (flutroline) or to 8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (an alternative flutroline intermediate).

Abstract: The compounds: ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, or alkyl;R.sup.2 is substituted or unsubstituted pyridinyl, pyrazinyl, quinolinyl or quinoxalinyl and said substituents are alkyl, alkoxy, alkoxycarbonyl, halogen, cyano or nitro;R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, halophenyl, methylphenyl, trifluoromethylphenyl, cyanophenyl or nitrophenyl; with the proviso that one of R.sup.5 and R.sup.6 is other than hydrogen;and n is an integer from 1 to 7;or a pharmaceutically acceptable salt thereof, are antipsychotic and anxiolytic agents.

Abstract: New .beta.-carboline-3-oxadiazolyl derivatives have the general formula I: ##STR1## wherein X is ##STR2## and wherein R.sup.4, R.sup.A and R have specified meanings. These new compounds exhibit surprising psychotropic properties.

Abstract: .beta.-carbolines of formula I ##STR1## wherein R=C.sub.1-5 alkylR.sup.4 =H, C.sub.1-5 alkyl or --(CH.sub.2).sub.n --OR with n=1 or 2 andR.sup.A =H, R, (CHR).sub.n --OR, OCH.sub.2 Ph, OPh, OPh(Cl,Br),OR,OCH.sub.2 Ph(Cl,Br) NRR, Cl or Br,wherein n and R have the above meanings and there are one or two R.sup.A 's are prepared, by dehydrogenation at reaction temperatures below ambient temperature in an inert solvent with tert-butyl hypochlorite and a tertiary amine.

Abstract: There are provided novel 2-(2-imidazolin-2-yl)pyridine and quinoline compounds, a process and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: The compounds: ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, or alkyl;R.sup.2 is substituted or unsubstituted pyridinyl, pyrazinyl, quinolinyl or quinoxalinyl and said substituents are alkyl, alkoxy, alkoxycarbonyl, halogen, cyano or nitro; andn is 2, 3, 4, 5 or 6;or a pharmaceutically acceptable salt thereof, are antipsychotic and anxiolytic agents.

Abstract: New .beta.-carboline-3-carboxylic acid esters have the general formula I: ##STR1## wherein R.sup.4, R.sup.5 and R.sup.6 have specified meanings. The new compounds exhibit surprising psychotropic properties.

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: Novel tetrahydro-.beta.-carboline derivatives of the formula: ##STR1## wherein R.sup.1 is carboxyl, a lower alkoxycarbonyl, carbamoyl, an N,N-di-lower alkylcarbamoyl, an N-(phenyl-substituted lower alkylidenamino)carbamoyl, a [N,N-di(lower alkyl)amino]-lower alkyl, or a nitrogen-containing monocyclic heterocyclic group;R.sup.2 is hydrogen atom, a lower alkyl, or a hydroxy-lower alkyl group, or R.sup.2 is combined with R.sup.1 to form a group: --CO--O--CH.sub.2 --;R.sup.3 is hydrogen atom, a lower alkyl, a phenyl-lower alkyl, or a group: --CSS--R.sup.4 ;R.sup.4 is hydrogen atom, an alkyl, or a group: --(CH.sub.2).sub.n Y.sup.1 ;n is 0, 1 or 2,Y.sup.

Abstract: Novel substituted .beta.-carboline derivatives of Formula I ##STR1## wherein R.sup.3 is an oxadiazolyl residue of the formula ##STR2## wherein R.sup.5 stands for lower alkyl of up to 3 carbon atoms or an ester ##STR3## with R.sup.6 being hydrogen or lower alkyl of up to 3 carbon atoms, R.sup.4 is hydrogen, lower alkyl of up to 3 carbon atoms, or CH.sub.2 OR.sup.9 wherein R.sup.9 is lower alkyl of up to 3 carbon atoms,R.sup.A is phenyl or a hydrocarbon residue containing 2-10 carbon atoms which can be cyclic or acyclic, saturated or unsaturated, branched or unbranched, and which can optionally be substituted by oxo, formyl OH, O-alkyl of up to 3 carbon atoms or phenyl, and wherein, in a cyclic hydrocarbon residue, a CH.sub.2 -group can be replaced by oxygen,exhibit an effect on the central nervous system and thus are suitable as psychopharmaceuticals.

Abstract: The present invention relates to new N-acyl derivatives of amino acids.These derivatives correspond to the general formula I below: ##STR1## in which A represents a linear or branched, saturated hydrocarbon radical containing from 1 to 6 carbon atoms or a saturated ring containing 6 carbon atoms,X represents a --COOH radical, a --COOAlkyl radical (alkyl from C.sub.1 to C.sub.4), a hydrogen atom or a --CH.sub.3 group when Y is --COOH or --COOAlkyl,Y represents a --COOH radical, a --COOAlkyl radical (alkyl from C.sub.1 to C.sub.4), an --NH.sub.2 group, an --SH group, an --SCH.sub.3 group, a --NH--CH(.dbd.NH)--NH.sub.2 group, a substituted or unsubstituted phenyl group, an indolin-3-yl group or a 5-hydroxyindolin-3-yl group, andQ represents an optionally substituted aromatic ring or an optionally substituted heterocycle containing 1 or 2 nitrogen atoms.Drugs having an antiallergic action.

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.

Abstract: 3-Substituted beta-carbolines of the formula ##STR1## wherein R.sup.A is H, F, Cl, Br, I, NO.sub.2, CN, CH.sub.3, CF.sub.3, SCH.sub.3, NR.sup.16 R.sup.17 or NHCOR.sup.16,wherein R.sup.16 and R.sup.17 are the same or different and each is hydrogen or alkyl, alkenyl or alkynyl each of up to 6 C-atoms, aralkyl or cycloalkyl each of up to 10 C-atoms,or wherein R.sup.16 and R.sup.17 together form a saturated or unsaturated 3-7 membered heterocyclic ring;said compounds possess valuable psychotropic properties which make them useful for example as tranquilizers.

Abstract: 2-Substituted 1-(3'-aminoalkyl)-1,2,3,4-tetrahydro-.beta.-carbolines of the formula ##STR1## where n, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings given in the description, and their preparation and use.The novel substances are useful for treating arrhythmia.

Abstract: 1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4, 3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyl)-]2,3,4,5 -tetrahydro-1H-pyrido[4,3-b]indole (flutroline) or to 8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (an alternative flutroline intermediate).

Abstract: A novel process for preparing various 2-substituted-5-aryl-1,2,3,4-tetrahydro-.gamma.-carboline derivatives is provided, which involves (1) condensing a corresponding 2-unsubstituted compound with formaldehyde and an appropriate acetylenic derivative in the presence of cuprous chloride or cuprous bromide, followed by (2) reduction of the corresponding unsaturated intermediate to yield the desired final product. The latter compounds are known to be useful as tranquilizing agents, with 2-[4-(p-fluorophenyl)-4-hydroxybutyl]-5-(p-fluorophenyl)-8-fluoro-1,2,3,4- tetrahydro-.gamma.-carboline representing a preferred final product. The aforesaid unsaturated intermediates are all novel compounds.

Abstract: Salts of 1,2,3,4-tetrahydro-.beta.-carbolines of the formula I ##STR1## where R is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, x is halogen and n is an integer from 2 to 5, and their preparation are described. The compounds are intermediates for the preparation of pharmacologically active substances.

Abstract: Pyridoindoles of the formula ##STR1## in which R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, which is optionally substituted by the radical ##STR2## R.sub.2 and R.sub.3 represent H or form a bond, or R.sub.1 and R.sub.2 together represent O, --O--CH.sub.2 --CH.sub.2 --O-- or --S--CH.sub.2 --CH.sub.2 --S--,R.sub.4 represents H or the ##STR3## or R.sub.3 and R.sub.4 represent O, orR.sub.1 and R.sub.4 are members of an N-containing six-membered ring andR.sub.8 and R.sub.9 represent H or C.sub.1 -C.sub.4 -alkyl, or optionally form, with the N atom, a heterocyclic 5-membered or 6-membered ring, which can optionally also contain a further hetero-atom from the series comprising N, O or S,R.sub.5 represents H, C.sub.1 -C.sub.4 -alkyl or the group ##STR4## or R.sub.5 and R.sub.3 form a bond, andR.sub.10 and R.sub.11 represent C.sub.1 -C.sub.4 -alkyl or are members of an N-containing 5-membered or 6-membered ring,R.sub.6 represents H or C.sub.1 -C.sub.4 -alkyl andR.sub.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is O, S or NHR.sup.3, wherein R.sup.3 is hydrogen, lower alkyl or cycloalkyl;R is loweralkyl, loweralkoxy, aralkoxy of up to 10 carbon atoms or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are, independently, hydrogen, lower alkyl, cycloalkyl or aminoalkyl; or R is alkoxymethyl or hydroxymethyl;n is one of the integers 2, 3 or 4;R.sup.1 and R.sup.2 are, independently, hydrogen, halo, nitro, cyano, SCH.sub.3, or NR.sup.6 R.sup.7, NHCOR.sup.6, COOR.sup.6, OR.sup.6 or SO.sub.2 NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 are independently hydrogen or loweralkyl;and their activity as anticonvulsants, having use in the treatment of epileptic conditions.

Abstract: Disclosed are 5,6-dihydro benzo[f]quinolines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure.

Abstract: A novel process for preparing various 2-substituted-5-aryl-1,2,3,4-tetrahydro-.gamma.-carboline derivatives is provided, which involves (1) condensing a corresponding 2-unsubstituted compound with formaldehyde and an appropriate acetylenic derivative in the presence of cuprous chloride or cuprous bromide, followed by (2) reduction of the corresponding unsaturated intermediate to yield the desired final product. The latter compounds are known to be useful as tranquilizing agents, with 2-[4-(p-fluorophenyl)-4-hydroxybutyl]-5-(p-fluorophenyl)-8-fluoro-1,2,3,4- tetrahydro-.gamma.-carboline representing a preferred final product. The aforesaid unsaturated intermediates are all novel compounds.