Abstract: 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, andR.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.

Abstract: 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, andR.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.

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: 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: 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: .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: New heterocyclic derivatives having the general formula: ##STR1## wherein X is ##STR2## or CO.sub.2 R' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, and--A-- 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, ecto- and endoparasiticides, insecticides and acaricides.

Abstract: New heterocyclic derivatives havingy the general formula: ##STR1## wherein ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, and--A-- is --(CH.sub.2).sub.n --Y--(CH.sub.2).sub.m --,wherein n and m are O 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, ecto- and endoparasiticides, insecticides and acaricides.

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: 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: 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: New heterocyclic compounds having the general formula ##STR1## wherein X is ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, phenyl, thienyl, or C.sub.1-3 -alkoxymethyl,R.sup.6 and R.sup.7 independently are hydrogen or halogen, and--A-- is --N(R")--C(O)--, --N(R")--CH.sub.2 --, or ##STR3## wherein R" is hydrogen, C.sub.3-7 -cycloalkyl, or C.sub.1-6 -alkyl The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: New heterocyclic compounds having the general formula ##STR1## wherein X is ##STR2## or CO.sub.2 R' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.3-7 -cycloalkymethyl,R.sup.6 and R.sup.7 independently are hydrogen, halogen, alkoxy, or trifluoromethyl, andR" hydrogen, C.sub.1-6 -alkyl, or C.sub.3-7 -cycloalkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: Compounds of formula I ##STR1## wherein X is COOR.sup.3 or an oxadiazolyl radical of the formula orR.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.A is -CHR.sup.1 -Z-R.sup.5,Z is sulfur or oxygen,R.sup.1 is lower alkyl or optionally substituted phenyl, and R.sup.5 is hydrogen, phenyl or optionally substituted lower alkyl,and wherein each compound can contain 1 or 2 R.sup.A radicals have valuable pharmacological properties.

Abstract: New heterocyclic compounds having the general formula ##STR1## wherein X is ##STR2## wherein R.sup.1 is C.sub.1-6 -alkyl, Cphd 3-7-cycloalkyl, phenyl, thienyl, or C.sub.1-3 -alkoxymethyl,R.sup.6 and R.sup.7 independently are hydrogen or halogen, and--A--is --N(R")--C(O)--, --N(R")--CH.sub.2 --, or ##STR3## wherein R" is hydrogen, C.sub.3.differential. -cycloalkyl, or C.sub.1-6 -alkyl The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 -cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: New heterocyclic compounds 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.3-7 -cycloalkylmethyl,R.sup.6 and R.sup.7 independently are hydrogen, halogen, alkoxy, or trifluoromethyl, andR" is hydrogen, C.sub.1-6 -alkyl, or C.sub.3-7 -cycloalkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: The application discloses novel benzodiazepine agonist compounds, namely, compounds having the formula ##STR1## wherein X is F, CF.sub.3, CH.sub.3, or CN, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for their production are also disclosed.

Abstract: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 -cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.