Abstract: Piperidine derivatives of formula ##STR1## wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R.sup.1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R.sup.2 is alkyl or phenyl; and R.sup.3 is phenyl optionally substituted, or R.sup.3 is ##STR2## wherein Z represents a 5- or 6-membered heterocyclic ring; or R.sup.2 and R.sup.3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.

Abstract: The present invention relates to therapeutically active piperidine derivatives, of formula 1 ##STR1## wherein, R.sup.1, R.sup.2, A, X and Y are as defined in the specification. The compounds are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.

Abstract: New substituted urea compounds of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 is a group of formula II, III or IV ##STR2## where n is 2 or 3, p is 1 or 2, q is 1 to 3, r is 1-3 and R.sup.4 and R.sup.5 are H, C.sub.1-7 alkyl or C.sub.3-6 cycloalkyl; and wherein R.sup.2 is an oxadiazole, substituted with C.sub.1[ alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-7 cycloalkyl, benzyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, amino or alkylamino; orwherein R.sup.2 --C--R.sup.6 .dbd.--N--O--R.sup.7 wherein R.sup.6 is hydrogen or methyl and R.sup.7 is C.sub.1-6 alkyl which may be substituted with C.sub.3-7 cycloalkyl;and wherein R.sup.3 is hydrogen, halogen, nitro, substituted amine, trifluoromethyl, C.sub.1-6 alkyl or C.sub.1-6 alkoxy.The compounds are useful in pharmaceutical preparations for treating psychotic disorders, nausea and vomiting.

Abstract: New substituted urea compounds of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein A is ##STR2## wherein R.sup.3 is an oxadiazol, substituted with C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 alkynyl, C.sub.3-7 cycloalkyl, benzyl, phenyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, amino or alkylamino;R.sup.2 is --H or lower alkyl;X is O or S;and R.sup.1 is a group of formula II, III, IV or V ##STR3## where n is 2 or 3, P is 1 or 2, q is 1 to 3, r is 1-3 and R.sup.4 and R.sup.5 are H,C.sub.1-7 alkyl or C.sub.3-6 cycloalkyl; and N-oxides thereof. The compounds are useful in pharmaceutical preparations for treating psychotic disorders, nausea and vomiting.

Abstract: From a synthesis gas mainly consisting of hydrogen and carbon oxides an acetic acid product consisting of acetic acid, acetic anhydride and/or methyl acetate is prepared by reactions known per se in a technically simple reaction sequence and a high conversion degree when the reactions are combined such that in a first step at a pressure of 5-200 bar and a temperature of 150.degree.-400.degree. C. the synthesis gas is converted in the gas phase in a first reactor to methanol, of which at least a substantial proportion is converted to dimethyl ether in the same reactor in the presence of one or more catalysts which together catalyze the reactionsCO+2H.sub.2 .revreaction.CH.sub.3 OH (1)2 CH.sub.3 OH.revreaction.CH.sub.3 OCH.sub.3 +H.sub.2 O (2)andCO+H.sub.2 O.revreaction.CO.sub.2 +H.sub.2 (3)and then passing the entire effluent from the first reactor to a second reactor in which methanol and dimethyl ether at a pressure of 1-800 bar and a temperature of 100.degree.-500.degree. C.

Abstract: A method of preparing methanol by reacting synthesis gas comprising hydrogen and carbon oxides in a fixed bed of methanol synthesis catalyst. The reaction of the synthesis gas is conducted under conditions where condensation of methanol occurs on the catalyst. Pressure, temperature and/or space velocity of the gas at the exit of the catalyst bed are adjusted to where conversion levels of the gas leads to formation of liquid methanol in the catalyst bed by exceeding the dew point of the reaction mixture.

Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.

Abstract: Piperazinyl derivatives of the general formula I ##STR1## wherein R.sup.1 represents substituted phenyl, 1- or 2-diazanaphthyl, azadiazanaphtyl or diazanaphtyl groups; n is 1, 2, 3 or 4; X is --O-- or ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-6 -alkyl or C.sub.3-8 -cycloalkyl; Y is .dbd.O or .dbd.S or .dbd.NZ wherein Z is hydrogen, C.sub.1-6 -alkyl or --CN and R.sup.3 is selected from a group consisting of various structures have been found to exhibit high affinity for various receptor subtypes including the 5-HT.sub.2 receptor, the 5-HT.sub.1A receptor, the alpha.sub.1 receptor the dopamine receptor or a combination of these and may therefore be useful for treating CNS system, cardiovascular system and gastrointestinal disorders.

Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; X represents oxygen or sulfur; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.

Abstract: The present invention relates to a process for preparing acetic acid, acetic acid methyl ester or acetic anhydride or mixtures thereof by converting a synthesis gas mainly containing hydrogen and carbon oxides, by first converting the synthesis gas catalytically into a gas mixture containing methanol and dimethyl ether and then carbonylating this mixture catalytically into acetic acid and/or methyl acetate and/or acetic anhydride.

Abstract: New substituted urea compounds of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## whereinA is ##STR2## wherein R.sup.3 is an oxadiazol, substituted with C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 alkynyl, C.sub.3-7 cycloalkyl, benzyl, phenyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, amino or alkylamino;R.sup.2 is --H or lower alkyl;X is O or S; andR.sup.1 is a group of formula II, III, IV or V ##STR3## where n is 2 or 3, p is 1 or 2, q is 1 to 3, r is 1-3 and R.sup.4 and R.sup.5 are H, C.sub.1-7 alkyl or C.sub.3-6 cycloalkyl; and N-oxides thereof.The compounds are useful in pharmaceutical preparations for treating psychotic disorders, nausea and vomiting.

Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.

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: 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: 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 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: 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.