Abstract: Acylation of nitrogen containing compounds utilizing esters as acylation agents in the presence of salts of substituted pyridine compounds.

Abstract: 3-Phenacylpiperidines, useful as depressants, stimulants, and anti-inflammatory agents, are obtained by preparing, from a 3-halomethylpiperidine, a 3-piperidylmethylmagnesium halide which is condensed with a benzonitrile.

Abstract: Novel N-substituted heterocyclic derivatives represented by the formula, ##SPC1##Wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkoxy, nitro, halogen or trifluoromethyl group; R.sub.2 is hydrogen atom or lower alkyl group; X is sulfur atom, sulfinyl or sulfonyl group; Y is ##EQU1## group (wherein R.sub.3 is phenyl or substituted phenyl group; R.sub.4 is hydrogen atom, hydroxy, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, carbamoyl, N-(lower alkyl)-carbamoyl or N,N-di(lower akyl)-carbamoyl group; R.sub.5 is hydrogen atom, morpholino, pyrrolidinyl, piperidinyl, hexamethylenimino, lower alkyl, cyclo(lower alkyl), cyclo(lower alkyl)-(lower alkyl), hydroxy-(lower alkyl), (lower alkoxy)-(lower alkyl), phenyl or substituted phenyl group; k is 0 or 1 and m is 0, 1 or 2); and n is 3 or 4, and pharmaceutically acceptable salts thereof, which have excellent tranquillizing, anti-psychotonic, anti-emotional, anti-convulsive, anti-psychosis, sedative, analgesic or anti-hypertensive activities.

Abstract: The new 1-alkyl-4-(10-oxo or -hydroxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-piperidine compounds are prepared from the corresponding 10-desoxy compounds having a double bond at the 10,11-position by a process involving bromination, dehydrobromination of the resulting dibromo compound, followed by enamine formation and hydrolysis to give the desired 10-oxo compound. The compounds prepared in this manner are active as antihistamines and as appetite stimulants.

Abstract: A new class of amino-imide compounds is disclosed in which a 2-oxo-cycloalkylimide group and an amino group are joined by a chain containing acetylenic unsaturation. The compounds are effective to antagonize the tremorogenic effect of oxotremorine and possess valuable pharmaceutical properties due to a strong central anti-cholinergic effect.

Abstract: 4,5-Dihydropyridines bearing an N,N-disubstituted amino group in the 2-position, carbonyl functions in the 3- and 5-positions and being optionally substituted in the 6-position by lower alkyl or phenyl and, in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group, are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-pyrrolidino-6-methyl-4-(3-nitrophenyl)-4,5-dihydropyridine-3,5-dicarboxy lic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and a substituted 3,3-diaminoacrylate.

Abstract: The title compound is a useful antifungal agent.

Abstract: 3-(Substituted-amino)-1,2,3,4-tetrahydrocarbazoles are prepared by reacting appropriate 4-substituted-aminocyclohexanones with a phenylhydrazine, by reacting a 3-(sulfonyloxy)-1,2,3,4-tetrahydrocarbazole with an appropriate substituted amine, or by reduction of an appropriate 3-(acylamino)-1,2,3,4-tetrahydrocarbazole. The 3-(substituted-amino)-1,2,3,4-tetrahydrocarbazoles of this invention have analgetic and psychotropic activities. Moreover, certain of these compounds also have antihistaminic activity.

Abstract: The invention relates to 1-phenyl-4-amino-cyclohex-2-ene-1-carboxylic-acid-esters of the general formula I ##SPC1##wherein R.sub.1 and R.sub.2 may be the same or different and may be H, alkyl, hydroxyalkyl, alkenyl, preferably with 1 to 4 C-atoms, aralkyl which may be bonded to each other, in which connection the heterocyclic system formed may be substituted further by the OH-- group and where attachment takes place by an oxygen or a nitrogen atom, if desired, which in its turn carries an H, alkyl with 1 to 4 C-atoms, aryl which may be substituted by chlorine, preferably in 3 or 4-position, and by methoxy, preferably in 2 or 4-position, acyl, preferably alkanoyl with 1 to 4 C-atoms, and aroyl, or aralkyl, and R.sub.3 represents an alkyl radical with 1 to 4 C-atoms, the salts thereof and quarternary ammonium compounds, and a process for their preparation. These compounds have analgesic and neuroleptic properties.

Abstract: 0,0-Bis(aryl)amidothiophosphates, useful as light stabilizers in polyolefins, are those having the formula: ##EQU1## wherein: R is hydrogen, alkyl of 1-12 carbons, or halogen; Ar is phenyl or naphthyl; n is 1 or 2; and R' and R", which may be the same or different, are each selected from the group consisting of hydrogen, alkyl of 1-18 carbons, 2,2,6,6-tetramethyl-4-piperidyl, cycloalkyl of 5-6 carbons or both R' and R", together with the N to which they are attached, form a morpholino or piperidino ring. Such compounds are made by reacting PSCl.sub.3 with two moles of a phenol and then the product thereof with an amine.

Abstract: Compounds of the formulae: ##SPC1##And the salts thereof with pharmaceutically acceptable cations wherein n and m are each two or three; X is oxygen or sulphur; R.sup.2 and R.sup.3, when taken separately, are each hydrogen or alkyl having 1 to 4 carbon atoms; R.sup.2 and R.sup.3, when taken together, are alkylene having 2 to 4 carbon atoms; Y is methylene or a single bond; R.sup.4 and R.sup.5, when taken separately, are each hydrogen, hydroxy or alkoxy having 1 to 5 carbon atoms, and R.sup.4 and R.sup.5, when taken together, are oxo or alkylene dioxy having 2 to 4 carbon atoms, each oxygen atom in R.sup.4 and R.sup.5, when taken separately, and in R.sup.4 and R.sup.5, when taken together, being separated from the nitrogen atom of the heterocyclic ring by two or more carbon atoms, said compounds being cerebral vasodilators.

Abstract: Compounds of the formulae: ##SPC1##And the salts thereof with pharmaceutically acceptable cations wherein R.sup.1 is 3-trifluoromethyl, chloro, bromo or fluoro; n and m are each two or three; X is oxygen or sulphur; R.sup.2 and R.sup.3, when taken separately, are each hydrogen or alkyl having 1 to 4 carbon atoms; R.sup.2 and R.sup.3, when taken together, are alkylene having 2 to 4 carbon atoms; Y is methylene or a single bond; R.sup.4 and R.sup.5, when taken separately, are each hydrogen, hydroxy or alkoxy having 1 to 4 carbon atoms, and R.sup.4 and R.sup.5, when taken together, are oxo or alkylene dioxy having 2 to 4 carbon atoms, each oxygen atom in R.sup.4 and R.sup.5, when taken separately, and in R.sup.4 and R.sup.5, when taken together, being separated from the nitrogen atom of the heterocyclic ring by two or more carbon atoms, said compounds being cerebral vasodilators.

Abstract: Piperidines of the formula ##SPC1##In which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.

Abstract: Novel 1-substituted-4-benzylpiperidines having .alpha.-substituents on the 4-benzyl moiety useful as antiinflammatory agents, sedatives, and tranquilizers are represented by the formula ##SPC1##Wherein R represents acetyl, aryloxyloweralkyl, aroylloweralkylcarbamoyl, N-lower-alkylcarbamoyl, N,N-dilower-alkylcarbamoyl, N-arylcarbamoyl, N-(.omega.-nitrogen containing heterocycle)lower-alkylcarbamoyl, N-(.omega.-aminolower-alkyl)carbamoyl, 2-hydroxy-3-(o-methoxyphenoxy)propyloxycarbamoyl, 2-carbamoylethyl, or 4-(p-fluorobenzoyl)piperidinoethyl; R.sup.1 represents hydrogen or hydroxy; R.sup.2 represents phenyl, p-fluorophenyl, m-trifluoromethylphenyl or cyclohexyl; Y represents hydrogen or fluorine with the proviso that when Y is hydrogen and R.sup.2 is phenyl, R is other than aroylloweralkyl. The pharmaceutically acceptable acid addition salts of the basic compounds of Formula I are included as part of the invention.

Abstract: The invention provides novel pyrazoline derivatives which are useful as optical brighteners.

Abstract: Piperidines of the formula ##SPC1##Wherein R is --CH.sub.2 OH, CO--NR,R.sub.2 in which R.sub.1 and R.sub.2 each are H or alkyl of 1-4 carbon atoms, --NHCH.sub.2 CH.sub.2 OH, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 CH.sub.2 SO.sub.3 H, --NHNH.sub.2 or --NHCH.sub.2 COOH, or --COOR.sub.3 in which R.sub.3 is 3-pyridylmethyl, 2-acetamidoethyl, 1-methyl-4-piperidyl or 2,3-dihydroxypropyl and the physiologically acceptable salts thereof, have cholesterol-level-lowering and triglyceride-level-lowering activity and can be prepared from 2-methyl-2-[4-(4-piperidinophenyl)-phenoxy]-propionic acid or a functional derivative thereof by reduction or by reaction with a compound of the formula HZ.

Abstract: Carbazoles of the formula ##SPC1##Wherein R.sub.1 is hydroxymethyl, alkanoyloxymethyl, tetrazolyl, cyano, oximinocarbonyl, aminocarbonyl, carboxyl and salts thereof with physiologically acceptable bases and the esters thereof with physiologically acceptable alcohols and amides thereof with physiologically acceptable amines,R.sub.2 through R.sub.6 each are a hydrogen atom, halogen atom, lower alkyl, trifluoromethyl, or lower alkoxy, orR.sub.5 and R.sub.6 collectively are a five- or six-membered isocyclic ring, andR.sub.7 is a hydrocarbon of 3-8 carbon atoms or, when at least one of the R.sub.2 through R.sub.6 is other than a hydrogen atom, a hydrogen atom, methyl or ethyl,And the corresponding compounds wherein R.sub.7 is a hydrogen atom, methyl or ethyl,And the 5,6,7,8-tetrahydrocarbazoles, possess topical anti-inflammatory activity.

Abstract: .beta.-[Benzo(b)thienyl-3]propionic acid derivatives in the form of their amino esters (and salts thereof) are prepared. These compounds have spasmolytic, vasodilatatric, antiserotanic and local anaesthetic activity.

Abstract: 1-[Methylated piperidino (and pyrrolidin-1-yl)]-3-(substituted phenoxy)-2-propanols of the formula: ##SPC1##Wherein R is a 2-thienylmethyl group, a 2-pyridylmethyl group, a 2-pyridyl group, a tetrahydrofurfuryloxy group, a furfuryloxy group, a 2-thienylmethoxy group, a 2-pyridyloxy group or a group of the formula R.sup.5 --X--A--O-- wherein R.sup.5 is a lower alkyl group, X is --O--, --S-- or --SO.sub.2 --, and A is a lower alkylene group or a --CH.sub.2 --C.ident.C--CH.sub.2 -- group, R.sup.1 is a hydrogen atom, a lower alkyl group or a halogen atom, R.sup.2, R.sup.3 and R.sup.4 are each a hydrogen atom or a methyl group, and n is zero or 1, and pharmaceutically acceptable acid addition and quarternary ammonium salts thereof are disclosed. They exhibit antiarrhythmic action, local anaesthetic action, analgesic action and gastric juice secretion inhibiting action.

Abstract: A compound having the formula:- ##SPC1##And salts thereof, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is hydrogen, an alkyl residue having from 1 to 9 carbon atoms, a cycloalkyl residue having from 5 to 14 carbon atoms or a cycloalkyl-alkyl residue having from 7 to 14 carbon atoms, Y is hydrogen, 0.degree., an alkyl residue having from 1 to 4 carbon atoms, or an aralkyl residue having from 7 to 12 carbon atoms and Z is hydrogen, an unsubstituted or substituted alkyl residue having from 1 to 20 carbon atoms, an alkenyl or alkynyl residue having from 2 to 20 carbon atoms, a cycloalkyl residue having from 5 to 12 carbon atoms, an aralkyl residue having from 7 to 12 carbon atoms, an aryl residue having from 6 to 12 carbon atoms, or the group having the formula: wherein Z.sub.1 has the same significance as Z as hereinbefore defined, or Z.sub.1 is a group --NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or an alkyl residue having from 1 to 4 carbon atoms and R.sub.