Abstract: Quinoline and substituted quinolines are prepared by reacting aniline or a substituted aniline with an .alpha., .beta.-monounsaturated aldehyde in a high-boiling mineral oil by a method in which the high-boiling mineral oil is replaced when it becomes enriched with by-products, and the said mineral oil enriched with by-products is removed.

Abstract: Disclosed are the compounds of formula I ##STR1## wherein X represents oxygen or sulfur; ring A is unsubstituted or substituted by one to three identical or different substituents selected from hydroxy, hydroxy-lower alkyl, etherified hydroxy, etherified hydroxy-lower alkyl, acyloxy, acyloxy-lower alkyl, halogen, lower alkyl, trifluoromethyl, amino, mono- and di-lower alkylamino and acylamino; or ring A is substituted by one lower alkylenedioxy; R represents hydrogen, lower alkyl or aryl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, lower alkylthio-lower alkyl, amino, acylamino, (amino, mono- or di-lower alkylamino)-lower alkyl, carboxy, lower alkoxycarbonyl, carbamoyl or mono- or di-lower alkylcarbamoyl; R.sub.2 to R.sub.5 represent hydrogen or lower alkyl; the dehydro derivatives thereof with a double bond at the 1,2-position, or at the 1,10b-position in which case R.sub.

Abstract: Substituted dihydropyridines and substituted and bridged tetrahydropyridines are disclosed which are useful as calcium entry blockers.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally interrupted by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is phenyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or together are a group X; SO.sub.2 NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X or S(O).sub.m R.sub.13 wherein m is 1 or 2 and R.sub.13 is C.sub.

Abstract: Hexahydroindolizines of the following formulae (I) and (II): ##STR1## are novel and have been found to possess antisecretory and antidepressant properties. Methods of preparation, intermediates thereto and use are also disclosed.

Abstract: Novel 7-fluoro-8-heterocyclyl-5-oxo-5H-thiazolo (3,2-a)-naphthyridine- and quinoline- 4-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.

Abstract: A novel [1] benzepino[3,4-b]pyridine derivative having antiulcer activity is represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a halogenated alkyl group, an alkoxy group or a halogen atom; R.sup.2 represents ##STR2## wherein Y represents an amino group, a substituted amino group, a heterocyclic group or a substituted heterocyclic group; Z represents a hydrogen atom, an alkyl group or an acyl group; and m is an integer of 1-3, ##STR3## wherein Z' represents a hydrogen atom or an alkyl group; Y has the same meaning as defined above, and n is 0, 1 or 2; or ##STR4## wherein Z and n have the same meanings as defined above; X represents an oxygen atom or a sulfur atom. Also disclosed are pharmaceutically acceptable acid addition salts of the compound represented by the formula (I).

Abstract: Novel benzothiopyranopyridinones of the formula ##STR1## wherein A,B,C and D are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 6 carbon atoms, nitro, halogen, amino and acylamino of 2 to 7 carbon atoms or A and B or C and D taken with the carbon atoms to which they are attached form a benzene ring, R is selected from the group consisting of hydrogen and R', R' is selected from the group consisting of alkyl of 1 to 9 carbon atoms, alkenyl of 2 to 9 carbon atoms optionally substituted with an --OH, cycloalkyl of 3 to 9 carbon atoms, phenyl, aralkyl of 7 to 9 carbon atoms and --(CH.sub.2).sub.

Abstract: New dihydropyridines are described. These compounds are useful in the treatment of asthma.

Abstract: Disclosed are tricyclic lactams and derivatives which are effective in increasing cardiac contractility in humans. These compounds are useful in the treatment of congestive heart failure.

Abstract: Novel N-(4-pyridyl)acetamide derivatives having the formula ##STR1## [where R.sup.1 and R.sup.2 are aryl or heteroarly (optionally linked together by a lower alkylene bridge) or one of R.sup.1 and R.sup.2 is aryl or heteroaryl and the other of R.sup.1 and R.sup.2 is lower alkyl or ar(lower)alkyl, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl] and their nontoxic acid addition salts are described. They are chemical intermediates for the preparation of 4-pyridinamine derivatives having the formula ##STR2## which show CNS activity and may be used as antidepressant drugs.

Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3, or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optional double bond, R.sup.2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.

Abstract: A process for the manufacture of a 2(3H)-benzothiazolone compound substituted in 3-position, or of a 2(3H)-naphthothiazolone compound substituted in 3-position which comprises treating a 2(3H)-iminobenzothiazoline compound substituted in 3-position or a 2(3H)-naphthothazoline compound substituted in 3-position with an alkali metal hydroxide or alkaline earth metal hydroxide in a solvent or diluent stable to alkalis, in the absence of water or with substantial exclusion of water, and cyclizing the alkali metal or alkaline earth metal salt of the ortho-mercapto-N-phenyl- or -naphthyl-urea compound substituted at the nitrogen atom so formed, optionally without intermediate isolation, by treatment with an acid to give the 2(3H)-benzothiazolone compound substituted in 3-position or the 2(3H)-naphthothiazolone compound substituted in 3-position. The process furnishes the final products with high yield and purity; waste water problems are excluded by this process.

Abstract: Aromatic-.alpha.-halo-{b} fused pyridines are made by reacting an aromatic acetamide, acid halide and amide in particular proportions, with the acid halide always in excess. The process permits the production of compounds having a wide range of substituents, that are new compounds, and that are of value as intermediates in the synthesis of, for instance, pharmaceutical compounds.

Abstract: Isoquinoline derivatives of the formula ##STR1## wherein the symbol A.sub.1 represents an isoquinol-8-yl, 3-methylisoquinol-8-yl, 3-hydroxymethylisoquinol-5-yl, 3-carboxymethylisoquinol-5-yl, quinol-5-yl, thienopyridyl, benzimidazolyl, thienyl or thiazolyl radical, a 4-(or 5-)carboxyalkylthiazol-2-yl radical in which the alkyl moiety is linear or branched and contains 1 to 4 carbon atoms, or a 1,3,4-thiadiazol-2-yl, pyrazolyl, imidazolyl, pyrimidinyl, pyridazinyl or pyrazinyl radical, monocyclic heterocyclic rings within the definition of A.sub.1 being optionally substituted by a linear or branched alkyl radical containing 1 to 4 carbon atoms, in the (S) or (R,S) form or mixtures thereof, and salts thereof possess useful pharmocological properties, in particular antiviral activity.

Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3 or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optical double bond, R.sup.2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.

Abstract: Novel compounds selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 or 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, halogen and methyl, R.sub.3, R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, --NH.sub.2 and mono- and dialkylamino of 1 to 3 alkyl carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant and neuroleptic activity and their preparation.

Abstract: Nitrogen containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl groups, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents by hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is chlorine, bromine or alkyl of 1 to 3 carbon atoms;R.sub.2 is hydrogen or, when R.sub.1 is alkyl, chlorine or bromine;R.sub.1 and R.sub.2, together with each other, are straight alkylene of 3 to 4 carbon atoms;R.sub.3 is hydrogen, fluorine, chlorine, bromine, alkyl of 1 to 2 carbon atoms; hydroxyl or trifluoromethyl; andR.sub.4 is hydrogen, straight or branched alkyl of 1 to 4 carbon atoms or phenyl lower alkyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antidepressants.

Abstract: Isoquinoline derivatives of the formula: ##STR1## wherein R.sub.1 represents alkyl of 1 through 8 carbon atoms, and n represents 1 or 2, are new compounds possessing useful pharmacological properties. They are particularly valuable as analgesic, anti-inflammatory, antipyretic or antiviral agents.

Abstract: 3,4-Dihydroxyphenyltetrahydrothieno[2,3-c] or [3,2-c] pyridines are prepared by cyclization of a N-thienylmethyl-2-(3',4'-dimethoxyphenyl)-ethanolamine. These compounds have renal vasodilating activity. A species is 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydrothieno[2,3-c]pyridine and its pharmaceutically acceptable acid addition salts or esters.

Abstract: Acetic acid derivatives having the formula, ##STR1## wherein X represents an oxygen or two hydrogen atoms, Y represents CH or N, A represents an oxygen or sulfur atom, and R represents hydroxy, amino or a lower alkoxy group having 1 to 5 carbon atoms possess excellent antiinflammatory activities.

Abstract: Thienopyridine derivatives of the formula: ##STR1## wherein the symbol A represents pyrid-3-yl, isoquinol-5-yl, or a 3-alkylisoquinol-5-yl group in which the alkyl radical is of 1 through 10 carbon atoms, and one of the symbols X and Y represents a single bond and the other represents the vinylene radical, are new compounds possessing useful pharmacological properties. They are particularly useful as anti-viral agents and, in certain cases, as analgesics, anti-inflammatory agents and anti-pyretics.

Abstract: Dyestuffs of the formula ##STR1## wherein R.sup.1, R.sup.2, R denote H, alkyl, alkenyl, cycloalkyl, aralkyl etc.R.sup.3, R.sup.4 denote H, alkyl, aralkyl, aryl, alkoxy, halogen, CN, COOH, alkoxycarbonyl, alkylsulfonyl, arylsulfonyl etc.Z denotes O, S or --N(R)--,p and q denote 0 or 1, but not simultaneously 0 andG stands for the remaining members of a ring system,with the proviso that R.sub.3 is not alkyl if G is a thiazole ring, are outstanding suitable for dyeing fibre materials of all kinds in clear yellow to violet shades with good fastness properties.

Abstract: Propionic acid derivatives having the formula ##STR1## wherein X represents an oxygen or two hydrogen atoms, Y represents CH or N, A represents an oxygen or sulfur atom, and R represents hydroxy, amino, or a lower alkoxy group having 1 to 5 carbon atoms are antiinflammatory agents.

Abstract: Compounds of the formula: ##STR1## where R is H or lower alkyl and a process for the preparation thereof are disclosed. The compounds are analgesic agents.

Abstract: This invention relates to compounds having the formula: ##STR1## in which: R.sup.1 represents hydrogen or a lower alkyl group; an aralkyl group optionally substituted on the aromatic nucleus with at least a halogen atom or a hydroxy, nitro, amino, cyano, carboxy, carboxamido, alkoxycarbonyl, lower alkyl, lower alkoxy or trifluoromethyl group; a nicotinyl group; an isonicotinyl group; a picolyl group; a furfuryl group; a 5-methyl-furfuryl group; a 2- or 3-thenyl group; a 5-methyl-2- or 3-thenyl group; or a 5-chloro-2-thenyl group;R.sup.2 represents hydrogen or a lower alkyl radical; andR.sup.3 and R.sup.4 represent each hydrogen, a halogen atom or a hydroxy, lower alkyl or lower alkoxy group,And their addition salts with inorganic or organic acids.Said new compounds have typically a therapeutically useful sedative and blood-platelet aggregation inhibiting activity.

Abstract: A compound having one of the structural formulae: ##STR1## AND HYDROGENATED, CHLORINATED AND BROMINATED DERIVATIVES THEREOF; ##STR2## WHEREIN R is H or lower alkyl; ##STR3## WHEREIN X is Cl or Br and n is an integer from 0 to 6; ##STR4## WHEREIN X is Cl or Br and m is an integer from 0 to 8; ##STR5## AND HYDROGENATED, CHLORINATED AND BROMINATED DERIVATIVES THEREOF; AND, ##STR6## USEFUL AS INSECTICIDES.

Abstract: The invention relates to new thiazoloisoquinolines of the formula (I), or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sup.1 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.2 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 is hydrogen, cyano, alkyl, aryl, nitro, carboxy, carboalkoxy or carboxamido, andY is oxygen, sulfur, or a group of the formula .dbd.N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkyl-sulfonyl or arysulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.

Abstract: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.

Abstract: Isoquinoline derivatives of the formula: wherein R represents alkyl of 1 through 10 carbon atoms, which are new compounds, possess pharmacological properties and are particularly active as anti-inflammatory, analgesic and antipyretic agents.

Abstract: Thienopyridine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, an alkyl, an aryl, an aralkyl or a halogen; R.sup.1 and R.sup.2 may, taken together, represent an alkylene group; X is hydrogen or an alkyl; Y is oxygen or sulfur; Z is phenyl which may optionally be substituted; R.sup.3 is hydrogen or an alkoxy; and R is a group of the formula: ##STR2## or of the formula: ##STR3## (wherein R.sup.4 is hydrogen, an acyloxy or a nucleophilic compound residue) or a pharmaceutically acceptable salt thereof are found to have activity against a broad spectrum of gram-positive and gram-negative bacteria, particularly against bacteria of the genus Pseudomonas .