Abstract: A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): ##STR1## whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuration (II) over the cis configuration (III) as defined in the following formulae: ##STR2## The preferred reaction conditions include use of a borane complex as the reducing agent and an acidic solvent such as trifluoroacetic acid.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: 5,6,-dihydro-pyrrolo[2,1-a]isoquinolines of the formula ##STR1## are prepared by heating a 1-(3-furyl)-3,4-dihydro-isoquinoline of the formula ##STR2## in a primary or secondary amine to at least 80.degree. C. for several hours, the amine is removed, the reaction product is treated with dilute acid, and the reaction product is purified and isolated.

Abstract: A process for the preparation of a compound of the formula ##STR1## having a trans 4a,10b-ring junction wherein X represents oxygen or sulfur; ring A is substituted by lower alkoxy; R represents lower alkyl; R.sub.1 -R.sub.5 represent hydrogen; which comprises (a) condensing the corresponding 2H[1]-benzopyran-3-one with the corresponding carboxy protected 3-aminopropanoic acid, (b) reducing and dehydrating the resultant product, and reducing the resulting double bond to a compound of formula I.

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: The invention relates to 5,6-dihydro-pyrrolo[2,1-a]isoquinolines of the formula ##STR1## wherein R, R.sup.2, R.sup.3, and R.sup.7, which may be identical or different, each represent a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms;R.sup.1 represents a cyano, hydroxycarbonyl, or alkoxycarbonyl group having from 1 to 4 carbon atoms or a primary or secondary, substituted or unsubstituted, aliphatic, cycloaliphatic, araliphatic, aromatic, or heterocyclic aminocarbonyl group;R.sup.4 and R.sup.8, which may be identical or different, each represent a hydrogen atom, a hydroxyl group, an alkoxy or alkylthio group having up to 4 carbon atoms, or an NR.sup.9 R.sup.10 group;R.sup.5 and R.sup.6, which may be identical or different, each represent a hydroxy atom or an alkoxy or alkylthio group having from 1 to 4 carbon atoms, or together represent an --O--CH.sub.2 --O--, --O--CH.sub.2 --CH.sub.2 --O--, or --O--CH.dbd.CH--O group;R.sup.

Abstract: Disclosed are the compounds of the formula ##STR1## wherein X represents oxygen (O) or sulfur (S); ring A is unsubstituted or substituted by one substituent or by two or three identical or different substituents selected from hydroxy, etherified hydroxy, acyloxy, halogen, lower alkyl and trifluoromethyl; or ring A is substituted on adjacent carbon atoms by one lower alkylenedioxy; R represents hydrogen, lower alkyl, aryl-lower alkyl, lower alkenyl, lower alkynyl, aroyl-lower alkyl or aryl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, lower alkylthio-lower alkyl, aryl-lower alkylthio-lower alkyl, (amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (hydroxy, acyloxy or etherified hydroxy)-lower alkyl, or cyano-lower alkyl; R.sub.2 -R.sub.7 represent hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof; which are useful as serotonin-2 receptor antagonists in mammals.

Abstract: A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms;A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; andR.

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: Compounds of the formula ##STR1## in which A denotes C-R.sup.4 or N; X denotes alkyl and Y denotes alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or benzoyl, or, together with X, cycloalkyl; R.sup.1 -R.sup.4 denote H, alkyl, alkoxy, alkoxycarbonyl, halogen, NO.sub.2, CN, phenoxy or (substituted) phenyl; R.sup.5 denotes H or alkyl; and R.sup.6 denotes H, (substituted) alkyl, halogenoalkenyl, cycloalk(en)yl, alkynyl, (substituted) phenyl or carboxylic acid ester, carboxylic acid amide, sulfo-ester or acyl radicals, are effective plant treatment agents, in particular herbicides.

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: The invention relates to pyrazolooxazines, pyrazolothiazines and pyrazoloquinolines defined herein by Formula I. The invention also includes compositions containing said Formula I compounds and methods for the use of said compounds and compositions for their lipoxygenase-inhibiting properties. Also included in the invention are methods for the manufacture of said compounds of Formula I.

Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bri

Abstract: The invention provides various medical compositions for use in treating or preventing certain of the side effects of diabetes or galactosemia. The active ingredients are selected from a series of novel aldose reductase inhibitory spiro-linked pyrrolidine-2,5-diones of the general formula: ##STR1## or a pharmaceutically acceptable salt, or a non-toxic, biodegradable precursor thereof. Processes for the production of these compounds are also provided. A particular compound suitable for use as an active ingredient is spiro[pyrrolidine-3,9'-xanthene]-2,5-dione.

Abstract: (1H-Tetrazol-5-yl)tetrazolo[1,5-a]quinolines and related compounds which are useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate halocyanoquinoline or isoquinoline with ammonium chloride and an azide such as sodium azide in an inert solvent such dimethylformamide.

Abstract: Pyrido (3,4', 4,5) furo (3,2-g) coumarins or pyrido (3,4-h) psoralens having formula I ##STR1## wherein R is a hydrogen radical or a lower alkyl group having from 1 to 4 carbon atoms and R" is a methyl group or a methoxy group. These compounds are photobiologically active and are useful or medicinals and pharmaceutical compositions in association with ultraviolet radiation for treating skin diseases and as cosmetic compositions for skin pigmentation.

Abstract: Monofunctional psoralen derivatives having the general formula ##STR1## wherein R represents a hydrogen atom, a lower alkyl group having from 1 to 4 atoms, preferably a methyl radical, or a lower alkoxy radical having from 1 to 4 carbon atoms, preferably a methoxy radical are described. The derivatives are photobiologically active and are useful in photochemical therapy and in cosmetics.

Abstract: Pyrrolo [3,4-c]quinolines are described which have various substitutions at the 2, 4, 5, 6, 7, 8 and 9 positions. The group of compounds has been found to possess unexpected pharmaceutical utilities including antipsychotic, analgesic and antidepressant activities. Also set forth are various methods of making the compounds as well as pharmaceutical compositions containing them.

Abstract: Quinolinecarboxylic acid derivatives, such as compound 7-fluoro-8-(4-methyl-1-piperazinyl)-5-oxo-1,2-dihydro-5H-thiazolo(3,2-a)-q uinoline-4-carboxylic acid, a pharmaceutical composition containing the same and methods of treatment of bacterial and fungal infections using the same.

Abstract: Anticholinergic 3-[2-(azabicyclo)ethyl]-1,2,3,4-tetrahydro-5H-[1]benzopyrano[3,4-c]pyridin -5-ones useful for treating bronchospastic diseases in mammals are disclosed. Also disclosed are methods for preparing said compounds, pharmaceutical compositions containing them and methods for using said pharmaceutical compositions.

Abstract: Anticholinergic 3-[2-(mono- and dialkylamino)-propyl]-1,2,3,4-tetrahydro-5H-[1]benzopyrano[3,4-c]-pyridin- 5-ones useful for treating bronchospastic diseases in mammals are disclosed. Also disclosed are methods for preparing said compounds, pharmaceutical compositions containing them and methods for using said pharmaceutical compositions.A method for preparing the intermediate which is required to prepare the unsubstituted benzopyrano-[3,4-c]pyridin-5-ones of the invention is also disclosed.

Abstract: The invention provides indole compounds useful for the treatment of hypertension, processes for the preparation of said compounds and pharmaceutical compositions containing these compounds.The compounds of the invention have the formula ##STR1## wherein n is 2 or 3, A is 1,4-cyclohexylidene or trimethylene and R.sub.1 is H or alkyl, or A together with NR.sub.1 is 4-piperidyl, R.sub.2 is hydrogen or alkyl, R.sub.3 is alkyl, cycloalkyl, amino, alkylamino, dialkylamino, phenylamino, unsubstituted or substituted phenyl or benzyl, pyridylmethyl or an heterocycle, R.sub.4 is hydrogen, chlorine, bromine or alkyl, R.sub.5 is hydrogen, alkyl, alkoxy or alkylthio, and X is --CO-- or --CS.

Abstract: Pyrrolo [3,4-c]quinolines are described which have various substitutions at the 2, 4, 5, 6, 7, 8 and 9 positions. The group of compounds has been found to possess unexpected pharmaceutical utilities including antipsychotic, analgesic and antidepressant activities. Also set forth are various methods of making the compounds as well as pharmaceutical compositions containing them.

Abstract: An antiphlogistic compound of the formula (I) ##STR1## or a pharmaceutically effective salt thereof wherein R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkoxy or together form a methylenedioxy group;R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n -R.sup.7 with the proviso that at least one of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen;R.sup.7 is a carboxylic group or a carboxylic acid derivative group; n=0, 1 or 2, provided that if R.sup.3, R.sup.4 and R.sup.5 are hydrogen and R.sup.7 in the group R.sup.6 is cyano or alkoxycarbonyl, and n=1, then R.sup.1 and R.sup.2 are hydrogen, C.sub.2-4 alkoxy, or together form a methylenedioxy group.

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: Disclosed are trans-2-substituted-amido-hexahydrobenzo[a]quinolizines represented by the formula: ##STR1## In the above formula, R.sup.1 and R.sup.2 are independently --H or --OCH.sub.3 or when taken together are ##STR2## R.sup.3 is --H or --CH.sub.3 and R.sup.4 is ##STR3## These compounds, and their pharmacologically acceptable, non-toxic, acid addition salts are useful as anti-hypertensive agents.

Abstract: 2-oxo-3-(.beta.-cyanoethyl)-9,10-methylenedioxy-1,2,3,4,6,7-hexahydro-11bH- benzo(a)quinolizidine (SC-118) especially and the corresponding 9,10-diethoxy compound are superior antiphlogistics which are used in effective amounts in antiphlogistic therapy.

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.