Abstract: This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.

Abstract: 1-Substituted-6-fluoro-7-heterocyclic-1,4-dihydroquino-1-(or dihydronaphthyridin)-4-one carboxylic acids have antibacterial properties. The 7-heterocyclic group is a bicyclic group, one of the rings of which is saturated and the other ring of which is unsaturated.

Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl;Y is CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.

Abstract: Novel tricyclic arylsulfonamides useful for treating hypertension and bronchoconstiction, as well as to their pharmaceutical compositions and methods for using the same.

Abstract: Novel 2,6-methano-1,3-benzodiazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain and for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease, utilizing compounds or compositions thereof are disclosed.

Abstract: New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy or alkylamino radical or an amine protective radical and either Hal is a fluorine, chlorine or bromine atom and R' is a hydrogen atom or Hal and R' are simultaneously fluorine atoms, their salts, their preparation and the compositions which contain them.These new products can be used as antimicrobial agents for topical application or as synthesis intermediates.

Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.

Abstract: A dye for heat sensitive transfer recording represented by formula (I): ##STR1## wherein Q.sup.1 represents an atomic group, which includes at least one nitrogen atom, which is required, together with the carbon atoms to which said atomic group is bonded, to form an at least five membered nitrogen containing heterocyclic ring; R.sub.1 represents an acyl group or a sulfonyl group; R.sub.2 represents a hydrogen atom or an aliphatic group which has from 1 to 6 carbon atoms; R.sub.3 represents a hydrogen atom, a halogen atom, an alkoxy group, or an aliphatic group which has from 1 to 6 carbon atoms; R.sub.4 represents a halogen atom, an alkoxy group, or an aliphatic group which has from 1 to 6 carbon atoms; n represents an integer of from 0 to 4; R.sub.3 may be joined to R.sup.1, R.sup.2, or R.sup.4 to form a ring; R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, an aliphatic group which has from 1 to 6 carbon atoms, or an aromatic group; R.sup.5 and R.sup.

Abstract: Trans-(.+-.)-2-(substituted)-6-(substituted)-5,5a,6,7,8,9,9a,10-octahydropy rido[2,3-g]quinolines are useful in treating a variety of disorders including Parkinsonism, anxiety, depression, hypertension, glaucoma, sexual dysfunction, and prolactin mediated disorders such as galactorrhea, amenorrhea, prolactinoma and the inhibition of postpartum lactation.

Abstract: New benzo[b][1,8]naphthyridine derivatives of general formula (I) in which R is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy, alkylamino or protected alkylamino radical, Hal is F, Cl or Br if R' is hydrogen, or Hal and R' are F, and Alk is an alkyl radical, and their preparation.These new products can be used as intermediates for the preparation of biologically active products.

Abstract: Trans-(.+-.)-2-(substituted)-6-(substituted)-5,5a,6,7,8,9,9a,10-octahydroph rido[2,3-g]quinolines are useful in treating a variety of disorders including Parkinsonism, anxiety, depression, hypertension, glaucoma, sexual dysfunction, and prolactin mediated disorders such as galactorrhea, amenorrhea, prolactinoma and the inhibition of postpartum lactation.

Abstract: The present invention includes compounds represented by the formula: ##STR1## wherein R.sub.1 is a hydroxy, a C.sub.1 to C.sub.6 alkoxy, benzoxy, or an alkylcarbonyloxymethoxy group, or R.sub.3 together with R.sub.1 forms a group of the formula --Y--NH-- where Y is oxygen or sulfur; or R.sub.3 is hydrogen; A is nitrogen or CR.sub.2, where R.sub.2 is hydrogen, or halogen, or R.sub.2 together with R forms a group of the formula --X--CH.sub.2 --CH(R.sub.6)-- or --X--CH.sub.2 --CH.dbd.CH.sub.2, wherein X is CH.sub.2, O, S, NH, or NCH.sub.3, and R.sub.6 is hydrogen, alkyl, or C.sub.1 -C.sub.3 haloalkyl; or R is (1) a C.sub.1 to C.sub.4 alkyl, (2) lower cycloalkyl, (3) alkylamino, (4) haloalkyl, (5) an aromatic heterocyclic ring or (6) a substituted phenyl group; and Z is a carbocyclic group;or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as antibacterial agents.

Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridge arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl,, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.6 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.

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: Bis-(2,2,6,6-tetramethyl-piperidyl)diimides are provided, having the formula: ##STR1## in which R is selected from the group consisting of hydrogen; oxyl; alkyl and alkenyl having from one to about eighteen carbon atoms; epoxy and hydroxyalkyl having from two to about eight carbon atoms; acyl having from two to about eight carbon atoms; and phenalkyl having from seven to about twelve carbon atoms; and Z is a tetravalent aliphatic or cycloaliphatic hydrocarbon group having from two to about eighteen carbon atoms; and stabilizer and synthetic polymer compositions containing such diimides having improved resistance to deterioration when exposed to light.

Abstract: Novel cyclized N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.

Abstract: Process for mass-coloring high molecular weight organic material, which comprises using a compound of the formula I ##STR1## in which one of R.sub.1 and R.sub.2 and one of R.sub.3 and R.sub.4 are, independently of each other, hydrogen, C.sub.1 -C.sub.12 -alkyl or benzyl and the other two radicals are, independently of each other, unsubstituted or halogen-, trifluoromethyl-, cyano-, C.sub.1 -C.sub.12 -alkyl-, --OR.sub.5 -, --SR.sub.5 -, --COR.sub.6 - or --SO.sub.2 R.sub.6 -substituted phenyl, biphenyl or naphthyl or a 5- or 6-membered aromatic heterocyclic ring containing one or more identical or different hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur without or with one or two fused-on benzene rings, R.sub.5 is hydrogen or C.sub.1 -C.sub.12 -alkyl, R.sub.6 is C.sub.1 -C.sub.12 -alkyl, and X and Y are independently of each other hydrogen, halogen or cyano.The invention also relates to new pyridoquinolones of the formula I.

Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.

Abstract: Compounds suitable for being used as lubricants, having general formula:(I) RO--(C.sub.3 F.sub.6 O).sub.m --(CFXO).sub.n --CFX--L,or(II) R"CFXO--(C.sub.3 F.sub.6 O).sub.x (CFXO).sub.y --(C.sub.2 F.sub.4 O).sub.z --CFX--L,whereR=--CF.sub.3, --C.sub.2 F.sub.5, --C.sub.3 F.sub.7X=F, --CF.sub.3R"=F, --CF.sub.3, --C.sub.2 F.sub.5m=an integer from 3 to 100n=a finite integer, or=zero, wherefore m+n ranges from 3 to 100, provided that, if n is finite, m/n ranges from 5 to 20 and R is preferably=CF.sub.3, if n=zero, R is preferably --C.sub.2 F.sub.5 or --C.sub.3 F.sub.7x=a finite integer, or=zeroy, z=finite integers, such that x+y+z ranges from 5 to 200, while (x+z)/y ranges from 5 to 0.5, provided that when x=zero, z/y ranges from 1 to 0.5 and y+z ranges from 5 to 200 n while X is is preferably F, and R"=LL=group Y-Z,where:Y=--CH.sub.2 O--, --CH.sub.2 --OCH.sub.2, --CF.sub.2, --CF.sub.

Abstract: There are disclosed compounds of the formula ##STR1## where .dbd.X--Y-- is ##STR2## R.sub.4 being loweralkyl and R.sub.5 being hydrogen or loweralkyl, --Z-- is ##STR3## n is 1, 2 or 3, R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl or arylloweralkyl, and R.sub.3 is hydrogen or loweralkyl, with the proviso that when .dbd.X--Y-- is ##STR4## n is 2 or 3, R.sub.1 is hydrogen and R.sub.2 is hydrogen or loweralkyl, Z is not ##STR5## which compounds are useful for enhancing memory and for treating Alzheimer's disease.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is pyridl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino, R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, R.sup.4 NCH.sub.2 CH.sub.2 OCH.sub.3, SCH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkylor phenyl; andR.sup.6 and R.sup.

Abstract: There is described a method of synthesizing 1,4-dihydro-benzo[c]-1,5-naphthyridin-2(3H)-ones having the formula ##STR1## where X is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl or hydroxy, which method consists essentially of the aromatization and rearrangement of 1,10a-dihydropyrrolo[1,2-b]isoquinoline-3,10(2H,5H)-dione oximes of the formula below: ##STR2##

Abstract: There are disclosed novel compounds of the formula ##STR1## where m is 1 or 2; each X is independently H, halogen, loweralkyl, loweralkoxy, --CF.sub.3, or --OH; R is H, loweralkyl, chloroloweralkyl, bromoloweralkyl, iodoloweralkyl, aminoloweralkyl, loweralkylaminoloweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, thienylloweralkyl, furylloweralkyl, loweralkanoyl, chloroloweralkanoyl, bromoloweralkanoyl, iodoloweralkanoyl, aminoloweralkanoyl, loweralkylaminoloweralkanoyl, diloweralkylaminoloweralkanoyl, aroyl, arylloweralkanoyl or diarylloweralkanoyl, thienylloweralkanoyl, furylloweralkanoyl; and R.sub.1 is .dbd.O, ##STR2## or --NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being independently H or loweralkyl, or taken together with the nitrogen atom to which they are attached constituting ##STR3## R.sub.4 in turn being H, loweralkyl, hydroxyloweralkyl, aryl, arylloweralkyl or diarylloweralkyl, with the proviso that when R.sub.1 is --NR.sub.2 R.sub.3, R is nonexistent, that when R.sub.1 is .

Abstract: Process for mass-coloring high molecular weight organic material, which comprises using a compound of the formula I ##STR1## in which one of R.sub.1 and R.sub.2 and one of R.sub.3 and R.sub.4 are independently of each other hydrogen, C.sub.1 -C.sub.12 -alkyl or benzyl and the other two radicals are independently of each other unsubstituted phenyl, phenyl which is substituted by halogen, trifluoromethyl, cyano, C.sub.1 -C.sub.12 -alkyl, phenyl or by the groups --OR.sub.5, --SR.sub.5, --COR.sub.6 or --SO.sub.2 R.sub.6, or a 5- or 6-membered aromatic heterocyclic ring containing one or more identical or different hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur without or with one or two fused-on benzene rings, R.sub.5 is hydrogen or C.sub.1 -C.sub.12 -alkyl, R.sub.6 is C.sub.1 -C.sub.12 -alkyl, and X and Y are independently of each other hydrogen, halogen or cyano.The invention also relates to new pyridoquinolones of the formula I.

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.

Abstract: Substituted quinoline, [1,5]- and [1,8]-naphthyridine and pyrido[2,3-b]pyrazine derivatives are anti-allergic, anti-inflammatory and cytoprotective agents. Methods for their preparation and use are disclosed.

Abstract: This invention describes tricyclic derivatives which are useful as histamine H.sub.1 -antagonists. A particular compound of this invention is 3-[3-(pyrido[3,2-b][1,4]-benzothiazin-10-yl)propylamino]-4-(pyrid-4-ylmeth ylamino)-1,2,5-thiadiazole-1-oxide.

Abstract: Polyfluorinated substituted quinoline mono- and dioxo compounds and a method for preparing them are described. The fluorinated oxo compounds are useful as antifungal agents.

Abstract: There are disclosed novel compounds of the formula ##STR1## where X is H, halogen, loweralkyl, loweralkoxy, --CF.sub.3, or --OH; R is H, loweralkyl, arylloweralkyl, diarylloweralkyl, loweralkanoyl, arylloweralkanoyl or diarylloweralkanoyl; and R.sub.1 is H.sub.2, O or --NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being independently H or loweralkyl, or taken together with the nitrogen atom to which they are attached constitute ##STR2## R.sub.4 in turn being H, loweralkyl, hydroxyloweralkyl, aryl, arylloweralkyl or diarylloweralkyl or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.

Abstract: Tetrahydro-.beta.-carboline derivative of the formula: ##STR1## wherein R.sup.2 is lower alkyl, and either (A)R.sup.1 is hydroxymethyl or carboxy,R.sup.3 and R.sup.4 are both hydrogen, andX is halogen, lower alkyl, lower alkoxy, hydroxy or benzyloxy; or(B)R.sup.1 is hydrogen, carboxy-lower alkyl or a group of the formula: --CH.sub.2 OY,Y is lower alkyl, lower alkanoyl or an oxygen-containing monocyclic heterocyclic group,R.sup.3 is hydrogen, hydroxy-lower alkyl or carboxy,R.sup.4 is hydrogen or hydroxy-lower alkyl, andX is hydrogen,or a salt thereof, which has excellent activities for alleviating, curing and preventing hepatic damages and is useful as a therapeutic or prophylactic agent for hepatic diseases.

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: New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.

Abstract: Disclosed are 5,6-dihydro benzo[f]quinolines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure.

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

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: Compounds having activated methylene radicals are oxidized to various oxidation products by an improved process comprising contacting the compound with an oxidizing agent and a base of sufficient strength to deprotonate at least one hydrogen from the activated methylene radical in the presence of a catalytic amount of a synergistic combination of elemental carbon and a phase-transfer catalyst. For example, flourene is oxidized to flourenone by contacting the flourene with elemental oxygen and sodium hydroxide in the presence of a catalytic amount of the synergistic combination of charcoal and benzyltriethyl-ammonium chloride.

Abstract: Cationic dyestuffs of the formula ##STR1## wherein A represents oxygen, sulphur or the groupings >N--R.sub.3, ##STR2## wherein R.sub.3 denotes an alkyl, aryl or aralkyl radical,R.sub.4 and R.sub.5 independently of one another denote an alkyl radical,R.sub.6 and R.sub.7 independently of one another denote hydrogen or an alkyl radical,R represents hydrogen or an alkyl group,R.sub.1 and R.sub.2 independently of one another represent hydrogen or an alkyl, aryl or aralkyl radical, orR.sub.1 can be bonded to R.sub.2 or to the ring b, andAn.sup.- represents an anion,and whereinthe rings a and b and the radicals R, R.sub.1, R.sub.2 and R.sub.3 can contain non-ionic substituents which are customary in dyestuff chemistry or carboxyl groups,are suitable for dyeing synthetic and natural materials, in particular paper.

Abstract: Quinoline and aniline compounds have been synthesized from aromatic nitro compounds and ethylenically unsaturated hydrocarbons in the presence of complexes of Group VIII metals used as catalysts.

Abstract: Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Abstract: Novel chemical compounds of the formula: ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, phenyl, alkali metal, or an amine cation;X and Y can be the same or different and are selected from the group consisting of hydrogen, alkyl or from one to six carbon atoms, inclusive, cycloalkyl of 5 or 6 carbon atoms, inclusive, phenyl, hydroxyl, alkoxy having from one to three carbon atoms, inclusive, halogen, trifluoromethyl, cyano, carboxyamide and ##STR2## where Q is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, alkali metal, and an amine cation, with the proviso that whereR is hydrogen, alkali metal or an amine cation, then Q is the same as R, and whereR is phenyl or alkyl from one to three carbon atoms, then Q is phenyl or alkyl from one to three carbon atoms; andZ is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, and phenyl.