Abstract: The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.

Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.

Abstract: Compounds of Formula (I), and their N-oxides and agriculturally-suitable salts, are disclosed which are useful in controlling undesired vegetation, wherein J is Formula (II), Q is represented by Q-1 through Q-4 and X, Y, Z, R.sup.1-19, m, n, p, q, and r are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (I).

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: A process for preparing thioxanthone and derivatives thereof is disclosed. In the process, an aromatic compound, such as cumene, is reacted with thiosalicylic acid (TSA) or dithiosalicylic acid (DTSA) in the presence of sulfuric acid. The reaction mixture, which includes thioxanthone or a derivative thereof, is thereafter distilled under reduced pressure to recover the thioxanthone compound.

Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.

Abstract: A process for preparing thioxanthone and derivatives thereof is disclosed. In the process, an aromatic compound, such as cumene, is reacted with thiosalicylic acid (TSA) or dithiosalicylic acid (DTSA) in the presence of sulfuric acid. The reaction mixture, which includes thioxanthone or a derivative thereof, is thereafter distilled under reduced pressure to recover the thioxanthone compound.

Abstract: A photochromic compound, in particular, for tinting optical elements made of a plastic material has reduced mobility in plastic material. The photochromic compound is a photochromic 2H-pyran and is distinguished by the aromatic residues being chemically rigidly attached in the 2-position to a spiropyran.

Abstract: Compounds of Formula I and their agriculturally suitable salts are disclosed which are useful for controlling undesired vegetation ##STR1## wherein Q is ##STR2## and R.sup.1 through R.sup.7, m, n, p and q are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.

Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).

Abstract: ConstitutionTricyclic heterocyclyl compounds having a general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 each represents H, a lower alkyl or lower alkoxy group, a halogen atom or halogeno-lower alkyl; R.sup.3 represents H or a lower alkyl group; R.sup.4 represents a substituted phenyl or naphthyl group; R.sub.5 represents H or a lower alkyl group; A represents a lower alkylene group; B represents an --O-- or --S-- group; and n is 0-1.EffectThe compounds have an excellent activity in the inhibition of acyl-CoA: cholesterol acyltransferase (ACAT) and are useful for the treatment and prophylaxis of atherosclerosis.

Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.

Abstract: Thioxanthone derivatives of the general formula I ##STR1## wherein R.sup.1 wherein R.sup.1 represents a halogen atom or a C.sub.1-10 alkoxy group, R.sup.2 and R.sup.4 each represent a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.6 alkyl group, X represents oxygen or sulphur, and R.sup.3 represents a C.sub.1 -C.sub.10 alkyl group optionally substituted by a hydroxy group which hydroxy group may be alkylated by an optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkenyl or a benzyl group or acylated by a C.sub.1-8 alkanoyl or C.sub.1-8 alkenoyl group, a C.sub.1-10 alkenyl group, a C.sub.3 -C.sub.6 cycloalkyl group, a C.sub.1 -C.sub.8 alkanoyl group, a C.sub.1-8 alkenoyl group, an optionally substituted phenyl group, an optionally substituted benzyl group or an optionally substituted benzoyl group.

Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.

Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.

Abstract: Compounds of the formula I ##STR1## in which X is O, S, SO, SO.sub.2 or NR.sub.13, R.sub.13 is, for example, methyl, and R.sub.1 to R.sub.12, independently of one another, are, for example, H, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 Alkoxy, halogen or --CN. The compounds are photosensitive and photochromic and are suitable as photosensitizers and simultaneously as color indicators, and as photoswitchable color filters.

Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: The present invention discloses a new class of calcium specific fluorescent indicator dyes having visible excitation and emission wavelengths. The new fluorescent indicator dyes combine at least one tricyclic chromophore with a tetracarboxylate parent CA.sup.2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of BAPTA to give a rhodamine-like or fluorescein-like fluorophore. Binding of calcium.sup.2+ increases the fluorescence of the new compounds by up to 40-fold. The calcium.sup.2+ dissociation constants are in the range 0.37-2.3 microM, so that the new indicators give better resolution of high [CA.sup.2+ ] levels than were previously obtainable with predecessor compounds such as quin-2 or fluo-2. The visible excitation wavelengths of the new compounds are more convenient for fluorescent microscopy and flow cytometry than the UV required by previous indicators.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

Abstract: The invention relates to photoinitiators having a combined structure ##STR1## and their use as photoinitiators in the photopolymerization of ethylenically unsaturated compounds or binder systems containing them.

Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.

Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.

Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.

Abstract: The invention provides thioxanthone derivatives of general formula ##STR1## wherein one of R.sup.2, R.sup.3 and R.sup.4 is a group of formula ##STR2## in which one of R.sup.5, R.sup.6 and R.sup.7 is an alkyl or a benzyl group, the others being alkyl groups and A.sup.- represents an anion, and R.sup.1 and the others of R.sup.2, R.sup.3, and R.sup.4 are independently selected from hydrogen atoms, alkyl groups and alkoxy groups; and the use of such derivatives as photoinitiators, particularly in aqueous photopolymerizable compositions for the production of stencils for screen printing.

Abstract: Compounds of formula (I) ##STR1## wherein n is 0, 1 or 2;one or R.sup.1 and R.sup.2 is hydrogen and the other is selected from carbamoyl, N-C.sub.1-4 alkylcarbamoyl, N,N-di-C.sub.1-4 alkylcarbamoyl, carbamimidoyl, N.sup.1 -C.sub.1-4 alkylcarbamimidoyl, N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1 -C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl and imidazolin-2-yl (optionally substituted by one or more C.sub.1-4 alkyl groups); andR.sup.3 is selected from hydrogen, saturated and unsaturated aliphatic hydocarbon moieties containing from 1 to 4 carbon atoms, groups OR.sup.4 (where R.sup.4 is selected from hydrogen and saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms), halo, groups of formula--NR.sup.5 R.sup.6 (where R.sup.5 and R.sup.6 are independently selected from hydrogen, C.sub.1-4 alkyl and hydroxy C.sub.

Abstract: Novel xanthones and thioxanthones of the formula I ##STR1## in which A, X, Y, Z, E and E' are as defined in patent claim 1, are described. A is preferably --S-- and E and E' are preferably bonded in the ortho-position relative to one another. The compounds (I) are suitable, for example, as sensitizers for photocrosslinkable polymers or photocurable compositions, or for use in mixtures with polymers with H donor groups for image formation, in particular electrically conductive coatings and patterns, by means of electroless deposition of metals.

Abstract: A method for preparing a compound of formula I ##STR1## in which X is O or S;both groups R together with the two carbon atoms to which they are attached form a fused aromatic group;R.sub.1 is an organic radical; andn is 0, 1, 2 or 3comprising reacting a compound of formula II ##STR2## where R, R.sub.1 and n are defined above and where each R.sub.3, independently, is C.sub.1-12 alkoxy or one R.sub.3 is C.sub.1-12 alkoxy and the other R.sub.3 is halogen,with elemental sulphur in an alkaline medium, a metal sulphide or a metal hydrosulphide.Compounds of formula I and formula II are useful as photoinitiators.

Abstract: 3-N-methylcarbamoylthioxanthen-9-one 10,10-dioxide of formula (I) ##STR1## is an inhibitor of monoamine oxidase-A, and is therefore useful in the prophylaxis and treatment of certain mental disorders such as depression.

Abstract: The invention relates to novel thiopyrones, especially novel benzothiopyranones of the general formula ##STR1## in which R.sub.1 represents hydrogen or an aliphatic radical, n represents 0, 1 or 2, Ph represents substituted or unsubstituted 1,2-phenylene and A represents a group of the formula --NH--CO--R in which R represents carboxy or esterified carboxy, and to their salts, processes for the manufacture of compounds of the formula (I) and their salts, pharmaceutical preparations containing such compounds and to the use of compounds of the formula (I) and their salts as the active ingredients of medicaments and/or for the manufacture of pharmaceutical preparations. The compounds of the formula (I) and their salts have anti-allergic properties.

Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: m is an integer selected from 1 to 4;n is zero or an integer selected from 1 to 4;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH.sub.2).sub.p C(.dbd.A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino, the group --NHC(.dbd.B)NR.sup.7 R.sup.8 in which B is oxygen or sulfur and R.sup.7 and R.sup.8 are hydrogen or alkyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; andR.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl.

Abstract: Photoinitiators of the formulaG--O--(CH.sub.2 CH.sub.2 O).sub.n --CH.sub.2 --CH.sub.2 --O--Qwherein G is a photoinitiator moiety, R is hydrogen or lower alkyl, n has a value of at least 10, and Q is G or a lower alkyl are soluble in water and common organic solvents and are useful in polymerization systems employed in coatings used in screen printing.

Abstract: Novel xanthones and thioxanthones of the formula I ##STR1## in which A, X, Y, Z, E and E' are as defined in patent claim 1, are described. A is preferably --S-- and E and E' are preferably bonded in the ortho-position relative to one another. The compounds (I) are suitable, for example, as sensitizers for photocrosslinkable polymers or photocurable compositions, or for use in mixtures with polymers with H donor groups for image formation, in particular electrically conductive coatings and patterns, by means of electroless deposition of metals.

Abstract: 1,4-Aminoalkylamino-9H-thioxanthen-9-ones have antimicrobial activity and activity against leukemic cells. Methods for their preparation, use and pharmaceutical compositions are described.

Abstract: Certain 5-substituted chromones and thiochromones and pharmacologically acceptable salts thereof are disclosed. The compounds possess antiallergic properties and are represented by the formula: ##STR1## wherein: X is selected from the group consisting of --O--, --S--, and --SO.sub.2 --;R.sub.1 and R.sub.2 are each independently H or lower alkyl having from 1 to 4 carbon atoms or together with C.sub.2 and C.sub.3 from a cyclohexane ring having the structure: ##STR2## wherein R.sub.3 and R.sub.4 are each independently H or a lower alkyl having from 1 to 4 carbon atoms.Also taught are valuable intermediates useful in the preparation of said 5-substituted chromones and thiochromones represented by the formula: ##STR3## wherein B is selected from the group consisting of --NHCOC(CH.sub.3).sub.3, 1,3-oxazolinyl and --CONHR, wherein R is methyl, phenyl, or t-butyl; Y is selected from the group consisting of CO.sub.2 H, CHO, CO.sub.

Abstract: The novel thioxanthones of the formula I ##STR1## in which R.sub.1, R.sub.2, X and W are as defined in patent claim 1, are suitable, for example, for the preparation of photosensitive, compositions of matter which are capable of undergoing condensation or addition reactions and may or may not be crosslinkable, and which in turn are used for image formation, in particular by means of electroless deposition of metals. Such compositions of matter contain, for example, a thioxanthone of the formula I, an oligomer or polymer with terminal glycidyl groups and, where relevant, a crosslinking agent and/or a salt of a metal or group Ib or VIII of the Periodic Table.

Abstract: 7-Hydroxylucanthone and 7-hydroxyhycanthone derivatives have been found to have significant antitumor effect. The derivatives are of the general formula: ##STR1## wherein the radicals R.sup.1 and R.sup.2 are lower alkyl groups or other simple groups and R.sup.3 is OH where X.dbd.O, and H or OH where X.dbd.S.

Abstract: Thioxanthonecarboxylic acid esters, thioesters or amides of the formula I ##STR1## in which X and Z are hydrogen or one of the substituents defined in more detail in claim 1 and Y is --OR.sub.1, --SR.sub.1 or --N(R.sub.1)(R.sub.2), in which R.sub.1 is C.sub.1-24 alkyl and R.sub.2 is H or R.sub.1, are suitable, if desired together with amines, as initiators for the photopolymerization of ethylenically unsaturated compounds or for photochemical crosslinking of polyolefines. They are also used an sensitizers for photocrosslinkable polymers. They can be prepared by methods known per se, for example by cyclization of phenylthio-phthalic, -isophthalic or -terephthalic acids, which can be correspondingly substituted, and subsequent reaction with suitable alcohols, thiols or amines.

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: Compounds of the formula ##STR1## wherein A, X, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, n and m are defined hereinbelow are effective photoinitiators especially for the photopolymerization of ethylenically unsaturated compounds and for the curing of printing inks.

Abstract: A composition of the formula: ##STR1## wherein X is lower alkyl, and Z is an amino acid a peptide residue or a good leaving group, the composition is adaptable as a blocking or protecting group for an amine composition useful in peptide synthesis and a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.

Abstract: The invention provides novel thioxanthone photoinitiators having the formula: ##STR1## wherein R.sub.1 alkyl, alkoxy, alkylthio, halogeno, nitro, amino, alkyl-amino, di-alkyl-amino, hydroxy alkyl-amino, alkanoylamino, benzoylamino, N-alkanoyl-N-benzoyl-amino, sulphonamido, or acetyl, R.sub.2 is alkylene, A is --COOH, --SO.sub.3 H, --OSO.sub.3 H, or --O--CO--X--COOH (where X is such that HO--CO--X--COOH is a di- or tri-carboxylic acid of up to 8 carbon atoms), n is 0, 1, or 2 and m is 1 or 2, provided that when A is --COOH, m is 2, the aforesaid alkyl, alkoxy, alkanoyl, and alkylene residues containing up to 4 carbon atoms each, as the free acid or as a salt thereof. The photoinitiators may advantageously be used in water-based photopolymerizable compositions, e.g. for use in screen stencil production.

Abstract: The present invention relates to a dialkylthioxanthone compound of formula (I): ##STR1## wherein X and Y may be the same or different, and represent a straight-chain or branched alkyl group having 1-12 carbon atoms with a proviso that sum of carbon atoms of alkyl groups X and Y is in the range of 3-15; a process for producing said compound; a process for hardening a photopolymerizable resin compound having an ethylenically unsaturated double bond which is radically crosslinkable or polymerizable using the above compound; and a photopolymerizable resin composition containing the same.

Abstract: Novel heterobicyclic compounds of Formula I, processes for preparing same and pesticidal compositions and methods are described.