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 oxypyrone 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 method produces calcium fulvate from naturally-occurring humus material, such as leonardite, or humic shales. The humus material containing solid fulvic acid and solid humic acid is mixed with water and sodium hydroxide for a first selected period of time to form a solution having a pH of approximately 10.0 thereby solubilizing the fulvic acid and the humic acid. The pH of the solution is reduced to approximately 4.5 and is maintained at the approximately pH 4.5 for second selected period of time thereby precipitating the humic acid as a solid while the fulvic acid remains in solution. The fulvic acid solution is separated from the solid humic acid. The pH of the fulvic acid solution is increased to approximately 13 with calcium hydroxide thereby precipitating the solubilized fulvic acid as calcium fulvate.

Abstract: A method produces magnesium fulvate from naturally-occurring humus material, such as leonardite, or humic shales. The humus material containing solid fulvic acid and solid humic acid is mixed with water and sodium hydroxide for a first selected period of time to form a solution having a pH of approximately 10.0 thereby solubilizing the fulvic acid and the humic acid. The pH of the solution is reduced to approximately 4.5 and is maintained at the approximately pH 4.5 for second selected period of time thereby precipitating the humic acid as a solid while the fulvic acid remains in solution. The fulvic acid solution is separated from the solid humic acid. The pH of the fulvic acid solution is increased to approximately 13 with magnesium hydroxide thereby precipitating the solubilized fulvic acid as magnesium fulvate.

Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilatation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.

Abstract: Compounds of general Formula I in which the substituents of R.sub.1 -R.sub.7 are hydrogen, hydroxy group, C.sub.1-6 alkyl group, C.sub.1-6 alkoxy group, or epoxypropoxy, but at the most, six of the substituents can simultaneously be hydrogen, methoxy group, or hydroxy group, or epoxypropoxy group for activity against hepatoma. There are also described processes for the preparation of the novel compounds and useful intermediates. Substitute benzophenones are described.

Abstract: Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also disclosed are methods for the treatment of infectious diseases using such compounds.

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 removing aromatic heterocyclic compounds from a product-containing solution, in particular a protein solution, by bringing the solution into contact with a support material. The process is preferably carried out following a virus inactivation with acridine or acridine derivatives and makes it possible to remove these virus-inactivating agents from the solution without there being any significant product losses or changes in the biological activity of the solution.

Abstract: Methods for forming combinatorial libraries and the libraries produced thereby are provided. According to a preferred aspect of the invention, a plurality of core molecules are reacted with a plurality of different tool molecules to form a library of molecules having non-naturally occurring molecular diversity. The libraries are useful for identifying lead compounds which modulate the functional activity of a biological molecule. Protease inhibitors that have been isolated from the libraries also are disclosed.

Abstract: Compounds of general Formula I in which the substituents of R.sub.1 -R.sub.7 are hydrogen, hydroxy group, C.sub.1-6 alkyl group, C.sub.1-6 alkoxy group, or epoxypropoxy, but at the most, six of the substituents can simultaneously be hydrogen, methoxy group, or hydroxy group, or epoxypropoxy group for activity against hepatoma. There are also described processes for the preparation of the novel compounds and useful intermediates. Substitute benzophenones are described.

Abstract: Intermediates for fluorescent dyes based on 9-carboxyethyl-6-hydroxy-3-oxo-3H-xanthene which are useful as reporters for reporter-labeled DNA fragments are described. The intermediates are protected fluorescent dyes bearing acyloxy groups at the 3 and 9 positions and an alkoxy group at the 9 position. Deprotection of the protected fluorescent dye by treatment with aqueous ammonia regenerates free dye.

Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.

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 novel compounds 3,6-Disubstituted xanthen-9-one of formula I ##STR1## in which R is a C.sub.3 -C.sub.8 linear, branched or cyclic alkyl and R.sub.1 is linear, branched C.sub.1 -C.sub.8 alkyl or cyclic C.sub.3 -C.sub.8 alkyl or --OR in which R is as defined hereinabove, exhibit bone resorption inhibiting activity. Pharmaceutical compositions are described.

Abstract: A compound, and salts thereof, represented by either formula I or formula II below:(1) Formula I: ##STR1## wherein substituents R.sub.1 -R.sub.7 can be, independently, hydrogen, hydroxy group, C.sub.1-6 alkyl(oxy) group, acetyl ester, or C.sub.1-12 alkyl propanolamine; at least three but no more than four of the substituents are alkyl(oxy) group, hydroxyl group or acetyl ester; no more than one of the substituents can be C.sub.1-12 alkyl propanolamines; R.sub.1, R.sub.3, R.sub.7 cnnnot all be hydroxy groups at the same time; and R.sub.6 is either an hydroxy group or an oxygen-containing glucose.(2) Formula II: ##STR2## wherein substituents R.sub.1 -R.sub.9 can be, indenpendently, hydrogen, hydroxy group and C.sub.1-6 alkyl(oxy) group; and no more then four of the substituents can be methoxy group, hydroxy group, or acetyl ester. These compounds were tested to be capable of inhibiting platelet aggregation, atrioventricular conduction, and calcium influx in myocardiac cells.

Abstract: Novel compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moleties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms.The compounds are producible by aerobic cultivation on suitable nutrient media under suitable conditions of a strain of the fungus Ascochyta sp., subsequent recovery of the active component from the fermentation medium, and optionally modifying the active compound to obtain a compound of the desired formula I.Disclosed is also microorganisms capable of producing said compounds, compositions containing said compounds, and the use of such compositions for controlling fungi in valuable crops, animals, including birds and mammals, and in the preservation of wood, paints and edible products.

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: 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: The novel class of xanthenone-4-acetic acids represented by the general formula (I) ##STR1## where R.sub.1 represents up to two of the groups lower alkyl, halogen, CF.sub.3, CN, NO.sub.2, NH.sub.2, CH.sub.2 COOH, OR.sub.2, OH, NHCOR.sub.2, NHSO.sub.2 R.sub.2, SR.sub.2, SO.sub.2 R.sub.2, CH.sub.2 CONHR.sub.2 or NHR.sub.2 (where R.sub.2 is lower alkyl optionally substituted with hydroxy, amino or methoxy functions), at any of the positions 1-8 which are available, R.sub.1 may also represent the substitution of an aza (--N.dbd.) group for one or two of the methine (--CH.dbd.) groups in the carbocyclic rings and two of R.sub.1 on any two available adjacent positions may also represent the grouping --CH.dbd.CH--CH.dbd.CH-- to form an additional fused benzene ring;and basic addition salts thereof, possess antitumour and antibacterial properties.

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: According to the present invention, there is provided a non-linear optical device comprising a non-linear optical medium comprising an organic compound, which remarkably improves the non-linear optical properties. The non-linear optical device according to the present invention is suited for the second and third harmonic generations, photomixing optical parametric oscillations, optical switches and optical bistable devices.

Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.

Abstract: The xanthosulfonamido and benzensulfonamido derivatives corresponding to the formula: ##STR1## wherein x represents hydrogen, alkyl, alkoxy or halogen, Y represents an alkyl, alkoxy or halogen and Z represents the group ##STR2## or Y and Z taken together form the group: ##STR3## wherein R.sub.1 in turn is a group selected among electron attracting groups, halogens and the group: ##STR4## itself, possess activity in inhibiting the aldose-reductase enzyme system and are thus useful in the treatment of the complications, at the eye and peripheral neuropathy levels, as induced by diabetes.

Abstract: Novel flavone carboxylic acid derivatives, intermediates therefor, and method for the preparation thereof, and their use in the differentiation of certain types of malignant cells, are all disclosed, certain of the novel compounds disclosed to be superior to retinoic acid in their activity.

Abstract: Xanthone derivatives of the formula (I): ##STR1## wherein W, X, Y and Z which may be the same or different represent a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; A is a hydrogen atom B is a hydroxymethyl group, a lower alkoxycarbonyl group having 1 to 4 carbon atoms, or a carboxyl group, provided that a --O--CH.sub.2 --B group is bonded to the 2- or 3-position of the xanthone ring and that there is no case in which X, Y, and Z are each a hydrogen atom concurrently; as well as intoxic salts thereof when B is a carboxyl group, and a process for preparing the same are disclosed.The compounds of formula (I) in accordance with the present invention are useful as diuretics having uricosuric activity and can be used in the treatment of edema or hypertension.

Abstract: Xanthone derivatives of the formula (I): ##STR1## (wherein W, X, Y and Z which may be the same or different represent a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; A is hydrogen atom or together with Z forms a --CH.sub.2 -- group which binds to a phenyl carbon adjacent the phenyl carbon to which the oxygen of the group ##STR2## is attached to form a cyclic methylene chain; B is a hydroxymethyl group, a lower alkoxycarbonyl group having 1 to 4 carbon atoms, or a carboxyl group, provided that W is neither a hydrogen atom nor a 7-position methyl group when X, Y and Z are each a hydrogen atom, and A is a hydrogen atom and B is a carboxyl group or a lower alkoxycarbonyl group), as well as non-toxic salts thereof when B is a carboxyl group, and a process for preparing the same are disclosed.The compounds of formula (I) in accordance with the present invention are useful as diuretics having uricosuric activity and can be used in the treatment of edema or hypertension.

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: 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: 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: UV stable linear polyesters, e.g. PET, contain in their chain copolymerized bis(hydroxyalkoxy)xanth-9-ones, preferably 3,6-bis-(2-hydroxyethoxy)xanth-9-ones. The polymers are obtained by polymerization in the presence of a tetrahydroxy benzophenone, preferably the 2,240 ,4,4'-isomer. The method of polymerizing in the presence of dihydric phenols to obtain ethoxyaryloxy polyesters is also described.