Abstract: A compound of formula I wherein A is a moiety which provides UV absorbing activity to the compound of formula I that comprises 1 divalent group or 2 monovalent groups, with at least one group having carbonyl (C═O) functionality, and each R is independently linear or branched C1-C8 alkyl. Sunscreen formulations which contain these compounds and methods using these compounds to prepare formulations are also provided.

Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.

Abstract: Benzoylcyclohexanedione derivatives of the formula (I) and their use as herbicides are described.

Abstract: A method for the production of substituted aromatic aldehydes or ketones and optionally substituted heteroaromatic aldehydes or ketones of formula (I) by reacting a compound of formula (II) in a suitable solvent in the presence of a carbonyl compound of formula (III), optionally in the presence of oxygen at a normal pressure or high temperature and at temperatures of 5-200° C.

Abstract: A compound of formula (I), wherein &agr;X is ═O, ═N—OR6, &bgr;NHR or &bgr;OH wherein R6 is H or C1-C6 alkyl, bond a is oriented &ggr; or &dgr; and R is H, C1-C6 alkyl which is unsubstituted or substituted by C6-C10 aryl, or C3-C6 cycloalkyl; &egr; is a bond when &zgr; and &eegr; are not bonds or, when X is ═O, &zgr; and &eegr; are both bonds and &egr; is not a bond; R1 and R2, which are the same or different, are H or a halogen; R3 and R4, which are the same or different, are H, C1-C6 alkyl, C3-C6 cycloalkyl, a heterocyclic group or an aromatic group; bond e is oriented &ggr; or &dgr;; and R5 is C1-C6 alkyl; or formula (Ib), or formula (II), or formula (III), has activity as a cytokine production inhibitor and an inhibitor and an inhibitor of tyrosine kinase.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: Pharmaceutically active compounds are prepared as described and used to produce pharmaceutical preparations for treating diseases.

Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: New compounds of formula I are described: 1

Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: A process for the preparation of an allylic aromatic compound in which an aromatic amine is reacted first with a nitrite and then with an allylic olefin having an eliminatable terminal substituent. Novel allylic derivatives of disubstituted benzene compounds are also described.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: The present invention has its objects to provide a method for reducing &agr;-aminoketone derivatives under mild conditions with high stereoselectivity.

Abstract: A method for treating cancer comprising administering a 1,3,4,6-tetrahydroxy-helianthrone derivative. The compounds can be used in the absence of light irradiation or for photodynamic therapy of solid tumors wherein the tumor site is subjected to light irradiation after administration of the active ingredient. A preferred compound is 10,13-dimethyl-1,3,4,6-tetrahydroxy-helianthrone.

Abstract: A novel process for the preparation of compounds of formula I by aminolysis of a p-halophenyl alkyl ketone of formula II with a cyclic amine of formula III in water at a temperature of at least 130° C., in which formulae X is a halogen atom and R1, R2 and R3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.

Abstract: Iodopropargylamine compound of the general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 combine with each other to form a tetramethylene group or a pentamethylene group, R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, and X and Y each independently represent a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a phenylcarbonyl group or a phenylsulfonyl group, provided that the phenyl group of a phenylcarbonyl group or a phenylsulfonyl group may be optionally substituted by halogen atoms, alkyl groups having 1 to 3 carbon atoms, alkoxy groups having 1 to 3 carbon atoms, nitro groups or trifluoromethyl groups.

Abstract: The present invention provides a method of purifying an aqueous dye solution having an aldehyde and/or ketone impurity including a step of reacting the impurity with a hydrazine derivative, forming a water-insoluble hydrazone compound. The hydrazone compound is then removed from the solution to form a dye having an increased purity.

Abstract: The invention is based on new methods for making and using compounds and arrays of novel .alpha.-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 .alpha.-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutic agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.

Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.

Abstract: The preparation of aromatic ketones substituted with a thioether group at the ortho position is accomplished by the initial reaction of an aromatic nucleus substituted with a halide and an ortho nitro group with a nitroalkane in the presence of a hydroxide base. The resulting ortho-nitroalkyl nitroarene compound is converted to the corresponding ortho-nitroaryl ketone by an oxidative Nef reaction. The aromatic nitro group of the ortho-nitroaryl ketone is replaced with a thioether group by reaction with a thiolate anion, most preferably under phase-transfer conditions. Aromatic ketones may be used to prepare various pharmaceutical and herbicidal compounds.

Abstract: A process for recovering a 1,1,1,5,5,5-hexafluoro-2,4-pentanedione ligand from a metal-ligand complex byproduct such as Cu.sup.+2 (1,1,1,5,5,5-hexafluoro-2,4-pentanedionate.sup.-1).sub.2, comprising: providing a copper-ligand complex byproduct of Cu.sup.+2 (1,1,1,5,5,5-hexafluoro-2,4-pentanedionate.sup.-1).sub.2 in a process stream; cooling and condensing the copper-ligand complex byproduct of Cu.sup.+2 (1,1,1,5,5,5-hexafluoro-2,4-pentanedionate.sup.-1).sub.2 to separate it from the process stream; contacting the copper-ligand complex byproduct of Cu.sup.+2 (1,1,1,5,5,5-hexafluoro-2,4-pentanedionate.sup.-1).sub.2 with a protonation agent, such as: sulfuric acid, hydrochloric acid, hydroiodic acid, hydrobromic acid, trifluoroacetic acid, trifluoromethanesulfonic acid, acid ion exchange resin, hydrogen sulfide, water vapor and mixtures thereof; and recovering 1,1,1,5,5,5-hexafluoro-2,4-pentanedione.

Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Abstract: 2-Amino-4,5,3',4'-tetramethoxybenzophenone of the formula: ##STR1## is prepared by mononitration of 3,3',4,4'-tetramethyoxybenzophenone using nitric acid in the presence of acetic acid, and subsequent reduction of the nitro group. The compound is an intermediate in the synthesis of active ingredients against rheumatoid arthritis.

Abstract: The present invention features biarsenical molecules. Target sequences that specifically react with the biarsenical molecules are also included. The present invention also features kits that include biarsenical molecules and target sequences. Tetraarsenical molecules are also featured in the invention.

Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.

Abstract: Stereospecific synthesis of the racemic threo isomers of 2-nitro-1-phenylpropanols by reacting a benzaldehyde derivative with nitroalkane in the presence of a tertiary amine and reducing 2-nitro-1-phenylpropanols with, for example, lithium aluminum hydride to 2-amino-1-phenylpropanols is described. Also described are phase transfer resolution of racemic mixtures of 2-amino-1-phenylpropanol and its derivatives into their optically pure isomers by reacting a racemic mixture with the mono alkali metal salt of a tartaric acid ester in a two phase system of a hydrocarbon and water. The specification further describes therapeutically useful optically pure isomers of threo-2-amino-1-(dialkoxy or alkoxy) phenylpropanols and acid addition salts thereof.

Abstract: A process for the nitration of an aromatic or heteroaromatic compound with a nitrating agent comprising nitric acid or a mixture of nitric and sulphuric acids, characterised in that nitration is performed in a solvent comprising at least 50% v/v of a C.sub.1 -C.sub.6 alkyl ester of a C.sub.1 -C.sub.4 carboxylic acid. The process is of particular use for the nitration of diphenyl ethers to give compounds which are useful as herbicides or as intermediates in the synthesis of herbicides.

Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

Abstract: Processes for efficiently producing .alpha.-halo ketones, .alpha.-halohydrins and epoxides on an industrial scale. The prosesses include one for producing an .alpha.-halo ketone of general formula (3) by decarboxylating a product of reaction between a carboxilic acid derivative of general formula (1) and a metal enolate prepared from an .alpha.-haloacetic acid of general formula (2) or an acceptable salt thereof, one for producing an by reducing the .alpha.-halo ketone (3), and one for producing an epoxide (13) by treating the .alpha.-halohydrin (11) with a base to effect ring closure. The above prosesses are particularly suitable for producing optically active .alpha.-halo ketones, .alpha.-halohydrins and epoxides from the corresponding .alpha.-amino acid derivatives.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: The invention provided methods and compositions for oligonucleotide synthesis and labeling. The subject compounds have either rigid ring or long linear linker structures and provide enhanced coupling efficiencies over prior art labeling reagents because of lack of stereo hindering and/or provide more convenient and cost-effective syntheses. These novel linkers also contain a base labile structure which provides: labeling at 3' end with regular solid supports, cleaving under mild conditions, and achieving higher yield because of the complete cleavage and higher purity because the mild conditions will not bring down the impurities on the solid support. When used in a solid support pre-attached with either a nucleotide for unlabeled oligonucleotide synthesis, or a label for 3' end labeled oligonucleotide synthesis, or an alternate structure to use as an universal support, these linkers provide solid supports requiring only mild cleavage conditions.

Abstract: A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a temperature of at least 130.degree. C., in which formulae X is a halogen atom and R.sub.1, R.sub.2 and R.sub.3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.

Abstract: A fullerene derivative of the formula I ##STR1## where the symbols and indices have the following meanings: F is a fullerene radical of the formula (C.sub.20+2m), where m is a number from 1 to 50R.sup.1 to R.sup.8 are identical or different and are each H, CO.sub.2 R.sup.9, CN, COR.sup.10, Cl, Br, I, F, OR.sup.11, C.sub.1 -C.sub.20 -alkyl, phenyl or H, R.sup.1 -R.sup.4 and/or R.sup.5, R.sup.7 can also be part of a cycloalipathic, cycloaromatic or cycloheteroaromatic system which in turn is substituted by C.sub.1 -C.sub.20 -alkyl, aryl, carboxyl, carbonyl, alkoxy, aryloxy, halogen, nitro, alcohol or amine, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, R.sup.3 and R.sup.4 can together be ##STR2## where R.sup.15 -R.sup.18 are each H, C.sub.1 -C.sub.20 -alkyl, F, Cl, Br, I or phenyl, andAR is the radical of a fused cyclo-aromatic system, and n is from 1 to 20 and a process for its preparation.

Abstract: 3-Chloro-3'-nitro-4'-methoxybenzophenone with substantially lower contents of dinitro derivatives than hitherto is obtained if 3-chloro-4'-methoxybenzophenone is nitrated in from 65 to 85% strength by weight sulfuric acid with nitric acid at temperatures in the range from -20.degree. to +60.degree. C.

Abstract: The invention relates to polyhydric phenol compounds of the general formula ##STR1## wherein R is a hydrogen atom or a saccharide moiety;A and B are hydrogen atoms or form together a C--C bond;R.sub.1 is a hydroxy group and R.sub.2 is a hydrogen atom, orR.sub.1 and R.sub.2 form together an oxygen atom;Z is a hydroxy group, an amino group, a carboxy group or a N-(carboxymethyl)carbamoyl group;X* is a radioactive halogen isotope; andm and n are 0 or 1, with the proviso, that m is 1 if n is 0, and that m is 0 if n is 1.The radiolabelled phenol compounds can be used for diagnosis and therapy.

Abstract: This invention relates to a novel thermoplastic and amorphous polyimide which is readily soluble in organic solvent, a novel aromatic diamino compound used for the polyimide, a preparation process thereof, a polyimide-based resin composition comprising the thermoplastic polyimide and a fibrous reinforcement, a process for preparing the resin composition, an injection molded article of the resin composition, a polyimide-based composite obtained by molding the above soluble and thermoplastic polyimide in combination with a fibrous reinforcement, and a fibrous reinforcement having a surface modified with the above polyimide.

Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.

Abstract: Disclosed are bis-meta-benzotrifluoride compounds having the general formula ##STR1## where each A is independently selected from the group consisting of NO.sub.2, NH.sub.2, and NH.sub.3.sup.+ Z.sup.-, Z.sup.- is an anion and B is selected from the group consisting of O, CO, S, SO, and SO.sub.2. The diamine compounds are useful as monomers in making polyimides, polyamide-imides, and polyamides.

Abstract: A particularly advantageous process for the preparation of 2,2-dialkyl-arylidene-cycloalkanones is characterized in that 2-alkyl-arylidene-cycloalkanones are reacted with alkyl halides in the presence of metal hydroxides and tertiary alcohols.

Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.

Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.

Abstract: Compounds of the formula ##STR1## having retinoid like biological activity.

Abstract: Fluorinated benzils and a process for their preparation A process for the preparation of fluorinated benzils of the formula (1) ##STR1## in which X.sub.1 -X.sub.6, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen, fluorine, chlorine or bromine atoms, or alkyl(C.sub.1 -C.sub.10), phenyl or naphthyl groups which may be substituted, or are groups reducing the electron density, at least one of the substituents X.sub.1 -X.sub.6 being a fluorine atom, by reacting 1 mol of a benzil of the formula (1), in which X.sub.1 -X.sub.6 and R.sub.1 and R.sub.2 have the abovementioned meanings, with the proviso that at least one of the substituents X.sub.1 -X.sub.6 is a chlorine atom, with about 0.8 to about 2.5 mol of potassium fluoride, rubidium fluoride, cesium fluoride or tetraalkyl (C.sub.1 -C.sub.18)-ammonium fluoride per chlorine atom to be exchanged, at temperatures of from about 100.degree. C. to about 280.degree. C.

Abstract: The present invention is to provide phenethyl alcohol derivative represented by the general formula (I), which is a stabilizing agent for colored images, particularly improved in resistance to plasticizers for the use in recording materials. ##STR1## (wherein Y: formula (II) or formula (III) R.sup.1 : H, alkyl, aralkylR.sup.2, R.sup.3 and R.sup.4 : halogen, nitro, alkyl, alkoxy, alkenyl, alkenyloxy,R.sup.5, R.sup.6 and R.sup.7 : H, alkyl,Z: --SO.sub.2 --, --CO--, --C(CH.sub.3).sub.

Abstract: There is provided o-nitrophenyl cyclopropyl ketone, a key intermediate in the manufacture of the crop-selective, herbicidal agent 1-{[o-(cyclopropylcarbonyl)phenyl]sulfamoyl}-3-(4,6-dimethoxy-2-pyrimidiny l)urea and a method for the preparation of said ketone from dihydro-3-acetyl-2(3H)-furanone and o-nitrobenzoyl halide.

Abstract: The present invention provides a method for the preparation of a 4-halo-2'-nitrobutyrophenone compound having the structural formula I ##STR1## The formula I compound is an important intermediate in the manufacture of a sulfamoyl urea herbicidal agent.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.