Abstract: High-voltage insulators are disclosed that are capable of handling diverse requirements, such as providing high standoff voltages, high temperature cycling, and the ability to withstand flexural stress. One high-voltage insulator includes a first piece formed from a first material, a second piece formed from a second material, and an interface section where the first piece contacts with and forms a seal with the second piece. The interface includes a first groove located that accommodates a first gasket, sets of matching threads on the first and second pieces. The interface section further accommodates a second gasket. In this multi-piece high-voltage insulator, the first material can have a first set of flexural, heat resistance, and electrical standoff characteristics suitable for a first environment, and the second material can have a second set of flexural, heat resistance and electrical standoff characteristics suitable for a second environment.

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The invention relates to pharmacology and can be used for treating liver diseases of various etiologies, inter alia, in combination with other preparations. Claimed is a drug with hepatoprotective activity comprised of 3-(4-bromophenyl)-6,6-dihydroxy-5-hydroxyiminohexahydro-2,4-pyrimidinedione and salts thereof of general formula (I), where X is selected from the group: H, Na, K, or from the group of hydroxyalkylammonia derivatives of general formula (II), where R1, R2 are selected from the group: H, CH3, CH2CH3, CH2CH2OH; R3 is selected from the group: H, CH2OH; and n=1, 2; the drug can be prepared in the form of tablets or capsules for enteral administration; or in the form of a liquid or lyophilized substance for parenteral administration; or in the form of rectal suppositories; or in the form of capsules or tablets, or sweets for sucking; and may additionally contain the hepatoprotector Heptral; or the hepatoprotector Essentiale; or the hepatoprotector ursodeoxycholic acid.

Abstract: Process for preparing 4,6-bis(aryloxy)pyrimidine derivatives. A process is provided for preparing 4,6-bis(aryloxy)pyrimidine derivatives. The process is conducted in water as reaction medium and catalyzed by one or more tertiary-amine catalyst(s). It has been found that a water based reaction substantially free of organic solvents can be carried out providing excellent yields by the addition of one or more tertiary-amine catalysts to the reaction medium. This provides a clean reaction and produces the desired product in high yields.

Abstract: The present invention relates to methods of inhibiting shikimate pathway, comprising administering to a subject a pharmaceutically acceptable composition comprising a compound having a formula: or pharmaceutically acceptable salts thereof.

Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.

Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.

Abstract: A protective film of polarizer comprising an organic acid that has a solubility in water at 25° C. of at most 0.1% by mass and has an acid dissociation constant in a mixed solvent of tetrahydrofuran/water=6/4 by volume at 25° C. of from 2 to 7 can improve polarizer durability.

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.

Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The invention is directed to methods and compositions for inhibiting caspase-independent apoptosis. In particular, methods and compositions for inhibiting Omi/HtrA2 activity, as well as method for identifying other inhibitors of Omi/HtrA2. Also disclosed are Omi/HtrA2 specific substrates and methods for identifying other substrates of Omi/HtrA2.

Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.

Abstract: The present invention relates to the identification of inventive pyrimidine-2,4,6-triones (PYT compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the inventive PYT compounds.

Abstract: An exchange membrane containing modified maleimide oligomers comprising sulfonated poly(aryl ether ketone) (S-PAEK) and modified maleimide oligomers. The exchange membrane uses the modified maleimide oligomers having a hyper-branched architecture as matrix, and introduces them into S-PAEK to constitute semi-interpenetration network (semi-IPN), so as to intensify water holding capacity, chemical resistance, the electrochemical stability and thermal resistance of the ionic/proton exchange membrane. The exchange membrane can be used to fabricate the membrane electrode assemblies, fuel cells, and be applied them to the fields of seawater desalination, heavy water and sewage treatment, and biomass-energy resources.

Abstract: Tissue solubilizing compositions are provided. The compositions comprise 3-(decyl dimethyl ammonio) propane sulfonate and polyethylene glycol dodecyl ether, such as tetraethylene glycol dodecyl ether. The compositions may be useful to solubilize tissue, including skin, mucosal membrane, and other tissue. The compositions may be further useful to preserve and recover analytes contained within the solubilized skin, mucosal membrane, and other tissue.

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract: The invention is directed to methods and compositions for inhibiting caspase-independent apoptosis. In particular, methods and compositions for inhibiting Omi/HtrA2 activity, as well as method for identifying other inhibitors of Omi/HtrA2. Also disclosed are Omi/HtrA2 specific substrates and methods for identifying other substrates of Omi/HtrA2.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

Abstract: The present invention relates to compositions and methods for targeting c-Rel. In particular, the present invention provides compositions and methods for treating cancers, inflammatory diseases, autoimmune diseases, and transplant rejection by inhibiting c-Rel activity and for regulating c-Rel for research and drug screening applications.

Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.

Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.

Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).

Abstract: The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.

Abstract: An exchange membrane containing modified maleimide oligomers comprising sulfonated poly(aryl ether ketone) (S-PAEK) and modified maleimide oligomers. The exchange membrane uses the modified maleimide oligomers having a hyper-branched architecture as matrix, and introduces them into S-PAEK to constitute semi-interpenetration network (semi-IPN), so as to intensify water holding capacity, chemical resistance, the electrochemical stability and thermal resistance of the ionic/proton exchange membrane. The exchange membrane can be used to fabricate the membrane electrode assemblies, fuel cells, and be applied them to the fields of seawater desalination, heavy water and sewage treatment, and biomass-energy resources.

Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

Abstract: The present invention provides a novel process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid. In particular, the present invention provides a process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid by reacting 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid with a Lewis acid to selectively remove one methoxymethyl group from 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid.

Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the specification. The invention also provides related pharmaceutical compositions, methods of use, and combinations.

Abstract: The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione; metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, W, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

Abstract: N-substituted derivatives of 5-oximinobarbituric add of the general formula where X is sulfur; R1 is selected from the group consisting of saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl; and R2 is selected from the group consisting of hydrogen, saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl possessing a biological activity.

Abstract: The present invention provides a novel process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid. In particular, the present invention provides a process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid by reacting 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid with a Lewis acid to selectively remove one methoxymethyl group from 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid.

Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Abstract: The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the specific deprotection of any substituent ono the saccharide ring, and greatly facilitates targeted or library-focused carbohydrate-related syntheses. In particular, the invention provides a universal monosaccharide building block of General Formula (I) or General Formula (II) in which A is a leaving group; X is hydrogen, O, N or N3; X1 is hydrogen, —CH2O—, —CH2NH—, —CH3, —CH2N3 or —COO—; and B, C, D and E are protecting groups that can be cleaved orthogonally, and in which B, C, D and E are absent when X is hydrogen or N3, and E is absent when X1 is hydrogen, CH3 or N3.

Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, W, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydr

Abstract: This invention relates to compounds of formula (I)

Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.

Abstract: Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.

Abstract: This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups that are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis.

Abstract: The invention provides a system for solid-phase synthesis of oligosaccharides, based on the discovery that a 2-substituted-1,3-dioxocycloalkyl linker group of general formula (I) can be used to couple saccharide groups of both the O-glycoside and N-glycoside type to a polymer support. The invention provides reagents, reagent kits and methods for solid-phase oligosaccharide synthesis.

Abstract: Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds, which have specific substituents and are useful in diazo thermal recording materials; and diazo thermal recording materials containing the barbituric acid derivative.

Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.

Abstract: A colored dispersion comprising a polymer and a dye represented by General Formula (1):

Abstract: Method of producing thiobarbituric acid derivatives of formula I wherein R1 is SH, S−M+ or CH3S—, and M+ is an alkali metal ion, by hydrogenolysis of a compound of formula II wherein R2 is chlorine or CH3O—, with a) a hydrogenolysis agent in the presence of an inert solvent and by a direct reaction of the hydrogenolysis product with an alkali metal methylate in methanol, or b) with a hydrogenolysis agent in the presence of an inert solvent and in the presence of a methylation reagent, and subsequently with an alkali metal methylate in methanol, as well as the use of these compound of formula I in the production of 7-[(4,6-dimethoxy-pyrimidin-2-yl)thio]-3-methylphthalide.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.