Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed

Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.

Abstract: The present invention relates to the use of a novel class of cancer stem cell pathway (CSCP) inhibitors; to methods of using such compounds to treat refractory, recurrent, or metastatic cancers; to methods of selective killing cancer cells by using such compounds with specific administration regimen; to methods of targeting cancer stem cells by inhibiting Stat3 pathway; to methods of using novel compounds in the treatment of conditions or disorders in a mammal related to aberrant Stat3 pathway activity; and to processes for preparing such compounds and intermediates thereof, and to the pharmaceutical composition of relevant compounds, and to the specific methods of administration of these compounds.

Abstract: Use of a phosphorus compound of the formula (I) as flame retardant, where the definitions of the symbols in the formula (I) are as follows: A is one of the following groups: Y is —P(?X2)SR3R4, H, a straight-chain or branched C1-C12-alkyl group, C5-C6-cycloalkyl, C6-C12-aryl, or benzyl, where the four last-mentioned groups are unsubstituted or have substitution by one or more radicals from the group of C1-C4-alkyl or C1-C4-alkenyl; R1, R2, R3, and R4 are identical or different and are hydrogen, OH, C1-C16-alkyl, C1-C16-alkenyl, C1-C16-alkoxy, C1-C16-alkenoxy, C3-C10-cycloalkyl, C3-C10-cycloalkoxy, C6-C10-aryl, C6-C10-aryloxy, C6-C10-aryl-C1-C16-alkyl, C6-C10-aryl-C1-C16-alkoxy, SR9 COR10, COOR11, CONR12R13 or two radicals R1, R2, R3, or R4 form, together with the phosphorus atom to which they are bonded, or the P—O-A-O—P group, a ring system; R5, R6, R7, and R8 are identical or different and are H, C1-C16-alkyl, C1-C16-alkenyl, C1-C16-alkoxy, C1-C16-alkenoxy; R9, R10, R11, R12, R13 are identical or

Abstract: The invention relates to novel caged ceramide 1-phosphate (C1P) and the method of using them for delivering C1P intracellularly in vitro and in vivo, for research and therapeutic purposes.

Abstract: The present inventions provides crystalline forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-(1-{4-[(diethoxyphosphoryl)methoxy]phenyl}-3-hydroxy-4-[4-methoxy-N-(2-methylpropyl)benzenesulfonamido]butan-2-yl)carbamate, methods of preparing the crystalline forms, pharmaceutical compositions containing the crystalline forms, and therapeutic uses thereof.

Abstract: Compositions for use in lubricating thin film storage media are provided, as well as storage media formed using the compositions, the compositions including one or more central cores having a cyclic group, and a plurality of arms extending from the central cores, wherein each arm comprises phenol or piperonyl. Methods of preparing the compositions are also provided. Methods of preparing storage media that incorporate the compositions therein are further provided.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

Abstract: An optically active compound represented by the following formula (5): wherein, in the formula (5), R1 and R2 may be the same or different are an alkyl group optionally having a substituent group selected from the group consisting of an alkoxy group and a halogen atom, a cycloalkyl group optionally having a substituent group selected from the group consisting of an alkoxy group and a halogen atom, an aryl group optionally having a substituent group selected from the group consisting of an alkyl group, an alkoxy group and a halogen atom, an alkoxy group optionally having a substituent group selected from the group consisting of a halogen atom and an aryl group or an aryloxy group optionally having a substituent group selected from the group consisting of an alkyl group, an alkoxy group and a halogen atom; a1 and a2 independently are 0 or 1; and * is axial asymmetry.

Abstract: A method for preventing, reducing, ameliorating or treating ophthalmic disorders associated with neurodegenerative diseases or trauma, comprising the topical, periocular, or intraocular application of an ophthalmic formulation comprising a therapeutically effective amount of one or more ophthalmic agents selected from the group consisting of alpha-tocotrienol, beta-tocotrienol, gamma-tocotrienol, delta-tocotrienol, or esters or mixtures thereof is disclosed. Use of tocotrienols for the prevention, reduction, amelioration or treatment of ophthalmic disorders that are, or that are associated with, mitochondrial diseases is also discussed. Topical ophthalmic formulations comprising tocotrienols are also discussed.

Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.

Abstract: A compound of formula (I) is described; wherein the substituents are as defined in the text and wherein the compound is intended for use in the production of a vascular damaging effect in a warm-blooded animal.

Abstract: Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.

Abstract: There is provided an emulsion composition for therapeutic administration comprising: (a) at least one mono-(electron transfer agent) phosphate derivative; (b) at least one di-electron transfer agent phosphate derivative; wherein the amount of transfer agent phosphate derivatives is no less than equimolar to the amount of di-electron transfer agent phosphate; and (c) a suitable carrier.

Abstract: The present invention provides amide-substituted xanthene fluorescent dyes and reagent for the introduction of phosphonate or sulfo groups into the fluorescent dyes.

Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.

Abstract: The present invention relates to a use of a cyclic imidate as a ligand for catalysis in which the ligand contains sub-structure (Y) as a minimal structural motive, wherein the carbon atoms and the nitrogen atom can be optionally substituted by a chemical substituent.

Abstract: Compositions and methods are directed to covalent adducts between reducing agents and optionally substituted 3-hydroxyflavans, wherein the reducing agent is covalently bound to the B-ring of the 3-hydroxyflavan. Such adducts exhibit markedly increased stability towards oxidation as compared to the unmodified 3-hydroxyflavan. Particularly preferred 3-hydroxyflavans include green tea catechins, and especially EGCG, while especially preferred reducing agents include NAC and glutathione.

Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.

Abstract: A phosphine ligand suitable for use in telomerizing butadiene comprises two phenyl groups and a xanthene moiety.

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

Abstract: The present invention provides rhodamine lactone phosphoramidites and polymer compositions, methods for making these phosphoramidites and polymer compositions, and methods for using these phosphoramidites and polymer compositions for labeling oligonucleotides. In particular, the present invention provides compositions and methods for labeling the 3?- and 5?-end of oligonucleotides during synthesis of the oligonucleotides.

Abstract: Described herein are substrates composed of a base coated with a fluorophore-labeled calcium phosphate coating. The substrates are useful in culturing and studying the activity of a variety of cells. The substrates described herein can be used for both solution- and image-based analysis of cultured cells. New methods for producing and using such coated substrates are also disclosed.

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: This invention relates to novel hydroxyethylamino sulfonamides and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.

Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.

Abstract: In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions. Also provided are a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement agent I.

Abstract: Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same.

Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).

Abstract: [Problem to be Solved] To provide an axially asymmetric optically active biarylphosphorus compound that can easily produced without the step of optical resolution which was almost indispensable in conventional methods. [Means for Solving the Problems] A method for producing an axially asymmetric phosphorus compound represented by the general formula (1), comprising a cycloaddition reaction of a compound having a triple bond with the use of a catalyst containing rhodium metal and an optically active bisphosphine. (In the formula (1), R1 and R2 may be the same or different and independently are an alkyl group optionally having a substituent group, a cycloalkyl group optionally having a substituent group, an aryl group optionally having a substituent group, an alkoxy group optionally having a substituent group or an aryloxy group optionally having a substituent group; * is axial asymmetry.

Abstract: The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

Abstract: Embodiments of the invention relate to natural and synthetic inositolphospholipid (IPL) materials, their preparation and applications. They provide compositions of the parent IPL comprising phosphatidylinositol (PI), PI-phosphates (phosphoinositides) and derivatives and analogues, and a process for their production starting from natural IPL. The embodiments further provide functional derivatives of PI for biomedical applications including a platform for drug design and delivery to therapeutic targets in the phosphoinositide mediated cellular signaling and allied cascades. The embodiments pertain to IPL having absolute stereo-structure. The embodiments further pertain to unique IPL and PI product compositions for defined applications, particularly pharmaceutical compositions for prophylaxis and treatment of diseases related to aberrant cellular and nuclear signaling mediated by PI and PI derived phosphates, and associated phosphoinositide specific enzymes including PI-PLC and PI 3-kinase.

Abstract: The present invention relates to novel compounds which are capable as acting as fluorescent sensors or which are precursors for these and for the use of these for the assay of biological processes such as posttranslational modifications of biological molecules such as phosphorylation, de-phosphorylation, proteolytic cleavage, phosphodiesterase mediated hydrolysis of cyclic nucleotides, methylation, acetylation of proteins peptides, DNA, lipids and the detection of biomolecule interactions (e.g., protein-protein interactions). A small molecule sensor is described which can associate to phosphorylated biological targets via metal ion—phosphate association. The association event can be monitored as fluorescence quench, sensitized emission, fluorescence polarization or a combination thereof.

Abstract: The invention concerns novel 1,2-dioxetane derivatives of general formula (I) as defined in the description, capable of emitting a detectable luminescent signal, their use in a method for detecting and/or quantizing a physical, chemical or biological, in particular enzymatic, phenomenon, as well as a kit for implementing said method.

Abstract: A specific culture medium for growth, detection, identification and/or counting of Staphylococcus aureus bacteria, said medium includes at least one fluorogenic, chromogenic or luminescent substrate of phospholipase C. Said medium permits differentiation between Staphylococcus aureus and coagulase-negative staphylococci.

Abstract: The disclosure provides novel trioxane sulfur dimers having Formula I: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer, proliferative disorders, and/or malaria using these compounds and/or compositions.

Abstract: Compounds of the formula (I), in the form of mixtures comprising predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1 (I) in which Z1 is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals, or Z1 is the —P*R0R1 group; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group Z1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*R0R1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally i

Abstract: The present invention relates to a sesamol derivative or its salt, and a skin external composition containing the same. More particularly, the invention relates to a sesamol derivative or its salt, which consists of sesamol and 3-aminopropane phosphoric acid, linked with each other by a phosphoric acid diester bond, and can be degraded into sesamol and 3-aminopropane phosphoric acid by enzymes present on the skin so as to simultaneously show the physiological activities of sesamol and 3-aminopropane phosphoric acid, as well as a preparation method thereof and a skin external composition containing the same.

Abstract: Autotaxin (ATX) is a prometastatic enzyme initially isolated from the conditioned media of human melanoma cells that stimulates a myriad of biological activities including angiogenesis and the promotion of cell growth, survival, and differentiation through the production of lysophosphatidic acid (LPA). ATX increases the aggressiveness and invasiveness of transformed cells, and ATX levels directly correlate with tumor stage and grade in several human malignancies. To study the role of ATX in the pathogenesis of malignant melanoma, we developed antibodies and small molecule inhibitors against recombinant human protein. Immunohistochemistry of paraffin embedded human tissue demonstrates that ATX levels are markedly increased in human primary and metastatic melanoma relative to benign nevi. Chemical screens identified several small molecule inhibitors with binding constants ranging from nanomolar to low micromolar.

Abstract: This invention relates to anti-cancer compounds and to methods for treating or preventing cancer. In one aspect the invention concerns mitochondrially delivered pro-oxidant anti-cancer compounds that generate reactive oxygen species and induce apoptosis of cancerous cells. The delivery moiety can be a lipophilic cation and the pro-oxidant vitamin E analogue, such as ?-tocopheryl succinate, ?-tocopheryl maleate, ?-tocopheryl maleyl amide, or 2,5,7,8-tetramethyl-2R-(4R,8R,12-trimethyltridecyl)-chroman-6-yloxyacetic acid (?-tocopheryloxyacetic acid).

Abstract: Compounds of the formula I, in the form of mixtures comprising predominantly one enantiomer or in the form of pure enantiomers, secondary phosphine-Q-P*(?O)HR1 (I) in which secondary phosphine is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*(O)HR1 is bonded to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally interrupted by heteroatoms from the group of O, S, N, Fe or Si; P* is a chiral phosphorus atom; and R1 is a hydrocarbon radi

Abstract: Disclosed are electroluminescent materials comprising a homopolymer based on recurring structural units of the formula (I) wherein R9, R9? R9?, R11, R13? R14, R11?, R13?, R14? independently are H or an organic substituent, where at least one of R9, R9? R9?, R11, R13 R14, R11?, R13?, R14? comprises a group R10 of the formula —(Sp)x10-[PG?]< wherein Sp is a divalent organic spacer, PG? is a group derived from a polymerisable group, and x10 is 0 or 1, with substituents and spacer as defined in claim 1. Further disclosed are some novel polymers of this class as well as monomers for their preparation. The homopolymers are advantageously used as a host material in devices further comprising a luminiscent component, which is usually selected from phosphorescent metal complexes and fluorescent dopants.

Abstract: Novel CE-phosphoramidites and CPG reagents have been synthesized from a serinol backbone. These reagents are useful to introduce functional groups or directly label oligonucleotides. The versatile serinol scaffold allows for labeling at any position (5? or 3? termini, or any internal position) during automated DNA synthesis. Multiple labels or functional groups can be achieved by repetitive coupling cycles. Optimal spacer arms and protected label moieties have been specially designed. Further, the natural 3-carbon atom internucleotide phosphate distance is retained when inserted internally.

Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.

Abstract: Provided are an organic light-emitting compound of Formula 1 and an organic light-emitting device using the organic light-emitting compound: where Ar, R1, R2, R3, R4, and R5 are the same as defined in the detailed description. The organic light-emitting device manufactured using the organic light-emitting compound has a low turn-on voltage and high efficiency and color purity.

Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.

Abstract: The present invention relates to a method for forming a calcium-based carrier particle consisting of the calcium-based material, an active, with or without a surface modification, a stabilizing agent, and the related composition. The calcium-based particle is illustrated by the general formula Cax(PO4)y(OH)zR and may also include a silica or silica oxide substituent. R is an active or actives such as an organic or inorganic molecule that includes markers, amines, thiols, epoxies, organosilicones, organosilanes, sulfates, and water soluble agents and, as needed, a surface modification, S, which may be either organic or inorganic. A stabilizing agent may be necessary to maintain dispersion of the particles in aqueous media. Examples of a surface modifying material and stabilizing agents are inorganic salts of aluminum and boron or organic materials such as organosilanes or low molecular weight polymers.

Abstract: The present invention relates to a method for forming a calcium-based carrier particle consisting of the calcium-based material, an active, with or without a surface modification, a stabilizing agent, and the related composition. The calcium-based particle is illustrated by the general formula Cax(PO4)y(OH)zR and may also include a silica or silica oxide substituent. R is an active or actives such as an organic or inorganic molecule that includes markers, amines, thiols, epoxies, organosilicones, organosilanes, sulfates, and water soluble agents and, as needed, a surface modification, S, which may be either organic or inorganic. A stabilizing agent may be necessary to maintain dispersion of the particles in aqueous media. Examples of a surface modifying material and stabilizing agents are inorganic salts of aluminum and boron or organic materials such as organosilanes or low molecular weight polymers.