Abstract: A solid-supported palladium(II) complex which catalyzes the Mizoroki-Heck coupling reaction efficiently and a method of employing the solid-supported palladium(II) complex to synthesize cinnamic acid and derivatives thereof. The solid-supported palladium(II) complex is also stable and can be recycled without significantly losing catalytic activity.

Abstract: A solid-supported palladium(II) complex which catalyzes the Mizoroki-Heck coupling reaction efficiently and a method of employing the solid-supported palladium(II) complex to synthesize cinnamic acid and derivatives thereof. The solid-supported palladium(II) complex is also stable and can be recycled without significantly losing catalytic activity.

Abstract: A solid-supported palladium(II) complex which catalyzes the Mizoroki-Heck coupling reaction efficiently and a method of employing the solid-supported palladium(II) complex to synthesize cinnamic acid and derivatives thereof. The solid-supported palladium(II) complex is also stable and can be recycled without significantly losing catalytic activity.

Abstract: A solid-supported palladium(II) complex which catalyzes the Mizoroki-Heck coupling reaction efficiently and a method of employing the solid-supported palladium(II) complex to synthesize cinnamic acid and derivatives thereof. The solid-supported palladium(II) complex is also stable and can be recycled without significantly losing catalytic activity.

Abstract: A method for the preparation of an alkali metal cinnamate powdery product, preferably potassium cinnamate or sodium cinnamate, is disclosed herein. The resulting product has novel structural properties. The powder of the present disclosure is made via spray-drying and/or spray agglomeration and has a higher flowability, is less cohesive and less dusty, has an improved dissolution rate and in particular has a very favorable organoleptic profile. The disclosure is also directed to product applications in which the novel cinnamate product of the present disclosure may be applied.

Abstract: An in-situ method for preparing a hydrolyzed, acyl halide-containing compound by combining a reactant including a plurality of acyl halide functional groups containing reactant, a tri-hydrocarbyl phosphate compound and water within a hydrocarbon or halogenated hydrocarbon solvent.

Abstract: A method for preparing a high purity (e.g. greater than 70 wt. %) mono-hydrolyzed acyl halide compound as a precipitate from solution comprising the steps of preparing a solution comprising: i) at least 80 v/v % of a hydrocarbon solvent, ii) water at a molar concentration greater than its solubility limit within the solvent but less that its solubility limit in solution, iii) a tri-hydrocarbyl phosphate compound, and iv) a polyfunctional acyl halide compound at molar ratio to both water and the tri-hydrocarbyl phosphate compound of at least 1:1.

Abstract: The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.

Abstract: The invention relates to certain compounds, salts of these compounds and mixtures containing or consisting of two or more such compounds, two or more such salts or one or more such compounds and one or more such salts, each for use in a method for the prophylaxis and/or treatment of inflammation, in particular of inflammation of the skin.

Abstract: Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.

Abstract: A method for preparing a high purity (e.g. greater than 70 wt. %) mono-hydrolyzed acyl halide compound as a precipitate from solution comprising the steps of preparing a solution comprising: i) at least 80 v/v % of a hydrocarbon solvent, ii) water at a molar concentration greater than its solubility limit within the solvent but less that its solubility limit in solution, iii) a tri-hydrocarbyl phosphate compound, and iv) a polyfunctional acyl halide compound at molar ratio to both water and the tri-hydrocarbyl phosphate compound of at least 1:1.

Abstract: The present invention provides a method of treating cancer using the sodium salt of a benzoic acid derivative, alone or in combination with standard treatments such as chemotherapy and radiotherapy.

Abstract: The present invention discloses 4-nerolidylcatechol and its derivatives isolated from South American/Amazon plants (Pothomorphe species) and their potential use as therapeutical agent for treatment of malarial symptoms, including malarial patients resistant to traditional drugs. The present invention also discloses a method for producing 4-nerolidylcatechol and their derivatives.

Abstract: There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.

Abstract: A salt represented by the formula (I-Pa): wherein Xpa represents a single bond or a C1-C4 alkylene group, Rpa represents a single bond, a C4-C36 divalent alicyclic hydrocarbon group or a C6-C36 divalent aromatic hydrocarbon group, and one or more methylene groups in the divalent alicyclic hydrocarbon group can be replaced by —O— or —CO—, Ypa represents a polymerizable group, and Zpa+ represents an organic cation.

Abstract: The invention relates to the use of at least one compound, selected from the group consisting of tebuconazole, epoxiconazole, metconazole, cyproconazole, prothioconazole and any mixtures thereof, for increasing the resistance of plants to abiotic stress factors.

Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.

Abstract: The invention relates to certain compounds, salts of these compounds and mixtures containing or consisting of two or more such compounds, two or more such salts or one or more such compounds and one or more such salts, each for use in a method for the prophylaxis and/or treatment of inflammation, in particular of inflammation of the skin.

Abstract: One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition metal-catalyzed: aryl amination reactions; aryl amidation reactions; Suzuki couplings; and Sonogashira couplings. In certain embodiments, the invention relates to catalysts and methods of using them that operate in aqueous solvent systems.

Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.

Abstract: A method for the preparation of an alkali metal cinnamate powdery product, preferably potassium cinnamate or sodium cinnamate, is disclosed herein. The resulting product has novel structural properties. The powder of the present disclosure is made via spray-drying and/or spray agglomeration and has a higher flowability, is less cohesive and less dusty, has an improved dissolution rate and in particular has a very favorable organoleptic profile. The disclosure is also directed to product applications in which the novel cinnamate product of the present disclosure may be applied.

Abstract: A traceable treatment composition for treating a subterranean formation having multiple zones penetrated by a well bore comprising a homogenous blend of a tracking composition and a resin composition. The tracking composition comprises a substantially non-radioactive tracking material selected from the group consisting of a metal salt. The metal portion of the metal salt may be selected from the group consisting of gold, silver, lithium, molybdenum, and vanadium.

Abstract: The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.

Abstract: Salts and/or co-crystals of (+)-3-[2-(dimethylamino)-methyl-1-hydroxycyclohexyl]-phenol or of (?)-3-[2-(dimethylamino)methyl-1-hydroxy-cyclohexyl]phenol, present in crystalline form, with cinnamic acid, C8- to C10-alkane-monocarboxylic acids, C6- to C10-alkanedicarboxylic acids, C15- to C17-alkane-monocarboxylic acids, fumaric acid, tartaric acid, mandelic acid, hippuric acid and/or embonic acid, a process for their production, and the use of such salts and/or co-crystals as medicaments.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy. Carboxylic acid-containing compounds having a terminal cyclic moiety, a carboxylic acid group, and a C3-12 hydrocarbon chain optionally containing at least one double bond, at least one triple bond, or at least one double bond and one triple bond linking the cyclic moiety and the carboxylic acid group are inhibitors of histone deacetylase.

Abstract: The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.

Abstract: The present invention discloses novel and useful intermediates for the synthesis of ezetimibe (EZT), which intermediates share a characteristic Z-isomeric structure. Based on Z-5-(4-fluorophenyl)-pent-4-enoic acid, and proceeding the synthesis through further Z-intermediates, a total synthesis is presented to obtained final ezetimibe in high yields.

Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type I1 diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.

Abstract: The present invention discloses 4-nerolidylcatechol and its derivatives isolated from South American/Amazon plants (Pothomorphe species) and their potential use as therapeutical agent for treatment of malarial symptoms, including malarial patients resistant to traditional drugs. The present invention also discloses a method for producing 4-nerolidylcatechol and their derivatives.

Abstract: A salt represented by the formula (I-Pa): wherein Xpa represents a single bond or a C1-C4 alkylene group, Rpa represents a single bond, a C4-C36 divalent alicyclic hydrocarbon group or a C6-C36 divalent aromatic hydrocarbon group, and one or more methylene groups in the divalent alicyclic hydrocarbon group can be replaced by —O— or —CO—, Ypa represents a polymerizable group, and Zpa+ represents an organic cation.

Abstract: A method of enhancing production of a phenylpropanoid compound in a plant or plant cell is disclosed. The method comprising: (a) expressing in the plant or plant cell a heterologous polynucleotide which produces a myb gene of the phenylpropanoid pathway; and (b) contacting the plant or plant cell with at least one substrate of the phenylpropanoid pathway, the substrate being upstream to the production of the phenylpropanoid compound, thereby enhancing the production of a phenylpropanoid compound in the plant or plant cell.

Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition with the above-mentioned properties.

Abstract: The invention relates to use of a compound of Formula (I) as a preservative, or to enhance the anti-mould efficacy of another preservative and a product comprising a compound of Formula (I), wherein: the second carbon is optionally substituted; the bond between R and the second carbon is unsaturated; R is a C1 to C20 alkyl, aryl, alkaryl, alkenyl or alkynyl; and wherein R may be optionally substituted; Z is H or OH; and when Z is OH, the bond between R and the second carbon is a triple bond.

Abstract: The present invention is related to a family of N-phenyl-prenylamine derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.

Abstract: This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.

Abstract: Methods of treating blood disorders are described.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from a UV-absorbing molecule has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds of formulas (I) and (V) having an alkoxy radical preferably in the four (para) position (hereinafter methoxycrylenes) on one or both of the phenyl rings: wherein at least one of R1 and R2 is a straight or branched chain C1-C12 alkoxy radical, preferably C1-C8, more preferably C1-C4, and most preferably methoxy, and any non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C24 alkyl radical, preferably C12-C24, more preferably C20; wherein A and B are the same or different and are selected from the group consisting of oxygen, amino and sulfur; R1 and R3 are the same or different and are selected from the group consisting of C1-C30 alkyl, C2-C30 alkylene, C2-C30 alkyne, C3-C8 cycloalkyl, C1-C30 substituted alkylene, C2-C30 substituted alkyne, aryl, substituted aryl, hete

Abstract: A method of producing a first ethynyl compound represented by the following formula (1), the method including reacting a second ethynyl compound represented by the following formula (2) in a liquid phase in the presence of a reducing agent to obtain the first ethynyl compound, wherein Q1 represents an organic group; R1 and R2 each independently represent a hydrogen atom or a hydrocarbon group; and R1 and R2 may be bonded to each other.

Abstract: The present invention relates to a process for the formation of carbon-carbon bonds starting from a copper compound of an aryl, heteroaryl, alkene or alkine and an aryl, heteroaryl, alkene or alkine compound having a suitable leaving group. The copper compounds can be prepared inter alia by means of transmetalliziation from a Grignard or lithium compound. Cross-coupling of these compounds with e.g. a halogen-substituted aryl compound is carried out by means of an iron or cobalt catalyst using suitable solvents and suitable additives.

Abstract: Polyhalogenated cinnamic acids and cinnamic acid derivatives are prepared by reacting diazonium salts accessible from polyhalogenated anilines with acrylic acid or acrylic acid derivatives in the presence of a homogeneous, palladium-containing catalyst at about ?5 to about +100° C. Some of the cinnamic acids and cinnamic acid derivatives obtainable in this way are new. Cinnamic acids and cinnamic acid derivatives which can be prepared according to the invention can be used for the preparation of indanones which are precursors for agro- and pharmaceutical chemicals and for substances having liquid-crystalline properties.

Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.

Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.

Abstract: Compounds of formula (II) are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted into a hydroxylactone and then the hydroxy group into a leaving group, the leaving group is replaced with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I).

Abstract: A photocurable hyaluronic acid derivative of the present invention comprises hyaluronic acid and a photoreactive crosslinking group bonded thereto, wherein a 1.0 wt. % aqueous solution of the photocurable hyaluronic acid derivative obtained by dissolving the solid photocurable hyaluronic acid derivative in an aqueous solvent, is capable of passing through a porous filter having a pore size of 0.45 &mgr;m and a diameter of 25 mm at a rate of not less than 2 ml/minute at 24° C. under a pressure of 5.0 Kg/cm2; and a process for producing the photocurable hyaluronic acid derivative; and a photocured crosslinked-hyaluronic acid derivative; a medical material using the photoreactive hyaluronic acid derivative and a medical material using the photocured crosslinked-hyaluronic acid derivative.

Abstract: There is disclosed a genus of optionally substituted Schiff base condensation products (and the carba analogs thereof) comprising an amino acid component and a benzaldehyde component, that have MIF (macrophage migration inhibitory factor) antagonist activity. The compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases, asthma, arthritis, EAE, ARDS and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization.

Abstract: The present invention relates to a process for the arylation of olefins by reaction of haloaromatics or arylsulfonates with olefins in the presence of a palladium catalyst, a bulky nitrogen base and a dipolar aprotic solvent.

Abstract: The present invention relates to a process for the arylation of olefins by reaction of haloaromatics or arylsulfonates with olefins in the presence of a palladium catalyst, a bulky nitrogen base and a salt.

Abstract: The present invention relates to a process for the synthesis of cinnamic esters and/or cinnamic acids by condensation of aldehydes with carboxylic anhydrides, using iron(II) salts as catalyst.

Abstract: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The acrylic acid esters of Formula I are useful for the delivery of organoleptic compounds, especially for flavors, fragrances, masking agents and antimicrobial compounds. They can also deliver fluorescent whitening agents.