Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

Abstract: Cellular migration is a normal part of the normal development of the human being and, in certain pathologies, its alteration damages physiological performance, so that it is necessary to learn about its molecular and cellular foundations and establish methodologies to identify those molecules that modulate this cellular behavior. A screening method using zebra fish embryos is used to follow the advance in the migration of the lateral line primordium upon contact with a test compound. Modulators N found are Fenritinide, PGD2 and is-deoxy-PJE2. The invention refers to a biological method for the IN VIVO, fast, massive and simultaneous tracking of molecules capable of affecting cellular migration, in order to facilitate the for of potential candidates to be used in the diagnosis, prevention, and, principally, for the preparation of pharmaceutical compositions for the treatment of congenital pathologies, immune system dysfunctions, tissue regeneration failure, inflammation, cancer.

Abstract: A non-water soluble polymeric surfactant is prepared by reacting a polymerized/bodied unsaturated oil with maleic anhydride followed by a further partial or complete reaction with an amine to form an amide; or an alcohol to form an ester.

Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.

Abstract: The present invention provides a protecting reagent that can be removed in a high yield even under acidic conditions and can afford a resulting product at a high purity in an organic synthesis reaction such as peptide synthesis and the like. The inventive protecting reagent is particular benzylic compound having only one hydroxyl group substituted by an organic group having an aliphatic hydrocarbon group having a carbon number of not less than 14.

Abstract: The present invention provides a new pharmaceutical application of a 15,15-difluoroprostaglandin F2? derivative. As a result of intensive studies in order to find a new pharmaceutical application of a 15,15-difluoroprostaglandin F2? derivative, it was found that, in a European Phase III clinical trial for tafluprost, one of the 15,15-difluoroprostaglandin F2? derivatives, with patients with open-angle glaucoma or ocular hypertension, tafluprost has actions of growing eyelashes, making eyelashes thicker, and changing the color thereof, that is, has an effect of promoting the growth of hair (eyelashes). Therefore, a 15,15-difluoroprostaglandin F2? derivative is useful as a hair growth promoting agent, and is expected to be useful as an active ingredient of a preventive or therapeutic agent for a disease associated with hair such as alopecia and a hair care product or a hair cosmetic product for regrowing hair, growing hair, increasing hair density, nourishing hair, or the like.

Abstract: An oxylamino group-containing compound represented by the following formula: R1—B-A-B—R2, wherein R1 represents a polymerizable group, R2 represents an oxylamino group-containing group or an oxylamino derivative-containing group, B represents an ester linkage or an amide linkage, and A represents an optionally substituted alkylene group having 2 to 12 carbon atoms.

Abstract: Stable ultrapure colchicine compositions comprising ultrapure colchicine and a pharmaceutically acceptable excipient are described. The compositions can be tablets. Methods for preparing such compositions and methods of use are also disclosed. Methods of treating gout flares with colchicine compositions are also disclosed.

Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.

Abstract: In the present specification we describe a new class of compounds, designed to modulate the ability of blood vessels to synthesize NO from L-arginine. In particular we have identified novel compounds which enhance the entry of L-arginine into cells. These compounds improve endothelial function, and thereby have the potential to retard the progression of vascular disease in conditions such as hypertension, heart failure and diabetes. This new class of drugs may also have other potentially, relevant pharmacological actions, including anti-hypertensive and anti-anginal actions.

Abstract: A paper softening composition that is capable of providing paper with excellent flexibility while suppressing decrease in paper strength. The paper softening composition contains a specific diamide diamine compound or a salt thereof and a specific amide amine compound or a salt thereof in a mass ratio of 5/95 to 90/10.

Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.

Abstract: The present invention provides a method for separating an amide from an amino acid ionic liquid. The method includes the step of providing a polar solvent and an extracting agent to the amino acid ionic liquid, so as to separate the amide from the amino acid ionic liquid. In the method of the present invention, there is no need to add ammonium for neutralization, such that no byproduct, ammonium sulfate, is formed. In addition, after the amide is separated from the amino acid ionic liquid, the amino acid ionic liquid can be recycled.

Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers using acylhydrazide compounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers using acylhydrazide compounds.

Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Abstract: Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.

Abstract: Zn2+-chelating motif-tethered fatty acids as histone deacetylase (HDAC) inhibitors. Compounds performed well in in vitro and in vivo tests.

Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.

Abstract: The invention relates to tuned multifunctional linker molecules for charge transport through organic-inorganic composite structures. The problem underlying the present invention is to provide multifunctional linker molecules for tuning the conductivity in nanoparticle-linker assemblies which can be used in the formation of electronic networks and circuits and thin films of nanoparticles. The problem is solved according to the invention by providing a multifunctional linker molecule of the general structure CON1-FUNC1-X-FUNC2-CON2 in which X is the central body of the molecule, FUNC1 and FUNC2 independently of each other are molecular groups introducing a dipole moment and/or capable of forming intermolecular and/or intramolecular hydrogen bonding networks, and CON1 and CON2 independently of each other are molecular groups binding to nanostructured units comprising metal and semiconductor materials.

Abstract: Provided is a novel extractant for palladium capable of improving an extraction rate compared to the conventional extractant, DHS, and also capable of back-extracting palladium using an ammonia solution, and a method of separating and recovering palladium using the novel extractant.

Abstract: The present invention provides a catalyst composition for preparing an amide, including an amino acid ionic liquid having a cation of formula (I) and an anion selected from the group consisting of an inorganic acid group, an organic acid group and a combination thereof, wherein the numbers of the anion and the cation are such that the amino acid ionic liquid is electroneutral; and a Bronsted acid. The present invention also provides a method for preparing an amide in the presence of the catalyst composition, and the method has advantages such as decreasing viscosity of ionic liquid, and increasing conversion rate of ketoximes and selectivity of amides.

Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumours, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumours, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.

Abstract: Described is a new cooling agent represented by Formula I and compositions with known coolers having cooling properties and the application of Formula I in foodstuffs and chewing gum: wherein X, Y is independently selected from a C1-C4 straight or branched alkyl or H atom; and R1 is selected from a linear or branched alkyl, alkenyl, alkynyl, alkoxyalkyl containing from 1 to 6 carbons or group (CH2)n-Z, where n is 0 to 6 and Z is a group with non-bonding electrons. Useful groups with non-bonding electrons are halogens, OH, OMe, OEt, NO2, CN, Ac, SO2NH2, CHO, CO2H, CONH2, CONHR2, where R2 is selected from C1-C4, and C1-C4 alkyl carboxylates such as CO2Me or CO2Et.

Abstract: Described is a new cooling agent represented by Formula I and compositions with known coolers having cooling properties and the application of Formula I in foodstuffs and chewing gum: wherein X, Y is independently selected from a C1-C4 straight or branched alkyl or H atom; and m is 0, 1 or 2, Z when present is nitrogen, W and W? are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy or W is group (CH2)n-R, where n is 0 or 1 and R is a group with non-bonding electrons. Useful groups with non-bonding electrons are halogens, OH, OMe, OEt, NO2, CN, Ac, SO2NH2, CHO, CO2H, CONH2, CONHR2, where R2 is selected from C1-C4, and C1-C4 alkyl carboxylates such as CO2Me or CO2Et.

Abstract: Since an amide compound represented by the formula (1) is effectiveness for controlling plant diseases, it is useful as an effective ingredient of a composition for controlling plant diseases.

Abstract: The present invention refers to cooling compounds of formula I wherein R1, R2, R3, X, Y, Z, and m have the same meaning as given in the specification. The present invention refers furthermore to a process for their production and to product compositions comprising them.

Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.

Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.

Abstract: The present invention relates to a catalyst for reacting carbonitriles with water, wherein the catalyst comprises at least 60% by weight of manganese dioxide with an empirical formula MnOx where x is in the range from 1.7 to 2.0, and at least one plasticizer. The present invention further relates to a process for preparing the catalysts detailed above and to a process for preparing carboxamides by reacting carbonitriles with water in the presence of the present catalyst.

Abstract: A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, whi

Abstract: The present invention provides for a polyketide synthase (PKS) capable of synthesizing a dicarboxylic acid (diacid). Such diacids include diketide-diacids and triketide-diacids. The invention includes recombinant nucleic acid encoding the PKS, and host cells comprising the PKS. The invention also includes methods for producing the diacids.

Abstract: The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1 may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.

Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolving, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

Abstract: A highly pure asiaticoside and a pharmaceutical grade asiatic acid can be prepared, along with salts of asiatic acid, for use in formulating therapeutic compositions that are suitable for treating arthritis, psoriasis and other inflammatory diseases, as well as pulmonary fibrosis, diabetic nephropathy, and other fibrotic diseases.

Abstract: A process for converting an olefin having x carbon atoms into an olefin having x+1 carbon atoms wherein the process comprises the steps of: (i) reacting an olefin having x carbon atoms with carbon monoxide and hydrogen in the presence of a hydroformylation catalyst to produce an alcohol having x+1 carbon atoms, and (ii) dehydrating the alcohol produced in step (i) in the presence of a dehydration catalyst to produce an olefin having x+1 carbon atoms characterized in that the hydroformylation catalyst used in step (i) is based on: (a) a source of cobalt, and (b) a ligand which contains phosphorus and nitrogen.

Abstract: Peripheral Benzodiazepine Receptor (PBR) is an attractive target for tumor imaging and treatment due to its up-regulation in numerous cancer cell types. DAA1 106 is a selective PBR ligand with high binding affinity. Aspects of the present invention are series of functionalized DAA1 106 analogs, which can be conjugated to a variety of signaling and treatment moieties, and are widely applicable in PBR targeted molecular imaging and drug delivery.

Abstract: There are provided a novel onium salt and a method for optimizing the interface of a negative electrode by the use of the novel onium salt and/or a conventional onium salt. Such a method is characterized in that an electrolyte comprising novel 2,2,2-trifluoro-N-(trifluoromethanesulfonyl)acetamide.tetraethyl ammonium salt is made to intervene between a negative electrode and a positive electrode in an electrochemical device having the constitution: a negative electrode| an electrolyte| a positive electrode, thereby constructing an electrode structure in the electrochemical device, and applying a voltage between the negative electrode and the positive electrode so as for the negative electrode to have a potential of ?1 V to ?5 V in terms of the potential relative to a reference electrode of I?/I3?, thereby forming a passive-state layer comprising a decomposition product of the above electrolyte or salt on the surface of the above negative electrode.

Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.

Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I processes for preparing such compounds, pharmaceutical formulations comprising these compounds, methods of making such pharmaceutical formulations and the related methods of treating or inhibiting certain conditions or disorders.

Abstract: The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.

Abstract: A high throughput neurophysiological assay for identifying anti-psychotic compounds is disclosed. In particular, a high throughput neurophysiological assay using information obtained from injecting a neural activity blocker, such as tetrodotoxin (TTX), into one hippocampus persistently coactivated pyramidal cells in the uninjected hippocampus that initially discharged independently. In accord with the definition of cognitive disorganization, pyramidal cell firing rates only changed for 15 min and did not accompany the coactivation. The disclosed assay uses the TTX-induced coactivity of hippocampal pyramidal cell discharge to identify compounds that may prevent or attenuate the changes in the hippocampal pyramidal cell discharge observed when a neural activity blocker is administered. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that have anti-psychotic properties.

Abstract: The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of ?, -diaminocarbonyl-?,?-pentamethylene glutarimide.

Abstract: Fluoroalkyl amidoalkyl alcohols of the formula are disclosed and their corresponding (meth)acrylate esters. These fluoroalkyl amidoalkyl (meth)acrylate monomers can be copolymerized with a wide variety of conventional ethylenically unsaturated monomers. The resulting copolymers are useful as water, oil- and grease-proofing agents for paper, textiles and hard surfaces such as masonry and wood.

Abstract: The present invention relates to novel ionic liquids comprising a docusate, docusate variant, or other sulfonate anion. The ionic liquids may be conveniently made via, for example, metathesis. The ionic liquids are often hydrophobic and useful in many hydrocarbon compositions, polymer compositions, and in supercritical carbon dioxide applications. The ionic liquids are capable of hindering static electricity buildup in the hydrocarbon compositions and can therefore minimize flammability and/or explosiveness.