Abstract: A process for preparing EDDN and/or EDMN by conversion of FA, HCN and EDA, the reaction being effected in the presence of water, and, after the conversion, water being depleted from the reaction mixture in a distillation column, which comprises performing the distillation in the presence of an organic solvent which has a boiling point between water and EDDN and/or EDMN at the distillation pressure existing in the column or which forms a low-boiling azeotrope with water.

Abstract: A process for reacting formaldehyde cyanohydrin (FACH) with ethylenediamine (EDA) in a reactor with limited backmixing at a temperature in the range from 20 to 120° C., wherein the residence time in the reactor is 300 seconds or less.

Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

Abstract: The present invention provides novel amino-lipids, compositions comprising such amino-lipids and methods of producing them. In addition, lipid nanoparticles comprising the novel amino-lipids and a biologically active compound are provided, as well as methods of production and their use for intracellular drug delivery.

Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.

Abstract: The present invention reacts ethylenediamine with one or more additional ethyleneamines in the presence of a transamination catalyst to provide a different, preferably more desirable product mix of one or more ethyleneamines.

Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

Abstract: The present invention provides novel amino-lipids, compositions comprising such amino-lipids and methods of producing them. In addition, lipid nanoparticles comprising the novel amino-lipids and a biologically active compound are provided, as well as methods of production and their use for intracellular drug delivery.

Abstract: Disclosed is a method of treating cancer in a patient comprising administering to the patient an effective amount of a diazeniumdiolated (N2O2-containing) compound or a pharmaceutically acceptable salt thereof, wherein the cancer cell has an elevated level of reactive oxygen species (ROS) and/or a decreased level of one or more of PRX1, PRX6, and OGG1, compared to a normal cell of the same tissue or tissue type. An example of a diazeniumdiolated compound is Formula (I), wherein X and Q are defined herein. Also disclosed are diazeniumdiolated compounds, pharmaceutical compositions, and methods of use including enhancing the chemotherapeutic treatment of chemotherapeutic agents and high energy radiation.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.

Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.

Abstract: A composition that includes aldimines of Formula (I). The composition can be a two-component polyurethane composition. The composition can have a long open time, but build up an early strength quickly, and in the cured state can have high tensile strength and a high modulus of elasticity. The composition can be odorless or at least low-odor before, during and after curing.

Abstract: Disclosed is a novel ionic liquid gel electrolyte having high photoelectric conversion efficiency. Also disclosed are a novel dye-sensitized photoelectric conversion device using such an ionic liquid gel electrolyte, and a solar cell composed of such a dye-sensitized photoelectric conversion device. Specifically disclosed is an ionic liquid gel electrolyte obtained by gelling a liquid electrolyte by using an ionic organic oligomer gelling agent represented by the general formulae (1) and (2) below. Also specifically disclosed are a dye-sensitized photoelectric conversion device, wherein the ionic liquid gel electrolyte is arranged between a counter electrode and a dye-absorbed semiconductor substrate which is arranged in contact with a transparent conductive substrate, and a solar cell.

Abstract: A compound represented by formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group, excluding a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.

Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.

Abstract: The invention relates to a method for the synthesis of exocyclic derivatives of cycloalkyl-hydrazines and exocyclic derivatives of heterocycloalkyl-hydrazines The invention is characterised in that the method comprises a step consisting in demixing a solution containing said synthesised derivative, by reacting a heterocyclic amine with monochloramine, in an organic phase and an aqueous phase with the addition of anhydrous sodium hydroxide. According to the invention, the starting amine which has not reacted is collected and reused directly without any additional treatment. The inventive method can also be used to obtain the corresponding exocyclic heterocycloalkyl-hydrazine or cycloalkyl-hydrazinederivative derivative at a low cost compared to that of other known methods.

Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The invention relates to a process for preparing triethylenetetramine (TETA), which, comprises the following steps: a) reaction of ethylenediamine (EDA) with formaldehyde and hydrocyanic acid (HCN) in a molar ratio of EDA to formaldehyde to HCN of from 1:1.5:1.5 to 1:2:2 to give ethylenediaminediacetonitrile (EDDN), b) hydrogenation of the EDDN obtained in step a) in the presence of a catalyst and a solvent.

Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.

Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R5 represents a halogen atom, cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R6 represents a C5-7 cycloalkyl group, a substituted C5-7 cycloalkyl group, a 5 to 7-membered completely saturated heterocyclic group or a substituted 5 to 7-membered completely saturated heterocyclic group, X represents a single bond, oxygen atom, sulfur atom, NR7, —O—CH2— or —N(R8)—CH2—, R7 represents hydrogen atom or a C1-4 alkyl group, or R7 may combine with a substituent of R6 to represent a single bond, methylene group or ethylene group, R8 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, which is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases caused by an activation of

Abstract: The present invention discloses multifunctional bioactive compounds of formula (I) constituted of an immunoregulatory portion linked to a stabilizer moiety and pharmaceutical compositions thereof useful in the treatment of immune disorders and hemopoietic disorders such as immune cytopema, multiple myeloma, chronic lymphoid leucosis, lymphocytic lymphomas, lymphosarcomas.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.

Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.

Abstract: A compound of Formula (A), wherein R1 is C1-C5 alkyl, C3-C6 branched alkyl, C4-C7 cycloalkyl, C8-C12 fused or bridged polycycloalkyl, or heterocyclic ring, where any of the preceding alkyl, cycloalkyl or heterocyclic ring groups may be singly or multiply substituted with X; R2 is H or R1; and X is halo, carbonyl carboxylic acid, carboxylic ester, carboxamide, substituted carboxamide, hydroxy, alkoxy, thioalkyl, sulphoxide, sulphone, sulphonamide, substituted sulphonamide, phenoxy, substituted phenoxy, phenyl, substituted phenyl, amino, substituted amino (including quaternary ammonium salts), N-oxide, imino, 5-7 membered heterocycle, or substituted heterocycle.

Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X) ??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.

Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with MEK that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, Wherein: R1 and R2 are independently hydrogen or C1-3 alkyl; X represents a bond, CH2 or O; R3 and R4 are independently hydrogen, C1-6 alkyl, OCH3, CF3, allyl or halogen; X1 is CH2, SO2, or CO; R5 is —C1-6 alkyl (optionally substituted by C1-6alkoxy or C1-6alkylthio), —C2-6 alkenyl, —C0-6 alkyl phenyl (wherein the phenyl is optionally substituted by one or more CF3, halogen, C1-3 alkyl, C1-3 alkoxy), —COC1-6 alkyl, SO2C1-6 alkyl; R6 is phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 N atoms wherein the phenyl or heteroaryl group is optionally substituted with 1, 2 or 3 moieties selected from the group consisting of C1-6 alkyl, halogen, —OC1-6 alkyl, —SO2C1-3 alkyl, phenyl (optionally substituted by one or more groups selected from halogen, CF3, C1-3 alkyl, OC1-3 alkyl, acetyl, CN).

Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: A method for obtaining compounds having selected properties for a particular application by forming base modules having at least two structural diversity elements from the reaction of a first compound having at least one structural diversity element and a first reactive group, with a second compound having at least one structural diversity element and a second reactive group, wherein the first and second groups combine by an addition reaction; producing a first array of molecules by varying at least one of the structural diversity elements of the compounds when producing the base modules; and screening the array to determine a first suitable compound for the particular application. The base modules are preferably formed form oxazolone- and aminimide-derived compounds.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.

Abstract: A metal complex of a piperazineNONOate derivative of the formula: wherein a) R1 and R2 independently represent hydrogen, linear or branched (C1-C4) alkyl, optionally substituted by 1 or 2 groups selected from the group consisting of hydroxy, (C1-C4) alkoxy, (C1-C4) alkylthio, amino, (C1-C4) alkylamino, di-(C1-C4) alkylamino, carboxy, carbo(C1-C4) alkoxy, aryl, aryloxy, arylthio; or b) R1 and R2 taken together, represent one of the following groups ?CR3-aryl, where R3 represents hydrogen, (C1-C4) linear or branched chain alkyl, optionally substituted by 1 or 2 groups selected from the group consisting of hydroxy, carboxy, aryl; n represents a whole number ranging from 2 to 4; M+ represents a cation of a transition metal or zinc; x represents a whole number which varies from 1 to 3, and indicates the charge units of the cation of the transition metal or of the zinc in relation to its stable oxidation state; A ? represents an inorganic or organic anion which forms stable salts with the NONOate metal complex

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Abstract: The present application describes novel cyclic &bgr;-amino acid derivatives of formula I: 1

Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: The present invention relates to a class of compounds represented by the Formula I 1

Abstract: The present invention provides estrogen receptor (ER) ligands of structural formula (I) 1

Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: The invention is to provide an antidementic and/or antiamnesic potency enhancer that comprises an aminopiperazine or aminopiperidine derivative of a formula: 1

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Process for removing a residual fragment of a chiral auxiliary from a diastereomeric compound with formula (2) 1

Abstract: The present invention relates to a novel process for the preparation of a diastereomeric mixture of piperidinylaminomethyl trifluoromethyl cyclic ether compounds of formulae Ia and Ib: 1