Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.

Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: Method for controlling rust infections in leguminous plants by using orysastrobin, mixtures of orysastrobin and a fungicidally active compound II from the group of the azoles, acylalanines, amine derivatives, anilinopyrimidines, dicarboximides, dithiocarbamates, heterocylic compounds, phenylpyrroles, cinnamides, and analogs, or other fungicides according to the description, and also compositions and seed comprising these mixtures.

Abstract: Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.

Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.

Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.

Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.

Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C?—C—(CH2)2CO2H, meta-C?—C—(CH2)2OH, meta-C?C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C?

Abstract: Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.

Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases

Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.

Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

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

Abstract: A composition for controlling harmful bio-organisms comprising (a) at least one imidazole compound represented by formula (I): wherein R represents a lower alkyl group or a lower alkoxy group; and n represents an integer of 1 to 5, as an active ingredient, and (b) at least one inorganic phosphorus compound and/or at least one fungicide for Phycomycetes as an active ingredient or (c) a spreader as an activity-enhancing ingredient, and a method for controlling harmful bio-organisms comprising applying the composition for controlling harmful bio-organisms onto harmful bio-organisms.

Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.

Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract: The invention relates to acyl-4-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention particularly relates to compounds of formula I, in which the radicals have the given meanings described herein, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.

Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

Abstract: Methods for preventing damage to epithelial tissue during PDT induced using a photosensitizing agent or pre-photosensitizing agent are provided. The methods of the present invention utilize spatial confinement to control photoactivation of the photoactive species to protect the epithelial tissue. In one embodiment, epithelial tissue surrounding a targeted treatment site can be protecting by decreasing the oxygen-content in the tissue, thereby preventing the conversion of the photosensitizer into the phototoxic species in the epithelial tissue.

Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2–10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5–10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4–20% of at least one inorganic solid carrier; and d) 3–20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.

Abstract: Disclosed is an insect repellent composition. The composition has an amount of an insect repellent active effective to repel insects when the composition is applied to the skin, and an amount of a urethane polymer sufficient to form a film on the surface of the skin. The composition also has a cosmetically-acceptable vehicle. Also disclosed is a method of repelling insects from the skin by applying the composition to the skin.

Abstract: A composition of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of the compound, and a diagnostically acceptable carrier. A method for detecting malignant tumors, by administering a tumor detecting effective amount to a host in need of tumor detection of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of said compound and detecting the malignant tumors using NMR.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alky

Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.

Abstract: A series of N-cycloalkylcarboxamide derivatives of N-benzyl benzenesulfonamides of Formula I are described. The compounds inhibit ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of ?-amyloid. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.

Abstract: The present invention relates to plant-protecting active ingredient mixtures having synergistically enhanced action and to a method of improving the growth of plants, comprising applying to the plants or the locus thereof at least three active ingredient components together. Specifically, a mixture of fludioxonil (I), metalaxyl (II) and a strobilurin fungicide (III) achieves markedly enhanced action against plant pathogens and is suitable for improving the growth of plants when applied to plants, parts of plants, seeds, or at their locus of growth.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.

Abstract: (R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparation and pharmaceutical preparations thereof are also described. The quaternary salts of the invention are useful in the inhibition of chemotaxis of neutrophils and monocytes induced by the fraction C5a of the complement and are used in the treatment of psoriasis, pemphigus and pemphigoid, rheumatoid arthritis, intestinal chronic inflammatory pathologies including ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, cystic fibrosis, chronic obstructive pulmonary disease and glomerulonephritis. The compounds of the invention are advantageously used in the prevention and the treatment of injury caused by ischemia and reperfusion.

Abstract: A pharmaceutical composition for the treatment of an increased urge to urinate or urinary incontinence, comprising an effective amount of at least a compound selected from the group consisting of codeine, dihydrocodeine, dextropropoxyphene, meptazinol and tilidine. Also disclosed are methods of treatment using the pharmaceutical compositions and preferred dosages for the treatment methods.

Abstract: The present invention relates to a pharmaceutical composition containing a cycloalkene compound, a salt thereof or a prodrug thereof, and a nonionic surfactant and/or a cyclodextrin derivative readily soluble in water, and a method for improving solubility, stability or coloring property of the compound, a salt thereof or a prodrug thereof.

Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.

Abstract: It has now been found that N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester (APM) lowers whole blood viscosity in patient, including those suffering from sickle cell disease and plasma cell dyscrasias. Upon in vivo APM treatment patients experienced a significant lowering of whole blood viscosity. In vitro addition of APM to patients samples having elevated whole blood viscosity resulted in reduced viscosity over time. These in vivo and in vivo results identify APM as a therapeutic agent for molecular diseases which lead to elevated whole blood viscosity. A method by which APM treatment can be monitored is also disclosed.

Abstract: An agent for diagnosing or photokinetically treating malignant tumors, comprising as an active ingredient a compound in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, or an ester, amide, salt, hydrate or solvate of the compound.

Abstract: Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.

Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.

Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5-10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4-20% of at least one inorganic solid carrier; and d) 3-20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.

Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: The present invention relates to N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives having the general formula I 1

Abstract: The present invention relates to a new field of indication for phenoxyacetic acid derivatives as described in European Patent Application EP 1095932. It has now been found that the compounds described therein are suitable for the preparation of a medicament for treating hyperactive bladder (overactive bladder). Accordingly, by means of these active substances, a method is provided for treating this urological syndrome.

Abstract: The subject invention provides compounds which are easily metabolized by the metobolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract: A method of inducing the viral resistance of plants comprises treating the plants, the soil or seeds with an effective amount of the compound of the formula I 1

Abstract: The subject-matter of the invention is the B form of ethyl [(7S)-7-[(2R)-2-(3-chlorophenyl)-2-hydroxyethylamino]-5,6,7,8-tetrahydronaphth-2-yloxy]acetate hydrochloride, of use as a medicament, which exhibits in particular the following physical characteristics:

Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.

Abstract: A composition and an associated method of treating cancer cells by impeding cancer cell growth with the composition are disclosed. The composition includes at least a first and a second HMG-CoA reductase inhibitor, wherein the total amount of the first and second HMG-CoA reductase inhibitors is effective in synergistically impeding cancer cell growth and wherein the cancer cell growth synergistic impedance from the total amount of the first and second HMG-CoA reductase inhibitors is greater than a theoretical additive effect from the combined first and second HMG-CoA reductase inhibitors. The present composition does not simultaneously contain both a tocotrienol and an ionone when the composition contains only a first and a second HMG-CoA reductase inhibitor. The method includes treating cancer cells with the claimed composition to impede cancer cell growth.

Abstract: The invention relates to compounds of formula (I), to salts and stereoisomers thereof, to their production and to their use for producing medicaments used for treating cardiovascular diseases.

Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.

Abstract: The novel compound 3-amidinobenzoyl-D-phenylglycine-3-phenylanilide is useful as a serine protease inhibitor.