Abstract: Methods and compositions for treating cells with cytokines are provided herein.

Abstract: The invention provides for the use of carbonic anhydrase activators; protein kinase C activators and FGF-18 to treat depressive disorders. The invention also relates to improved animal models and methods for screening and identifying compounds the treatment of depressive disorders.

Abstract: The invention relates to compounds of the general formula (I) wherein X, Y and W have the significances given in claim 1 and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites in and on warm-blooded animals.

Abstract: Compositions comprising terpene compounds for the treatment of negative sensory phenomena (NSP). Negative sensory phenomena is characterized by a decreased ability to sense light touch, pin prick, vibration, temperature, pain and/or reduced proprioception. The terpene compounds are preferably aromatic terpene compounds such as geraniol and citronellol and analogs thereof. The terpenes may also be used in combination. The terpenes are derived form plant essential oils or are manufactured synthetically.

Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.

Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Abstract: Provided are novel a target and drugs in the treatment of neurological disorders related to amyloid beta pathology/amyloidosis. More specifically, the use of phosphatase inhibitors for the treatment of brain impairments mediated by A?-oligomers is described.

Abstract: The present invention relates to methods of decreasing the infectivity, morbidity and rate of mortality, in treating diseases associated with a variety of pathogenic organisms, specifically diseases involving one or more pathogens that require neuraminidase as a virulence factor. In addition, the present invention uses biology based therapy to treat neuraminidase dependent infections or diseases dependent on sialic acid metabolism.

Abstract: This invention relates to the use of oleuropein, specifically oleuropein in non-glycated form, and its derivatives in the treatment of type 2 diabetes mellitus. Furthermore, this invention relates to the use of oleuropein, specifically oleuropein in non-glycated form, and its derivatives both from synthesis and from degradation, in the treatment of pathologies associated with protein aggregation phenomena. Specifically, this invention relates to the use of oleuropein to prepare a pharmaceutical formula for the prophylactic and therapeutic treatment of pathologies connected to or deriving from amyloid deposit.

Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and vinca alkaloids, which have anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and vincristine. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.

Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and an alkylating agent, which has anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and cyclophosphamide. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.

Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a platinum compound which has anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and carboplatin. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.

Abstract: The present invention relates to synergistic combinations of the compound 5, 6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from anthracyclines and topisomerase II inhibitors, which have anti-tumor activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from etoposide, and doxorubicin. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.

Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.

Abstract: Nebivolol has been shown to be beneficial in the treatment of cardiovascular diseases such hypertension, congestive heart failure, arterial stiffness and endothelial dysfunction. The present invention features a pharmaceutical composition comprising nebivolol and at least one other active agent, wherein the at least one other active agent is a cardiovascular agent.

Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.

Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.

Abstract: Nebivolol has been shown to be beneficial in the treatment of cardiovascular diseases such hypertension, congestive heart failure, arterial stiffness and endothelial dysfunction. The present invention features a pharmaceutical composition comprising nebivolol and at least one other active agent, wherein the at least one other active agent is a cardiovascular agent.

Abstract: The present invention relates to alkyl-substituted tetrahydropyrans, mixtures containing these alkyl-substituted tetrahydropyrans, their respective use and corresponding flavored products.

Abstract: The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.

Abstract: Novel compounds of the formula I in which R, X and n are as defined herein, are inhibitors of tyrosine kinase and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.

Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Abstract: The invention relates to compositions intended for external topical use comprising a true solution containing a chromane or chromene derivative having formula (I), preferably a flavonoid, dissolved in a suitable solvent. The invention also relates to a method for preparing such compositions and the use of said compositions as sun protection agents for the skin, advantageously as agents having an anti-erythemal, anti-oxidant, anti-radical, anti-inflammatory or vasculotropic activity.

Abstract: The invention relates to any isolated or synthetic compound and, in particular, to compounds having formula which can: modulate the cell specification of neural stem cells, promote the differentiation and subsequent survival of differentiating glial cells and neurones, and promote the differentiation of oligodendrocyte precursor cells into mature oligodendrocytes. In addition, the inventive compounds can reduce the inflammatory component of diseases that affect the nervous system, for example, by reducing activation of the microglia an/or astrocytes and/or by reducing reactive gliosis. The invention also relates to the methods of preparing such compounds and to the use of same in the preparation of a pharmaceutical composition that is intended for the prevention or treatment of diseases that affect the nervous system. More specifically, the inventive compounds have general formula.

Abstract: A compound of formula (1) Including pharmaceutically acceptable salts thereof, wherein: R1 is aryl or heteroaryl optionally substituted with R8; R2 is H or alkyl or CH2 (when forming part of a ring with R3, R4 or R5); R3 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R4 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R5 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R6 is H, alkyl, COH, COOR9, CON(R9)2, COR9, COR10, COR11, P(O)nR9, P(O)nR10S(O)nR10 or S(O)nR9 and can be part of a ring with R2, R3, R4 or R5; R7 is H, alkyl, COOR9, COOR11, COR9 or CON(R9)2, and can be part of a ring with R2, R3, R4, R5 or R6; R8 is alkyl, CF3, OR9, OCOR9, CONH2, CN, F, Cl, Br, I, N(R9)2, NO2, NHCHO, NHCONH2, NHSO2R9, CON(R9)2, S(O)nR9, CH2OH Or OCON(R9)2; R9 is H, alkyl or cycloalkyl; R10 is aryl or heteroaryl (optionally substituted with R8) or a four to seven membered ring (which is optionally substituted with R8 and can contain one or more additional heteroatoms selected from

Abstract: The present invention describes the identification and purification of 7-hydroxychromes that exhibit potent antioxidant activity. In one embodiment the present invention includes a method for providing an antioxidant to a host in need thereof, comprising administering an effective amount of a 7-hydroxychrome or a mixture of 7-hydroxychromones. The present invention includes methods that are effective in inhibiting free radical and oxidation caused damage through the simultaneous suppression of free radical generation and the suppression of the production of reactive oxygen species (ROS). The present invention also includes methods for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes.

Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular naphthoquinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.

Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Abstract: Provided are novel a target and drugs in the treatment of neurological disorders related to amyloid beta pathology/amyloidosis. More specifically, the use of phosphatase inhibitors for the treatment of brain impairments mediated by A?-oligomers is described.

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: The present invention relates to an improved assay for identifying compounds that may be of use in conjunction with cancer chemotherapeutic agents and anti-proliferative agents, to improve efficacy of such agents and/or render effective compounds with relatively little therapeutic activity. There is also provided a class of compounds of formula (I) and retinoids identified by said assay which may be used in a combination therapy, with current and novel agents, to treat cancers and other diseases associated with abnormal host cell proliferation, such as psoriasis.

Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Abstract: Pesticidal compounds of general formula (I) Wherein ?represents a double bond; A— represents ?C(R5)—C(?O)—, wherein R represents hydrogen or halogen, R1 and R2 represent, independently, hydrogen, halogen, alkoxy, substituted alkoxy or an ester group; or R1 and R2, together with the carbon atoms to which they are attached, represent an oxirane ring; or R1 and R2, taken together, represent an alkylidenedioxy or substituted alkylidenedioxy group; and R3 represents —CH2R6, wherein R6 represents an ester group, oxiranyl, or a group of formula wherein R7 represents hydrogen or alkyl, R8 represents phenylsulfanyl, phenylselenyl, phenylsulfoxy or phenylselenoxy, and R9 represents hydrogen, ethoxycarbonyl or carbamoyl and R4 represents, independently, hydrogen, alkoxy or substituted alkoxy; and methods of making the compounds of formula (I) and methods for controlling pests wherein the pest dies as a result of contact with a compound of formula (I).

Abstract: The present invention relates to photosensitive derivatives of optically active L-threo-?-benzyloxyaspartate or its benzene ring-substituted analogs, represented by the following formula (1) or (2): (1) (2) wherein R1 represents hydrogen atom, amino group, straight or branched lower aliphatic acylamino group optionally substituted at the acyl group portion, alicyclic acylamino group or aromatic acylamino group optionally having a substituent on the aromatic ring, R2 represents hydrogen atom or one or more straight or branched optionally substituted lower aliphatic alkyloxy groups on the benzene ring, R3 represents hydrogen atom, methyl group or carboxyl group, and R4 and R5 each represent hydrogen atom, hydroxyl group, straight or branched lower alkyloxy group optionally substituted at the alkyl portion, amino group, straight or branched lower alkyl-substituted amino group, or a halogen atom, which upon photoirradiation can produce compounds exhibiting a function of suppressing the glutamate uptake activity o

Abstract: Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R1, R2, R3, R4, R5, and R6 are described herein.

Abstract: This invention relates to a novel herbal composition comprising an extract of flowering and fruiting heads of the plant, Sphaeranthus indicus. The said extract of Sphaeranthus indicus contains a compound, 3a-hydroxy-5a,9-dimethyl-3-methylene-3a,4,5,5a,6,7,8,9b-octahydro-3H-naphtho[1,2-b]furan-2-one (7-Hydroxy-4,11(13)-eudesmadien-12,6-olide) (compound 1), as a bioactive marker. The invention also relates to a composition comprising 3a-hydroxy-5a,9-dimethyl-3-methylene-3a,4,5,5a,6,7,8,9b-octahydro-3H-naphtho[1,2-b]furan-2-one (compound 1) as an active ingredient. The invention also relates to methods of manufacture of the said compositions. The invention also relates to methods of administration of the said compositions to a subject in need of treatment for an inflammatory disorder. The invention also relates to tumor necrosis factor- (TNF-?) and interleukin (IL-1, IL-6, IL-8) inhibitory activity of the said compositions.

Abstract: A compound of general formula (I): wherein Xi is H or COR1 and X2 is H or COR2 but X1 and X2 are not both H; R1 and R2 are the same or different and are each C1-4 alkyl substituted with R3, or a four to seven-membered ring which can be optionally substituted with R8 and can contain one or more additional heteroatoms selected from O, S(O)n and NR9; R3 is F, CF3, OR4, NR5R6 or S(O)nR7; R4, R5 and R6 are the same or different and are each H or C1-4 alkyl optionally substituted with R3, or NR5R6 is a C4-6 heterocycloalkyl ring containing one or more heteroatoms selected from O, NR8 and S(O)n; each n is 0-2; R7 is C1-4 alkyl; R8 is as defined for R3 or C1-4 alkyl optionally substituted with R3 or halogen; R9 is H or C1-4 alkyl; Y is NR9R10R11; and R10 and R11, are the same or different and are each H or C1-6 alkyl optionally substituted with R3 or halogen, or NR10R11, is a four to seven membered ring which can be optionally substituted with R8 or COR1, and can contain one or more additional heteroatoms selected fr

Abstract: This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-?, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.

Abstract: A preparation process is provided for preparing a novel flavonoid compound having a high level of antioxidative action. The flavonoid compound is obtained by subjecting hesperidin to microbial fermentation treatment with Aspergillus saitoi.

Abstract: The present invention describes leucascandrolide analogs of the formula (I), intermediates of the formula (III), pharmaceutical compositions containing the same, methods for preventing cell proliferation, and methods for treating cancers and other proliferative diseases.

Abstract: The present invention provides a novel method for inhibiting sugar-induced weight gain resulting from fructose and glucose driven lipogenesis. The method for inhibiting sugar-induced weight gain is comprised of administering a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the Scutellaria and Acacia genus of plants to a host in need thereof. The present also includes novel methods for the prevention and treatment of diseases and conditions resulting from high carbohydrate ingestion. The method for preventing and treating these sugar-induced diseases and conditions is comprised of administering to a host in need thereof a therapeutically effective amount of a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the Scutellaria and Acacia genus of plants and a pharmaceutically acceptable carrier.

Abstract: Internally masked neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.

Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, R, R1, R2, R3 and n are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.

Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

Abstract: A compound of formula (1) wherein X is H or —OCR1 and Y is H or —OCR2, provided that X and Y are not both H; and R is CH2OR9, CONR11R12, CN, tetrazole or COOR17; or a salt thereof, has therapeutic utility.

Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.

Abstract: The present invention is directed to the use of sterol absorption inhibiting compounds, pharmaceutical compositions thereof, therapeutic combinations and their use in combination with other lipid lowering agents to treat or prevent sitosterolemia and/or to lower the concentration of sterol(s) other than cholesterol in plasma or tissue of a mammal. Methods of treating or preventing vascular disease and coronary events also are provided.

Abstract: The present invention relates to an environmental friendly antifouling agent, and more particularly, to a novel Sargassum-derived antifouling agent which is harmless to environment, has antifouling activity against a broad spectrum of fouling organisms, can be extracted from nature, resulting in a relative reduction in production cost as compared with the existing antifouling substances, and can effectively prevent the pollution of marine environment caused by the use of toxic antifouling agents, such as TBT.