Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.

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

Abstract: The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

Abstract: The present invention relates to an extended release pharmaceutical tablet composition comprising guanfacine comprising: a core containing guanfacine or a pharmaceutically acceptable salt thereof and one or more of pH-independent rate controlling polymer(s) and other pharmaceutically acceptable excipients; optionally a coating over the core as in (a) wherein, the coating comprises one or more of pH-independent rate controlling polymer(s).

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: Disclosed are pharmaceutical compositions, particularly oral dosage forms, which comprise two or more enteric coating materials, either as a coating or as part of a matrix dosage form, and methods of making and using the same. The compositions are characterized by having a sustained release profile at lower pH and an accelerated dissolution profile at higher pH.

Abstract: Methods for therapeutic renal denervation are disclosed herein. One aspect of the present application, for example, is directed to methods that block, reduce and/or inhibit renal sympathetic nerve activity to achieve a reduction in central sympathetic tone. Renal sympathetic nerve activity may be altered or modulated along the afferent and/or efferent pathway. The achieved reduction in central sympathetic tone may carry several therapeutic benefits across many disease states.

Abstract: The present invention relates to a method of controlling pests and/or increasing the health of a plant as compared to a corresponding control plant by treating the cultivated plant, parts of a plant, seed, or their locus of growth with a carboxamide compound.

Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract: The present disclosure describes methods for enhancing an overall cooling sensation of an oral mucosa comprising administering a liquid composition comprising a thickening agent and/or a mucoadhesive polymer, a non-menthol coolant; and contacting the oral mucosa with the liquid composition. The disclosure also describes the liquid compositions.

Abstract: The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.

Abstract: The invention provides for a method for screening compounds that bind to and modulate the hair-specific G-protein coupled receptor, P2RY5. The invention further provides for methods for controlling hair growth by administering a P2RY5 modulating compound to a subject.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as neurodegenerative diseases and heart failure.

Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.

Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

Abstract: An object is to provide a novel therapeutic drug for adult T-cell leukemia having an ATL cell specific antitumor effect. The therapeutic drug for adult T-cell leukemia according to the invention is characterized by containing a compound represented by the formula I or a prodrug thereof, wherein R1 is H, OH, an alkoxy group, an acyl group, or a thioacyl group, R2 is an acyl group, a thioacyl group, CONR7R8, or CSNR7R8 (R7 and R8 being each independently H, an alkyl group containing 1 to 3 carbon atoms, or a phenyl group), or R1 and R2 together may form a ring, X1 and X2 may be the same or different and are each —CR3R4—, —SiR3R4— or oxygen, and R3 and R4 may be the same or different and are each an alkyl group containing 1 to 6 carbon atoms.

Abstract: In the specification and drawings a method of treating cancer is described and shown. The method includes delivering an amount of at least one compound to an area containing a cancer cell. A compound and a method of preparing a compound are also described and shown.

Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and R2 have the meanings given in the description. and at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.

Abstract: This disclosure relates to amides, aryl sulphonamides, aryl ureas, and ?,?-diketones derivatives useful as carboxylesterase esterase inhibitors. The disclosure is also directed to the use of these compounds as selective human intestinal carboxylesterase inhibitors and insect carboxylesterase inhibitors. The disclosure is also directed to pharmaceutical compositions and pesticide formulations containing these compounds, and to methods for treating or ameliorating the toxic effects following administration of drugs such as cancer therapy drugs, treating or ameliorating the effects of a drug overdose, and to the use of the compounds for increasing the effectiveness of insecticides and pesticides.

Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.

Abstract: Disclosed is a process for modifying the morphology and/or polymorphism of an organic substance, which process comprises treating the solid substance, or a solution or dispersion thereof, with one or more amphiphilic proteins.

Abstract: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that exhibits alpha-adrenergic activity and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and/or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.

Abstract: Analogs of 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-napthalenyl)-1-propenyl]benzoic acid and methods of manufacture and use thereof, such as for use in cancer prevention and treatment.

Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae ?wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R

Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.

Abstract: A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia. The composition contains a therapeutically effective amount of a binding-inhibiting compound selected from Compounds 1 through 15, and at least one diluent, carrier or excipient. The Compounds competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions can be administered to a human prior to or after infection by a Norovirus, to prevent or ameliorate an infection.

Abstract: This invention provides a compound of the formula (I): (I) These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor, such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.

Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

Abstract: A fuel cell is provided. The fuel cell includes at least one of a plant essential oil and a plant essential oil ingredient in an effective amount so as to function as a biological repellent.

Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.

Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: The present invention relates to the use of a particular group of carbonylamino derivatives for the treatment or alleviation of a disease or condition relating to certain inflammatory disorders.

Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.

Abstract: The present invention relates to the use of agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, on its own or in association, in obtaining medicaments intended for the treatment of bipolar disorders, especially bipolar disorders of types I and II, and more especially bipolar disorders of type I.

Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

Abstract: Described herein are compositions and articles containing a polymeric matrix and an active liquid intermixed with at least a portion of the polymeric matrix. Methods of making and using the compositions and articles are also described herein.

Abstract: The present invention relates to the use of tranilast and derivatives thereof for the preparation of a pharmaceutical composition for treating and/or preventing a neuronal condition where there is a need of neuroprotection and neuroregeneration. The invention furthermore relates to the use of tranilast and derivatives thereof for the in vitro differentiation of neuronal stem cells and the use of such pre-treated cells for stem cell therapy von neurological conditions.

Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.

Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.

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: The present invention relates to the use of compounds which have the following general formula (I), wherein R1 and R2 are independently selected from optionally substituted aryl, optionally substituted C1 to C12 alkyl and H; and R3 and R4 are independently selected from hydroxy, optionally substituted C1 to C6 alkyl, optionally substituted phenyl and H, in a method of preventing or reducing fouling, particularly in the marine environment. The compounds of the present invention have the considerable advantage of providing the antifouling coating market with an organic alternative to the existing technology which relies heavily on the addition of copper to obtain significant antifouling effects. The compounds we have developed may be used as cheap, easy to prepare additives that do not contain metals and therefore have reduced toxicity in marine environment.

Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.

Abstract: The present invention relates to skin coating compositions and methods and, in particular, to coatings containing an active agent. In some embodiments, the coating may be applied to a skin surface and may be essentially colorless and transparent. In some aspects, the coating comprises a polymer and an active agent, and the polymer may be configured for sustained release of the active agent. In some aspects, the coating forms a barrier essentially impermeable to microorganisms yet permeable to water vapor. The coating may also be flexible and conformable to the surface. The coating may be applied to the skin using any suitable method. In some embodiments, the polymer and/or active agent are dissolved and/or suspended in an alcohol solvent. In some embodiments, the alcohol may function as an antiseptic on skin.

Abstract: The present invention relates to compounds with activity as inhibitors of sAPP? and A? production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.

Abstract: Crystalline form IV of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.