Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).

Abstract: The present invention relates to an anti-inflammatory use of macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A and 7-O-succinyl macrolactin A, which are produced from a novel Bacillus strain of Bacillus polyfermenticus KJS-2 (KCCM10769P). The macrolactin compounds provided by the present invention were confirmed to greatly suppress the expression and formation of inducible nitric oxide synthetase (iNOS) and cyclooxygenase-2 (COX-2) which are proteins related to the formation of inflammatory mediators, and to accordingly inhibit the formation of nitric oxide (NO) and of prostaglandin E2 (PGE2) which are the metabolites of the proteins. In addition, the macrolactin compounds provided by the present invention were confirmed to have excellent effects in inhibiting the formation of tumor necrosis factor-alpha (TNF-?), interleukin-1? (IL-1?), interleukin-6 (IL-6) and granulocyte macrophage colony-stimulating factor (GM-CSF), which are pro-inflammatory cytokines.

Abstract: Disclosed is a compound of formula 1, as shown below, where R1, R2, R3, R4, R5, R6 and R7 are as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin.

Abstract: The present invention relates to rosmarinic acid and to the derivatives thereof, expressed by the compounds of general formula (I), for the use thereof to prevent and/or treat disorders caused by ciguatoxin poisoning and for preparing a pharmaceutical composition for preventing and/or treating disorders caused by ciguatoxin poisoning.

Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

Abstract: This invention provides for novel antiparasitic and pesticidal forms of moxidectin, including a long-acting polymeric implant. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections in animals.

Abstract: The present invention relates generally to the field of lipids and in particular aims at improving lipid absorption, for example under conditions of lipid maldigestion or malabsorption. One embodiment of the present invention relates to a composition comprising a sn-2 monoacylglycerol derivative, wherein the sn-1 and sn-3 positions are blocked by protective groups. The acyl group may be a fatty acid, for example one with anti-inflammatory properties.

Abstract: Provided herein, inter alia, are anticancer polyketides. The uses of the polyketides described herein include treatment of cancer, for example, through regulation of the spliceosome and detection of spliceosome inhibition.

Abstract: Stable formulations of Olopatadine, methods of making such formulations and methods of treatment using such formulations are provided.

Abstract: The present invention provides an aqueous antifungal composition comprising a polyene antifungal compound and a thickening agent. The composition can be used in the protection against the development of fungi on food, feed and agricultural products.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

Abstract: Embodiments of the present invention are directed to methods and dosage forms for treating inflammation and rejection in transplantation injuries with Bryostatin-1, Bryostatin-1 analogs and pharmaceutically acceptable salts thereof.

Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.

Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.

Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.

Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.

Abstract: The present invention provides methods and compositions for modifying fertility in a male mammalian subject by contacting the subject's testis cells, germ cells or sperm with a sufficient amount of a composition comprising a ligand that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Also described are methods for screening a test molecule for its effect on fertility by examining changes in male germ cells, testis cells or sperm resulting from contact with a molecule that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Compositions for modifying fertility in a mammalian subject, e.g., contraceptive products, include a ligand that binds, inhibits or activates a TAS2R receptor in a pharmaceutically acceptable carrier.

Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

Abstract: The present invention provides formulations which may comprise macrocyclic lactones and at least one spirodioxepinoindole derivative or a spirooxepinoindole derivative for combating parasites in birds and mammals. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

Abstract: The present invention provides compositions and methods for treating, preventing, and inhibiting viral replication, viral infections and viral diseases and disorders, comprising the use of artemisinin derivatives having anti-viral activity.

Abstract: The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.

Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).

Abstract: In one aspect, the present invention provides a method for treating colon and/or ovarian cancer in a subject comprising administering to a subject in need thereof a compound of general formula (I): wherein R1-R6, R, -R, Q, Y1, Y2 and n are as defined herein, wherein the compound is present in an amount effective to inhibit colon and/or ovarian tumor metastasis.

Abstract: Methods of treating disorders mediated by ?-catenin comprising administration of Nefopam compounds are provided In particular, the treatment of disorders arising from excessive or undesired expression of ?-catenin is contemplated Said compounds include Nefopam, analogues thereof, prodaigs thereof, and salts and solvates of Nefopam The ?-catenin mediated disorders are preferably selected from the group consisting of fibroproliferative disorders (such as scars, aggressive fibramtoses, and fibroses) and cancer (such as colon cancer, melanoma, liver cancer, ovarian cancer, endometrial cancer, medullobalstoma pilomatricomas, and prostate cancer)

Abstract: The invention provides novel compounds of Formulas (I)-(IV), as described herein. Also provided are compositions of these compounds, method of making the compounds, and methods of using the compounds. The compounds can be used to regulate cholesterol homeostasis and to treat conditions and diseases associated with cholesterol homeostasis, including lysosomal lipid storage disorders such as Niemann-Pick Disease type C.

Abstract: The present invention relates to a long-acting composition for the treatment of an animal in need thereof wherein the composition includes a therapeutically effective amount of a bioactive agent, characterised in that the composition includes a non-aqueous carrier and a solvent system comprising castor oil and at least one cyclic amide.

Abstract: The invention generally relates to environmental friendly pesticide compounds, formulations, methods of preparation and application and utilities thereof. More particularly, the invention relates to pesticide compounds and formulations that include terpenes or terpenoids having chemical formula of (C5H8)n, and its derivatives and analogs thereof, as active insecticidal ingredients; certain botanical essential oils as synergists, and other select ingredients as additives.

Abstract: The discovery of clonally pure populations of serosal cancer stem cells (CSCs) as well as methods of producing CSCs, culturing the CSCs and using them in screening assays, has lead to the development of methods of treating serosal and ovarian cancers by targeting removal or inhibition of the glycocalyx coat surrounding such cells, and includes combination therapies using particular chemotherapeutics in conjunction with glycocalyx inhibitors, as well as the same new chemotherapy treatments without targeting the glycocalyx, where the chemotherapeutic agent is any one of LBH-589 (Panobinostat), NVP-AUY922, LAQ824 (NVP-LAQ824, Dacinostat), colchicine, brefeldin A, diphenyleneiodonium chloride, any combination thereof or another agent identified herein. These treatment methods of the invention can also be used in combination with radiation treatment or other conventional cancer therapy.

Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.

Abstract: The present invention relates to an anti-angiogenic composition containing macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A, and 7-O-succinyl macrolactin A as active ingredients. The macrolactin compounds according to the present invention strongly suppress angiogenesis in in vivo experiments and can be used as a pharmaceutical composition for preventing or treating diseases caused by angiogenesis.

Abstract: In certain aspects, the invention relates to methods of treating proliferative cervical disorders (such as cervical cancer and cervical dysplasia) and treating virus infection by administering artemisinin-related compounds. In certain aspects, the invention relates to methods of treating a tumor induced by an oncogenic virus, methods of killing or inhibiting a squamous cell carcinoma, and methods of inhibiting the replication of a virus, by administering artemisinin-related compounds.

Abstract: The present invention is a method for the treatment of mania and/or bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined.

Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.

Abstract: Biodegradable and nutritionally attractive composition comprising biocidal or antibiotic compounds and/or microbes having bio-adhesion and controlled buoyancy properties are selectively fed to an aquatic organism in open or closed water-bodies, and bioactive components are released upon contact with mucosal tissues such as gill, skin or along the digestive tract of the selected aquatic organism.

Abstract: The present invention relates to novel chemical compounds, to methods for synthesis of such compounds, and to the use of these novel compounds in the synthesis of other chemical compounds that, inter alia, may be used in the treatment of sexual dysfunction, and for eliciting enhancing effects on sexual behavior. The invention also relates to remarkable biological properties of the novel compounds in their capacity of inducing aggressive behavior.

Abstract: The present invention relates to use of DHA analogs and their pharmaceutical compositions for treating ALS, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

Abstract: An avermectin-based topical formulation is disclosed which is useful for prevention and treatment of head lice (Pediculus humanus capitis). This topical formulation may be formulated as a shampoo-condition which comprises an effective amount of avermectin, solubilizers, suspending agents, preservatives, non-ionic surfactants, humectants, a silicone compound, and water. Also disclosed are methods of using the topical formulations disclosed within this specification to treat either a susceptible or treatment-resistant strain of lice, as well as uses in the manufacture of a medicament for treating or preventing a lice infestation from a susceptible or treatment-resistant strain in a human patient.

Abstract: An object of the present invention is to provide a novel antischistosomal agent, and more specifically, to provide a novel drug capable of inhibiting a growth of schistosomes in vivo to prevent development of liver dysfunction due to eggs of the schistosomes in the case of infection with the schistosomes. The novel antischistosomal agent includes as an active ingredient a peroxide derivative. Specifically, the novel antischistosomal agent includes as an active ingredient a peroxide derivative represented by the general formula (I): where C represents an alicyclic hydrocarbon ring group which may be substituted, and n represents an integer of 1 to 6.

Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.

Abstract: Disclosed is a novel C-aryl ansa compound having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. Also provided are a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.

Abstract: A targeted osmotic lysis (TOL) of tumor cells that over-express voltage-gated sodium channels (VGSCs) has been developed that uses a combined therapy of a drug that blocks sodium, potassium-adenosine triphosphatase (Na+, K+-ATPase) that is then followed by an activation of VGSCs, for example, by electrical or pharmacological stimulation. Activation of VGSCs conducts sodium into the cancer cells in much greater amounts than non-cancer cells. Water follows this sodium gradient into the cancer cells, causing swelling and lysis. Because non-cancerous cells do not over-express VGSCs, less sodium and less water will enter the cells, and the non-cancerous cells will not lyse. This method is applicable to all cells that over-express VGSCs, including, but not limited to, highly invasive breast cancer, prostate cancer, small cell lung cancer, non-small cell lung carcinoma, lymphoma, mesothelioma, neuroblastoma, and cervical cancer.

Abstract: The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.

Abstract: The present invention is an aqueous pharmaceutical composition that includes an ionized therapeutic agent, an ionic component and guar gum. The guar gum is present in the composition a concentration sufficient to limit interactions between the ionized therapeutic agent and the ionic component thereby imparting stability to the composition. The composition is preferably at or near physiologic pH. The aqueous pharmaceutical composition has been found particularly useful as an aqueous ophthalmic, otic or nasal composition. The pharmaceutical composition, due to its characteristics, is particularly suitable as an ophthalmic composition.

Abstract: The present invention provides methods and devices related to markers (or biomarkers) associated with chronic lymphocytic leukemia (CLL). Examples of these markers include drivers of CLL progression. The invention contemplates, inter alia, detecting the clonal, including subclonal, profile of CLL in a subject and the presence (or absence) of subclonal driver mutations, and utilizing this information in predicting disease progression, need, timing and/or nature of treatment regimen, and likelihood and frequency of relapse.

Abstract: A method of treating hyperesthesia, paresthesia, dolor, and pruritus caused by an insect or arthropod sting or bite, or a skin contact with a noxious weed or plant is disclosed. The method includes topically applying a dermatological composition containing an avermectin compound to an affected area immediately after said sting or bite, or said skin contact occurs. The method further includes moistening the affected area first prior to application of the dermatological composition.

Abstract: Disclosed are compositions and methods for the inhibition of biofilm formation or reduction of existing or developing biofilms in a patient. These methods also inhibit the aggregation of bacteria that form biofilms in the airways. The methods include administering to a subject that has or is at risk of developing biofilms a compound or formulation that inhibits the formation or polymerization of actin microfilaments or depolymerizes actin microfilaments at or proximal to the site of biofilm formation. Such a compound can be administered in combination with a compound or formulation that inhibits the accumulation or activity of cells that are likely to undergo necrosis at or proximal to the site of biofilm formation (i.e., neutrophils). The methods and compositions can further include the use of anti-DNA and/or anti-mucin compounds, as well as other therapeutic compounds and compositions.

Abstract: Small-molecule scaffolds based on 1,2-diphenylacetylene that accurately replicate the spatial and angular projections of several side chains on both faces of an ?-helix, specifically the i and i+7 side chains on one face, and the i and i+2 side chains on the other. The amphipathic ?-helix mimetic can be used to disrupt disease-promoting protein-protein interactions that are mediated by ?-helices.

Abstract: The present invention relates to a composition consisting of ellagitannins rich extracts originated from plant extracts of the Fagaceae family, for use in a method for improving sexual fitness or wellness of both sexes, the male sexual enhancement, the treatment of sexual dysfunction and the health of the sexual vascular system of both sexes.

Abstract: The present invention relates to a new use of a known medicament. Specifically, the invention relates to methods and compositions for enhancing the therapeutic efficacy of a therapeutic agent by increasing the uptake of the therapeutic agent by target cells, and in particular relates to a pharmaceutical composition comprising a regulating agent of lipid raft/caveolae-dependent endocytic pathway and some therapeutic agents, such as anti-tumor agents. The invention also relates to a method for screening a regulating agent of lipid raft/caveolae-dependent endocytic pathway capable of enhancing the therapeutic efficacy of anti-tumor agents.

Abstract: Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.