Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Disclosed are methods of enhancing cognitive impairment in a patient wherein the cognitive impairment is due to ADDL neurotoxicity. The methods employ non-peptidic compounds having a molecular weight of less than 1000 and which can antagonize against formation of neurotoxic ADDLs from A?1-42 monomers.

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer, stereoisomer or deuterated analogue thereof, wherein X, R, R1, R2, R3, R4, M1, M2, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.

Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).

Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.

Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.

Abstract: The invention provides a screening assay for selecting inhibitors of NFAT:Transcription factor interactions. The invention also provides compositions and methods for inhibiting immune response in a subject.

Abstract: In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.

Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.

Abstract: Provided herein are bioactive agents comprising a compound that inhibits the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR) and that is linked to a macromolecule that interacts with a cell that expresses CFTR. The bioactive agents described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.

Abstract: The present invention provides new ?-phenylethylidenehydrazine derivatives, processes for preparing them and their use as pharmaceutical compostions.

Abstract: The present invention provides materials and methods for modulating an immune response. The materials and methods may be used to treat diseases associated with an aberrant immune response. In some embodiments, materials and methods of the invention may be used to treat autoimmune diseases, for example, rheumatoid arthritis.

Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: A composition comprises surface-modified nanoparticles of at least one amphoteric metal oxide or oxyhydroxide. The nanoparticles bear, on at least a portion of their surfaces, a surface modification comprising (i) at least one surface modifier selected from lactate, thiolactate, and mixtures thereof, and (ii) at least one surface modifier selected from halide, nitrate, acetate, carbonate, formate, propionate, sulfate, bromate, perchlorate, tribromoacetate, trichloroacetate, trifluoroacetate, carboxylate comprising from one to about four alkyleneoxy moieties, chlorate, and mixtures thereof.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: The present invention provides, inter alia, methods for ameliorating an adverse effect in a patient caused by an acute transfusion into the patient of a composition containing aged red blood cells using an iron chelator. Apparatuses and kits for ameliorating such adverse effects are also provided.

Abstract: Subjects having elevated signaling of a mammalian target of rapamycin (mTOR) are treated with compositions that include at least one compound that activates a Group 1 mGluR. In an embodiment, the subject has tuberous sclerosis complex (TSC). In an embodiment, the compound is a Group 1 mGluR agonist. In another embodiment, the compound is a Group 1 mGluR positive allosteric modulator.

Abstract: Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described.

Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Disclosed herein are compositions comprising a compound represented by structural formula (I): 2 g of which is reconstitutable in 10 mL of a water in less than 10 minutes, and methods for preparing these compositions. Also disclosed are compositions comprising a compound represented by structural formula (I) and a pharmaceutically acceptable excipient, wherein the molar ratio of said compound to said excipient is from 1:20 to 1:1, and methods for preparing these compositions.

Abstract: The present invention provides an effective method and composition for the prevention, amelioration or control of external parasites on a human or animal via the administration of a prophylactically, therapeutically or pharmaceutically effective amount of a neuronal sodium channel antagonist to a human or animal in need thereof.

Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.

Abstract: The present invention provides new ?-phenylethylidenehydrazine derivatives, processes for preparing them and their use as pharmaceutical compostions.

Abstract: A copolymer obtainable by polymerization of a) at least one compound of the formula (I) (monomer ?) where R1 and R2, independently of one another, are in each case H or CH3, R3 is C6-C10-aryl or C7-C12-aralkyl which can carry one or more identical or different C1-C9-alkyl and/or C1-C5-alkoxy substituents, and n is an integer from 0 to 100, b) at least one compound chosen from the group of N-vinylamides, N-vinyllactams, N-vinylimines and N-vinylamines with 2 to 15 carbon atoms (monomer ?), c) if appropriate one or more different difunctional crosslinker components and d) if appropriate one or more different regulators and e) if appropriate one or more further copolymerizable components (monomer ?) is useful for increasing the systemicity of a pesticide.

Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.

Abstract: A method is disclosed for treating hyperproliferative body surface lesions, including cancerous or precancerous lesion, such as warts or anogenital cancers, by applying a polyaryl mononitro- or dinitrophenylhydrazone such as (I) wherein R1 is hydrogen, hydroxy, 2- or 4-hydroxyphenyl, acetate, nitroso, phosphate, azido, nitrile, amino, dimethylamino, sulfate, methylsulfonate, phosphate, succinate or another water soluble electrophilic group capable of hydrogen bonding; R2 is C6H4OH, C6H4N3, C6H4CN, 4-HO—C6H4—C6H4, C6H4OPO2OH, C6H4OSO2H, C6H4NH2, C6H4NHMe2, C6H4OSO2Me, C6H4OCO(CH2)xCO2H, or C6H5Cl; and X is C6H3-2,4(NO2)2, C6H4-4(NO2), C6H4-3(NO2), or C6H3-2,4(NO2)2. In a particular example, R1 is OH, R2 is C6H4OH and X is C6H3-2,4(NO2)2.

Abstract: A composition of matter is disclosed that comprises a compound of the formula: wherein R1 is selected from the group consisting of unsubstituted and substituted biphenyl moieties, unsubstituted and substituted fluorenyl moieties, unsubstituted and substituted carbazolyl moieties, and unsubstituted and substituted pyridyl moieties; and R2 is hydrogen or alkyl. The compositions are useful as insecticides, acaricides, and fungicides.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: This invention relates to methods for treating retinopathy and repairing tissue damage. The methods include administering to a subject in need thereof an effective amount of one or more compounds of the following formula. Each variable in this formula is defined in the specification.

Abstract: The present invention is directed to methods of enhancing insulin release, GLP-1 release, and insulin sensitivity, methods of increasing insulin gene expression, methods of decreasing gastric secretion and emptying and glucagons secretion, and methods of inhibiting food intake, and methods of treating diabetes mellitus, insulin resistance syndrome, hyperglycemia, and obesity comprising administering to a subject an effective amount of a TRPM5 inhibitor.

Abstract: The present invention relates to therapeutic compositions for treating or preventing obesity and obesity-related disorders in a subject. The present invention also relates to the use of PGC-1 expression levels to determine the safe dosage range for known or putative respiration uncoupling agents for use as anti-obesity therapeutics. The present invention further relates to methods for identifying new compounds that have respiration uncoupling activity.

Abstract: Provided herein are bioactive agents comprising a compound that inhibits the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR) and that is linked to a macromolecule that interacts with a cell that expresses CFTR. The bioactive agents described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.

Abstract: This invention relates to a method for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, or tissue injuries. The method includes administering to a subject in need thereof an effective amount of one or more compounds of the following formula. Each variable in this formula is defined in the specification.

Abstract: A fungicidally active compound of the formula: a) wherein Q is —NY—NH—, —N?N—, or X is oxygen, sulfur, sulfoxide, or sulfone; n is 0 or 1; Y is hydrogen, C1–C4 alkanoyl, C1–C4 haloalkanoyl, C1–C6 straight chain or branched alkoxycarbonyl, C1–C4 alkoxy(C1–C4)alkoxycarbonyl, C1–C4 alkyl, or C1–C4 haloalkyl; R1 is C1–C6 alkoxy, C3–C6 branched alkoxy, C3–C6 cycloalkoxy, phenoxy, benzyloxy, C2–C6 alkenyloxy, C2–C6 alkynyloxy, C1–C6 haloalkoxy, silyloxy, (C1–C6 alkoxy)-carbonylmethoxy, C1–C6 thioalkoxy, C1–C6 alkylamino, C1–C6 alkyl, C3–C6 branched alkyl, (C1–C6 alkoxy) C1–C6 alkoxy, or (C1–C6 alkoxy)carbonyl; R2 and R3 are each, independently, hydrogen, halogen, C1–C6 alkyl, C3–C6 branched alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, C1–C6 haloalkoxy, cyano, or (C1–C6 alkoxy)carbonyl; R4 is C1–C6 alkyl; and Z1 and Z2 are each independently, carbon or nitrogen, with the proviso that when Z1 is carbon, X is oxygen, and R2 is hydrogen, then R3 cannot be hydrogen; b) wherein R5 is C1–C6 alkoxy; and R6 and

Abstract: A substituted apicidin derivative, a method of synthesis therefore, and an anti-tumor composition comprising the same are disclosed. The substituent of the derivative is preferably semicarbazone, thiosemicarbazone, hydrazone, tert-butylhydrazone, phenylhydrazone, 2,4-dinitrophenylhydrazone, 4-methoxyphenylhydrazone, 3-methoxyphenylhydrazone, 4-nitrophenylhydrazone, benzylhydrazone, methanesulfonylhydrazone, benzenesulfonylhydrazone, 4-methylbenzenesulfonylhydrazone, benzoylhydrazone, 4-nitrobenzoylhydrazone, carbohydrazone, benzyloxime or acetoxime. The compound has strong inhibition effect against histone deacetylase and detransforming activities and specifically inhibit growth of cancer cells. Therefore, it is useful in preparation of an anti-tumor composition.

Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.

Abstract: Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.

Abstract: Compounds having the structure: 1

Abstract: The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.

Abstract: Compounds having a structure according to Formula (I): 1

Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): 1

Abstract: Compounds having a structure according to Formula (I): are effective in a method of increasing erythropoietin and vascularization of tissue in a subject in need thereof.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.