Abstract: A ethyl 2-[9-(6-chloro-2-hydroxyquinolin-3-yl)-3,6-diphenyl-1,8-dioxo-3,4,9,10-tetrahydroacridine-10-yl]-acetate compound, its synthesis, and its use as an antimicrobial agent.

Abstract: An 9-(2-hydroxyquinoline-3-yl)-10-[3-(dimethylamino)propyl]-3,4,6,7,9,10-hexahydroacridine-1,8(2H,5H)-dione compound, its synthesis, and its use as an antimicrobial agent.

Abstract: A pharmaceutical composition comprises a taxane (e.g., paclitaxel, docetaxel, cabazitaxel, larotaxel, ortataxel, and/or tesetaxel) in a mixture of first and second surfactants. The absorption of the taxane is increased from the pharmaceutical composition is greater than the sum of the absorption of docetaxel from either the first or the second surfactant. The increase in absorption is especially enhanced when the ratio of the first surfactant to the second surfactant in the pharmaceutical composition is between 60:40 and 85:15 by weight, and the total surfactant weight does not exceed 98% of the total weight. Polysorbate 80, polysorbate 20, and caprylocaproyl polyoxylglycerides serve as suitable first surfactants, and polysorbate 80 or polyethyoxylated castor oil serve as suitable second surfactants. The stability of the pharmaceutical composition may be enhanced by further including a stabilizer (e.g., citric acid and/or ascorbic acid).

Abstract: An 2-[9-(2-hydroxypyridin-3-yl)-1,8-dioxo-1,2,3,4,5,-6,7,8,9,10-decahydroacridin-10-yl]-acetate compound, its synthesis, and its use as an antimicrobial agent.

Abstract: An 9-(2-hydroxypyridin-3-yl)-10-(2-hydroxyethyl)-3,6-diphenyl-3,4,6,7,9,10-hexahydroacridine1,8(2H,5H)-dione compound, its synthesis, and its use as an antimicrobial agent.

Abstract: An 9-(2-hydroxypyridin-3-yl)-10-(2-phenyletnyl)-3,3,6,6-tetramethyl-3,4,6,7,9,10-hexahydroacridine1,8(2H,5H)-dione compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Described herein are PPAR? agonists, including, but not limited to, endocannabinoids that can be used for treatment of a neuropsychiatric disorder and/or symptom thereof. Also described herein are pharmaceutical formulations containing an effective amount of a PPAR? agonists, including but not limited to endocannabinoids, where the effective amount is effective for treating a neuropsychiatric disorder and/or symptom thereof. Also described herein are methods of treating a neuropsychiatric disorder and/or a symptom thereof in a subject in need thereof.

Abstract: The invention provides 20-nor-salvinorin A, an analog of the kappa-opioid agonist salvinorin A. The 20-nor-salvinorin A is an active kappa-opioid modulator and can be used for treatment of medical conditions wherein modulation of the kappa-opioid receptor is medically indicated, such as pain, pruritis, depression, or inflammation, or conditions implicating perception and consciousness. 20-nor-salvinorin A can be less additive when used in treatment compared to a mu-opioid receptor agonist, and 20-nor-salvinorin A is more stable in vivo than is parent compound salvinorin A. The invention further provides synthetic intermediates and procedures for preparation of 20-nor-salvinorin A.

Abstract: Local delivery formulations of the antineoplastic and microbicide agent acriflavine, and methods of making and using thereof are significantly more efficacious at increasing the median survival of subjects with proliferative disease than systemic administrations of acriflavine. The local delivery formulations of acriflavine show a dose-dependent increase in the median survival of subjects. The local delivery forms provide the increased efficacy without the toxicity associated with systemic administration of the agent.

Abstract: The present technology is directed to compounds, compositions, and methods related to non-morphinan-like mu opioid receptor agonists. Compounds of the present technology demonstrate remarkable potency and selectivity for the mu opioid receptor over the kappa opioid receptor, while also exhibiting a significant reduction (or, essentially, absence) of the negative side effects of many morphine-derived compounds.

Abstract: It relates to the use of compounds of formula (I?), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, as anticancer agents and as agents for generating induced pluripotent stem cells. Compounds of formula (I?), wherein R2? is an alcoxy group, a hydrocarbon chain or a ring system, and R1, R3, and R4 are as defined herein, are dual inhibitors of histone methyltransferases and DNA methyltransferases. It also relates to the compounds of formula (I?), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein R2? is phenyl or 5- to 6-membered heteroaromatic ring, both optionally fused to another rings (i.e., compounds of formula (I)). It also relates to pharmaceutical or veterinary compositions containing compounds of formula (I).

Abstract: The present invention relates to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine salts and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine salts; especially to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride as well as to the use of these salts for preventing or treating migraine or pulmonary hypertension.

Abstract: Provided are a fluoreneol-based monomer, a polymer for preparing a resist underlayer film obtained therefrom, a resist underlayer film composition containing the polymer, and a method for forming a resist underlayer film using the resist underlayer film composition, wherein the fluoreneol-based monomer is represented by Chemical Formula 2 below:

Abstract: The invention includes methods of treating a subject having hepatitis B viral (HBV) infection. In certain embodiments, the method of the invention comprises stimulating the innate cytokine response in macrophages, dendritic cells and/or liver non-parenchymal cells with small molecular STING agonists, thus suppressing HBV replication in hepatocytes. In other embodiments, the method of the invention can be used to treat chronic HBV infections. The invention further provides methods of identifying compounds useful in treating HBV infection in a subject.

Abstract: The present invention relates to methods and compositions for characterization of global cellular changes in response to introduction of viral vector compositions into target cells. It more particularly refers to a method for assessing the quality of a viral vector composition for a transgene transfer into target cells comprising measuring the expression level of at least one biomarker selected in the group consisting of CXCL2 and EREG and/or of at least one biomarker selected in the group consisting of ASPM, AURKB, CENPA, CENPF, CKS1B, E2F8, ERCC6L, FAM83D, KIFC1, MKI67, NEK2, NUSAP1, OIP5, PRC1, RRM2, SGOL1, SPC25, TOP2A and TTK.

Abstract: Compositions of hepatic therapeutic actives from one or more acridone compounds, one or more xanthone compounds, one or more thioxanthone compounds, one or more tocotrienol compounds, and one or more oleanolic triterpenoid compounds. Also, methods for treating various liver diseases or certain cancers with such hepatic therapeutic actives, as well as providing liver health maintenance.

Abstract: Compositions of hepatic therapeutic actives from one or more acridone compounds, one or more xanthone compounds, one or more thioxanthone compounds, one or more tocotrienol compounds, and one or more oleanolic triterpenoid compounds. Also, methods for treating various liver diseases or certain cancers with such hepatic therapeutic actives, as well as providing liver health maintenance.

Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.

Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.

Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End 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: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.

Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.

Abstract: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.

Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.

Abstract: A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.

Abstract: The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.

Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: As disclosed herein, co-administration of pimavanserin with an agent that ameliorates one or more cholinergic abnormalities can have a synergistic effect on the efficacy of the agent. Disclosed herein are compositions which include pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities. Also disclosed herein are methods for ameliorating or treating a disease condition characterized by one or more cholinergic abnormalities that can include administering pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities.

Abstract: The present invention relates to a compound of general formula (I) in which: —R1 and R2 are simultaneously or independently H, OH, OCH3 or a C1-C5 alkyl radical, —R3 and R4 are simultaneously CH3, —or R3 is H and R4 is CH3, CH2CH3 or an isopropyl radical or a phenyl radical, —R5 is a C4-C24 alkyl radical or a 3-phenylpropanyl or 2,2-diphenylethanyl radical.

Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.

Abstract: Described herein are compositions and methods for treating or preventing a sexually transmitted infection in a subject

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, A, X, D1, D2 and Y3 are as defined in the claims. The invention further provides intermediates used in the preparation of these compounds, to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The invention relates to novel hybrid cholinesterase inhibitors containing the melatonin or its oxidation products unit and tetrahydroacridine unit linked via a carbamate bond. Due to the high selectivity of action, which is expressed with high ratio of IC50 for acetylcholinesterase inhibition to IC50 for butyrylcholinesterase inhibition ([IC50(AChE)]/[IC50(BChE)]), the novel compounds may be used in relief and/or treatment of the neurodegenerative diseases, among them the Alzheimer's disease.

Abstract: A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.

Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).

Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. 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: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.

Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an antitumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, said rings being linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.

Abstract: The present invention provides compounds of formula (I) wherein G1, G2, G3, G4, G5, G6, Y1, Y2, Y3, Y4, Y5 and Y6 and p and q are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.