Abstract: Novel resorcinol derivatives and methods of preparation and use are presented. These compounds can stimulate angiogenesis as a biological function triggered by the activation of one cannabinoid receptor distinct from CB1 and CB2. Thus, these compounds are specific ligands for one cannabinoid receptor distinct from CB1 and CB2. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.

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 phthalimide derivatives of non-steroidal and/or TNF-? modulating anti-inflammatory compounds as well as the process of obtaining the so-called derivatives, pharmaceutical compositions containing such derivatives and their uses, including use in the treatment of inflammatory diseases, especially those related to chronic inflammatory processes, such as rheumatoid arthritis and intestinal inflammatory diseases (for instance, Chron's disease) and the use of the referred to pharmaceutical compositions as antipyretic, analgesic and platelet antiaggregating medications.

Abstract: The present inventions relate to compositions and methods for imaging and treating atherosclerotic diseases, pathogen infections, and tumors by administering actively targeting magnetic nanoparticles. In particular, the present inventions provide new types of targeting ligands attached to magnetic nanoparticles for magnetic resonance imaging. The use of these targeted magnetic nanoparticles is contemplated as a means to treat atherosclerotic diseases, including but not limited to inhibiting and removing atherosclerotic plaques. Further, actively targeting magnetic nanoparticles are contemplated for use with multiple labels for use in nuclear medicine imaging, computed tomography (CT) techniques and other types of imaging for medical and research applications.

Abstract: Provided herein are compounds of formula (I) as well as compounds of formula (I) which are prodrugs in which the (R7)a-phenyl-S(O)2NH group represents a sulphonamide-bond compound, compositions and methods for preventing or treating gastrointestinal diseases such as inflammatory bowel disease and colorectal cancer, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulphonamide inhibitor as a prodrug or a derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in vivo.

Abstract: Provided herein are methods for treating certain conditions, including fibrosis, inflammatory, and autoimmune conditions, with conjugated compounds having Toll-like receptor modulatory activity.

Abstract: Phosphotyrosine phosphatase (PTP) encoded by PF13_0027 is a desirable drug target for the human malaria parasite Plasmodium falciparum. This PTP is critical for intraerythrocytic parasite development and invasion of erythrocytes by malaria merozoites. Mutation of the PF13_0027 gene or blocking expression of PTP function to create a PTP-null parasite severely attenuates the malaria parasite's ability to survive, making the PTP-null parasite suitable as an attenuated blood-stage parasite vaccine.

Abstract: Methods and systems are described for a rapid and sustainable change in the pigment melanin content of melanocytes of the iris stroma, thereby to change the color of the eye. Also described are nanoparticle compositions for lightening the pigmented tissues or treating a pigmented tissue related disease.

Abstract: The present invention discloses a method to induce fatty liver in an animal. The steps of the method comprise: feeding an animal with a high calorie diet, and injecting a mitochondrial inhibitor into the animal to inhibit the mitochondrial activity of the animal, then resulting in fat accumulation and inflammation in the liver of the animal.

Abstract: The instant application provides methods and compositions for the treatment of male subjects having ulcerative colitis.

Abstract: The present disclosure relates to amphiphilic compounds, self assembling compositions formed from the amphiphilic compounds and methods of making such compositions.

Abstract: Disclosed herein are diagnostic and prognostic methods for determining drug sensitivity and resistance in Ewing's sarcoma patients. Treatments for drug-resistant Ewing's sarcoma are also disclosed. The assays involve the detection of GSTM4 gene expression alone or in combination with other clinical factors. The tests are suitable for diagnosing and monitoring treatment of patients having or suspected of having Ewing's sarcoma. The disclosure also relates to inhibitors of GSTM4 for the treatment of Ewing's sarcoma, including drug-resistant forms thereof.

Abstract: Disclosed are methods and compositions comprising mGluR modulators and procysteine drugs. The methods and compositions can be used to treat subjects with prior addiction in order to reduce drug use, drug seeking or relapse.

Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

Abstract: The Notch signal transduction pathway has been identified as a target for screening and treatment methods for the prevention and/or reduction of short- and long-term UVB-induced skin damage, e.g., the prevention and/or reduction of UVB-induced wrinkles. The invention thus features screening and treatment methods for prevention or reduction of UVB-induced sin damage, and related compositions, e.g., cosmetic compositions.

Abstract: The present invention features a composition for killing fire ants. In some embodiments, the composition comprises an insecticide and a triclosan composition. In some embodiments, the composition is a liquid composition.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.

Abstract: Methods are provided for increasing utrophin promoter activity, utrophin expression or utrophin activity, and treating or reducing the symptoms of muscular dystrophy by administering to a subject in need thereof an effective amount of a composition comprising a utrophin promoter or activity upregulator. Muscular dystrophy includes but is not limited to Duchenne muscular dystrophy, Becker's muscular dystrophy, limb girdle muscular dystrophy, or a disease characterized by mutation or dysregulation of the dystrophin gene or an aberrant or dysfunctional dystrophin.

Abstract: The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine.

Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.

Abstract: The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner.

Abstract: Method of identifying compounds that modulate intermolecular interactions between a target protein and a modifier are disclosed. Pharmaceutical composition comprising compounds that inhibit intermolecular interactions between a target protein and a modifier are disclosed. Methods of treating individual suffering from inflammatory conditions, undesirable immune responses, immunological conditions and bacterial infections are disclosed.

Abstract: The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.

Abstract: Certain embodiments in the present invention provide for methods for therapy of lung diseases and other conditions such as infection are provided. In certain embodiments, the methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e., ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments can include the use of agents to modulate transport of thiol-containing compounds from the cell such as thiocyanate. In certain embodiments, therapeutic methods involve the administration of such agents to a patient afflicted with an inflammatory condition or infection responsive to stimulation of thiol-containing compound transport.

Abstract: Methods and systems are described for a rapid and sustainable change in the pigment melanin content of melanocytes of the iris stroma, thereby to change the color of the eye. Also described are nanoparticle compositions for lightening the pigmented tissues or treating a pigmented tissue related disease.

Abstract: The present disclosure relates to bisphenyl compounds that are useful for inhibiting the ADP-ribosyl cyclase (ADPR-cyclase). More particularly, the disclosed compounds can be used for treatment and prevention of hypertension, hypertensive cardiac hypertrophy, diabetes, and diabetic nephropathy, in which pathogenesis ADPR-cyclase is involved. The compounds and compositions of the invention can be used for treatment and prevention of cardiovascular disease and related disease states, particularly, hypertension or diabetes related disorders, such as, hypertensive cardiac hypertrophy, diabetic nephropathy, and the like.

Abstract: Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active agent and at least one CB1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined KATP channel opening and CB1 antagonistic properties is used.

Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.

Abstract: In this disclosure, methods and systems for drug delivery utilizing high shear are disclosed. In an embodiment, a method comprises (1) subjecting a therapeutic fluid containing a drug to high shear; and (2) obtaining a processed therapeutic fluid, wherein the processed therapeutic fluid contains the drug in nano-size. In an embodiment, a method comprises (1) subjecting a drug carrier and a therapeutic fluid containing a drug to high shear; and (2) obtaining a processed therapeutic fluid, wherein the processed therapeutic fluid contains the drug carrier loaded with the drug. In an embodiment, a method comprises (1) applying high shear to a drug carrier and a therapeutic fluid containing a drug; (2) obtaining a processed therapeutic fluid, wherein the processed therapeutic fluid contains the drug-loaded carrier; and (3) modifying the drug-loaded carrier with a targeting moiety to obtain a modified drug-loaded carrier.

Abstract: Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.

Abstract: The present invention relates to novel triazene compounds, to a process for their preparation, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans. The novel triazene compounds are distinguished, as compared with the known triazene compounds, by improved activity while at the same time having reduced toxicity, that is to say by fewer side-effects.

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: Azido-diarylpyrimidine (azido-DAPY) compounds, and compositions containing such compounds, are provided. In addition, methods of using azido-diarylpyrimidines to inactivate reverse transcriptases, prepare inactivated viruses, and treat or prevent viral infections are also provided.

Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Abstract: Synergistic pesticidal mixtures are provided.

Abstract: The present application relates to processes for the preparation of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate compounds and to pharmaceutical compositions containing said compounds. The application further relates to a method of using the novel intermediates to treat or prevent influenza.

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: This invention relates to novel carboxylic acid 4-phenylazo-phenyl ester derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: Provided are methods and compositions for treating ocular conditions characterized by the presence of unwanted choroidal neovasculature, for example, neovascular age-related macular degeneration. The selectivity and sensitivity of, for example, a photodynamic therapy (PDT)-based approach can be enhanced by combining the PDT with an anti-FasL factor, for example, an anti-FasL neutralizing antibody.

Abstract: An embodiment of the invention provides a pharmaceutical composition comprising a compound of formula (I)a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Another embodiment of the invention provides a method of treating or preventing a condition associated with increased expression and/or activity of an NF?B pathway using same compounds. A further embodiment of the invention provides a method of diagnosing a condition in an individual using same compounds.

Abstract: The compounds, pharmaceutical compositions, and methods of using such compounds or compositions thereof described herein are useful for treating a disease modulated by B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein expression.

Abstract: Described herein are compositions useful in anticancer treatment and prevention. The compositions are composed of (a) an O2-aryl substituted diazeniumdiolate and (b) an amphiphile, wherein the amount of amphiphile is sufficient to produce a liposome or micelle. The compositions described herein provide numerous advantages such as increased solubility and stability of the O2-aryl substituted diazeniumdiolate in vivo. The compositions also do not induce hypotension. Methods for using the compositions in anticancer treatment and prevention are also described herein.

Abstract: The present invention discloses a method to induce fatty liver in an animal. The steps of the method comprise: feeding an animal with a high calorie diet, and injecting a mitochondrial inhibitor into the animal to inhibit the mitochondrial activity of the animal, then resulting in fat accumulation and inflammation in the liver of the animal.

Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include naphthalenesulfones, phenylsulfones, and certain peptides with unnatural amino acids and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

Abstract: The use of enhancers with possibly riboflavin, as well as the corresponding compositions for the treatment of keratoconus or other ectasic corneal disorders by the method of corneal cross-linking.

Abstract: Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described.

Abstract: This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.

Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.