Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.

Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.

Abstract: This invention relates to a pharmaceutical composition for treating cancer, comprising an effective amount of a compound represented by formula (I): wherein R is —CCOCCOCC— or —CCOCCOCCOCC—; and a pharmaceutical acceptable carrier. This invention also relates to a method for treating cancer, comprising administering a therapeutically effective amount of said compound to a subject; and a method for stabilizing G4 structure of telomere by using this compound.

Abstract: A pharmaceutical composition for inhibiting cancer stem cells growth or carcinoma metastasis and an application thereof are disclosed. The pharmaceutical composition includes: a berberine compound; and a pharmaceutically acceptable carrier. The application is the use of the berberine compound in the manufacture of a medicament for the inhibition of cancer stem cell growth or carcinoma metastasis.

Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.

Abstract: Described herein are substituted norindenoisoquinoline compounds, and pharmaceutical compositions and formulations comprising the norindenoisoquinoline compounds. Also described herein are methods for using the compounds for the treatment and/or prevention of topoisomerase mediated diseases, such as cancer.

Abstract: Reduction of HSP27 expression is in beneficial in the treatment of pleural and pulmonary fibrosis and in particular subpleural fibrosis and IPF. Pharmaceutical compositions for this purpose contain an inhibitor of HSP27 and a pharmaceutically acceptable carrier.

Abstract: The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated.

Abstract: We have found that exposure of an aqueous tryptophan solution to window sunlight results in the production of multiple tryptophan photoproducts that have the capability of activating the aryl hydrocarbon receptor and increasing the production of AhR target genes and proteins in hepatocytes. We have isolated three of those photoproducts not previously identified as AhR activators, their chemical identification and synthesis and the demonstration that all three have biologic activities as novel AhR activators. Further, one of the three is a completely novel, not previously described, chemical compound.

Abstract: The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.

Abstract: Hypoxia-activated prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: The invention provides formulations containing sanguinarine, chelerythrine or chelidonine or their salts or extracts containing them, mixed with suitable vehicles and/or excipients, for the treatment of common skin warts and verrucas, anal and vulvar warts and psoriatic plaques.

Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.

Abstract: The invention provides compounds of formula I: (I) wherein A, B, W, Y, Z, R1, R3 and R4 have any of the meanings defined in the specification and their salts as well as additional compounds and their salts. The invention also provides pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer, a bacterial infection or a fungal infection using compounds of the invention.

Abstract: The invention provides novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein, compositions including the compounds and methods of preparing and using the compounds.

Abstract: An anti-inflammatory and anti-fibrotic antioxidant formulation for treatment of hepatic oxidative stress and cirrhosis is disclosed. The antioxidant formulation can further include at least one of a hepatitis C virus-specific or a non-alcoholic steatohepatitis-specific formulation comprising one or more compounds to retard the progression of liver fibrosis and possibly reverse an established fibrosis. Methods of treatment or therapies for treating chronic liver disease and chronic hepatitis are also provided.

Abstract: Described are methods of improving insulin sensitivity, and treating fatty liver disease (including non-alcoholic steatohepatitis (NASH)), by administering specific inhibitors of PKC delta.

Abstract: The invention provides formulations containing sanguinarine, chelerythrine or chelidonine or their salts or extracts containing them, mixed with suitable vehicles and/or excipients, for the treatment of common skin warts and verrucas, anal and vulvar warts and psoriatic plaques.

Abstract: The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla. The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic-D2, Cholinergic (muscarinic) and Serotonergic (5HT2A) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10-der?ethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and ?-yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkabids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla. The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R.

Abstract: The invention pertains to topical pharmaceutical formulations of berberine and its biologically equivalent analogues, such as palmatine and coptisine, for the treatment of rosacea and other red face-related skin disorders. The topical pharmaceutical formulations of this invention contain purified berberine as the primary active drug ingredient at concentrations higher than 0.1%. The invention also pertains to methods of treating rosacea and other red face related skin disorders, such as steroid-induced rosacea-like dermatitis, comprising the administration of topical pharmaceutical formulations that contain berberine or its biologically equivalent analogues, such as palmatine.

Abstract: The invention relates to the utilization of a substance for diagnostic determination of sgk1 (serum and glucocorticoid dependent kinase 1) and to the utilization of an active agent in order to influence sgk1 for therapeutic treatment of diseases associated with disordered activity of the tissue factor and to a diagnostic kit related to such substances or such active agents.

Abstract: The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.

Abstract: Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds.

Abstract: 13-substituted 5,6-dihydrodibenzo[a,g]quinolizinium salt compounds of the general formula (I): processes for the preparation of said compounds, pharmaceutical compositions containing said compounds and the use of said compounds for the manufacture of medicaments suitable for the treatment of cancerous diseases.

Abstract: The present invention relates to methods of using botanical-based compositions to treat or prevent microbial dental disease. The claimed invention is directed to methods of using botanical-based compositions in a rinse, gel- or paste-like form to prevent microbe invasion of dental cavities, including the root canal.

Abstract: The invention provides compounds of formula I: wherein A, B, X, and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds, processes for preparing such compounds, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.

Abstract: Disclosed is a novel crystalline form of topotecan monohydrochloride pentahydrate, which is a pentahydrate of 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3?,4?:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)dione monohydrochloride, corresponding pharmaceutical compositions, methods preparation and/or use thereof to treat anti-viral and/or cancer-related diseases.

Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Abstract: The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an topoisomerase inhibitor for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer. In particular, the present invention relates to such a therapy wherein the topoisomerase inhibitor is irinotecan, or a pharmaceutically acceptable salt thereof, and the disorder is colorectal cancer involving a tumor comprising b-Raf having the V600E mutation.

Abstract: Provided are methods of treating cellulite, the methods comprising applying to skin in need of cellulite treatment a composition comprising paulownin or an extract of Paulownia wood.

Abstract: The present invention relates to the use of butaclamol and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases.

Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.

Abstract: The present invention provides compounds of formula I: formula (I) wherein X1-X4 and R1-R12 have any of the values defined in the specification, as well as salts and prodrugs thereof, which inhibit major molecular mechanisms associated with bacterial cell division and proliferation so as to be useful for the treatment and/or prevention of bacterial infections. The invention also provides compositions comprising these compounds as well as methods for using these compounds to inhibit bacterial cell division and proliferation and to treat bacterial infections.

Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Abstract: The invention provides methods and pharmaceutical compositions for treating certain cancers with compounds of formula (I) wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts and prodrugs.

Abstract: The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.

Abstract: The present invention provides a controlled release pharmaceutical composition which exhibits reduced food effect.

Abstract: We have discovered that p63 inhibition results in increased cellular proliferation. We have also performed a screen for agents capable of increasing cellular proliferation, (e.g., of stem cells such as skin-derived precursors (SKPs)). The invention therefore invention provides compositions, methods, and kits for increasing proliferation of cells, using compounds that decrease p63 expression or activity or using the compounds described herein. The invention also features methods of using these compounds for increasing hair growth, improving skin health, or promoting skin repair in a subject.

Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.

Abstract: The compositions and methods disclosed herein are of use for the treatment and prevention of weight gain and obesity. In particular, the compositions and methods include treatment of weight gain and obesity with berberine and/or berberine analogs alone or in combination thereof to cause a reduction in an individual's weight or prevent weight gain or obesity. In certain embodiments, the weight gain and obesity are associated with administration of anti-psychotic drugs. In an alternative embodiment, the compositions and methods provide berberine or berberine analogs alone or for coadministration with an anti-psychotic agent. In an additional embodiment, the compositions and methods further include a natural product. The usefulness of the present invention is that berberine and berberine analogs do not have synergistic effects with other drugs and administration results in few side effects.

Abstract: Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.

Abstract: The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to patients in need thereof.

Abstract: The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria.

Abstract: In one aspect, the present invention is directed to a stable aqueous composition including (a) SN-38; (b) a sulfoalkyl derivative of a cyclodextrin; and (c) water; in which the concentration of SN-38 in the composition is at least about 0.13 mg/g of the composition. In another aspect, this invention is directed to a process for making the composition which process comprises mixing SN-38 and a sulfoalkyl derivative of a cyclodextrin in an aqueous medium wherein the water content of the mixture is less than about 60% by weight.

Abstract: A method of treating inflammation and joint deterioration in mammals includes administering a therapeutically effective dose of alpha 1A receptor antagonists alone or in combination with a beta 2 adrenergic antagonists or beta 2 adrenergic antagonists and beta 2 adrenergic agonists.

Abstract: The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

Abstract: Isolated and purified chemokine peptides, variants, and derivatives thereof, as well as chemokine peptide analogs, are provided.

Abstract: According to an aspect of the invention, urological medical devices are provided, which comprise a prostatically beneficial agent selected from alpha-adrenergic blockers, antispasmodic agents, anticholinergic/antimuscarinic agents, calcium channel blockers, anti-inflammatory agents, hormone affecting agents, anti-cancer agents, and combinations thereof, among others. The urological medical devices are adapted for implantation or insertion into a subject's urinary tract, whereupon at least a portion of the prostatically beneficial agent is released into the subject's prostatic urethra. The release profile of the prostatically beneficial agent is effective to treat a prostatic disorder, for example, benign prostate hypertrophy, prostate cancer or prostatitis, among others. Other aspects of the invention are directed to treating prostatic disorders.

Abstract: Methods and compositions containing a berberine compound or berberine related or derivative compound are provided for the prevention and treatment of hyperlipidemia, elevated cholesterol, and/or cardiovascular disease in mammalian subjects. The methods and compositions of the invention are effective for prevention and treatment of atherosclerosis, coronary artery disease, angina pectoris, carotid artery disease, stroke, cerebral arteriosclerosis, high blood pressure, myocardial infarction, cerebral infarction, restenosis following balloon angioplasty, intermittent claudication, dyslipidemia post-prandial lipidemia or xanthoma.

Abstract: Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.