Abstract: The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethroid insecticides, and anthelmintics, such as benzimidazoles and imidazothiazoles. The inventive formulation provides a larger duration of parasite control at a faster rate of control. The inventive formula remains effective up to three months from the first application. Moreover, the inventive formulations prevent tick attachment to the animal, thereby providing protection against tick borne diseases. The ectoparasites which may be controlled, treated or prevented by the present invention includes ticks, fleas, mites, mange, lice, mosquitoes, flies and cattle grubs.

Abstract: The present invention provides anhydrous compositions for topical delivery of a medicament comprising (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol, or any combination of any of the foregoing; and (C) an anhydrous vehicle. In an alternate embodiment, the present invention provides anhydrous compositions for topical delivery of a medicament which comprise (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol or any combination of any of the foregoing; (C) an anhydrous vehicle; and (D) a medicament.

Abstract: Disclosed are an Schisandrae fructus extract for inhibition or prevention of influenza and its application, wherein the Schisandrae fructus extract is obtained by water, methanol, or ethanol extraction process and the extract comprises compounds such as schisandrone, benzoylgomisin P, wulignan A1, epigomisin O, epiwulignan A1, and tigloylgomisin P. The extracts and purified compounds of Schisandrae fructus has anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities, therefore the extracts and the purified compounds of Schisandrae fructus can be applied as an inhitibory agent of a pharmaceutical composition for treatment or prevention agent for influenza infection.

Abstract: Nano-sized particles are provided comprising at least one multi-headed amphiphilic compound, in which at least one headgroup of said multi-headed amphiphilic compound is selectively cleavable or contains a selectively cleavable group, and at least one biologically active agent, which is both encapsulated within the nano-particle and non-covalently associated thereto.

Abstract: Tellurium-containing compounds identified for use in a method of treating, or prophylaxis against, a viral infection caused by an influenza virus, uses thereof and pharmaceutical kits and pharmaceutical corn positions comprising the same, are disclosed. The tellurium-containing compounds disclosed herein are suitable for co-administration with an antiviral agent.

Abstract: Provided herein are methods, drug formulations, and dosing regimens for improving cognitive function in a normal or cognitively impaired subject. For instance, methods provided herein comprise administering a GABAA receptor antagonist so that peak concentration of the GABAA receptor antagonist occurs when the subject is asleep.

Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.

Abstract: Several terpene glycosides (e.g., mogroside V, paenoiflorin, geniposide, rubusoside, rebaudioside A, steviol mono-side and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, celecoxib, clofazimine, digoxin, oleandrin, nifedipine, and amiodarone. The use of the diterpene glycoside rubusoside and monoterpene glycoside paenoiflorin increased solubility in all tested compounds. The terpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries.

Abstract: The invention relates to a formulation comprising formoterol and budesonide for use in the treatment of respiratory diseases. The composition further contains HFA 227, PVP and PEG, preferably PVP K25 and PEG 1000.

Abstract: The present invention is a method for the treatment or prevention of migraine 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. The present invention is directed to a method for the treatment and/or prevention of migraine, which includes mono-therapy and alternatively, co-therapy with at least anti-migraine agent.

Abstract: A biologically active composition to treat colorectal cancer includes an extract of the plant Schisandra chinensis and a suitable pharmaceutical formulation. The extract can be at least one of gomisin A, angeloylgomisin H, deoxyschisandrin and gomisin N, showing activities against human tumor cell line HT-29 in the range of about 716 ?M to about 43 ?M. A suitable pharmaceutical formulation can be any one of a pill, a tablet, a capsule, a liquid solution, a liquid suspension, a powder, an intravenous solution, a gel and a suppository form. The extract is prepared by grinding the dried berries, extracting with hexane, extracting the marc with dichloromethane, extracting the dichloromethane soluble fraction with ethyl acetate, removing fatty materials in the dichloromethane-ethyl acetate soluble fraction with hexane, and fractionating the total hexane insoluble material extract using analytical high performance liquid chromatography equipped with automated repeat injection/collection cycles.

Abstract: A method of packaging and applying toxic anti-neoplastic pharmaceutical agents for the prevention and treatment of premalignant and malignant lesions of the skin is described. The packaging of liquid formulations containing these toxic anti-neoplastic agents in plastic or glass bottles with control-flow applicators and caps enables patients to apply such formulations to affected areas of skin without having to have physical contact on the part of their hands with the medicaments.

Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by the Wnt/?-catenin pathway by selecting a subject with a condition mediated by the Wnt/?-catenin pathway and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly inhibiting the Wnt/?-catenin pathway in a subject is also disclosed.

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: Disclosed are compounds based on C- and D-ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.

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 invention relates to the use, or methods (especially with regard to animals, especially human, that are in need of such treatment) comprising the use, of an extract and/or one or more natural compounds from plants or parts of plants, respectively, from a genus selected from the group consisting of Schisandra, Illicium, Kadsura, Steganotaenia and Magnolia, alone or as supplement, as active ingredient in the regulation of body weight and/or fat loss and/or for the management of obesity, either in humans or in animals, to the use of said extract and/or natural compound(s) or mixtures in the manufacture of a pharmaceutical or nutraceutical formulation for the regulation of body weight and/or fat loss and/or for the management of obesity either in humans or in animals. The above extract and/or compound(s) can further be used to reduce one or more adverse metabolic parameters in a subject.

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: This invention is directed to compounds useful as intermediates in the synthesis of lipoxin A4 analogs of the following formulas (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

Abstract: There is disclosed use of certain picro derivatives of cyclolignans for prophylaxis or treatment of diseases or conditions characterised by a hyperactive immune system. Examples of cyclolignans according to the invention include picropodophyllin, deoxypicropodophyllin, anhydropicropodophyllol or deoxyanhydropicropodophyllol.

Abstract: The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C1-4alkyl, —A represents CO(CH2)n or CONH(CH2)n where n=2, 3, 4, or 5, —R1 and R2 are as described herein.

Abstract: Novel methods of treating proliferative disorders characterized by elevated Her-2, and the patient is then administered an effective amount of an HSP90 inhibitor.

Abstract: The present invention relates to compounds that modulate the replication of negative-sense, single-stranded RNA viruses, such as influenza virus, and the use of such compounds. The invention relates to methods for increasing the titer of negative-sense, single-stranded RNA viruses, such as influenza virus, in substrates for virus propagation (e.g., tissue culture). The invention also relates to the use of compounds that decrease virus replication as antiviral agents. The invention further relates to methods for identifying compounds that modulate the replication of negative-sense, single-stranded RNA viruses, in particular, influenza virus.

Abstract: A method of producing water-insoluble anti-cancer drug in the form of particulates, the method including preparing a water-insoluble anti-cancer drug having at least one multiple bond in the structure, and irradiating said water-insoluble anti-cancer drug with a laser beam having a wavelength of a low absorption portion in the vicinity of the foot of an absorption curve on the long wavelength side within the absorption band until said water-insoluble anti-cancer drug is formed into particulates having an average particle diameter of 50 to 200 nm.

Abstract: The present invention relates to naphthoquinone derivatives isolated from solid callus cultures from two species of the palaeotropical plant families Dioncophyllaceae and Ancistrocladaceae. It further relates to methods of their production as well as to their use as antiinfective and antitumoral pharmaceuticals.

Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.

Abstract: The present invention relates to solid forms of 13-(N-Boc-?-isobutylserinyl)-14-?-hydroxybaccatin III 1,14-carbonate (Ortataxel). Amorphous Form A, crystalline Form B, mixtures thereof and processes for preparing them are disclosed. Amorphous Form A is prepared by fast precipitation of Ortataxel from a mixture of acetone and water. Form A transforms in Form B when suspended and stirred in a mixture of ethanol and water for 4-8 hours. If the suspension is stirred for less than 4 hours, mixtures of Form B and Form A are obtained. Form B or mixtures of Forms A and B can also be obtained dissolving Ortataxel in a protic organic solvent, followed by addition of water.

Abstract: The invention relates to the use of 2,2?-cyclolignanes in the cosmetic or pharmaceutical field for inducing, restoring or stimulating the pigmentation of the skin, hair or hairs.

Abstract: Several diterpene glycosides (e.g., rubusoside, rebaudioside, steviol monoside and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, and celecoxib. The use of the diterpene glycoside rubusoside increased solubility in all tested compounds. The diterpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries. Aqueous solutions by using rubusoside to increase the solubility of otherwise insoluble drugs will have several new routes of administration. In addition, aqueous solutions of therapeutic compounds with rubusoside were shown to retain the known pharmacological activity of the compounds.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.

Abstract: The present invention relates to the inhibition of melanogenesis with para-aminobenzoic acid (PABA) and its use in treating melanotic cancer.

Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.

Abstract: Disclosed herein are compositions that exhibit viscosities suitable for injectable formulations. The compositions comprise bioactive agent-loaded microparticles and hyaluronic acid or a salt thereof in a suitable liquid pharmaceutical carrier. Also disclosed are methods of making and using the compositions.

Abstract: The present invention includes both sterilized and unsterilized hemostatic compositions that contain a continuous, biocompatible liquid phase having a solid phase of particles of a biocompatible polymer suitable for use in hemostasis and which is substantially insoluble in the liquid phase, and a discontinuous, biocompatible gaseous phase, each of which is substantially homogenously dispersed throughout the continuous liquid phase, methods for making such compositions, medical devices that contain sterilized hemostatic compositions disposed therein and methods of making such devices.

Abstract: A method of increasing an activity of a podophyllotoxin or a derivative thereof is disclosed. The method comprises contacting the podophyllotoxin or the derivative with a liquid composition having a liquid and nanostructures, each of the nanostructures comprising a core material of the nanometric size surrounded by an envelope of ordered fluid molecules, the core material and the envelope of ordered fluid molecules being in a steady physical state, thereby increasing the activity of the podophyllotoxin or the derivative. Pharmaceutical compositions comprising same and uses thereof are also disclosed.

Abstract: To provide an antiseptics, a detergent, an antimicrobial, a deodorizer against nitrogenous odor, an insecticide, a repellent and a bactericide, containing an ozonized surfactant obtained by adding ozone to a surfactant having at least one olefin-based double bond in a hydrophobic group moiety. These are highly safe to the human body and have features and performance that ordinary surfactants do not have.

Abstract: The present invention relates to the use of vanilloid receptor (VR) antagonists, and more particularly vanilloid receptor 1 (VR1) antagonist, as analgesics in the treatment and/or prohylaxis of cnidaria envenomations.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.

Abstract: This invention is directed to compounds useful as intermediates in the synthesis of lipoxin A4 analogs of the following formulas (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

Abstract: The invention relates to a formulation comprising formoterol and budesonide for use in the treatment of respiratory diseases. The composition further contains HFA 227, PVP and PEG, preferably PVP K25 and PEG 1000.

Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.

Abstract: The present invention relates to the use of insecticides which are selected among GABA antagonists and nicotin receptor agonists/antagonists, if appropriate in combination with at least one gibberellin, as safener for fungicides which have a phytotoxic effect. Moreover, the invention relates to a method of reducing or preventing the phytotoxic effect of fungicides on plants treated therewith or on plants whose seeds or growth substrate have been or are treated with these fungicides. The invention finally also relates to compositions which comprise at least one GABA antagonist, at least one azole fungicide or strobilurin fungicide and, if appropriate, at least one gibberellin, and to compositions which comprise at least one nicotin receptor agonist/antagonist, at least one azole fungicide or strobilurin fungicide and, if appropriate, at least one gibberellin.

Abstract: Compounds which inhibit the insulin-like growth factor-1 receptor (IGF-1 R) and methods for using them for treating IGF-1 R dependent diseases, such as cancer.

Abstract: Inositol derivatives are described that are represented by the structural formula I wherein X is a radical of scyllo-inositol wherein one or more of R1, R2, R3, R4, R5, and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl, or carboxamide and the other of R1, R2, R3, R4, R5, or R6 are hydroxyl, or pharmaceutically acceptable salts thereof. The compounds, compositions comprising same and methods using same are described for use in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, desposition, accumulation or persistence.

Abstract: The invention relates to compounds of the general formula and optionally the enantiomers thereof. These compounds have advantageous pesticidal properties. They are especially suitable for controlling parasites in warm-blooded animals.

Abstract: Membrane permeable prodrugs of creatine phosphate analogs, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate analogs, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine phosphate analogs, or pharmaceutical compositions thereof are disclosed.

Abstract: The present invention relates to agonists of the hTAS2R14 bitter taste receptor and its role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R14 bitter taste transduction or bitter taste response.

Abstract: Nanoparticles made from a select group of lipids and optionally containing a therapeutically active agent are employed in pharmaceutical compositions for delivery to targeted tissues and/or cells for the treatment or diagnosis of such diseases as cancer.