Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a COX-2 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.

Abstract: The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them.

Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols according to formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.

Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.

Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The present invention relates to a eutectic mixture wherein poloxamer is added to the poorly soluble drug celecoxib to significantly increase the solubility and bioavailability of celecoxib.

Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.

Abstract: The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component.

Abstract: One subject of the invention is a soap-free, self-foaming gel comprising, in a cosmetically acceptable medium: a) at least one aqueous phase; b) at least one N-acylsarcosine where the acyl radical is a C10-C20 radical in an amount less than 4 wt % relative to the total weight of the composition; c) at least one mineral or organic base in an amount sufficient to dissolve the N-acylsarcosine and produce a pH of 4 to 8; d) at least one amphoteric or zwitterionic surfactant; e) at least one non-ionic surfactant; and f) at least one self-foaming agent. The present invention also relates to a shaving method consisting in applying a self-foaming gel as defined above to the surface of the skin to be shaved, then in shaving the hairs using a razor. The present invention also relates to a method for cleansing the skin and more particularly the face, consisting in applying a self-foaming gel as defined above to the surface, followed by rinsing with water.

Abstract: The present invention provides a novel nanoparticle drug delivery system generated from poly(ortho ester) polymers with sustained drug release capability and can be functionalized to allow for systemic delivery to various organ systems throughout the body. One important aspect of this invention is that the nanoparticle drug delivery system generated from poly(ortho ester) polymers encapsulate several types of drugs in poly(ortho ester) nanoparticles, including but not limited to lipophilic, hydrophilic small and large molecules and also hydrophilic and lipophilic dyes by adopting appropriate emulsion techniques. These poly(ortho ester) nanoparticles are biodegradable, biocompatible and controlled release drug delivery system with zero order kinetics, which can be used in various biomedical applications such as eye-related diseases, cancer, arthritis, etc.

Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.

Abstract: The invention provides compositions and methods for determining the increased risk for recurrence of certain cancers and the likelihood of successful treatment with one or both of chemotherapy and radiation therapy. The methods comprising determining the type of genomic polymorphism present in a predetermined region of the gene of interest isolated from the subject or patient. Also provided are nucleic acid probes and kits for determining a patient's cancer risk and treatment response.

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

Abstract: Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2?, R3, R4, R5, R6, R7, R8, R9 are as described herein.

Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.

Abstract: This invention is to provide multiple specific inhibitors of cytochrome P450 isozyme CYP2C9. These inhibitors can be derived from any combinations with the following compounds including: Tamarixetin, Formononetin, isoliquritigenin, Phloretin, luteolin, Quercitrin, quercetin, myricetin, Wongonin, Puerarin, Genistein, Nordihydroguaiaretic acid, Narigenin, Capillarisin, Chrysin, Fisefin, eriodictyol, 6-Gingerol, Isorhamneti, isoquercitrin, Morin, (+)-Taxifolin, isovitexin, 3-Phenylpropyl Acetate, Oleanolic acid, ursolic acid, ?-Myrcene, cinnamic acid, Luteolin-7-Glucoside, Liquiritin, (+) Limonene, Homoorientin, Swertiamarin, Embelin, Daidzein, Poncirin, (?)-Epicatechin, ergosterol. These natural products can be used to enhance the bioavailability of therapeutic agents (drugs).

Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract: The present invention relates to oral pharmaceutical compositions comprising co-crystals of tramadol and celecoxib and processes for the preparation of these oral pharmaceutical compositions. The present invention also relates to methods of using oral pharmaceutical compositions comprising co-crystals of tramadol and celecoxib as medicaments, more particularly for the treatment of pain.

Abstract: This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections.

Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

Abstract: There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent.

Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.

Abstract: The invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in humans, including three or four active principles selected as: a nucleoside reverse transcriptase inhibitor (NARTI) selected from lamivudine and emtricitabine; a nucleoside or nucleotide reverse transcriptase inhibitor (NARTI) selected from didanosine, abacavir and tenofovir; and the combination of ritonavir with a protease inhibitor (PI) selected from lopinavir, fosamprenavir, atazanavir and darunavir; or an non-nucleoside reverse transcriptase inhibitor (NNRTI) selected from efavirenz and etravirine; for daily administration to said human being one to four days per week.

Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease and related disorders. In particular, the invention concerns compounds which, alone or in combination(s), can effectively modulate synapse function and/or angiogenesis and/or cell stress response. The invention also relates to methods of producing a drug or a drug combination for treating Alzheimer's disease and to methods of treating Alzheimer's disease or a related disorder.

Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.

Abstract: The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.

Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

Abstract: The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component.

Abstract: Compositions and methods to treat lymphoma and cancer are disclosed. In particular, the method teaches treatment of lymphoma and cancer using anti-HERV-K(HML-2) therapies. Further taught are compositions and methods for characterizing patient samples to, for example, select or identify therapeutic options or assess the impact of therapies.

Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.

Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.

Abstract: Pellets are made by combining a direct compression binder and a waxy spheronizing agent. The pellets may further contain additional pharmaceutical ingredients and/or a drug. The pellets may be compressed to form tablets or loaded into a capsule shell for oral administration, and the pellets may or may not have an additional coating.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.

Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

Abstract: The compositions of the present invention comprise a therapeutically effective amount of particles consisting of diphenhydramine or pharmaceutically acceptable salts thereof, optionally in combination with another drug such as pseudoephedrine, or phenylephrine and hydrocodone, in combination with rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol and/or a saccharide. These compositions are useful in treating the symptoms of one or more diseases or conditions in which diphenhydramine (alone or in combination with one or two other drugs) is a therapeutically effective, e.g. allergic rhinitis, sinusitis, upper respiratory tract infections, motion sickness, Parkinson's disease, insomnia, the common cold, and nighttime pain management, particularly for subjects or patients with dysphagia, and people ‘on the move’.

Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.

Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

Abstract: Diuretic bioactivity profiles of phase inversion micronized furosemide and furosemide co-precipitated with Eudragit L100, and mixtures of those formulations with stock furosemide, reduced or eliminated the rapid spike in diuresis associated with immediate release formulations and maintained cumulative urine output. Of the formulations tested, each of a mixture of micronized furosemide with stock furosemide, and Eudragit L100 polymer with stock furosemide demonstrated optimal diuretic bioactivity profiles in subjects.

Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.

Abstract: The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection.

Abstract: The present invention relates to a pharmaceutical dosage form comprising an active ingredient combination of nifedipine or nisoldipine and at least one angiotensin II antagonist and/or at least one diuretic, characterized in that nifedipine or nisoldipine is released in the body in a controlled (modified) manner and the angiotensin II antagonist and/or the diuretic is released rapidly (immediate release (IR)), and also to processes for their preparation, to their use as medicaments and to their use for the prophylaxis, secondary prophylaxis or treatment of disorders.

Abstract: Provided are a variable geometry turbocharger in which a drain pipe from a hydraulic servo drive device can be omitted and in which a member for transmitting power of the hydraulic servo drive device can be efficiently lubricated, and a method of returning oil from the hydraulic servo drive device. The variable geometry turbocharger includes a slide mechanism for changing an opening degree of a nozzle, the hydraulic servo drive device for driving the slide mechanism by hydraulic pressure, and drain flow paths for delivering oil exhausted from the hydraulic servo drive device into an oil return chamber adjacent to a turbocharger body.

Abstract: Methods, compounds and compositions for promoting motor neuron survival and the treatment of a neurodegenerative disorders such as Spinal Muscular Atrophy (SMA) are described herein.

Abstract: This invention provides new lipoxin analogs, compositions containing analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond theoral cavity that are related to periodontal disease using the composition containing lipoxin analogs, COX-2 inhibitors, or both.

Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.