Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The invention relates to Cebranopadol or a physiologically acceptable salt thereof for use in the treatment or the prevention of pain and/or opioid drug dependence in a subject with impaired hepatic and/or renal function.

Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and their uses for the treatment of REM sleep behavior disorder.

Abstract: The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and/or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis.

Abstract: The present disclosure relates to methods for treating a neurodegenerative disorder by administering an effective amount of an agent that inhibits or reduces translation of amyloid precursor protein. In some embodiments, the neurodegenerative disorder is Alzheimer's disease or Down syndrome. Also disclosed are methods for decreasing amyloid-beta production in a subject's brain. Further disclosed is a method for restoring or maintaining iron homeostasis in a subject's brain.

Abstract: The present invention encompasses combinations comprising a plurality of amino acids, formulations thereof for use in humans and animals, as well as methods for increasing muscle protein synthesis, muscle strength, and/or muscle function in a subject with chronic heart failure, cardiac cachexia or a combination thereof.

Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to 1,9-diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Abstract: Described herein are polymeric nanoparticles that comprise 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]-triazolo-[3,4-fJ[1,6]-naphthyridin-3-one (Compound A), or a pharmaceutically acceptable salt thereof, and methods of making and using such nanoparticles. The nanoparticle comprises about 50 to about 99.8 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic acid-co-glycolic acid)-poly(ethylene)glycol copolymer, wherein the total amount of poly(ethylene)glycol in the nanoparticle is about 10 to about 30 weight percent poly(ethylene)glycol and about 0.2 to about 30 weight percent of Compound A.

Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.

Abstract: The present invention provides a method for treating an allergy disease or disorder or symptoms related thereto, in a subject in need thereof, the method comprising: administering a therapeutically effective amount of an anti-allergy benzocycloheptathiophene derivative compound of Formula I: or a pharmaceutically acceptable salt thereof, solvate, or prodrug thereof, and a pharmaceutically acceptable carrier, vehicle or excipient.

Abstract: The invention provides pharmaceutical stable semisolid topical compositions comprising between 0.2 to 5% of a des-fluoroquinolone compound, and a suitable carrier to manufacture an ointment or a cream.

Abstract: The present invention relates to the field of molecular biology and cancer biology. Specifically, the present invention relates to methods of treating a subject with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on genotyping and expression profiling of certain immunological genes and RAS mutation status in the subject.

Abstract: A liposome of irinotecan or irinotecan hydrochloride and its preparation method are disclosed. The liposome contains irinotecan or irinotecan hydrochloride, neutral phospholipid and cholesterol, wherein the weight ratio of the cholesterol to the neutral phospholipid is 1:3 to 1:5. The liposome is prepared by an ion gradient method.

Abstract: Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

Abstract: The disclosure provides extended release pharmaceutical formulations comprising an opioid, particularly buprenorphine, a biocompatible organic solvent, and, optionally, a glycol, for use in the treatment of pain or opioid dependence. The pharmaceutical formulations are in the form of a pharmaceutical solution.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.

Abstract: This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.

Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.

Abstract: This invention provides a method for treating a subject afflicted with glioblastoma multiforme comprising administering a therapeutically effective regimen of temoxolomide to be glioblastoma multiforme-afflicted subject, wherein the subject's glioblastoma multiforme cells are known to be caveolin-1-positive. This invention also provides a method for determining whether a subject afflicted with glioblastoma multiforme is likely to progress therapeutically in response to a therapeutically effective regimen of temoxolomide comprising determining whether the subject's glioblastoma multiforme cells are caveolin-1-positive, whereby if the subject's glioblastoma multiforme cells are caveolin-1-positive, the subject is likely to progress therapeutically in response to a therapeutically effective regimen of temozolomide.

Abstract: The present invention relates to a pharmaceutical composition comprising posaconazole and a carrier material, wherein the carrier material comprises a vinylpyrrolidone-vinyl acetate copolymer or a polymer containing ethylene glycol units. The present invention also relates to a method for the preparation of the pharmaceutical composition, a method for the prevention and/or treatment of fungal infections and related diseases in a mammal using the pharmaceutical composition, and a pharmaceutical formulation comprising the pharmaceutical composition.

Abstract: Disclosed herein are protein kinase inhibitors, more particularly pyridazine derivatives and pharmaceutical compositions thereof, and method of use thereof.

Abstract: The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents.

Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A? are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR?SO2—R?, etc., where R? and R? are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and Ro and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2? are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.

Abstract: Disclosed herein are compositions and methods for the treatment of pulmonary hypertension, including pulmonary arterial hypertension. The methods include administering to a patient in need thereof an effective amount of anagrelide or derivative thereof. The compositions include an effective amount of anagrelide or derivative thereof, in some instances combined with one or more additional agents for the treatment of pulmonary hypertension.

Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.

Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and a partner drug, processes for the preparation thereof, and their use to treat certain diseases.

Abstract: A cell permeable iron chelator, optionally in combination with an autophagy inhibiting agent, is used for treating a solid cancer tumor in a person. A preferred chelator is an alkyl substituted N-(1-pyridine-2-yl-methylidene)-N-(9H-1,3,4,9-tetraaza-fluoren-2-yl)-hydrazine. A preferred autophagy inhibiting agent is chloroquine. Also disclosed is a pharmaceutical composition comprising iron chelator, pharmaceutically acceptable carrier and, optionally, autophagy inhibiting agent; and a method of treating cancer by administering cancer combating-effective amount(s) of the iron chelator or the combination of iron chelator and autophagy inhibiting agent.

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

Abstract: Provided are novel compounds which are capable of inhibiting an activity of RNA polymerase I, and uses thereof in treating diseases or disorders modulated by RNA polymerase I, preferably autoimmune diseases such as multiple sclerosis and proliferative diseases.

Abstract: A method of treating a condition of in a human patient comprising pharmacologically activating a translocator protein of 18 kDa (TSPO), wherein the condition is one of a chronic methamphetamine addiction, a medical consequence of methamphetamine use; a behavioral consequence of methamphetamine use, an HIV associated cognitive motor disorder, an HIV-associated neurodegenerative disorder, and a neuroinflammatory response.

Abstract: The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.

Abstract: Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.

Abstract: In one aspect, the invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by providing to an animal in need thereof an effective amount of a compound. 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 provides aza-heteroaryl derivatives of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A, W, R4, R5, and R6 are defined herein, that inhibit the activity of phosphoinositide 3-kinases-gamma (PI3K?) and are useful in the treatment of diseases related to the activity of PI3K? including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

Abstract: The present invention is directed to methods of treating or preventing fibrosis comprising an oxidized lipid or pharmaceutical composition comprising the same.

Abstract: New drugs useful in the prevention or treatment of constipation are provided, in which SGLT1 inhibiting compounds, in particular, a 4-isopropylphenyl glucitol compound represented by the following formula (I), or pharmaceutically acceptable salts thereof are contained as an active ingredient:

Abstract: Phosphoramidate derivates of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.

Abstract: A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.

Abstract: The invention relates to a novel use of a pharmaceutical composition comprising at least one methyl cyclodextrin having a molar substitution (MS) degree of between 0.05 and 1.5 in the treatment and/or prevention of diseases that can be treated and/or prevented by an increase in the HDL cholesterol level. The invention also relates to the use thereof in the treatment and/or prevention of atherosclerosis or complications relating to an atheroma, and/or diseases of the central nervous system. The pharmaceutical compositions of the invention can also be used to stimulate the reduction of circulating fatty acid and triglyceride levels and to reduce or prevent atheromatous plaques.

Abstract: Described herein are methods of treating a subject that has been or will be exposed to radiation, trauma or shock, the method comprising identifying a subject that has been or will be exposed to radiation, and treating the subject with a compound that treats, reduces the severity or delays the onset of sepsis or reduces the likelihood of mortality in a subject upon administration of a therapeutically effective amount the compound to the subject.

Abstract: The present invention relates to the use of hydroxymethyl-group-containing glycosaminoglycans, such as in particular hydroxymethyl-hyaluronic acid, for the treatment and prevention of infectious diseases or malignant or premalignant diseases, in particular of the skin or mucosa. The invention additionally provides a preparation method for glycosaminoglycans modified with hydroxymethyl groups.

Abstract: The subject matter of the invention relates to the method of administering the polypropyleneimine dendrimer of the fourth generation, coated with maltotriose, of a general formula I, wherein 25 to 45% of R substituents stand for a maltotriose residue and each of the remaining R substituents is H, to a human subject. The dendrimer of the formula I is designated in short as PPI-G4-OS-Mal-III, where PPI-G4 stands for the 4th generation of polypropyleneimine dendrimer, OS (Open Shell)—for open coat, Mal-III for maltotriose (trisaccharide made of 3 ?-glucose residues).

Abstract: Compositions and methods useful in treating dermatological disorders are described. The methods include applying to the skin a composition comprising a reactive reinforcing component and a cross-linking component, wherein the cross-linking component facilitates a reaction to form a film in situ on the skin.

Abstract: The invention disclosed provides means of inhibiting, ameliorating, and/or treatment of rheumatoid arthritis through the use of Noble gas containing mixtures. In one embodiment, the invention provides means of reducing inflammation and immune associated pathology through administration of Noble gas mixtures. In one specific embodiment, Xenon gas is administered to a patient in need at concentrations and frequencies sufficient to inhibit inflammatory and autoimmune processes. In another embodiment Noble gas mixtures are administered to reduce pain and provide symptomatic relieve to a patient suffering from rheumatoid arthritis. In another embodiment the use of Noble gas containing mixtures is disclosed as a means of reducing joint destruction through inhibition of matrix metalloprotease production and activity.

Abstract: A supplemented antacid formulation comprising at least one primary component and at least one supplemental component. In one embodiment, a primary component is selected from the group consisting of calcium carbonate, magnesium carbonate, and potassium bicarbonate, and a supplemental component is selected from the group consisting of L-glutamine, deglycyrrhizinated licorice, D-limonene, papain, ginger extract, zinc L-carnosine complex, and a probiotic blend. In one further embodiment, a supplemented antacid formulation comprises a plurality of primary components in combination with a plurality of supplemental components, wherein the primary components are selected from the group consisting of calcium carbonate, magnesium carbonate, and potassium bicarbonate, and the supplemental components are selected from the group consisting of L-glutamine, deglycyrrhizinated licorice, D-limonene, papain, ginger extract, zinc L-carnosine complex, and a probiotic blend.

Abstract: A dietary nutritional supplement that provides relief for light to moderate wine consumers who experience headaches triggered by light to moderate wine consumption. The nutritional composition consists of at least one member selected from the group of ingredients consisting of: Molybdenum, Selenium, Vitamin B1, Vitamin B2, Vitamin B3, Vitamin B6, Folic acid, Quercetin, and Vitamin E. Alternative embodiments may include nitrogreens. The ingredients for the composition form a synergy with each other to improve metabolism of wine constituents. A method of use requires six sequential weeks of administering the composition in pill form and in predetermined quantities with predetermined amounts of wine. A survey questionnaire is given to experimental subjects to help assess the efficacy of the nutritional composition.

Abstract: The present invention relates to a composition for modulating tumor cell dissemination, in particular metastatic cancer cells. In particular, the invention relates to an agent for modulating metastatic tumor cell dissemination for use in the treatment and/or prevention of a metastatic cancer wherein the agent is a capture agent and/or a chemoattractant for tumor cells. The invention also relates to a product, comprising an agent for modulating metastatic tumor cell dissemination, and to a method of treatment or prevention of cancer.

Abstract: [Problem] The purpose of the present invention is to provide a novel pharmaceutical for use in cellular immunotherapy for the prevention and/or treatment of diseases in which Th2-type cytokines are effective, such as cardiovascular disease and the like. [Solution] The present invention relates to a pharmaceutical containing dendritic cells pulsed with ?-galactosylceramide for the prevention and/or treatment of diseases in which Th2-type cytokines are effective, and a method for producing the same.