Abstract: The present invention relates to compounds that may be used for binding and imaging tau aggregates and related beta-sheet aggregates including, for example, beta-amyloid aggregates or alpha-synuclein aggregates.

Abstract: The invention provides for treatment of cancers using a rapamycin analog, optionally including bortezomib. In particular, the invention addresses the treatment of bortezomib-resistant cancers using seco-rapamycin and optionally a second proteasome inhibitor. This invention relates to oncology and medicine, and more particularly to treatment of cancer. In particular, rapamycin analogs such as seco-rapamycin may be used advantageously to target the proteasome in cancer cells, optionally in conjunction with proteasome inhibitors such as bortezomib.

Abstract: The disclosure provides methods for predicting and/or determining whether a subject has cancer based on the level of expression of BPTF. The disclosure also provides methods for determining whether a cancer in a subject is progressing or regressing based upon the change of expression levels of BPTF between two time points. The disclosure further provides methods to treat a subject with a cancer by administering a polynucleotide comprising an inhibitory BPTF nucleic acid and/or an agent that inhibits the expression or activity of BPTF.

Abstract: The present invention provides methods of delivering a composition comprising nanoparticles that comprise a macrolide and an albumin by directly injecting the nanoparticle composition into the blood vessel wall or the tissue surrounding the blood vessel wall. The methods can be used for inhibiting negative remodeling or vascular fibrosis in the blood vessel and are useful for treating various diseases.

Abstract: The present invention relates to a pharmaceutical composition containing FK506 derivative for treating a fungal infection caused by the genus Cryptococcus or the genus Candida, and a use thereof. In addition, the present invention relates to a therapeutic agent for fungal infection caused by the genus Cryptococcus or the genus Candida, the therapeutic agent containing FK506 derivative. The pharmaceutical composition of the present invention is harmless to the human body, and can make a great contribution to providing antifungal drugs with an excellent antifungal effect.

Abstract: A method of treating or preventing keratin hyperproliferation skin disorders is set forth. The method includes the administration of an mTOR inhibitor to a subject afflicted with the hyperproliferation disorder. The mTOR inhibitor can be administered to the subject via any means known in the art including oral, topical, and transdermal administration.

Abstract: The present invention provides compositions, and related kits and methods, for formation of hydrogels. The compositions comprise one or more chemically crosslinkable agents dissolved in an aqueous solution to form a precursor solution. The chemically crosslinkable agents useful in the present invention are selected from polymers modified with a molecule selected from acrylate, maleimide, vinylsulfone, N-hydroxysuccinimide, aldehyde, ketone, carbodiimide, carbonate, iodoacetyl, mercaptonicotinamide, quinone, thiol, amine, and combinations thereof. The precursor solution is characterized as being in an aqueous form at a non-physiologic physical-chemical condition and undergoing gelation when in contact with another fluid or body at a physiologic physical-chemical condition.

Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.

Abstract: There are described ROR? modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.

Abstract: This invention relates to use of probiotics, particularly P acidilactici and S boulardii, for use in conjunction with steroids and other immune suppressor agents to ameliorate symptoms of autoimmune diseases, especially disease symptoms arising from the body's production of antibodies against autologous blood cells. The practice of the invention sustains ameliorative response associated with immune suppressor agents while lowering the amount of immune suppressor agents required for treatment.

Abstract: A cocrystal of tiotropium bromide and lactose monohydrate is herein disclosed. In the cocrystal the components tiotropium bromide and lactose are preferably present in an almost stoichiometric ratio. Said cocrystal has a single endothermic event at about 191-193° C. determined by DSC. A process for the preparation of the cocrystal is also disclosed. Preferably, the cocrystal has a particle size distribution of D90<10 ?m. The cocrystal is also disclosed for use as medicament, in particular for the treatment of a respiratory complaint, such as chronic obstructive pulmonary disease (COPD), bronchitis, emphysema and asthma. A pharmaceutical composition comprising the cocrystal as active ingredient is also disclosed, in particular for administration by inhalation. In the latter case, said cocrystal has a mean particle size of 0.5 to 10 ?m, preferably 1 to 6 ?m, more preferably 1.5 to 5 ?m.

Abstract: The present invention relates to a sterile pharmaceutical composition comprising tiotropium or a pharmaceutically acceptable salt thereof, for inhalation via nebulization to a subject (e.g. a human). The invention also relates to a process for preparing the pharmaceutical composition and its use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease (COPD) in a subject.

Abstract: The present disclosure provides methods of using protein kinase inhibitors for treating diseases and conditions, including diseases and conditions associated with activity of any protein kinase selected from Fms protein kinase including any mutations thereof, Kit protein kinase any mutations thereof, Flt-3 protein kinase any mutations thereof and combinations thereof.

Abstract: Aryl-quinolin derivatives for use in inhibiting vasculogenic mimicry, treating diseases characterized by abnormal vascular morphology or function and/or by the presence of vasculogenic mimicry in a subject in need thereof are disclosed. In one embodiment of the invention, the compounds are for use in treating metastatic tumor, hyperproliferative, or angiogenic diseases. In another embodiment of the invention, the compound for use may combine an additional therapeutic agent such as anti-cancer agents, anti-inflammatory agents, anti-proliferative agents, anti-hormonal agents, or any combination thereof for use.

Abstract: This invention provides a method of inducing a lacrimal acinar cell in a tissue to degrade a secretory vesicle and its content protein or proteins from the trans-Golgi network (TGN) by contacting the cells with an effective amount of an agent that induces autophagy. Also provided is a method for treating a mammal suffering from defective trans-Golgi network-secretory vesicle (TGN-SV) sorting by administering to the mammal an effective amount of an agent that induces autophagy in the tissue having the defective TGN-SV.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Abstract: The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and/or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and/or panic episode.

Abstract: The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.

Abstract: The disclosure provides evidence that the abundance of this particular “oncogenic HSP90” species, which is not dictated by HSP90 expression alone, predicts for sensitivity to HSP90 inhibition therapy, and thus is a biomarker for HSP90 therapy. The disclosure also provides evidence that identifying and measuring the abundance of this oncogenic HSP90 species in tumors predicts of response to HSP90 therapy. “Oncogenic HSP90” is defined herein as the HSP90 fraction that represents a cell stress specific form of chaperone complex, that is expanded and constitutively maintained in the tumor cell context, and that may execute functions necessary to maintain the malignant phenotype. Such roles are not only to regulate the folding of overexpressed (i.e. HER2), mutated (i.e. mB-Raf) or chimeric proteins (i.e. Bcr-Abl), but also to facilitate scaffolding and complex formation of molecules involved in aberrantly activated signaling complexes (i.e. STATS, BCL6).

Abstract: A compound delivery device for delivering a plume derived from a propellant and a drug formulation. The drug formulation is in an intranasal dosage form in the form of powder, suspension, dispersion or liquid. The propelled intranasal dosage form is deposited within the olfactory region of the nasal cavity. The drug deposited within the olfactory region is delivered to the brain avoiding the blood-brain-barrier. Hydrofluoroalkane propellant from a pressurized canister is channeled to a diffuser and drug-containing chamber where the intra-nasal dosage form is aerosolized. The aerosolized intra-nasal dosage form passes through a nozzle thus delivering a plume to the olfactory region of a user's nasal cavity.

Abstract: A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N?-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

Abstract: Embodiments of the invention provide methods of treating a disorder or disease characterized by cellular proliferation and migration by co-administering a synergistically effective amount of an mTOR inhibitor and a ?-opioid receptor antagonist.

Abstract: The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity.

Abstract: The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and/or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and/or panic episode.

Abstract: An automated apparatus and method for coating medical devices such as an intravascular stent, are disclosed in the method, a 2-D image of a stent is processed to determine (1) paths along the stent skeletal elements by which a stent secured to a rotating support element can be traversed by a dispenser head whose relative motion with respect to the support element is along the support-element axis, such that some or all of the stent skeletal elements will be traversed (2) the relative speeds of the dispenser head and support element as the dispenser head travels along the paths, and (3), and positions of the dispenser head with respect to a centerline of the stent elements as the dispenser head travels along such paths The rotational speed of the support and relative linear speed of the dispenser are controlled to achieve the desired coating thickness and coating coverage on the upper surfaces, and optionally, the side surfaces, of the stem elements.

Abstract: Novel rapamycin analogues and methods for their production with FKBP and/or MIP inhibitory activity with reduced mTOR inhibitory activity with therapeutic potential e.g. as bacterial virulence inhibitors.

Abstract: The present invention provides nanoparticles, methods of making the nanoparticles, and methods of using the nanoparticles to deliver therapeutic agents and/or imaging agents.

Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.

Abstract: Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.

Abstract: The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and/or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and/or panic episode.

Abstract: Methods and compositions for enhancing fertility and/or inhibiting pregnancy failure, restoring glucose tolerance and/or preventing glucose intolerance and/or maintaining glucose homeostasis and/or inducing or enhancing weight loss, treating dyslipidemia, treating hypertestosteronism or hyperandrogenism, and/or treating type 2 diabetes in an individual in need thereof are provided. These involve compositions that inhibit expression of interferon-gamma (IFN-?) or a downstream IFN-?-stimulated gene, which is preferably a macrolide immunosuppressant compound.

Abstract: The present invention relates to methods for improving muscle strength and treating muscular dystrophy.

Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-member

Abstract: This invention relates to use of probiotics, particularly P acidilactici and S boulardii, for use in conjunction with steroids and other immune suppressor agents to ameliorate symptoms of autoimmune diseases, especially disease symptoms arising from the body's production of antibodies against autologous blood cells. The practice of the invention sustains ameliorative response associated with immune suppressor agents while lowering the amount of immune suppressor agents required for treatment.

Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.

Abstract: The invention provides compounds having the formula: wherein R1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof. The disclosed compounds have CCR1 antagonist activity.

Abstract: An antimicrobial therapeutic hydrogel composition comprises a pharmaceutical and/or medical grade silver salt, and an Aloe vera gel or extract. The composition could also include stabilizing agents, a non-ionic surfactant, polyol, and hydrophilic hygroscopic polymers. The resulting product has potent antimicrobial activity against bacteria, protozoa, fungi and viruses. The antimicrobial therapeutic composition can serve as a treatment for burns and as a wound/lesion dressing that either donates or receives moisture to provide a physiologic environment for accelerated wound healing and the relief of pain.

Abstract: The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol.

Abstract: Provided herein are methods and systems of molecular profiling of diseases, such as cancer. In some embodiments, the molecular profiling can be used to identify treatments for a disease, such as treatments that were not initially identified as a treatment for the disease or not expected to be a treatment for a particular disease.

Abstract: The present invention relates to functional composite particles for the oral care sector, more particularly for toothpastes and mouthwashes, which are charged with active ingredients which ensure a long-term antimicrobial or antibacterial effect in the oral cavity and hence reduce the formation of plaque and halitosis. The invention further relates to a process for producing these composite particles and also to their use for producing oral hygiene articles.

Abstract: The present invention relates to methods for synthesizing tiotropium bromide following the scheme: Using the above scheme, tiotropium bromide (compound 6C) is obtained under mild conditions and with high yields.

Abstract: Composition and method for preventing and/or treating dementia and ameliorating memory impairment and/or improving memory, comprising one or more arylnaphthalene lignan derivatives, namely Justicidin A, 5-methoxyjusticidin A, Chinensinaphthol, and a pharmaceutically-acceptable salt thereof, as active ingredient.

Abstract: A method of treating or preventing keratin hyperproliferation skin disorders is set forth. The method includes the administration of an mTOR inhibitor to a subject afflicted with the hyperproliferation disorder. The mTOR inhibitor can be administered to the subject via any means known in the art including oral, topical, and transdermal administration.

Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.

Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.

Abstract: The present invention relates to a method of suppressing organ rejection in a patient receiving an organ transplant by initiating oral treatment with a once-daily extended release tacrolimus dosage form, for example, at an initial dose of from about 0.15 to about 0.20 mg/kg/day within 24 or 48 hours following transplantation. The once-daily extended release tacrolimus dosage form (i) provides low fluctuation and/or swing of tacrolimus, (ii) provides a significantly lower Cmax than an immediate release formulation of tacrolimus while providing the same or greater area under the curve (AUC), (iii) releases the tacrolimus substantially in the colon and/or the lower ileum, (iv) releases at most 63.5% of the tacrolimus in the dosage form at the 12 hour time point, or (v) any combination of any of the foregoing.

Abstract: This invention relates to new water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins. More particularly the invention relates to new water-soluble solid pharmaceutical inclusion complexes and their solutions in aqueous solvents, said compositions containing a) as an active ingredient a macrolide such as Rapamycin, Pimecrolimus, Temsirolimus, Everolimus or Tacrolimus in an amorphous form and optionally in the form of their polymorphic hydrates or solvates e.g. solvates formed with acetone or ethanol. b) a large surface cyclodextrin, such as gamma cyclodextrin—whereby the weight ratio of said macrolide to said cyclodextrin ranges between 1:111 and 1:333.

Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the general formula:

Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.