Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).

Abstract: The present invention relates to the field of hematopoietic stem cells. More specifically, the present invention provides methods and composition useful for peripheral blood stem cell mobilization. In one embodiment, a method of treating an organ transplant recipient comprises administering to the recipient a low dose of Tacrolimus in an amount sufficient to mobilize stem cells to the peripheral blood of the recipient. In a specific embodiment, the low dose of Tacrolimus is in the range of about 0.05 mg/kg to about 0.5 mg/kg.

Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).

Abstract: It is provided a method of treating a disorder, the method comprising implanting in a patient an implantable device including a polymer formed of fluorinated monomers and hydrocarbon monomers and another biocompatible polymer.

Abstract: A biobeneficial coating composition for coating an implantable device, such as a drug eluting stent, a method of coating the device with the composition, and an implantable device coated with the composition are provided.

Abstract: It is provided an implantable device including a polymer blend that contains a polymer formed of fluorinated monomers and hydrocarbon monomers and another biocompatible polymer.

Abstract: This invention provides for biocompatible, biodegradable eye drop pharmaceutical formulations useful for the treatment of ocular indications. In particular, tocopherols and their esters of low water solubility, notably ?-tocopheryl acetate, are exceptional vehicles for biocompatible, nonirritating topical eye drop formulations that provide sustained release of active agents.

Abstract: A method for treating a mammal having an infection with an organism that persists intracellularly in a mammalian cell by inducing an autophagy defect includes administering to the mammal an effective dose of a bioavailable agent that restores autophagy function, by inhibition of the mTOR pathway.

Abstract: The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formulas (I)-(XXVI) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.

Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.

Abstract: The invention relates to the use of cystamine, cysteamine, or a salt thereof, or of calcineurin inhibitors for treating a MeCP2-associated disorder such as Rett syndrome.

Abstract: An external medicine of the present invention includes a gel composition or an ointment composition, each of which contains sirolimus and/or a derivative thereof. Accordingly, provided is an external medicine which enables sirolimus, in an amount sufficient to treat a skin disease, to be absorbed into an affected part without causing a side effect.

Abstract: The invention provides methods for treating or preventing an age-related disease, condition, or disorder comprising administering a therapeutically effective amount of an inhibitor of TOR to a patient in need thereof. The invention also provides pharmaceutical compositions and topical formulations for treating or preventing an age-related disease, condition, or disorder comprising an inhibitor of TOR and a pharmaceutically acceptable carrier. In particular, the invention provides methods, pharmaceutical compositions, and topical formulations comprising rapamycin or an analog of rapamycin.

Abstract: A stent is provided in combination with delivery of a tocopherol agent, and in particular a des-methyl tocopherol agent, and further beneficially a gamma-tocopherol agent, so as to reduce restenosis along the vessel or other lumenal wall where the stent is implanted. In particular applications, the stent is an endolumenal stent, and more specific beneficial applications is an endovascular stent, and the gamma-tocopherol elutes from a coating or carrier coupled with the stent. Certain combinations are provided with the des-methyl-tocopherol or phytyl substituted chromanol, e.g. gamma-tocopherol, combined with an additional agent such as an anti-restenosis agent, e.g. sirolimus, tacrolimus, everolimus, or paclitaxel, in order to provide synergistic benefit to tissues along the stented or recanalized regions. Other forms of tocopherol or tocotrienol, or other phytyl substituted chromanols, and other compounds such as palm oil, are ailso contemplated. for use to treat restenosis.

Abstract: A process is described for loading hydrophilic polymer particles with a water-insoluble solvent-soluble drug. The particles are preferably embolic agents. The method provides particles having little or no drug at the surface and in a surface layer, whereby the burst effect is minimised. The drug is precipitated in the core of the particle, leading to extended release. The drug is, for instance, paclitaxel, rapamycin, dexamethasone or ibuprofen.

Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.

Abstract: A medical device includes an implantable structure and a coating layer including a water-insoluble therapeutic agent and one or more additives selected from heparin, heparan sulfate, dextran and dextran sulfate, and physiologically-acceptable salts thereof. The one or more additives can be present in an amount effective to increase the rate of release of the water-insoluble therapeutic agent from the coating layer. The implantable medical device structure can be an expandable structure such as a balloon or stent. Also described are methods of making and using such implantable medical devices and coating layers.

Abstract: Compounds of formula (IIc); wherein X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different; Y1, Y2, Y3 and Y4 independently from each other are N or CR9 wherein R9 may be same or different and wherein up to 3 of the group Y1, Y2, Y3 and Y4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.

Abstract: A method of treating leukemia by administering an H4 agonist of histamine, 7-amino-4,5,6-triethoxy-3-(5,6,7,8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl) phthalide (tritoqualine), to a subject is provided.

Abstract: Compounds according to the general formula (I) wherein X1, X2, X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different, and wherein up to 3 of the group X1, X2, X3 and X4 may be N; A is a 5- or 6-membered aromatic or heteroaromtic cycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S wherein A may be substituted by 1 to 5 substituents R which may be same or different; their solvates, hydrates, and pharmaceutically acceptable salts for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal selected from a cell proliferative disorder, rheumatoid arthritis, increased bone density, aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis).

Abstract: The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent.

Abstract: The present invention provides tacrolimus containing ointment having low dermal irritation and excellent stability. It was found that an ointment comprising triacetin as a solubilizer for tacrolimus may sufficiently solubilize tacrolimus, has low dermal irritation and excellent stability. Preferably, the ointment of the present invention is an o/o type (oil-in-oil type) ointment in which tacrolimus-solubilized triacetin droplets are dispersed in an ointment base, preferably a mixture of beeswax and petrolatum.

Abstract: The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent.

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: One embodiment of an aspect of the present invention is a method for lessening the symptoms of depression, anxiety, and post-traumatic stress disorder comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of depression, anxiety, and post-traumatic stress disorder. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.

Abstract: Medical devices having a catalyst capable of catalyzing the generation of nitric oxide in vivo and methods of treating a vascular condition using the devices are provided.

Abstract: A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.

Abstract: The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.

Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying cancer by administering nanoparticles that comprise rapamycin or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof. The invention further provides combination therapy methods of treating cancer comprising administering to an individual an effective amount of nanoparticles that comprise rapamycin or a derivative thereof and a second therapy.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.

Abstract: Composition for delivery of at least one active principle at the implantation site of an implant device, including: at least one active principle, and at least a first excipient combined with the at least one active principle, wherein the at least a first excipient is selected among fatty acids with a linear or branched, saturated chain, including a number of carbon atoms between 14 and 36.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer as well as sepsis, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.

Abstract: Compounds of formula I?: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I?, processes for preparing compounds of formula I?, intermediates useful for preparing compounds of formula I? and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.

Abstract: The present application teaches a coating having a biologically compatible compound conjugated to, or blended with, a polymer, wherein the polymer includes at least one olefin-derived unit and at least one unit derived from a vinyl alcohol, an allyl alcohol, or derivatives thereof.

Abstract: The invention relates to an intraluminal device, in particular an intraluminal prosthesis, shunt, catheter or local drug delivery device. In order to increase the bio-compatibility of this device, it is provided with at least one coating. The coating contains a therapeutic agent which is comprised in a matrix that sticks to the intraluminal device. Instead of being formed by a little bio-compatible polymer, the matrix is formed by a bio-compatible oil or fat, such as cod-liver oil or olive oil. Preferably, the bio-compatible oil or fat further comprises alfa-tocopherol.

Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable shell containing a drug of abuse within an oil comprising physiologically tolerable unsaturated fatty acids.

Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion containing a drug of abuse.

Abstract: Methods and compositions are provided for treatment of disorders associated with aberrant adrenal cortex cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC), Cushing's syndrome and/or pituitary ACTH excess (Cushing's Disease). Such methods involve administration of an effective amount N-(2,6-bis(1-methylethyl)phenyl)-N?-((1-(4-(dimethylamino)phenyl)cyclopentyl)-methyl)urea hydrochloride to the patient.

Abstract: Medical devices may be utilized for local and regional therapeutic agent delivery. These therapeutic agents or compounds may reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the prevention of thrombosis. The drugs, agents, and/or compounds may also be utilized to treat specific disorders, including restenosis, vulnerable plaque, and atherosclerosis in type 2 diabetic patients.

Abstract: Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: wherein R, R1, R2, X and Y are as defined herein.

Abstract: Embodiments of the present invention include methods of treating, preventing, or ameliorating a vascular disease and/or disorder in a diabetic or pre-diabetic patient. The methods include implanting a stent in a vascular region in a diabetic patient, and during the implantation procedure, delivering a drug formulation from a source other than the stent to the vascular region. The stent may be a bare metal stent, or a drug eluting stent, such as a metal stent having a coating including a drug. The drug may be everolimus, sirolimus, or a combination thereof. The drug formulation may include dexamethasone, paclitaxel, or a combination thereof.

Abstract: The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent.

Abstract: A method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting activating phosphorylation of glutaminase C under conditions effective to reduce production of glutamate from glutamine. Methods for treating or preventing a condition mediated by the activating phosphorylation of glutaminase C, detecting a condition mediated by the activating phosphorylation of glutaminase C, and screening for compounds capable of treating or preventing cancer are also disclosed.

Abstract: The present invention provides compositions and uses of an ascomycin macrolactam for the treatment of an unwanted ocular condition occurring in a patient undergoing treatment with a therapeutically active agent for the treatment of cancer.

Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.

Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.

Abstract: Provided are over 300 mTOR kinase targets identified by a comprehensive phosphoproteomics assay. Methods of targeting mTOR kinase targets, methods to determine the level of mTOR activity by measuring the level of phosphorylation of an mTOR targeted phosphorylation site, methods for distinguishing different classes of mTOR activity in a cell based on phosphoproteomic analysis of mTOR-targeted proteins are also provided. Also provided is the classification of a hyperproliferative disease based on phosphoproteomic analysis of mTOR-targeted proteins, as well as the personalization of therapeutic methods for the treatment of hyperproliferative disease based on phosphoproteomics. Also provided are therapeutic methods including administering to a subject an mTOR inhibitor, an mTOR inhibitor and an additional kinase inhibitor, or a dual inhibitor of mTOR and an additional kinase based on the phosphorylation levels of mTOR targets determined in the subject.

Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.