Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: The present invention relates to a novel form of anhydrous tiotropium bromide, processes for the preparation of anhydrous tiotropium bromide, pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.

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 invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. The invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases.

Abstract: The present invention relates to methods for synthesizing tiotropium bromide following the scheme: Using the above scheme, tiotropium bromide (compound 5A) is obtained under mild conditions and with high yields.

Abstract: This document provides methods and materials for treating cancers including renal cancer (e.g., renal cell carcinoma) as well as ovarian, breast, prostate, colon, pancreatic, bladder, liver, lung, and thyroid cancers and melanoma. For example, methods and material for using one or more inhibitors of an SCD1 polypeptide to treat renal cell carcinoma (e.g., clear cell renal cell carcinoma (ccRCC)) or to increase the efficacy of a renal cell carcinoma treatment are provided. In addition, this document provides methods and materials for using elevated SCD1 expression levels in diseased tissues as an indication that an SCD1 inhibitor can be used as an appropriate therapeutic to ameliorate the disease.

Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

Abstract: The present invention includes biocompatible polymeric coatings, membranes, matrices, and films to be used with implantable medical devices. Medical devices containing such materials applied to a surface thereof contain a film-forming fluorous homo-polymer or copolymer containing the polymerized residue of a fluorous moiety, wherein the relative amounts of the polymerized residues of one or more moieties are effective to provide the coating and films with properties effective for use in coating implantable med devices.

Abstract: The present invention includes biocompatible polymeric coatings, membranes, matrices, and films to be used with implantable medical devices. Medical devices containing such materials applied to a surface thereof contain a film-forming fluorous homo-polymer or copolymer containing the polymerized residue of a fluorous moiety, wherein the relative amounts of the polymerized residues of one or more moieties are effective to provide the coating and films with properties effective for use in coating implantable med devices.

Abstract: Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives and their uses in the manufacture of pharmaceutical compositions and in the treatment of cancers.

Abstract: The present invention relates to substituted cellulose acetates and methods of use thereof. One embodiment of the present invention provides a coating having a substituted cellulose acetate having a polar substituent that has an oxygen atom covalently bonded to a nonmetal selected from the group of sulfur, phosphorus, and boron; wherein the nonmetal is present in at least about 0.01% by weight of the substituted cellulose acetate.

Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: Disclosed herein are methods of increasing retinal responsiveness to light in a subject, such as a subject with retinal degeneration. The disclosed methods include administering one or more compounds that decrease or inhibit ?-aminobutyric acid (GABA) signaling to a subject with retinal degeneration. In some embodiments, the methods include selecting a subject with retinal degeneration and administering a ?-aminobutyric acid C (GABAC) receptor antagonist to the subject. In one example, the GABAC receptor antagonist is (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA). In other embodiments, the methods include selecting a subject with retinal degeneration and administering a metabotropic glutamate receptor (mGluR) antagonist to the subject. In one example, the mGluR antagonist is a mGlu1 receptor antagonist (for example, JNJ16259685).

Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.

Abstract: Compositions and methods are disclosed for treating vitiligo and promoting the formation of collagen.

Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.

Abstract: A block copolymer comprising a fluorinated block and a non-fluorinated block and method of making the block copolymer are provided. Also provided herein are a coating on an implantable device comprising the block copolymer and method of using the implantable device.

Abstract: Methods of treating a head and neck cancer are disclosed.

Abstract: An amorphous PDLLA stent coating for drug delivery is disclosed.

Abstract: The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.

Abstract: The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABAA receptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic GABAA receptor antagonist.

Abstract: The present invention relates to a self-preserved oil dispersion. Especially, the present invention relates to a self-preserved oil dispersion including a dispersed oil phase, an aqueous phase and at least one surfactant, wherein said oil dispersion comprises boric acid in an amount ranging from 0.005% to 0.075% in weight of the total weight of the oil dispersion, said amount of boric acid being a preservative effective amount so that the oil dispersion has a preservative activity.

Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.

Abstract: The present invention is directed to therapeutic methods and compositions involving cyclohexenone compounds where said compounds inhibit farnesyltransferase or Ras. The therapeutic methods (e.g. for treating cancers) comprise contacting a tumor with a cyclohexenone compound and an anticancer agent.

Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.

Abstract: Methods and composition for tumor therapy, especially esophageal adenocarcinoma (EAC), are described. For example, in certain aspects methods for determining Hedgehog and mTOR signaling pathway status to select patients for administering a combination therapy of Hedgehog and mTOR signaling inhibitors are described. Furthermore, the invention provides compositions that involve testing kits for determining signaling status.

Abstract: The present invention is directed to the use of marker for Akt2 activation in podocytes as a biomarker to predict toxicity of mTOR inhibitors. Another aspect of the invention relates to a method for preventing graft rejection comprising administering a selective mTORC1 or Akt1 inhibitor in a subject in need thereof.

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

Abstract: A method of controlled in vivo drug delivery is provided. A porous silicon matrix having pores sized and configured to admit to trap and then release a predetermined molecular complex with a predetermined dose-time profile is selected. The matrix contains the predetermined molecular complex so that the predetermined molecular complex is disposed within the pores of the porous silicon matrix. The matrix is introduced into a human body. The drug releases according the dose-time profile. The introduction can be via transdermal introduction, intramuscular injection, intravenous introduction, surgical implantation, inhalation, and oral ingestion.

Abstract: A method for inhibiting formation of adhesions following abdominal surgery which involves application of an anti-static fatty acid ethoxylated amide (Cocamide DEA) in a matrix that is placed in the peritoneal cavity at the conclusion of an abdominal surgery and which releases this anti-adhesive chemical over a predetermined time in a range up to seven days. Tests conducted on laboratory rats established that the method reduced the incidence of adhesions from 100 percent (100%) in a test model to near zero in the majority of treated animals. In an alternative embodiment, andrographalide was delivered via a pump with similar results. In still another embodiment, an effective amount of 50% phosphatidylchorene and propylene glycol was delivered, via a pump, into the abdominal cavity, again with similar results.

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: 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: Provided are methods and compositions for the treatment of depression and anxiety. The compositions contain scopolamine, or an analog thereof, and can optionally include one or more psychoactive agents. Further provided is an inhaler containing scopolamine, or an analog thereof, in a pharmaceutically acceptable carrier.

Abstract: Disclosed are methods of treating viral infections or disorders of uncontrolled proliferation comprising, in one aspect, administering compounds that are phospholipase D inhibitors and/or Akt therapeutic agents. 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 for methods and pharmaceutical compositions for treating disorders using treatment regimens involving multiple agents. In one aspect, a method of treatment is provided resulting in reduced toxicity and/or synergistic effect by administration according to a described dosing schedule.

Abstract: Nano-constructs comprising nanoshells and methods of using the nano-constructs for treating or ameliorating a medical condition are provided.

Abstract: A method for identifying cancer patients that are likely to be responders or non-responders to a signal transduction pathway inhibitor is described.

Abstract: Provided herein is a prohealing piezoelectric coating and the method of making and using the same.

Abstract: A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof.

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: Disclosed are drug delivery systems comprising drugs admixed with polymers having drug solubility gradients and methods of making the polymers. Also disclosed are medical devices having coatings thereon comprising the drug solubility gradient-containing polymers and at least one drug.

Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible rapamycin composition comprising a specific mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers. In other aspects, the present invention is directed to a method of making the composition.

Abstract: An oral tacrolimus composition comprises minicapsules having a core containing tacrolimus in a solubilized liquid form. The minicapsules have a release profile to release the pre-solubilized tacrolimus throughout the entire gastrointestinal tract. The composition may be used, for example, for treatment or prevention of solid organ transplant rejection.

Abstract: A core-shell particle formulation for delivering multiple therapeutic agents is disclosed. More particularly, core-shell particle formulation configured to independently release therapeutic agents from the core and the shell. Moreover, the core-shell particle bearing therapeutic agents enables treatment against the diseases such as cancer, inflammatory and auto-immune diseases.

Abstract: Gene signatures for determining whether a neoplasm (such as a multiple myeloma neoplasm) is sensitive to mTORi/HDACi combination therapy and/or for determining the prognosis of a neoplasm in a subject are described. Some embodiments include determining whether a neoplasm is sensitive to mTORi/HDACi combination therapy by predicting whether mTORi/HDACi combination therapy will successfully treat the neoplasm, for example increasing survival of the subject with the neoplasm. In some embodiments, determining the prognosis includes predicting the outcome (such as chance of survival) of the subject with a neoplasm. Also disclosed are reagents, for example arrays, for use with the disclosed methods, as well as computer implementation of the disclosed methods.

Abstract: A biodegradable in vivo supporting device is disclosed. The in vivo supporting device comprises a biodegradable metal scaffold and a biodegradable polymer coating covering at least a portion of the biodegradable metal scaffold, wherein the biodegradable polymer coating has a degradation rate that is faster than the degradation rate of the biodegradable metal scaffold.

Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and methods for controlling the delivery of a therapeutic agent, and their use in the treatment and/or prevention of diseases and disorders.

Abstract: A drug coating layer which is a drug coating layer having a morphological form including a plurality of elongated bodies having long axes that each crystal of a water-insoluble drug independently has on a substrate surface, in which the long axes of the elongated bodies are nearly linear in shape, and the long axes of the elongated bodies form an angle in a predetermined range with respect to a substrate plane with which the long axis of the elongated body intersects. The drug coating layer can provide low toxicity and a high intravascular stenosis inhibitory effect.

Abstract: The present invention provides for methods and pharmaceutical compositions for treating proliferative disorders. In one aspect, the method comprises administration of two cell-cycle suppressors having a synergistic effect. In another aspect, two cell-cycle suppressors having a synergistic effect are provided in a pharmaceutical composition.