Abstract: Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: Treatment of pain and related conditions with oral dosage forms of zoledronic acid is described herein.

Abstract: Disclosed herein are methods of treating or preventing pain. Typically, a pharmaceutical composition having a therapeutically effective amount of the zoledronic acid is administered to a mammal suffering from pain. The pharmaceutical composition may further comprise an enhancer, which can be a medium chain fatty acid salt, an ester, an ether, or a derivative of a medium chain fatty acid and can have a carbon chain length of from about 4 to about 20 carbon atoms.

Abstract: The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Methods for treating neurodegeneration, e.g., sensorineural hearing loss, or a demyelinating disease, using bisphosphonates, ERK kinase inhibitors, and osteoprotegerin (OPG) proteins or nucleic acids.

Abstract: The invention provides a drug selected from eslicarbazepine acetate and eslicarbazepine, for use in treating or preventing a disorder selected from epilepsy, affective disorders, schizoaffective disorders, bipolar disorders, neuropathic pain and neuropathic pain related disorders, attention disorders, anxiety disorders, sensorimotor disorders, vestibular disorders, and fibromyalgia, in a patient suffering from or susceptible to absence seizures.

Abstract: The present invention provides for methods and compositions for treating, reducing and/or preventing cardiac dysfunction by administering to subject a therapeutically effective amount of a bisphosphonate, prodrug thereof, functional analogue or a pharmaceutically effective salt thereof in an amount sufficient to increase activity of at least one kinase in heart tissue of the subject.

Abstract: Provided herein are combination therapies for the treatment of progeroid diseases and conditions, cellular aging, bone diseases, and cardiovascular diseases. The provided combination therapies target the aberrant farnesylation of the mutant lamin A protein progerin, and inhibit farnesyl biosynthesis, lamin A prenylation, and increase progerin clearance.

Abstract: The described invention provides an ex vivo dynamic multiple myeloma (MM) cancer niche contained in a microfluidic device. The dynamic MM cancer niche includes (a) a three-dimensional tissue construct containing a dynamic ex vivo bone marrow (BM) niche, which contains a mineralized bone-like tissue containing viable osteoblasts self-organized into cohesive multiple cell layers and an extracellular matrix secreted by the viable adherent osteoblasts; and a microenvironment dynamically perfused by nutrients and dissolved gas molecules; and (b) human myeloma cells seeded from a biospecimen composition comprising mononuclear cells and the multiple myeloma cells. The human myeloma cells are in contact with osteoblasts of the BM niche, and the viability of the human myeloma cells is maintained by the MM cancer niche.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: A combination therapy for treating osteoarthritis is disclosed. The combination therapy includes the co-administration of a steroid and Zoledronic Acid. The coadministration of a steroid decreases the production of cytokines, and, therefore, decreases the pro-inflammatory effects of Zoledronic Acid. The co-administration of Zoledronic Acid with steroids treats osteoarthritis, and helps to prevent the onset of osteoarthritis in patients at risk for osteoarthritis.

Abstract: A combination therapy for treating osteoarthritis is disclosed. The combination therapy includes the co-administration of a steroid and Zoledronic Acid. The coadministration of a steroid decreases the production of cytokines, and, therefore, decreases the pro-inflammatory effects of Zoledronic Acid. The co-administration of Zoledronic Acid with steroids treats osteoarthritis, and helps to prevent the onset of osteoarthritis in patients at risk for osteoarthritis.

Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: Methods for treating diseases such as cancer comprising administering a Wnt pathway inhibitor, either alone or in combination with other anti-cancer agents, and monitoring for skeletal-related side effects and/or toxicity.

Abstract: The present invention relates to substituted diaryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to substituted 1H-pyrazol-1,2,4-oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to substituted pyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to a mixed agrochemical emulsion composition comprising: an organic phosphorous pesticide represented by formula (I) (wherein, R1 represents a C1-4 linear or branched alkyl group; R2 represents a C1-4 linear or branched alkyl group; R3 represents a nitrogenated heterocyclic group which may have a substituent or a group —OR4 (wherein R4 represents a nitrogenated heterocyclic group which may have a substituent; and X and Y each independently represent an oxygen atom or a sulfur atom, wherein Y is a sulfur atom when X is an oxygen atom, and Y is an oxygen atom when X is a sulfur atom); chloropicrin; and a nonionic surfactant. The composition has excellent storage stability and excellent emulsifying properties in water and can be sprayed and applied conveniently by diluting the composition with water, in spite of a fact that both chloropicrin and the organic phosphorous pesticide, which are effective for the control of pests, are contained.

Abstract: Metal-bisphosphonate nanoparticles are disclosed. Also disclosed are pharmaceutical compositions including the metal-bisphosphonate nanoparticles, methods of preparing the metal-bisphosphonate nanoparticles and materials comprising the nanoparticles, and methods of using the compositions to treat cancer or bone-related disorders (e.g., bone-resorption-related diseases, osteoporosis, Paget's disease, and bone metastases) and as imaging agents.

Abstract: The present invention relates to substituted dihydropyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to methods for in situ treatment of malignant cells from a cancer associated with bone. In one method, the treatment is for a primary cancer and entails positioning an implant containing and/or coated with at least one active agent for treating malignant cells directly in/on or indirectly among/near (e.g., by placing the implant in an area immediately proximal to) a site containing the malignant cells. In another method, the treatment includes positioning an implant containing and/or coated with at least one active agent for treating malignant cells directly in/on or indirectly among/near (e.g., by placing the implant in an area immediately proximal to) a surgical site from which malignant cells were previously removed/excised.

Abstract: The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R1, R2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of injuries, conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease.

Abstract: Bisphosphonamidate prodrugs of therapeutic bisphosphonate compounds and uses thereof to treat diseases are described.

Abstract: Administration of TH-302 or another hypoxia activated prodrug in combination with a pharmacological agent that down-regulates or inhibits homology directed repair (HDR) is useful for treating cancer.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: The present invention is directed to a method for treating aneurysms in vascular tissue. The method includes administering a bisphosphonate compound to a subject in an amount which is effective against the formation or progression of aneurysm, or which is effective to induce regression of an established aneurysm. In alternative methods, an anti-RANKL neutralizing antibody is administered to the subject to achieve analogous anti-aneurysm effect. The methods of particular advantage in the treatment of subjects having an abdominal aortic aneurysm, a relatively common, and life-threatening, condition.

Abstract: Provided herein is a method of treating cancer by the administration of binuclear gold(I) compounds in patients in need thereof. The pharmaceutical compounds possess anti-cancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

Abstract: To provide a novel compound that has S1P lyase inhibitory ability and induces a reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof.

Abstract: Methods and compositions useful for the treatment and/or prevention of muscle weakness in cancer patients. In certain embodiments, the methods of the present invention include administering to a cancer patient a therapeutically or prophylactically effective amount of one or more inhibitors of TGFbeta signaling in combination with one or more benzothiazepine derivatives.

Abstract: The present invention pertains to use of PKC-iota inhibitors for treatment of glioma. In a specific embodiment, the treatment method comprises administering ICA-1 or a salt thereof to a subject with glioma. In another embodiment, the treatment method comprises contacting glioma cells with an effective amount of ICA-1 or a salt thereof.

Abstract: Methods for treating neurodegeneration, e.g., sensorineural hearing loss, or a demyelinating disease, using bisphosphonates, ERK kinase inhibitors, and osteoprotegerin (OPG) proteins or nucleic acids.

Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

Abstract: The present invention relates to a method for the diagnosis or the prognosis of metastasis in prostate cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in prostate cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the prostate cancer.

Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.

Abstract: Compositions and methods for inhibiting the growth of solid tumors following radiation treatment are described. The compositions and methods target matrix metalloproteinases and bone marrow-derived cells expressing matrix metalloproteinases.

Abstract: Formulations and unit dose forms of TH-302 and other hypoxia activated prodrugs suitable for oral administration are useful for treating cancer.

Abstract: A method of detecting prostate tumorigenesis in a subject, the method including the steps of (a) obtaining a sample from the prostate of the human subject, (b) detecting quantitatively or semi-quantitatively in the sample a level of expression for PKC-? and (c) comparing the expression level in (b) to a level of expression in a normal control, wherein overexpression of PKC-?, with respect to the control, indicates the presence of prostate cancer in the subject. The present invention is based upon the discovery that PKC-? levels are elevated during prostate tumorigenesis. Furthermore, the proliferation rate of the tumor correlates with the level of PKC-?. The invention also provides methods of treating prostate cancer by administering to the subject a compound that inhibits the expression of PKC-?. The compound can be a small interfering RNA (siRNA) molecule.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.

Abstract: The identification of pO2 lowering agents as transient hypoxia-inducers is disclosed herein. Provided is a method of enhancing the efficacy of a hypoxia-sensitive agent in a subject, by administering to the subject a therapeutically effective amount of the hypoxia-sensitive agent and a therapeutically effective amount of a pO2 lowering agent. Methods of treating a subject with a tumor, by administering to the subject a therapeutically effective amount of a pO2 lowering agent and a therapeutically effective amount of a hypoxia-sensitive agent are also disclosed.