Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Abstract: The present invention provides a method for controlling toxicity of metallic particles and a low-toxicity composite of metallic nanoparticles and inorganic clay. The metallic nanoparticles are effective in preventing infection and in skinning over, and thus suitable for treating scalds/burns. In the composite, the weight ratio of metallic nanoparticles to inorganic clay preferably ranges 0.1/99.9 to 6.0/94.0 in a size of about 5 to 100 nm. Preferably, the metal is silver and the inorganic clay is nano silicate platelets.

Abstract: This invention features methods for prognosticating the efficacy of a cancer treatment comprising administration of a lymphotoxin-? receptor (LT-?-R) using TRAF3, TRAF2, and/or p53 markers, as well as combination therapies that include a composition that activates lymphotoxin-beta receptor signaling in combination with one or more other agents.

Abstract: The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.

Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.

Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.

Abstract: The present invention relates to methods of treating a hyperproliferative disease by administering a composition of lactoferrin alone or in combination with standard anti-cancer therapies.

Abstract: RNA interference using small interfering RNAs which are specific for the ICAM-1 gene inhibits expression of this gene. Diseases which involve ICAM-1-mediated cell adhesion, such as inflammatory and autoimmune diseases, diabetic retinopathy and other complications arising from type I diabetes, age related macular degeneration and many types of cancer, can be treated by administering the small interfering RNAs.

Abstract: The present invention provides, in part, compounds and compositions including a thiazole moiety, that may be useful, for example, for treating cancers, for example kidney cancer.

Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.

Abstract: The present invention provides a method of improving a therapeutic response to a cancer treatment, in a subject, the method comprising administering an effective amount of an agent that enhances the expression of microRNA-140-5p or an agent that mimics the effects of microRNA-140-5p. Further provided is a method of treating a cancer in a subject in need of such treatment comprising the step of administering an effective amount of a microRNA-140-5p or an agent that enhances the expression of microRNA-140-5p.

Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: A method for treating, preventing or ameliorating breast cancer is provided by administering a synergistic amount of digitoxin and either actein or an extract of black cohosh comprising triterpene glycosides, and optionally another chemopreventive agent which may be paclitaxel. Methods for treating or preventing a neoplasia using a synergistic combination, and compositions of a synergistic combination of a cardiac glycoside and either actein or an extract of black cohosh comprising triterpene glycosides, and optionally another chemopreventive agent which may be a taxane are also provided. The compositions may also be used in a method for modulating Na+K+ATPase activity. In addition, a method for inhibiting the progression or development of breast cancer in vivo by administering either actein or an extract of black cohosh comprising triterpene glycosides and optionally at least one other chemoprotective agent is provided.

Abstract: The present invention relates to mannopyranoside-derived compounds and to the use thereof as medicaments, in particular in the treatment of cancer diseases, and also to the method for preparing same and to pharmaceutical compositions comprising such compounds. Medical devices surface-treated with mannopyranoside-derived compounds according to the invention also form part of the invention.

Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal which is optionally being treated with ionising radiation, which comprises the administration of ZD6474 in combination with a platinum anti-tumour agent; to a pharmaceutical composition comprising ZD6474 and a platinum anti-tumour agent; to a combination product comprising ZD6474 and a platinum anti-tumour agent for use in a method of treatment of a human or animal body by therapy; and to a kit comprising ZD6474 and a platinum anti-tumour agent.

Abstract: A composite magnetic nanoparticle drug delivery system provides targeted controlled release chemotherapies for cancerous tumors and inflammatory diseases. The magnetic nanoparticle includes a biocompatible and biodegradable polymer, a magnetic nanoparticle, the biological targeting agent human serum albumin, and a therapeutic pharmaceutical composition. The composite nanoparticles are prepared by oil-in-oil emulsion/solvent evaporation and high shear mixing. An externally applied magnetic field draws the magnetic nanoparticles to affected areas. The biological targeting agent draws the nanoparticles into the affected tissues. Polymer degradation provides controlled time release delivery of the pharmaceutical agent.

Abstract: The present invention relates to substituted halophenoxybenzamide derivative compounds of general formula (I) in which R1, R2, R3, R3a, R4, R5, R6, Ra, Rb, Rc, and X are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: Lung cancer can be treated effectively by combination of amrubicin or a pharmaceutically acceptable salt thereof with cisplatin.

Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.

Abstract: The present invention relates to the method of treating chemotherapy-induced neuropathy in a subject in need thereof with the use of a poly(ADP-ribose)polymerase (PARP) inhibitor.

Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.

Abstract: A peptide including the amino acids sequence X9CGYX13X14AX16X17X18MX20X21X22X23X24X25X26X27CPLCX32X33, a nucleic acid coding for the peptide, and/or a recombinant vector including the nucleic acid for the preparation of a drug intended for the treatment of cancer.

Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.

Abstract: Antimicrobial coatings to protect surfaces and a method of applying such a coating are disclosed. An antimicrobial coating may be applied to a surface, such as the interior surface of a building's exterior wall. The interior surface must be accessed, and then an antimicrobial coating is provided and applied. The antimicrobial coating includes an inorganic antimicrobial additive and a colloidal polymeric medium. The inorganic antimicrobial additive may be silver, platinum, gold, palladium, copper, zinc, boron, or a compound of any of those elements. By including an ultraviolet tracer or color dye additive in the coating, it is possible to detect the coating at any time, provided that the surface is accessed.

Abstract: The present invention provides a method of improving a therapeutic response to a cancer treatment, in a subject, the method comprising administering an effective amount of an agent that enhances the expression of microRNA 29 or an agent that mimics the effects of microRNA 29. Further provided is a method of treating a cancer in a subject in need of such treatment comprising the step of administering an effective amount of a microRNA 29 or an agent that enhances the expression of microRNA 29.

Abstract: Provided herein is a method of reducing incidences of cancer recurrence. The method involves administering to an individual in cancer remission an isoflavonoid. In specific instances, the treated individual is in remission from epithelial cancer, such as ovarian cancer or breast cancer.

Abstract: A method of treating living mammals including humans uses x-rays to disrupt DNA in malfunctioning cells such as cancerous or tumorous cells. A compound comprising a pre-selected element is administered to the mammal so that the compound associates with DNA. Then a localized region of cells which contains the malfunctioning cells is irradiated with line emission x-rays of an energy selected to cause emission of Auger electrons from the pre-selected element of the compound to disrupt DNA proximate to the irradiated pre-selected element. A kit useful for the treatment comprises an x-ray tube capable of emitting monochromatic line emission x-rays and a compound which associates with DNA and has an element which when irradiated emits said Auger electrons.

Abstract: A method of inducing mineralization in a bone cell is described. The method comprises contacting a bone cell with a composition comprising nanoparticles. The nanoparticles can be single-walled carbon nanotubes, hydroxyapatite nanoparticles, TiO2 nanoparticles or silver nanoparticles. The bone cell can be an osteoblast cell. A method for increasing bone mass, bone healing or bone formation is also described which comprises administering to a subject in need thereof an effective amount of a composition comprising nanoparticles. The subject can suffer from a bone disease such as osteoporosis. The subject can suffer from a bone fracture and the method can comprise contacting bone cells near the bone fracture site with the composition. The composition can further comprise a pharmaceutically acceptable carrier.

Abstract: The present invention is directed to compositions and methods of delivering a chemotherapeutic agent via a polynueleotide-functionalized nanoparticle (PN-NP).

Abstract: The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative.

Abstract: This invention relates to novel diaryl urea compounds, their derivatives, 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 an inhibitor of multiple kinases.

Abstract: The present invention concerns a SIMP peptide (Short-interfering mutant p53 peptides) suitable to disrupt the protein complexes within tumour cells resulting from m-p53 and p73 proteins selectively in tumours wherein m-p53 contains His273 mutation.

Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: Epithelial cell transforming sequence 2 (Ect2) is a potential oncogene. Our invention uncovers key mechanisms of Ect2 oncogenicity and the development of a relevant therapies by modulation of Ect2 expression.

Abstract: Provided are methods for detecting bladder cancer in a subject. In some aspects, methylation of one or more of MYO3A, CA10, NKX6-2, SOX11, DBC1, NPTX2, and/or A2BP1 in DNA sediment from a urine sample may be evaluated to detect the presence or absence of a bladder cancer in a human patient.

Abstract: Embodiments of the present invention concern methods and compositions related to detection of ovarian cancer, including detection of the stage of ovarian cancer, in some cases. In particular, the invention encompasses use of expression of TFAP2A and in some embodiments CA125 and/or E2F5 to identify ovarian cancer, including detecting mRNA and/or protein levels of the respective gene products. Kits for detection of ovarian cancer are also described.

Abstract: The present invention relates to compositions containing nanoparticies and uses of said composition for transferring therapeutically active substances into cells by means of specifically coated nanoparticles. The chemical design of the particles is such that a large amount thereof is absorbed into the cells. No direct bond between nanoparticle and the therapeutically active substance is required for the transfer into the cells. Thanks to said transfer, an increased efficacy of the substance and simultaneously reduced systemic toxicity is achieved, i.e. an increase in the efficacy while the side effects are reduced.

Abstract: The present invention provides compounds of Formula I: and related compounds as further described herein, and pharmaceutical compositions comprising these compounds. The invention further provides methods to use these compounds and compositions for treating disorders associated with undesired levels of Pim kinase activity, including cancers and autoimmune disorders.

Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.

Abstract: In the present invention, a method of producing stable bare colloidal gold nanoparticles is disclosed. The nanoparticles can subsequently be subjected to partial or full surface modification. The method comprises preparation of colloidal gold nanoparticles in a liquid by employing a top-down nanofabrication method using bulk gold as a source material. The surface modification of these nanoparticles is carried out by adding one or multiple types of ligands each containing functional groups which exhibit affinity for gold nanoparticle surfaces to produce the conjugates. Because of the high efficiency and excellent stability of the nanoparticles produced by this method, the fabricated gold nanoparticle conjugates can have surface coverage with functional ligands which can be tuned to be any percent value between 0 and 100%.

Abstract: Disclosed herein are multifunctional nanoparticles, comprising: polymer nanoparticles formed by loading a drug into a polymer; a gold thin film deposited on a portion of the surface of the polymer nanoparticles; and an antibody to a substance expressed on the surface of a cell to which the drug is to be delivered, the antibody being conjugated to the gold thin film. Also disclosed is a method for preparing multifunctional nanoparticles, the method comprising the steps of: loading a drug into a polymer to prepare polymer nanoparticles; depositing a portion of the surface of the polymer nanoparticles with a gold thin film; conjugating to the gold thin film an antibody to a substance expressed on the surface of a cell to which the drug is to be delivered; and separating from the resulting nanoparticles those in which a portion of the surface of the polymer nanoparticles is deposited with the gold thin film and conjugated with the antibody.

Abstract: The present invention provides a composition comprising a sPLA2 hydrolysable liposome, an exterior solution, and an interior solution within the liposome, -wherein the concentration of osmolytes is higher in the interior solution than in the exterior solution. The composition improves storage stability of sPLA2 hydrolysable liposomes, in particular at when stored at 2-8 degrees Celsius. The liposome preferably encapsulates cisplatin. The invention also provides methods of preparing the composition of the invention.

Abstract: This invention provides methods of diagnosing or determining a cause of an autoimmune encephalitis or an epilepsy in a subject and of diagnosing a tumor in a subject, comprising the step of testing a biological sample of the subject for an anti-body to a GABAB receptor. This invention further provides methods of treating an autoimmune encephalitis or an epilepsy, comprising the steps of detecting an antibody to a GABAB receptor and treating a tumor associated with the disease.

Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.

Abstract: The invention relates to the use of an Raf inhibitor for the manufacture of pharmaceutical compositions for the treatment of thyroid cancer, more specifically papillary thyroid cancer (PTC); the use of a Raf inhibitor in the treatment of thyroid cancer, more specifically PTC; a method of treating warm-blooded animals including mammals, especially humans, suffering from thyroid cancer, more specifically PTC, by administering to a said animal in need of such treatment a dose effective against said disease of an Raf inhibitor. The invention also relates to the use of a Raf inhibitor in combination with a platin compound for the treatment of thyroid cancer, more specifically papillary thyroid cancer.

Abstract: A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a cephalotaxine and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments, the cephalotaxine comprises homoharringtonine (cephalotaxine, 4-methyl-2-hydroxy-2-(4-hydroxy-4-methyl pentyl)butanediocate ester). Antiproliferative agents of the invention comprise alkylating agents, intercalating agents, metal coordination complexes, pyrimidine nucleosides, purine nucleosides, inhibitors of nucleic acid associated enzymes and proteins, and agents affecting structural proteins and cytoplasmic enzymes.

Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.

Abstract: The present invention includes compositions and method to improve the therapeutic index of anti-cancer agents using a novel anti-cancer agent and a modulator or potentiator thereof