Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 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 proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: A method of treating a patient with a pulmonary disease, where the method includes delivering a dose of aerosolized medicament intermittently to a ventilator circuit coupled to the respiratory system of the patient. Also, a method of treating a patient with a pulmonary disease, where the method includes taking the patient off a ventilator, and administering to the patient, a nebulized aerosol comprising from about 100 ?g to about 500 mg of a medicament. Also a method of treating a patient with a pulmonary disease, the method comprising administering an aerosolized first medicament comprising amikacin to the patient and administering, systemically a second medicament comprising an antibiotic to the patient that also treats the pulmonary disease, wherein a resulting amikacin concentration in the lung and/or pulmonary system is therapeutically-effective, and an amount of the systemically administered antibiotics is reduced.

Abstract: The invention provides a method for treating target in need of such a treatments in a subject, comprising (a) administering a liposome containing a photosensitizer and a drug to a subject and (b) irradiating targets at least one time at appropriate time(s). In particular, the irradiation is performed at least two times.

Abstract: The present invention relates to plexin D1 for use as a targetable protein in the treatment or diagnosis of disorders that involve expression of plexin D1. Diagnosis is suitably effected by detecting the presence of plexin D1 in the body or a bodily tissue or fluid, whereas treatment is effected by targeting plexin D1 for delivery of therapeutics to the site where treatment is needed. The invention further relates to the use of molecules that bind plexin D1, a nucleic acid encoding plexine D1 or a ligand of plexin D1 for the preparation of a therapeutical composition for the treatment or diagnosis of disorders that involve expression of plexin D1. The disorders comprise disorders in which plexin D1 is expressed on tumor cells, tumor blood vessels or activated macrophages.

Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.

Abstract: Screening and diagnostic reagents, kits and methods for primary and/or metastatic stomach or esophageal cancer are disclosed. Compositions for and methods of imaging and treating primary and/or metastatic stomach or esophageal cancer are disclosed. Vaccines compositions and methods of for treating and preventing primary and/or metastatic stomach or esophageal cancer are disclosed.

Abstract: Described herein are compositions and methods for the diagnosis, prognosis, prevention and treatment of melanoma or melanoma associated symptoms. The compositions are microRNA molecules associated with melanoma, as well as various nucleic acid molecules relating thereto or derived therefrom.

Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.

Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. 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: An exosomal composition is provided that comprises a therapeutic agent encapsulated by an exosome. The therapeutic agent can be a phytochemical agent, a chemotherapeutic agent, or a Stat3 inhibitor. Pharmaceutical compositions comprising the exosomal compositions are also provided. Methods for treating an inflammatory disease or a cancer are further provided and include administering an effective amount of an exosomal composition to a subject in need thereof to thereby treat the inflammatory disorder or the cancer.

Abstract: RNA interference using small interfering RNAs which target HIF-1 alpha mRNA inhibit expression of the HIF-1 alpha gene. As HIF-1 alpha is a transcriptional regulator of VEGF, expression of VEGF is also inhibited. Control of VEGF production through siRNA-mediated down-regulation of HIF-1 alpha can be used to inhibit angiogenesis, in particularly in diseases such as diabetic retinopathy, age related macular degeneration and many types of cancer.

Abstract: This description applies to pharmaceutical compositions comprising a mixture comprising one or more hERG1 channel blockers in combination with one or more compounds for anticancer therapy for use in the treatment of chemoresistant or potentially chemoresistant leukaemias and in vitro systems for the screening of substances suitable for use in the treatment of chemoresistant or potentially chemoresistant leukaemias.

Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.

Abstract: The invention concerns compounds of the formula: X—(Y)t wherein: X is Formula (X), each Y is the same or different and is Formula (Y) —O—[CH2—CH(OH)—CH2—O—]m—H; or —C(OR5)3; R1, R2, R3, R6, R7, R8, R9, R10 are each, independently, —(CH2CH2O)m—R4, —[CH2CH(OH)CH2O]nH, OR11, —O(CH2)PR13, or —(CH2)R12; each R4 is independently OR5 or OH; R5, R11 and R12 are each, independently, H or C1-C30 alkyl; R13 is —NH3+Cl? or —NHBoc; t is an integer from 2 to 6; m, n, and p are each, independently, an integer from 1 to 12; and each q, r, and s is 0 or 1 and the sum of q+r+s is at least 2.

Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.

Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.

Abstract: The invention provides magnetic nanoparticles comprising a core, wherein the nanoparticles comprise at least one therapeutic agent linked to the core via a hydrazone linkage or via an oxime ether linkage, methods for making said nanoparticles, and methods for using said nanoparticles.

Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-I or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-I in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-I and another therapeutic agent.

Abstract: The present invention relates to a drug delivery composition comprising a hyaluronic acid-peptide conjugate micelle and a production method thereof. According to the drug delivery composition and the production method of the drug-loaded, hyaluronic acid-peptide conjugate micelle of the present invention, the reaction for encapsulating can proceed in a mixed solvent of an aqueous solvent and an organic solvent. Therefore, the present invention can be applied to various types of water-insoluble active components and the biocompatible and biodegradable derivative can encapsulate a drug to provide a drug-loaded micelle, which is safe to be applied for human bodies. Moreover, the micelle has a therapeutic effect from the peptide contained therein, which can act in combination with the drug as packing therein. Therefore, the drug delivery composition and its production method can be utilized in the field of producing a sustained release formulation with an extended duration of the medicinal effect.

Abstract: The invention relates to compositions and methods to inhibit gene expression. In particular, the invention provides co-therapies comprising oligonucleotides plus other therapies to treat cancer.

Abstract: Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed.

Abstract: A process for producing a small-sized, lipid-based cochleates. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structures by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca2+ or Zn2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing biologically relevant molecules.

Abstract: The present invention relates to a target-aiming drug delivery system for diagnosis and treatment of cancer containing liposome labeled with peptides which specifically targets interleukin-4 receptors, and a manufacturing method thereof. The liposome which contains anticancer drugs labeled with IL4RPep peptides prepared in accordance with the present invention can deliver drugs to cancer cells in which IL-4 receptors are overexpressed by IL4RPep peptides which specifically bind to IL-4 receptors, and the drug delivery can recognize cancer cells specifically by a label. Thus, IL4RPep peptides can increase the effect of drugs only on cancer tissues and at the same time significantly reduce the side effects on normal tissues, which makes possible in vivo(molecular) imaging and early diagnosis of tumors.

Abstract: An embodiment of the present invention comprises a method of treating malignancies in a subject in need of treatment comprising administering to the subject a high loading dose of a pegylated liposomal doxorubicin (PLD) in an initial cycle, followed by a reduced dose in a second cycle, wherein the second cycle reduced dose is in the range of 20% to 50%, preferably 50%, of the initial loading dose, and thereafter one or more maintenance doses in further cycles. The interval between dose cycles is in the range of about three-to-four weeks, preferably about four weeks. The initial loading dose is in the range of between the maximum tolerated dose (MTD) and the recommended dose, preferably the MTD (for instance, in the range of about 70 mg/m2 to 50 mg/m2, preferably 60 mg/m2). The one or more maintenance doses are in the range of about 40 mg/m2 to 50 mg/m2, preferably 45 mg/m2).

Abstract: Methods for treating ocular and periocular disorders by administration to a human patient of a therapeutically effective amount of a compound that modulates muscle action.

Abstract: A method of treating a warm-blooded animal, especially a human, having a proliferative disease or acute or chronic transplant rejection comprising administering to the animal a combination which comprises (a) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and (b) a chemotherapeutic agent selected from antineoplastic agents, especially as defined herein, and agents effective in treating acute or chronic transplant rejection; a combination comprising (a) and (b) as defined above and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.

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: 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: In accordance with certain embodiments of the present disclosure, a self-assembling biodegradable nanoparticle is provided. The nanoparticle includes Cys-Val-Val-Val-Val-Val-Val-Lys-Lys conjugated with a synthetic polymer and has a diameter of from about 50 nm to about 150 nm.

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: Proteasome inhibitors (PI) are used for inhibiting the maturation of dendritic cells (DZ) and thus in the treatment or the prophylaxis of allergies, asthma, tissue or transplant rejection or autoimmune diseases. The concentration of the proteasome inhibitors lies preferably in the range of 10 nM to 10 ?M, based on the peripheral blood or the cytoplasm.

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: 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: This invention provides methods for treating a subject afflicted with cancer, comprising concurrently administering (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide. This invention also provides methods for inducing the death of a transformed cell such as a cancer cell, comprising concurrently contacting the cell with (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide.

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 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: Methods and systems for treatment of hypoxic tumors are provided, including the steps of positioning a delivery device in a bodily cavity adjacent to tumor tissue, delivering an oxygenating agent to the tumor tissue via the delivery device and radiating the tumor tissue with radiation. Methods and systems of treatment of tumors are also provided, including the steps of positioning a delivery device in a bodily cavity adjacent to tumor tissue, delivering a photosensitizing agent to the tumor tissue via the delivery device, and radiating the tumor tissue with light.

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 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: Ezatiostat is useful for inhibiting multiple myeloma cell proliferation and treating multiple myeloma, alone or when added together with another anti-myeloma drug.

Abstract: Methods of treating cancer comprising administering inhibitors of glucose transporters (GLUTs) are provided. Methods of predicting whether a cancer will respond to treatment with a GLUT inhibitor also are provided.

Abstract: The present invention relates to methods for predicting the responsiveness of a patient to a breast cancer treatment regimen by assaying a biological sample to determine the level of expression of the long-chain fatty acyl-CoA synthetase 4 (ACSL4) in the biological sample. The present invention also provides ACSL4 inhibitors and uses of ACSL4 inhibitors as adjuvant therapies in breast cancer treatment regimens.

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: The invention relates to a passive solid tumor-targeted anticancer prodrug and a preparation method thereof, belonging to the field of antitumor drugs. The preparation method includes the following steps: reacting low molecular weight pectin with Mw of 5,000-45,000 with doxorubicin to obtain a pectin-doxorubicin conjugate with Mw of 100,000-1,000,000, preparing the conjugate into a suspension, and treating the suspension in an ultra-high pressure nano homogenizer to obtain the passive solid tumor-targeted anticancer prodrug with particle size of 100 nm-200 nm and melting point of 220-245°, wherein the pectin and doxorubicin are linked by an amide bond, and the pectin is linked by an ester bond formed by condensing carboxyl groups and hydroxyl groups of pectin molecules. Cell inhibition rate of the anticancer prodrug for humanized lung cancer cells NCI-H446 and A549 is equivalent to that of doxorubicin hydrochloride.