Abstract: The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.

Abstract: The present invention relates to pharmaceutical technical field, to melonine bisindole compounds, pharmaceutical compositions thereof, and preparation methods thereof. Specifically, the present invention relates to melonine bisindole compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts thereof. The present invention further relates to method for preparing the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof, and the use of the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of cancers.

Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.

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: A liposome of irinotecan or irinotecan hydrochloride and its preparation method are disclosed. The liposome contains irinotecan or irinotecan hydrochloride, neutral phospholipid and cholesterol, wherein the weight ratio of the cholesterol to the neutral phospholipid is 1:3 to 1:5. The liposome is prepared by an ion gradient method.

Abstract: This invention relates to pharmaceutical compositions consisting of a semisynthetic derivative of vinca alkaloid, stable at room temperature, in which said derivative is present in the form of a freeze dried product obtained in the presence of at least one carbohydrate.

Abstract: The present disclosure generally relates to 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. Other aspects of the invention include methods of making such nanoparticles.

Abstract: An embolic composition comprises microspheres formed of water-insoluble water-swellable anionic polymer having swollen diameter more than 100 ?m and a cationic camptothecin compound, preferably irinotecan. The microspheres are preferably formed of crosslinked polyvinylalcohol, preferably of ethylenically unsaturated polyvinylalcohol macromer, crosslinked with anionic ethylenically unsaturated anionic comonomer. The compositions are used to treat hypervascular tumours for instance colorectal metastases of the liver.

Abstract: A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as, is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.

Abstract: In one aspect, the present invention provides a method of treating breast cancer that is negative for ER, PR, and HER2, comprising administering to a subject at least one iodonitrobenzamide. In another aspect, the present invention provides a method of treating breast cancer comprising administering to a subject at least one iodonitrobenzamide in combination with at least one anti-tumor agent.

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: A combination of HKI-272 compound and a vinorelbine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.

Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.

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

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 provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg

Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.

Abstract: The invention provides compositions and methods for delivery of a bioactive agent to an individual. Delivery vehicles are provided that include a bioactive agent in disc shaped particles that include one or more lipid binding polypeptides circumscribing the perimeter of a lipid bilayer in which the bioactive agent is localized. Chimeric lipid binding polypeptides are also provided and may be used to add additional functional properties to the delivery particles.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: The invention relates to the identification of aprataxin (APTX) expression levels as a marker for the response to topoisomerase I inhibitor-based therapies in patients with cancer and, more particularly, colon cancer. The invention also relates to methods for treating patients with cancer who have low APTX expression levels by means of administering a topoisomerase I inhibitor to said patients.

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 provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of renal disease and cancer.

Abstract: To provide a therapeutic method using a water soluble, high molecular weight block polymer to enable that an intraperitoneally administered anti-cancer agent may maintain for a long-term retention in the abdominal cavity to enoughly exert the effect of the anti-cancer agent and reduce adverse side-effects thereof. A therapeutic agent as a micelle preparation, comprising a copolymer having a hydrophilic polymeric moiety and a polycarboxylic acid derivative moiety; and an anti-cancer agent bonding to or encapsulated in the copolymer, wherein the micelle preparation may exhibit sustained drug release capability, and enables an extension of a retention time period of the anti-cancer agent in an abdominal cavity, is provided. A superior life-prolonging effect was found in an intraperitoneal administration mouse model compared with a case in which only an encapsulated drug is administered, and thus the present invention was completed accordingly.

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: 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: To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. The marker for determining sensitivity to an anti-cancer agent is formed of a protein selected from the group consisting of a protein or a fragment thereof which is detected as a peak at m/z of 16,450 to 16,620, a protein or a fragment thereof which is detected as a peak at m/z of 22,080 to 22,310, and a protein or a fragment thereof which is detected as a peak at m/z of 17,100 to 17,270, the peaks being determined by means of a mass spectrometer.

Abstract: The present invention provides novel substituted quinoline 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: To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. The marker for determining sensitivity to an anti-cancer agent is formed of one or more substances selected from the group consisting of a substance or a fragment thereof detected as an anion at m/z of 149.05 to 149.06, a substance or a fragment thereof detected as an anion at m/z of 152.99 to 153.00, a substance or a fragment thereof detected as a cation at m/z of 724.34 to 724.35, the peaks being determined by means of a mass spectrometer, glycerol 3-phosphate, dihydrobiopterin, GABA, lactic acid, asparagine, aspartic acid, 2-methylbutyroylcarnitine, 1-methyladenosine, and glutathione, and a substance involved in a metabolic pathway of any of these substances.

Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-1 or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-1 in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-1 and another therapeutic agent.

Abstract: The present invention relates to injectable compositions comprising biocompatible, swellable, substantially hydrophilic, non-toxic and substantially spherical polymeric material carriers which are capable of efficiently delivering bioactive therapeutic factor(s) for use in embolization drug therapy. The present invention further relates to methods of embolization gene therapy, particularly for the treatment of angiogenic and non-angiogenic-dependent diseases, using the injectable compositions.

Abstract: The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or autoimmune conditions.

Abstract: The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: wherein each occurrence of M is independently a modifier having a molecular weight ?10 kDa; denotes direct of indirect attachment of M to linker LM; and each occurrence of LM is independently an optionally substituted succinamide-containing linker, whereby the modifier M is directly or indirectly attached to the succinamide linker through an amide bond, and the carrier is linked directly or indirectly to each occurrence of the succinamide linker through an ester bond. In another aspect, the invention provides compositions comprising the conjugates, methods for their preparation, and methods of use thereof in the treatment of various disorder, including, but not limited to cancer.

Abstract: Disclosed is a crystalline form of irinotecan hydrochloride (I) and processes for the preparation thereof from crude irinotecan hydrochloride or another polymorphic form of irinotecan. Said crystalline form is particularly suitable for industrial use, because it is easily filtered and possesses characteristics of high stability and purity.

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: Methods for treating a patient at risk for or diagnosed with colorectal cancer are disclosed herein. The method of the present invention determines the overall expression of MSH3 in cells suspected of being colorectal cancer cells from the patient and predicting the efficacy of therapy with a genotoxic anti-neoplastic agent for treating the patient, wherein a decrease in the overall expression of MSH3 in the patient cells when compared to the expression of MSH3 in normal colorectal cells indicates a predisposition to responsiveness to genotoxic anti-neoplastic agent therapy, wherein the therapy comprises administering an effective amount of the genotoxic anti-neoplastic agent therapy to patients.

Abstract: An embolic composition comprises microspheres formed of water-insoluble water-swellable anionic polymer having swollen diameter more than 100 ?m, and a cationic camptothecin compound, preferably irinotecan. The microspheres are preferably formed of crosslinked polyvinylalcohol, preferably of ethylenically unsaturated polyvinylalcohol macromer, crosslinked with anionic ethylenically unsaturated anionic comonomer. The compositions are used to treat hypervascular tumours for instance colorectal metastases of the liver.

Abstract: The present invention relates to methods for predicting and evaluating metastasis of solid cancers, such as melanoma, in a subject by measuring serum biomarkers associated with a metastatic phenotype. In particular, the present invention provides a serum gene expression signature that is different between highly aggressive and more metastatic versus less aggressive and less metastatic melanomas by quantitatively measuring the levels of, inter alia, lymphoid-specific helicase (HELLS) and condensing complex subunit 2 (NCAPH) transcripts in a subject.

Abstract: Provided are methods for treating a hematological malignancy comprising administering an effective amount of flubendazole alone or in combination with a vinca alkaloid. Also provided are compositions and kits comprising an effective amount of flubendazole and/or a vinca alkaloid for use in the methods of the disclosure.

Abstract: The invention concerns an improved method for treating tumor, including cancer, which combines the administration of a chemotherapeutic agent and an antagonist of a gene product the expression of which is upregulated by the chemotherapeutic agent. The invention further concerns methods and means for the diagnosis and classification of tumors, and for the prognosis of the outcome of tumor treatment, and patient response to a particular treatment modality.

Abstract: A liposome comprising bilayer and inner water phase is disclosed. Said inner water phase contains sulfobutyl ether cyclodextrin and active compound. Said sulfobutyl ether cyclodextrin is sulfobutyl ether ?-cyclodextrin, sulfobutyl ether ?-cyclodextrin, or sulfobutyl ether ?-cyclodextrin.

Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.

Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:

Abstract: The present invention relates to the salts of (+)-13a-(S)-deoxytylophorinine represented by the general formula (I), the preparation method thereof, the pharmaceutical compositions containing them, and their use as medicaments for prevention and/or treatment of cancer and/or inflammation disease.

Abstract: Non-Small Cell Lung Carcinomas (NSCLCs) are treated with Gel Micro-Particles (GMPs) that passively accumulate in the lungs and contain Nano-Particles (NPs) combining one or more therapeutic agents that are cytotoxic to the NSCLC with one or more NSCLC active targeting ligands, as well as one or more other optional agents that increase cellular uptake, enhance the pro-apoptotic effect of the chemotherapeutic agent(s), and the like. NPs targeting other cancer cells are also disclosed, as well as NP-containing GMPs that reduce the occurrence of tumor metastasis.

Abstract: The present invention provides compositions for delivering highly water-soluble drugs (such as vinca alkaloids) and methods of using such compositions.

Abstract: The present invention relates to medical use of liposomes, more particular the first medical use of sPLA2 hydrolysable liposomes. Such liposomes may be used for targeted delivery of therapeutic agents to cancerous tissue and in such embodiments; the therapeutic agents are typically small molecule antitumor agents. Other aspects of the inventions relates to methods of reducing the side effects of therapeutic agents, e.g. reducing nephrotoxicity, neurotoxicity and gastrointestinal toxicity of a therapeutic agent. Yet another aspect of the present invention relate to methods of prolonging the therapeutic effect of a therapeutic agent.