Abstract: A composition comprising microspheres of a polymer matrix, having two different pharmaceutical actives having complementary, usually synergistic, activity in killing cells. The compositions have particular utility for treating tumours. Useful combinations are doxorubicin with rapamycin, irinotecan with ibuprofen, ibuprofen with doxorubicin and irinotecan with doxorubicin. The polymer matrix is preferably a crosslinked polyvinyl alcohol. The drugs may be included in the same microsphere, or microspheres each with an individual pharmaceutical agent may be mixed together. The microspheres are preferably used in chemoembolisation of tumours.

Abstract: Compositions which comprise a liposomal water-soluble camptothecin and optionally a liposomal fluoropyrimidine in combination with a vascular epithelial growth factor (VEGF) inhibitor such as cetuximab or an epidermal growth factor receptor (EGFR) inhibitor such as bevacizumab are useful in achieving enhanced therapeutic effects for the treatment of cancer.

Abstract: The present disclosure is directed in part to a biocompatible nanoparticle composition comprising a plurality of non-colloidal long circulating nanoparticles, each comprising a ?-hydroxy polyester-co-polyether and a therapeutic agent, wherein such disclosed compositions provide a therapeutic effect for at least 12 hours.

Abstract: The present invention relates to anti-flavivirus compounds, including lycorine and derivatives thereof, and their use in treating a subject infected by a flavivirus. The present invention also relates to the use of the anti-flavivirus compounds for the prophylaxis of flavivirus infection. The present invention further relates to a method of suppressing viral RNA synthesis of a flavivirus. Also described is a method of preparing an anti-flavivirus compound for use in the treatment or prophylaxis of flavivirus infection.

Abstract: The present invention is directed to new oral formulations of chemotherapeutic agents, their process of preparation as well as their therapeutic uses. More specifically, said invention is related to nanoparticles comprising at least one chemotherapeutic agents as an active ingredient, at least one polymer and at least one cyclic oligosaccharide capable of complexing said camptothecin derivative, said nanoparticles being for therapeutic oral administration.

Abstract: The present invention is directed to a composition including: (a) an active ingredient other than bendamustine; (b) a charged cyclopolysaccharide comprising at least one charged group; and (c) a stabilizing agent comprising at least one charged group having a charge opposite to that of the cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma which contain entities (such as enzymes, other proteins and the like) and/or conditions which can decompose or deactivate the active ingredient.

Abstract: A novel compound having an excellent NF?B inhibitory effect is provided and specifically disclosed is a compound represented by the following formula (1) or a salt thereof: wherein, R1 represents a hydrogen atom, a lower alkyl group, a lower alkyloxy group, or a halogen atom; R2 represents a hydroxyl group, or a lower alkyloxy group; R3 represents a hydrogen atom, a lower alkyl group, or a halogen atom; R4 represents a hydrogen atom or a lower alkyloxy group; R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6; R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5; R7 represents a hydrogen atom or a lower alkyl group; and R8 represents a hydrogen atom, a hydroxyl group, an amino group, or a lower alkylcarbonyloxy group (excluding the case where R1, R3, R4 and R7

Abstract: A novel compound having an excellent NF?B inhibitory effect is provided. Specifically disclosed is a compound represented by the following formula (1) or a salt thereof: wherein, R1 represents a hydrogen atom, a lower alkyl group, or the like; R2 represents a hydrogen atom, a lower alkyl group, a halogen atom, or the like; R3 represents a hydrogen atom, a lower alkyl group, a hydroxyl group, or a halogen atom; R4 represents a hydrogen atom or a lower alkyloxy group; R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6; R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5; R7 represents a hydrogen atom or a lower alkyl group; and R8 represents a hydrogen atom, a hydroxyl group, an amino group, a lower alkylcarbonyloxy group, or a halogen atom.

Abstract: The invention relates to a novel therapeutic use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment of serious depression in humans, particularly for the treatment of a patients resistant to conventional anti-depressant treatments and for treatment of sleep/waking cycle disorders.

Abstract: Pyrazole urea compounds, pharmaceutical compositions which contain them and methods for treating cancer using them.

Abstract: A method of treating a resistant or refractory cancer in a mammal includes administering an effective amount of a compound of to the mammal. In preferred aspects, the cancer is resistant or refractory to CPT-11 or CPT therapy.

Abstract: The present invention relates to new quinoline inhibitors of tyrosine kinases, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A germicidal absorptive material for use in surgical packings, wound bandages, sanitary tampons and bed sore prevention and/or treatment uses is provided by a foam-like matrix of hydrophilic polyurethane polymer to which application-specific loads of a germicidal disinfectant dye have been made. Polyurethane polymer of various densities and thicknesses exhibits an exceptional ability to absorb different levels of a number of disinfectant dyes, both basic and acidic, such as gentian violet and methylene blue, respectively. The relationship between dye-load and application-specific uses permits a totally-bound gentian violet pad to be used as a conventional bandage or pad on a surface wound with the capability of preventing the incursion of external pathogens from entering the wound through the pad, where the pathogens are killed by the bound-dye. The wound exudate is absorbed safely by the pad, where wound-originating pathogens are also killed.

Abstract: Antitumor combinations comprising a taxane and at least one antibiotic for treating neoplastic diseases are described.

Abstract: A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium erythorbate, sodium thioglycolate, sodium pyrosulfite, and ?-thioglycerin. The pharmaceutical composition is useful in that, after storage for a long period of time or under light-irradiation conditions, camptothecin or a derivative thereof contained therein undergoes minimum degradation.

Abstract: The invention relates to methods of treating or preventing pathological cardiac remodeling and/or preventing heart failure. These methods include the administration of a PDE1 inhibitor to a patient under conditions effective to treat or prevent pathological cardiac remodeling, and therefore heart failure that occurs as a result of such remodeling. Pharmaceutical compositions and delivery vehicles that can be used in the methods of the present invention are also disclosed herein.

Abstract: Compositions and methods for modulating HSP70 function, particularly for the targeted killing of cancer cells, are disclosed.

Abstract: Antitumor combinations comprising a taxane and at least one therapeutically useful substance for treating neoplastic diseases are described.

Abstract: The use of dimiracetam in the treatment of chronic pain is disclosed. At doses higher than those previously disclosed in relation with its cognition enhancing activity (i.e. amelioration of learning and memory), dimiracetam was able to completely revert hyperalgesia or allodynia associated with several animal models of chronic pain. Dimiracetam showed high activity in iatrogenic neuropathies associated with antiviral and chemotherapeutic drug treatments and in painful conditions caused by osteoarthritis. In addition, dimiracetam was devoid of toxicity even at doses 10-fold higher than the highest therapeutic dose. The possibility of treating such debilitating pathologies with a highly effective and essentially non-toxic compound is therefore disclosed.

Abstract: Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.

Abstract: There is provided a powder composition for use in a pharmaceutical product, the composition including a) 5(S)-(2?-hydroxyethoxy)-20(S)-CPT; at least one cyclodextrin; wherein 5(S)-(2?-hydroxyethoxy)-20(S)-CPT includes less than 5% of 5(R)-(2?-hydroxyethoxy)-20(S)-CPT. Preferably, in the powder composition, 5(S)-(2?-hydroxyethoxy)-20(S)-CPT is substantially free from said 5(R)-(2?-hydroxyethoxy)-20(S)-CPT.

Abstract: Disclosed herein are methods used in the identification of cancer patients likely or unlikely to respond to systemic chemotherapy, methods of treating cancer patients based upon the identification, and kits that facilitate the identification. The methods and kits involve detecting the expression of specific microRNA.

Abstract: Polynucleotides encoding a mutant human carboxylesterase enzyme and polypeptides encoded by the polynucleotides which are capable of metabolizing a prodrug and inactive metabolites thereof to active drug are provided. Compositions and methods for sensitizing cells to a prodrug agent, inhibiting cell growth, treating drug addiction, and facilitating the metabolism of an organophosphate with this enzyme are also provided. In addition, a screening assay for identification of drugs activated by this enzyme is described.

Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.

Abstract: A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.

Abstract: The present invention relates to the use of a Shiga toxin B-subunit moiety as carrier for therapeutic agents, for example, anti-cancer agents such as anti-cancer agents that require intracellular uptake to exert their anti-cancer effects. In particular, the present invention provides conjugates comprising a Shiga toxin moiety covalently linked to an anti-cancer agent through a self-immolative spacer, and methods of using such conjugates to increase cellular uptake and/or specificity for cancer cells of the anti-cancer drug. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment.

Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

Abstract: This invention pertains to methods of increasing the bioavailability and/or cellular uptake of an amphiphilic drug when administered parenterally, which method comprises the step of parenterally co-administering the drug with a short-chain sphingolipid as described herein.

Abstract: Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.

Abstract: Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for inhibiting proteasomal activity and for treating cancer is also provided.

Abstract: A method for determining a therapeutically effective amount of suramin for administering to a patient, who is to receive a cytotoxic agent, which comprises the steps of determining the circulating suramin concentration in the patient; administering suramin, if required, to establish a low circulating concentration of suramin in the patient of below about 200 ?M; and administering the chemotherapeutic agent to the patient when the low circulating concentration of suramin is present in the patient. Conveniently a nomogram can be constructed for use in clinical settings with the suramin.

Abstract: The invention provides methods for treating and preventing a neurodegenerative disease associated with aberrant protein aggregation by modulating the expression and/or activity of XBP-1, IRE-1 alpha, and/or EDEM. The present invention also pertains to methods for identifying compounds that modulate the expression and/or activity of XBP-1, 1RE-1 alpha, and/or EDEM. The present invention further provides methods for determining whether a subject is at risk of developing or has developed a neurodegenerative disease associated with aberrant protein aggregation.

Abstract: The present invention relates to polyphenol compounds, compositions thereof, and methods for treating or preventing cancer in a subject, the methods comprising co-administering to a subject an effective amount of two or more polyphenol compounds or a polyphenol composition thereof.

Abstract: Disclosed herein are methods and compositions for determining the sensitivity or enhancing the sensitivity of cells to the effects of topoisomerase I inhibitors. Also disclosed are methods and compositions for inducing cell death, apoptosis and/or growth arrest which may be used for tumor suppression.

Abstract: An oil body carrier, its uses in target therapy and/or detection, and a fusion protein comprised therein are provided. The oil body carrier comprises: a) the fusion protein, comprising an oil body protein and a ligand peptide, an antibody peptide, a cell penetrating peptide, or combinations thereof, and b) a lipid, wherein the weight/volume (?g/?l) ratio of the fusion protein and the lipid is at least about 1/25, and the average particle size of the oil body carrier is about 10 nm to about 2,000 nm.

Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.

Abstract: Novel methods of treating proliferative disorders characterized by elevated Her-2, and the patient is then administered an effective amount of an HSP90 inhibitor.

Abstract: A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises poorly water soluble nanoparticles formed by the API together with a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.

Abstract: The present invention provides a PEGylated and fatty acid grafted chitosan oligosaccharide comprising a structural unit represented by the following Formula (I) and a structural unit represented by the following Formula (II) and synthesize method, wherein the chitosan oligosaccharide has a molecular weight of less than 200,000 Da, and a degree of deacetylation of 70%-100%, and part of free amino groups of chitosan oligosaccharide chain are replaced by a fatty acid or PEG, where n refers to degree of polymerization of the PEG, and R is an alkyl group having 11-21 carbon atoms. The grafting ratio of fatty acids is 1%-50%, and the grafting ratio of PEG is 0.05%-50%. The present invention also comprise a pharmaceutical composition comprising the PEGylated and fatty acid grafted chitosan oligosaccharide as a carrier, and use of the PEGylated and fatty acid grafted chitosan oligosaccharide in preparation of a pharmaceutical composition.

Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.

Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.

Abstract: The subject invention concerns materials and methods for treating oncological disorders in a person or animal using any agent or compound that inhibits uptake of glucose into a cell. The subject invention also concerns methods for inducing apoptosis and inhibiting the proliferation or survival of a cell. In one embodiment, the methods comprise administering an effective amount of an agent or compound that inhibits the activity of one or more glucose transporter proteins, such as Glut-1. An antibody that binds to and inhibits a glucose transporter protein can be used in the present methods.

Abstract: The invention relates to agents which possess anti-angiogenic activity and are accordingly useful in methods of treatment of disease states associated with angiogenesis in the animal or human body. More specifically the invention concerns a combination of an antagonist of the biological activity of Angiopoietin-2 and an antagonist of the biological activity of VEGF-A, and/or KDR, and/or Flt1, and uses of such antagonists.

Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.

Abstract: This invention relates to improved liposomal camptothecin compositions and methods of manufacturing and using such compositions for treating neoplasia and for inhibiting angiogenesis.

Abstract: The present disclosure provides lipid-containing compositions, including targeted liposomes encapsulating drug, and pharmaceutical formulations thereof, as well as methods for the making and using the lipid-containing compositions, including the use of the targeted liposomes in the treatment of cancer and other diseases.

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

Abstract: Provided is a novel therapeutic approach for the treatment of heart failure and diseases associated therewith. In particular, vinca alkaloids are used for improving the viability of cardiomyocytes and preventing myocardial infarction.

Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.