Abstract: The invention provides combinations comprising a) compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R5, R10, and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.

Abstract: A composition having a structure of: X-L-Y wherein X comprises at least one embelin moiety; L comprises a linker; and Y comprises a hydrophilic moiety. Also disclosed is a micelle that includes: a core that includes at least one hydrophobic active agent and at least one embelin moiety; and a hydrophilic zone surrounding the core and comprising at least one hydrophilic moiety.

Abstract: Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. The one or more HIF-1 inhibitors can be dispersed or encapsulated in a polymeric matrix. In some embodiments, the one or more HIF-1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.

Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying cancer by administering nanoparticles that comprise rapamycin or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof. The invention further provides combination therapy methods of treating cancer comprising administering to an individual an effective amount of nanoparticles that comprise rapamycin or a derivative thereof and a second therapy.

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

Abstract: The present invention provides novel substituted pyrazolone 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: The present invention provides liposomal compositions and methods of using such compositions in vitro and in vivo. In particular, the present invention provides stable, polymer-caged liposomes comprising a pH responsive delivery mechanism for delivery of nucleic acids, peptides, small molecules, drugs, etc. in vitro and in vivo.

Abstract: Described herein are methods and compositions for treating HER2-amplified cancer. The methods include administering to an individual in need thereof ibrutinib.

Abstract: The present invention relates generally to a method of treating a neoplastic condition and to agents useful for same. More particularly, the present invention is directed to a method of facilitating the treatment of a solid tumor in a localised manner via the co-administration of particulate material and a cellular toxin. The method of the present invention is useful in a range of therapeutic treatments including the treatment of primary and metastatic tumors.

Abstract: The present invention provides small molecules useful to affect cancer cells, along with related methods. The present compounds, formulations, kits and methods are useful for a variety of research, diagnostic and therapeutic purposes. STAT3 inhibitors, particularly LLL12, are disclosed. The STAT3 inhibitors are useful to treat breast cancer in general and breast cancer initiating cells in particular.

Abstract: The present invention relates to a high-density lipoprotein (HDL)-like particle composite which is a drug-encapsulating apoA-I comprising apoA-I and a drug encapsulated in the apoA-I capable of releasing the drug encapsulated in the apoA-I under acidic pH conditions, and a preparation method thereof. Since the HDL-like particle composite of the present invention can release the encapsulated drug under acidic conditions, while remaining stable under non-acidic conditions over a wide temperature range, it can be widely used for the development of target-specific drugs.

Abstract: The present invention provides novel substituted pyrazolone 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: A chemotherapy agent or a pharmaceutical composition including chemotherapy agent and artificial cerebrospinal fluid, wherein the chemotherapy agent at a concentration of between 0.01 mg/ml and 0.

Abstract: A mammal undergoing an energy-based therapy is treated by administering at least one vasoconstrictive agent to the mammal prior to or during the procedure. The at least one vasoconstrictive agent is added in amounts sufficient to reduce or prevent vasodilation. This treatment method increases or promotes the size of the coagulation zone created after energy-based therapy.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: Oral dosage compositions for drugs normally given intravenously such as Paclitaxel, containing a plant sterol to enhance solubility and a small intestine efflux inhibitor to prevent P-glycoprotein from being a barrier to absorption.

Abstract: A liposome comprising bilayer and inner water phase is disclosed. Said inner water phase may contain sulfobutyl ether cyclodextrin and an active compound.

Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.

Abstract: Gene mutations are associated with the progression of acute myeloid leukemia (AML). The invention relates to methods and systems for evaluating the progression of AML based on these gene mutations. The present invention also relates to methods and compositions for treating AML patients by modulating the expression or activity of certain genes involved in AML progression and/or their encoded proteins. The invention further relates to methods and compositions for determining the responsiveness of an AML patient to induction chemotherapy therapy.

Abstract: The present invention relates to pharmaceutical composition containing nemorubicin hydrochloride incorporated in microspheres. The compositions are useful for chemoembolization, particularly for loco regional treatment of tumors.

Abstract: N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy}-benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, alone or in association with surgery, chemotherapy or hormone therapy treatment or radiotherapy, for use in the treatment of cancer, characterised in that it is administered for 4 consecutive days, that period being followed by 3 consecutive days without any administration of compound of formula (I), with the proviso that the chemotherapy is not FOLFOX.

Abstract: A delivery device for a active agent comprises nanoparticles based on a biopolymer such as starch. The delivery device may also be in the form of an aptamer-biopolymer-active agent conjugate wherein the aptamer targets the device for the treatment of specific disorders, such as cancer. The delivery device survives for a period of time in the body sufficient to allow for transport and uptake of the delivery device into targeted cells. The degree of crosslinking can provide a desired release profile of the active agent at, near or inside the target cells. The nanoparticles may be made by applying a high shear force in the presence of a cross linker. The particles may be predominantly in the range of 50-150 nm and form a colloidal dispersion of crosslinked hydrogel particles in water.

Abstract: A liquid embolic material may include a mixture of a first solution comprising between about 1.2% and about 2.5% weight per volume (w/v) carboxymethyl chitosan (CCN) in a first solvent and a second solution comprising between about 1.2% and about 2.5% w/v oxidized carboxymethyl cellulose (OCMC) in a second solvent. The liquid embolic material may be used to embolize a targeted embolization location by mixing the first solution and the second solution to form a liquid embolic material (or hydrogel precursor material), introducing the hydrogel precursor material to a targeted embolization location within a body of a patient, and allowing the CCN and the OCMC to react to form the hydrogel material and embolize the targeted embolization location.

Abstract: The present invention generally relates to compositions containing chemical compounds and compositions and pharmaceutical formulations of the compounds which increase the expression of total hemoglobin or globin protein such as embryonic or fetal globin, or the proliferation of hemoglobin expressing and other blood cells. These compositions can be used to treat or prevent the symptoms associated with anemia, sickle cell diseases, thalassemia, and other blood cell deficiencies and blood disorders. The invention also relates to methods for administering these compositions to subjects and for use as medical aids for the treatment and prevention of blood and other disorders.

Abstract: A method is disclosed for the preparation of glycerol esters (triglycerides) of medium-chain length monocarboxylic fatty acids which consists of the reaction of the precursor free fatty acid and glycerol in the presence of a catalyst under partial vacuum. The process preferably uses a metal catalyst such as an oxide or a chloride of tungsten, molybdenum, calcium, zinc, chromium or magnesium. The method of the invention allows the preparation in high yield and high purity (>99.5%) of the final triglyceride. The present method allows the formation of triglycerides without solvent. Are also contemplated, the triglyceride obtained by the method, and the pharmaceutical composition containing the triglyceride as an excipient or as an active ingredient.

Abstract: The present invention relates to a carrier that is targeted at fucosylated molecule-producing cells, which comprises an effective amount of fucose for targeting said cells, to a composition comprising the carrier, and to a method for treating and diagnosing a disease related to fucosylated molecule-producing cells utilizing said carrier, etc. The carrier of the present invention enables to deliver a substance specifically to fucosylated molecule-producing cells.

Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.

Abstract: Curcumin analogues and methods are provided for treatment of disease.

Abstract: The present invention relates to the use of which are attached or anchored phospholipid biolayers further modified by CRLF-2 and CD 19 binding peptides which may be used for delivering pharmaceutical cargos, to cells expressing CRLF-2 and CD 19, thereby treating cancer, in particular, acute lymphoblastic leukemia (ALL), including (B-precursor acute lymphoblastic leukemia (B-ALL). Novel CRLF-2 binding peptides and CLRF-2 and CD19-binding viral-like particles (VLPs) useful in the treatment of cancer, including ALL are also provided.

Abstract: Methods are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.

Abstract: This invention relates to a method of treating B cell malignancies, which involves administering to a subject a compound having a structure of formula (I) to cause cell death of a B cell malignancy, thereby treating the B cell malignancy in the subject. Also disclosed are a method of causing cell death of malignant B cells, pharmaceutical compositions and therapeutic systems comprising a compound having a structure of formula (I), and a compound having a structure of formula (I).

Abstract: The present invention relates generally to the pathology of restenosis. In particular, provided herein are devices comprising a compound that selectively decreasing smooth muscle cell proliferation without a substantial decrease in endothelial cell proliferation. Also provided are methods of using such devices to treat, prevent, or reduce vascular disease or the likelihood of restenosis following angioplasty.

Abstract: The present invention relates to the cosmetic use by external topical route of steviol, of a steviol glycoside derivative or of one of their isomers to stimulate, restore or regulate the metabolism of the cells of the skin.

Abstract: Disclosed herein are ?-galactosylceramide (?-GalCer) analogs and compositions thereof, methods of activating invariant Natural Killer T (iNKT) cells using said analogs, methods of treating diseases by activating iNKT cells using said analogs, and combination therapy of said analogs.

Abstract: A therapeutic agent delivery system includes a therapeutic agent delivery platform and a therapeutic guest agent. The therapeutic agent delivery platform is capable of being implanted in a tissue being treated. The platform includes a substrate and at least one host molecule coupled to the substrate. The therapeutic guest agent is capable of reversibly coupling with the host molecule when administered to the tissue being treated. The reversible coupling is defined by the binding affinity between the host molecule and the therapeutic guest agent. The therapeutic guest agent is delivered at a rate determined by the affinity release rate between the host molecule and the therapeutic guest agent. The degradation rate of the therapeutic guest agent may be slower than the affinity release rate between the host molecule and the therapeutic guest agent.

Abstract: Liposomes with an entrapped amphipathic weak base and alkyl or aryl sulfonate are described as well as methods of making and using these liposomes.

Abstract: The present invention relates to compositions, kits, and methods for detecting, characterizing, preventing, and treating cancer (e.g., hematological malignancies in humans). A variety of biomarker chromosomal number alterations (CNAs) and biomarkers corresponding thereto, are provided, wherein alterations in the copy number of one or more of the biomarker CNAs and/or alterations in the amount, structure, and/or activity of one or more of the biomarkers comprised within the CNAs is associated with cancer status.

Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.

Abstract: The invention relates to therapeutic agents for use in the prevention or treatment of Alzheimer's disease. In particular the invention relates to use of inhibitors of cell cycle reentry and progression to the G1/S transition or inhibitors of progression of the cell cycle through the G1/S transition point in the prevention or treatment of Alzheimer's disease.

Abstract: This invention provides compounds capable of reducing drug resistance in a subject undergoing cancer treatment, methods using the compounds, compositions, and methods for identifying such compounds.

Abstract: The invention relates to (among other things) a method comprising the steps of (a) administering to a patient a topoisomerase II-inhibiting amount of a long-acting topoisomerase II inhibitor; and (b) administering to the patient a topoisomerase I-inhibiting amount of a long-acting topoisomerase I inhibitor.

Abstract: This disclosure describes methods of screening for compounds that disrupt the interaction between DNMT1 and the gamma-globin promoter or between LSD-1 and the gamma-globin promoter. This disclosure describes methods of screening for compounds that de-repress the gamma-globin gene.

Abstract: The invention provides methods for predicting or determining the response of a mammalian tumor to a chemotherapeutic agent and for treating a mammalian tumor comprising detecting and quantifying the SPARC protein or RNA in a sample isolated from the mammal. The invention further provides kit for predicting the response of a mammalian tumor to a chemotherapeutic agent, comprising a means for the isolation of protein or RNA from the tumor, a SPARC protein or RNA detection and quantification means, control RNAs, and rules for predicting the response of the tumor based on the level of SPARC protein or RNA in tumor.

Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.

Abstract: The invention encompasses micelle assemblies, compositions having micelle assemblies, and methods for preparing micelle assemblies and compositions thereof. The invention also encompasses a prolamine protein conjugated to a polymer, such as a polyethylene glycol (PEG) chain, which conjugates can be used to prepare micelle assemblies. The invention further encompasses methods of encapsulating molecules using the conjugates of the invention. The micelle assemblies can be used for a variety of applications, such as treating cancer, targeting tumors, reducing the toxicity of a drug in vivo, increasing the efficacy of an encapsulated agent in vivo, protecting an encapsulated agent against degradation, and enhancing the water solubility of a drug or other agent.

Abstract: This disclosure features optically active stereoisomers of (2-(4-methoxy)quinolin-4-yl)(piperidin-2-yl)methanol that reduce drug resistance, compositions containing the same, and methods of using and preparing the same.

Abstract: The present invention relates to a method of inhibiting growth of a cancerous cell. The method includes the step of exposing the cancerous cell to an anti-cancer therapy and an effective amount of a steroid saponin.

Abstract: The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.

Abstract: The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.

Abstract: The present invention provides a compound of Formula (I), wherein: each X is independently hydrogen or deuterium; and at least one X is deuterium.