Abstract: This invention relates to methods for treating, preventing and/or managing hematopoietic neoplasm in a subject by administering to the subject combretastatin A-4 phosphate, or a pharmaceutically acceptable salt thereof. The method may further comprise co-administering a chemotherapeutic agent.

Abstract: The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.

Abstract: The present invention is directed toward the use of thyromimetic compounds that are thyroid receptor ligands, pharmaceutically acceptable salts thereof, and to prodrugs of these compounds for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.

Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.

Abstract: The present invention relates to 21-deoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and or prophylaxis of cancer or B-cell malignancies.

Abstract: The present invention relates to new oxazaphosphorine alkylating agents and/or immuno-suppressive agents, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5? oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.

Abstract: The present invention relates to methods for decreasing cellular DNA repair in a target patient; decreasing cellular NAD+ biosynthesis in a target patient; increasing efficiency of radiation therapy in a target patient; modulating nicotinamide phosphoribosyl transferase activity in a patient; or sensitizing a patient to a DNA damaging therapy. The invention relates to methods for treating a patient who received a toxic dose of an nicotinamide phosphoribosyl transferase inhibitor. The invention also relates to pharmaceutical compositions comprising a physiologically acceptable carrier; an effective amount of a NMPRT inhibitor; and nicotinic acid. The invention also relates to methods for treating a patient diagnosed with or suspected to have a cancer deficient in nicotinic acid pathway.

Abstract: The present disclosure relates to a kind of sodium alginate microsphere vascular embolus that contains water-soluble drug and preparation and application thereof. The embolus preparation falls into dry microsphere type and wet one that are made of degradable materials. The drug carrier can be sodium alginate, human serum albumin, chitosan or sodium hyalurate, solidifying and forming microsphere together with calcium ion solution under presence of static charge. The microsphere can have a diameter in the range of 20-1000 ?m and can be divided into a wide variety of sizes in case of need. The present disclosure adopts raw materials that are good at mechanical strength, bio-compatibility, bio-degradability and stability.

Abstract: This invention relates to novel 2-{6-[4-(2-hydroxy-ethyl)-piperazin-1-yl]-2-methyl-pyrimidin-4-ylamino}-thiazole-5-carboxylic acid (2-chloro-6-methyl-phenyl)-amide derivatives, and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by the inhibition of kinases including Src-kinase and Bcr-Abl kinase.

Abstract: This invention is related to a pharmaceutical combination that contains a Casein kinase 2 (CK2) peptide inhibitor (termed P15) along with the standard chemotherapeutic drugs used in cancer treatment and which are administered together, separated or sequentially. The chemothearapeutic drugs include cisplatin, taxol, alkaloids from Vinca, 5-fluorouracil, doxorubicin, cyclophosphamide, etoposide, mitomicin C, imatinib, iressa and velcade (vortezomib). The synergism between the P15 peptide and the anticancer drugs achieves an efficient concentration of each cytostatic drug in the combination which is from 10- to 100-fold lower than that for each cytostatic drug alone. The pharmaceutical combination described in this invention exhibits lower toxicity compared to that reported by the anticancer therapeutics and therefore, it represents a crucial advantage for its use in cancer therapy.

Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.

Abstract: The present invention provides improved treatment methods by the administration of the non-physiologic D-isomer of an IDO inhibitor.

Abstract: The invention at hand concerns trofosfamide containing film-coated tablets for oral application and a procedure for their production.

Abstract: The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.

Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).

Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).

Abstract: Compounds of the general formula are disclosed with activity towards treating diseases related to inflammation, such as cancer, neurodegenerative and cardiovascular diseases. Pharmaceutical compositions and methods of use are also described.

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.

Abstract: The present invention provides improved treatment methods by the administration of both an inhibitor of indoleamine-2,3-dioxygenase in addition to the administration of an additional therapeutic agent.

Abstract: Compounds useful in the treatment of metastatic melanoma and other cancers containing a triazine ring scaffold are described. These compounds may be classified into two groups: (1) two disubstituted triazine rings are covalently linked by an organic linker to each other and (2) one trisubstituted triazine ring.

Abstract: The present invention relates to orally effective ligands of the peripheral cannabinoid receptor CB2, especially (+)-?-pinene derivatives, and to pharmaceutical compositions thereof, which are useful for prevention, alleviation or treatment of autoimmune neurodegenerative disorders, in particular multiple sclerosis and associated symptoms. Methods of the invention are useful when the active ingredient is administered alone or in combination with existing therapeutic modalities. The compositions are administered by oral route.

Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formula I, II, III, I?, II?, I?, II?, Ia, IIa, or IIIa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

Abstract: Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1-2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.

Abstract: The present invention provides to methods of preventing, treating or ameliorating one or more symptoms associated with an autoimmune or inflammatory disorder utilizing combinatorial therapy. In particular, the present invention provides methods of preventing, treating, or ameliorating one or more symptoms associated with an autoimmune or inflammatory disorder comprising administering to a subject in need thereof one or more integrin ?V?3 antagonists and at least one other prophylactic or therapeutic agent. The present invention also provides compositions and articles of manufacture for use in preventing, treating or ameliorating one or more symptoms associated with an autoimmune or inflammatory disorder.

Abstract: New substituted benzazole 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: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric Nanoparticle form of thyroid hormone agonist, partial agonist or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: The present invention relates to the surprising discovery that agents that increase intracellular accumulation of NADH+H+ enhance the anti-cancer effects of angiogenesis inhibitors. Furthermore, treatment of a mammal with a combination of at least one angiogenesis inhibitor and at least one agent that enhances intracellular accumulation of NADH+H+ allows for the enhanced treatment and/or prevention of angiogenic diseases and disorders.

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: The present invention is in the fields of cell biology, immunology and oncology. The invention relates to the discovery that there is a relationship between the expression levels of the tumor suppressor gene smad4 (also known as dpc4) and integrin ?v?6, and the responsiveness of patient populations to ?v?6-active compounds and compositions (e.g., antibodies and other ligands that bind ?v?6), particularly in cancer cells from such patient populations, more particularly on carcinomas such as pancreatic carcinomas.

Abstract: Disclosed are compositions and methods used to treat and/or prevent cancer and metabolic diseases, such as psoriasis. In one aspect, the present invention pertains to the use of cross-linking analogs of vitamin D and its metabolites employed for the treatment of prostate cancer.

Abstract: Disclosed are methods of purifying glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups that are useful as antibacterial agents. The methods include contacting a solution of the glycopeptide derivatives with a polystyrene-containing resin, eluting the resin with an aqueous solution, and isolating the purified glycopeptide derivative.

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: An injectable polymer-lipid blend is provided as a localized drug delivery system for a pharmaceutically active agent. The blend may be prepared from a chitosan-based material, fatty acid and phospholipid. The chitosan-based material may be a water soluble chitosan derivative. The fatty acid may be a fatty acid or a fatty aldehyde, such as laurinaldehyde, having an acyl chain length of C8-C16. The rheological properties of the blend relates to the ratio of the components and to the acyl chain length of the fatty acid. The injectable system is well suited for the delayed release of pharmaceutically active agents in the treatment of cancer and other diseases requiring localized drug delivery.

Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and an IGF1R inhibitor compound of Formula I combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and IGF1R inhibitor compound of Formula I combination with a pharmaceutically acceptable carrier. The IGF1R inhibitor is represented by Formula I: wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein.

Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.

Abstract: The invention provides methods of identifying and making compounds that inhibit the interaction between MUC1 and either p53 or TBP. Also embraced by the invention are in vivo and in vitro methods of inhibiting such an interaction and of inhibiting the expression of MUC1 by a cell.

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: 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: A method for inducing ER? expression in cancer cells in a subject affected with cancer cells which are ER? (?) is disclosed. The method involves administering to the subject an effective amount of a PPAR? antagonist alone or in combination with anti-estrogen therapy.

Abstract: A preventive/therapeutic composition for free radical diseases, characterized by containing as an active ingredient at least one kind of a fullerene, a fullerene derivative, and a composite comprising a fullerene or fullerene derivative and an organic compound with which the fullerene or derivative has been modified or clathrated. The composition is reduced in side effects, has the high ability to eliminate free radicals in the body, and further has excellent preparation stability.

Abstract: The invention is based on the observation that certain phenols, monophenols or benzenediols, can be metabolized into reactive quinones, in particular ortho-quinones and related reactive intermediates, which is brought about by oxidation of monophenols and benzenediols by proteins exhibiting tyrosinase activity, such as human tyrosinase and the related proteins TRP1 and TRP2. Although the substances and the produced reactive intermediates are toxic and can induce cell death, it is more relevant according to this invention that they function as haptens that become covalently bound to the tyrosinase enzymes, in particular to histidine moieties, in or near the catalytic site of proteins exhibiting tyrosinase activity, such as tyrosinase, TRP1 and TRP2. An immune response is then to be mounted against these haptenized auto-antigens, in order to treat melanocytic malignancies, in particular melanomas.

Abstract: The present invention concerns certain hydrolytic thalidomide metabolites, combinations thereof with other anti-neoplastic compounds and their use in the treatment of solid tumours.

Abstract: The present invention relates to compounds according to the general formula wherein the dotted lines denote a single bond which is optionally present, with 2 dotted lines denoting a double bond; wherein, in case no double bond is present and a free valence exists, this valence is occupied by H; and wherein the symbols have the meanings defined in the text, or a pharmaceutically acceptable salt thereof, and which lend themselves for the manufacture of drugs useful in the inhibtion of DNA methylation, the inhibition of DNA methyltransferases, and may therefore be useful for the manufacture of pharmaceuticals for the treatment of developmental disorders such as Prader-Willi-Syndrome, Angelman-Syndrome (Happy Puppet Syndrome), Beckwith-Wiedemann-Syndrome, and proliferative diseases, such as coronary restenosis and neoplastic diseases, particularly colon carcinoma, familiary adenomatous polyposis carcinoma and hereditary non-polyposis colorectal cancer, prostate carcinoma, melanoma, non-Hodgkin lymphoma, acu

Abstract: The present invention provides a pharmaceutical composition comprising (a) a phosphodiesterase (PDE)-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases to be administered simultaneously or separately with an interval comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, as active ingredients; and the like.

Abstract: The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.

Abstract: Compounds of the structure I: are useful for treating bacterial growth, wherein E is selected from the group consisting of B, P, and S, T1 and T2 are each independently selected from the group consisting of O, NR, and CH2, where R=H or C1-C8 alkyl, or C1-C8 oxoalkyl, and L is selected from the group consisting of ethylene, propylene, and four to six-membered alicyclic and aromatic rings, provided that structure I does not include AI-2-borate. The compounds may be used to treat bacterial infections in human beings and to regulate biofilm formation. Pharmaceutical compositions comprising one or more such compounds are useful for treating bacterial infections in human beings.

Abstract: This invention provides a method for treating tumor in a subject comprising administering to the subject an effective amount of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a nucleoside analog. This invention also provides a method for inhibiting tumor cell growth comprising contacting the tumor cell with effective amounts of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a nucleoside analog. The present invention relates to the treatment of cancer, comprising administering to a subject in need thereof an effective amount of VNP40101M in combination with a nucleoside.

Abstract: This invention relates to compositions comprising haptenized tumor cells and extracts thereof, methods for preparing the compositions, vaccines comprising such haptenized tumor cells, and methods for treating cancer with such vaccines. In a specific embodiment, melanoma cells are haptenized with a dinitrophenyl group, and used for treatment of melanoma patients having metastatic disease. Preferably, patients are given a first vaccine dose containing haptenized cells to “prime” the immune system. Subsequently, patients are injected with an immunomodulatory compound such as cyclophosphamide. In a preferred embodiment, an appropriate time period after the “priming” vaccine dose, additional vaccine doses containing a mixture of haptenized cells and an adjuvant are administered. The described treatment plan is more effective for eliciting favorable anti-tumor immune responses.