Abstract: Porous calcium phosphate implant compositions that approximate the chemical composition of natural bone mineral are provided. In addition to calcium phosphate, the compositions include an effervescent agent to promote the formation of interconnected pores and a cohesiveness agent to maintain the shape and hardness of the hardened composition. When introduced at an implant site, the calcium phosphate compositions are remodeled into bone. Methods for using the calcium phosphate compositions, e.g., to repair or replace bone, are also provided.

Abstract: The present invention provides fusion proteins comprising an extracellular domain of a VEGF receptor and a death ligand. The fusion proteins bind to VEGF and to death receptors on tumor cells thereby inhibiting VEGF activation of VEGF receptors and inducing apoptosis in the tumor cells. Fusion proteins of the present invention are useful for inducing apoptosis and cytotoxic effects in cells, treating cancer and diseases or disorders related to unregulated angiogenesis and/or vasculogenesis. Thus, this invention further provides methods for treating angiogenesis related diseases using the fusion proteins, polynucleotides encoding the fusion proteins, vectors containing the polynucleotides, pharmaceutical compositions and kits containing the fusion proteins or the polynucleotides encoding the fusion proteins.

Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.

Abstract: The present invention relates to the use of one or more compounds selected from the following classes of biologically active agents: an a-adrenergic antagonist, an anthelmintic agent, an antifungal agent, an antimalarial agent, an antineoplastic agent, an antipsychotic agent, an antioxidant, a vasodilator and/or a vitamin, or a pharmaceutically acceptable derivative thereof, for use in the treatment of a microbial infection and in particular for killing multiplying, non-multiplying and/or clinically latent microorganisms associated with such an infection.

Abstract: The present provides amphiphilic block copolymer coated surfaces (e.g., nanoparticles, medical devices, etc.) and methods of preparing such surfaces. In certain embodiments, the present invention provides amphiphilic block copolymer coated single dispersed nanoparticles, which are stable in buffer (e.g., PBS) and have neutral but functionable surfaces, and methods of preparing the same.

Abstract: The present invention provides a pharmaceutical preparation for tumor chemotherapy and a method for producing the same, the pharmaceutical preparation for tumor chemotherapy comprises cell vesicles derived from apoptotic tumor cells and chemotherapeutic drugs as active ingredients wrapped within the cell vesicles. The chemotherapeutic drugs contained within the pharmaceutical preparation are chemotherapeutic drugs containing active ingredients for the treatment of the tumors from which the cell vesicles are provided. The present invention also provides a method for producing the pharmaceutical preparation for tumor chemotherapy. The technical solutions provided by the present invention can selectively release the chemotherapeutic drugs to the tumor sites and maintain lasting medicinal effect, increasing their killing effects against tumor cells and reducing the toxic side-effect of the chemotherapeutic drugs to normal cells.

Abstract: Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.

Abstract: Provided are compositions and uses thereof in methods of inhibiting angiogenesis, metastasis, or both, wherein said compositions comprise phosphaplatins such as pyrodach-4. In some embodiments, provided are compositions and uses thereof in methods of treating sensitive and resistant cancers.

Abstract: Disclosed are methods and compositions for determining and/or predicting a response to a therapy, especially a cancer therapy, including chemotherapy. Specifically, the disclosure provides profiles of a set of marker genes in breast cancers from patients who were known to have responded or not responded to a chemotherapy for predicting response to the same therapy including different combination of chemotherapy in a patient diagnosed with breast cancer. The disclosure further provides computer complemented methods for the prediction based on genetic profiles as well as different clinical parameters. Furthermore, the disclosure provides kits for performing the method disclosed.

Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: The present invention is directed to a method for preparing colloidal dispersions of precious metal nanoparticles selected from the group consisting of Pt, Au, Pd, Ag, Rh, Ru and mixtures or alloys thereof, and to a method for isolating such precious metal nanoparticles from these colloidal dispersions. The colloidal dispersions are prepared by reducing suitable precious metal precursor compounds in aqueous alkaline solutions at reaction temperatures between 40 and 70° C. and a pH?12.0 in the presence of polysaccharides with average molecular weights (Mw) in the range of 300,000 to 1,000,000. The precious metal nanoparticles are isolated after decomposing the polysaccharide by heating the colloidal dispersions to temperatures >80° C. The nanoparticles can be used for the manufacture of core/shell-type catalyst materials and for electronic, decorative and medical applications.

Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.

Abstract: This invention describes a method for treating cancer by increasing the nuclear localization of the COMMD1 protein, which is associated with decreasing or blocking the proliferation of the cancer cell. The invention is also related to the use of agents that increase nuclear localization of the COMMD1 protein, in the manufacture of a medicament for cancer therapy. These agents can be peptides or proteins, among other compounds. The invention is also related to the optimization of a peptide, coming from the sequence HARIKPTFRRLKWKKYKGKFW, to increase the nuclear localization of the protein COMMD, and thus, to increase the antitumor effect of this peptide.

Abstract: The present invention relates to a method of increasing blood brain barrier (“BBB”) permeability in a subject. This method involves administering to the subject an agent or agents which activate both of the A1 and A2A adenosine receptors. Also disclosed is a method to decrease BBB permeability in a subject. This method includes administering to the subject an agent which inhibits or blocks the A2A adenosine receptor signaling. Compositions relating to the same are also disclosed.

Abstract: Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:

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: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes.

Abstract: Some embodiments of the present invention relate to methods and compositions for treating cancer. More embodiments include methods and compositions for modulating the activity of the Hedgehog pathway.

Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.

Abstract: Disclosed are heterocyclic derivatives, methods for making them, compositions containing the same and uses thereof. Particularly, their pharmaceutical use as inhibitors of PARP is disclosed.

Abstract: The invention provides methods for treating various types of cancer/tumor by administering the combination of Dll4 antagonists, in particular, Dll4 antibodies and fragments thereof that specifically bind human Dll4, and chemotherapeutic agents. Such combination therapies exhibit synergistic effects compared to the treatment with either agent alone. Thus, the methods of the invention are particularly beneficial for cancer patients who have low tolerance to the side effects caused by high dosages required for the treatment by either agent alone, by being able to reduce effective dosages. Pharmaceutical compositions and kits containing Dll4 antagonists and chemotherapeutic agents are also provided.

Abstract: The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing cancer and other related diseases that result in dysregulation of malic enzyme 2. In particular, the methods and compositions include combination therapy, such as with a combination of two or more ME2 inhibitors or a combination of an ME2 inhibitor and an anticancer agent.

Abstract: The present invention relates to a pharmaceutical composition for treating a neoplasm, a preneoplasm, a proliferative disorder and/or a precancerous lesion, the use of such compositions for the treatment of the listed conditions, and methods of treating the listed conditions. The composition of the present invention comprises an inhibitor of eIF4E, a methltransferase inhibitor, and a pharmaceutically acceptable carrier.

Abstract: In the present invention there is provided a pharmaceutical composition for oral administration which comprises bendamustine or a pharmaceutically acceptable, ester, salt or solvate thereof as an active ingredient, and a pharmaceutically acceptable excipient and which shows a dissolution of the bendamustine of at least 60% in 20 minutes, 70% in 40 minutes and 80% in 60 minutes, as measured with a paddle apparatus at 50 rpm according to the European Pharmacopoeia in 500 ml of a dissolution medium at a pH of 1.

Abstract: This invention relates to therapeutic combinations comprising a platinum-based anti-neoplastic agent, such as cisplatin, and an extract from a species of the genus Nerium, such as Nerium oleander, as well as methods of using such combinations to treat subjects, including humans, suffering from certain cancers, such as prostate cancer, melanoma, pancreatic cancer, lung cancer, breast cancer, or colorectal cancer.

Abstract: The present invention provides a pharmaceutical composition, useful for the treatment of diseases characterized by abnormal PTKs activity of erbB family in a mammal, comprising pharmaceutically acceptable salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy) phenylamino]quinazolin-6-yl}-acrylamide, optionally a pharmaceutically applicable carrier or diluent, and a stabilizer having a dispersing and/or protective effect on the active ingredient. The present invention further provides a pharmaceutical formulation comprising said composition, methods for preparation of said composition and said formulation, as well as use of said composition and said formulation for treating diseases characterized by abnormal PTKs activity of erbB family in a mammal.

Abstract: In the present invention there is provided an oral pharmaceutical composition, comprising bendamustine or a pharmaceutically acceptable, ester, salt or solvate thereof as an active ingredient, and a pharmaceutically acceptable excipient, which is a pharmaceutically acceptable non-ionic hydrophilic surfactant.

Abstract: Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.

Abstract: Expression of Forkhead-box protein A1 (FOXA1), a transcription factor important for the normal development of the prostate gland is thought to be controlled by steroid hormones and GATA-3. Expression of FOXA1, GATA-3 and androgen receptor (AR) was retrospectively analyzed by immunohistochemistry (IHC) in a series of 80 primary tumors and 28 metastatic prostate cancers including 15 matched paired samples. High nuclear FOXA1 expression was seen in 19% of primary tumors and 89% of metastatic tumors (p<0.0001). FOXA1 expression correlated positively with tumor size, extra-prostatic extension, angiolymphatic invasion, AR and metastasis but did not correlate with age, tumor stage, Gleason score, presence of PIN or multifocality, seminal vesicle or perineural invasion and status of surgical excision margins. Expression of GATA-3 was not seen in either normal epithelium or tumor. High FOXA1 expression is associated with development of metastatic prostate cancer.

Abstract: The invention is directed to methods of monitoring B-cell lymphoid proliferative disorders, such as B-cell acute lymphoblastic leukemias, by measuring the presence, absence and/or levels of correlating, or index, clonotypes and related clonotypes that have evolved therefrom, for example, as part of the disease condition. In one aspect, such methods are implemented by generating sequencing-based clonotype profiles and determining frequencies of correlating, or index, clonotypes present, including new clonotypes that have evolved therefrom, particularly, in the case of B-cell ALL, by VH substitution. The invention also includes use of such monitoring information to modify treatment status of a patient.

Abstract: In one aspect, a method for treating a subject having a hyperproliferative disorder is disclosed, including administering to the subject a composition including: IPM, an IPM analog, or a pharmaceutically acceptable salt thereof in the dosage from about 70 mg/m2/day to about 160 mg/m2/day; etoposide in the dosage up to about 100 mg/m2/day; and one or more of carboplatin, cisplatin, oxaliplatin, picoplatin, or a combination thereof in the dosage of from AUC 2 mg/mL/min to AUC 7 mg/mL/min; wherein the treatment does not result in a dose limiting toxicity.

Abstract: Provided are a self-assembled conjugate of a host molecule containing compound and a guest molecule containing compound, a delivery composition of a bioactive material comprising the self-assembled conjugate and a bioactive material to be delivered, and a composition for tissue engineering containing the self-assembled conjugate and a cell.

Abstract: A vascular embolization gelling agent for sustained release of drugs for treating tumors having a drug and a drug carrier. The drugs are antitumor drugs. The drug carrier includes poloxamer polymer and polyvinylpyrrolidone or gel made of the combination, and may be purified before use. The drug carrier accounts for 5-65% of the gel. The particle size of the gel is in the range of 10 nm-150 ?m. The embolization agent is a liquid gel at normal temperature, to facilitate direct transcatheter injection, and is rapidly solidified to the gel state in body with the increase of the temperature; it is used to encapsulate different drugs on demand, and can achieve dual efficacy of embolization and drug treatment through local sustained release of the drug. The present invention can be used as the embolization agent for endovascular interventional therapy for transcatheter arterial chemoembolization of various benign and malignant tumors.

Abstract: The present invention relates to imidazopyrazine compounds of general Formula (I): in which X, R1, R2, R3a, R3b, R4a, R4b, R4C, and R4D are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.

Abstract: The present invention relates to drug combinations and pharmaceutical compositions for treating hyperproliferative disorders such as cancer including non-small cell lung carcinoma, said drug combination comprising (1) a fluoro-substituted-diaryl urea of Formula (I), (2) at least one antifolate and optionally (3) at least one platinum complex antineoplastic nucleic acid binding agent, where any of these components can be present in the form of a pharmaceutically acceptable salt or other derivative thereof.

Abstract: Disclosed is a means for improving the clinical outcomes of cancer therapy. Specifically disclosed is an activity potentiator comprising a compound capable of inhibiting the expression of RFP (RET finger protein) gene or the activity of RFP as an active ingredient. The activity of an anti-cancer agent having an oxidative stress inducing ability can be potentiated by using the anti-cancer agent in combination with the activity potentiator. Further specifically disclosed are a biomarker useful for the recognition of prognosis in a cancer patient and use of the biomarker.

Abstract: A pharmaceutical combination comprising a topoisomerase II inhibitor, and an Hsp90 inhibitor according to the following formulae a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.

Abstract: The present invention relates to a pharmaceutical composition for elevating radiation-sensitivity of cancer cells, which comprises: a nanoparticle containing with a first element, which is iron, copper, or the combination thereof; and a pharmaceutically acceptable carrier, wherein the nanoparticle is a metal nanoparticle, an alloy nanoparticle, or a metal nanoparticle with core-shell structure, and the size of the nanoparticle is under a controllable range of 3 nm to 150 nm. In addition, the present invention provides a detection method to detect radiation-sensitivity of the cancer cells through different modalities such as CT or MRI due to its native high CT number and magnetic property. Furthermore, the present invention provides a pharmaceutical composition for elevating radiation-sensitivity of the cancer cells through preferential uptake of the nanoparticle, in order to enhance the radiation-sensitivity of the cancer cells and improve the efficiency of radiation therapy to the cancer cells.

Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.

Abstract: Novel Uses of an aromatic ester isolated from Armillaria mellea, particularly, armillaridin, are disclosed herein. The armillaridin is useful for manufacturing a medicament or a pharmaceutical composition for suppressing the growth of cancerous cells or for enhancing susceptibility of esophageal cancerous cells to a radiation treatment, in a subject.

Abstract: The invention provides a method for inhibiting EGF receptor activity comprising contacting an EGF receptor with an immunomodulatory protein (GMI) from Ganoderma microsporum, or a recombinant thereof. Also provided is a method for treating invasion and metastasis of cancer cells, comprising administering an effective amount of an immunomodulatory protein (GMI) from Ganoderma microsporum, or a recombinant thereof, to a subject in need of such treatment.

Abstract: The present invention relates to mannopyranoside-derived compounds and to the use thereof as medicaments, in particular in the treatment of cancer diseases, and also to the method for preparing same and to pharmaceutical compositions comprising such compounds. Medical devices surface-treated with mannopyranoside-derived compounds according to the invention also form part of the invention.

Abstract: This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.

Abstract: Hyperhalogens, a new class of highly electronegative species, are now invented. A hyperhalogen is a superhalogen-containing composition in which the electron affinity (EA) of the hyperhalogen is even larger than that of the superhalogens they are composed of. Novel production methods are provided in which highly electronegative species are produced by surrounding a central metal atom by superhalogen moieties.

Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract: Methods to sensitize tumor cells to radiation therapy through the administration of an endothelin agonist such as the ETB agonist IRL1620.

Abstract: The invention provides drug compositions with synergistic effects, which includes alcohol-soluble and water-insoluble liquorices extracts and at least one kind of anti-tumor or glucose-and-lipid-lowering drug/eatable substance, and can be used to treat tumor or lower blood glucose and lipid. Besides, the invention also provides pharmaceutical preparation, pharmaceutical application, therapeutic and preparation methods, etc. related to this drug compositon.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.