Abstract: The present invention provides an aminopyrazole compound, or a pharmaceutically acceptable salt thereof, that inhibits Chk1 and is useful in the treatment of cancer.

Abstract: A liposome and preparation method thereof; the liposome is prepared from drugs, a phospholipid, a cholesterol-based compound, an internal buffering system and a pH adjusting agent; the drugs, the phospholipid and the cholesterol-based compound are in a weight ratio of 1:2-100:1-35; the drugs is a combination of a chloroquine-based drug and an adriamycin-based drug.

Abstract: The present invention concerns a method for predicting the responsiveness of an individual suffering from leukemia to a chemotherapeutic drug. In particular, this method comprises determining the proportion of leukemic cells expressing cytoplasmic PCNA in a biological sample of the individual. The present invention also relates to a tyrosine kinase inhibitor for use for the treatment of an individual suffering from leukemia and having a proportion of leukemic cells expressing cytoplasmic PCNA in a biological sample lower than a predetermined threshold. The invention also pertains to a method for diagnosing whether an individual suffers, or is at risk of suffering, from leukemia.

Abstract: This invention provides compositions, methods and process of producing extracts from Xanthoceras sorbifolia. The extract comprises alkaloids, coumarins, saccharides, proteins, polysaccharides, glycosides, saponins, tannins, acid, flavonoids and others. The composition can be used for treating cancer, arthritis, rheumatism, poor circulation, arteriosclerosis, Raynaud's syndrome, angina pectoris, cardiac disorder, coronary heart disease, headache, dizziness, kidney disorder, impotence and premature ejaculation; for preventing cerebral aging; for improving memory, cerebral functions; or for curing enuresis, frequent micturition, urinary incontinence, dementia, weak intelligence and Alzheimer's disease, autism, brain trauma, Parkinson's disease or other diseases caused by cerebral dysfunctions, and treating arthritis, rheumatism, poor circulation, arteriosclerosis, Raynaud's syndrome, angina pectoris, cardiac disorder, coronary heart disease, headache, dizziness, kidney disorder.

Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are 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 of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.

Abstract: The present invention relates to hydroxyalkyl starch (HAS) conjugates and to a method for preparing the hydroxyalkyl starch (HAS) conjugates, the hydroxyalkyl starch (HAS) conjugates comprising a hydroxyalkyl starch derivative and a cytotoxic agent, said conjugate having a structure according the following formula HAS?(-M)n wherein M is a residue of a cytotoxic agent, the cytotoxic agent comprising a carbonyl group, HAS? is a residue of the hydroxyalkyl starch derivative comprising at least one functional group X, n is greater than or equal to 1, and wherein the cytotoxic agent is linked via the carbonyl function present in the cytotoxic agent to the functional group X comprised in the hydroxyalkyl starch derivative, wherein the linkage via the carbonyl function is a cleavable linkage, which is capable of being cleaved in vivo so as to release the cytotoxic agent.

Abstract: A composition for preventing, improving, or treating renal diseases, the composition including as an active ingredient a Maillard browning reaction product obtained by reacting ginsenoside Re, an extract of Panax species plant including ginsenoside Re, or glucose with amino acid at a temperature of 100 to 130° C. for 0.5 to 12 hours.

Abstract: A pharmaceutical composition comprising protein micro and/or nanoparticles are provided. The particles have a predetermined geometric shape and a broadest dimension less than about 10 micrometers. The particles may further comprise active agents.

Abstract: The invention belongs to the pharmaceutical field, and particularly relates to a lyophilized formulation of pectin-adriamycin conjugate and a preparation method thereof. In order to solve insolubility problem of the pectin-adriamycin conjugate (hereinafter referred to as PAC), improve bioavailability and facilitate preparation, the inventor prepared the PAC into a nanosuspension. However, as long-term stability of the nanosuspension is poor, the inventor proposed to prepare the nanosuspension into a lyophilized formulation, that is, an insoluble pectin-adriamycin conjugate is prepared into a suspension or nanosuspension, and a lyophilized support agent is added to the suspension for lyophilization treatment to prepare the lyophilized formulation. Lyophilized products prepared from the nanosuspension are characterized by enhanced stability of nano-particle size and enhanced stability of drug loading rate, which provides a new solution for clinical application of the PAC.

Abstract: Nanocells allow the sequential delivery of two different therapeutic agents with different modes of action or different pharmacokinetics. A nanocell is formed by encapsulating a nanocore with a first agent inside a lipid vesicle containing a second agent. The agent in the outer lipid compartment is released first and may exert its effect before the agent in the nanocore is released. The nanocell delivery system may be formulated in pharmaceutical composition for delivery to patients suffering from diseases such as cancer, inflammatory diseases such as asthma, autoimmune diseases such as rheumatoid arthritis, infectious diseases, and neurological diseases such as epilepsy. In treating cancer, a traditional antineoplastic agent is contained in the outer lipid vesicle of the nanocell, and an antiangiogenic agent is loaded into the nanocore. This arrangement allows the antineoplastic agent to be released first and delivered to the tumor before the tumor's blood supply is cut off by the antianiogenic agent.

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 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: 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: Use of an animal model of spontaneous metastasis bearing a tumor derived from a cell line RM72 (Accession No. NITE BP-1110) allows simultaneous evaluation of tumorigenesis and spontaneous cancer metastasis. Use of a screening method using the animal model of spontaneous metastasis allows the obtainment of a substance having an anticancer activity and/or an anti-metastatic activity. Use of another screening method for selecting a substance that increases the expression of RECK in a cancer cell allows the obtainment of a substance that can serve as an active ingredient in an anticancer drug.

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: The present invention provides a nanodisc without a membrane scaffold protein. The nanodisc includes a telodendrimer and a lipid; the nanodisc does not include a membrane scaffold protein. The telodendrimer has the general formula PEG-L-D-(R)n, wherein D is a dendritic polymer; L is a bond or a linker linked to the focal point group of the dendritic polymer; each PEG is a poly(ethylene glycol) polymer; each R is and end group of the dendritic polymer, or and end group with a covalently bound hydrophobic group, hydrophilic group, amphiphilic compound, or drug; and subscript n is an integer from 2 to 20. Methods of making the nanodiscs are also provided.

Abstract: The present invention relates to a method for the production of functional dendritic cells wherein CD34 positive cells are contacted with compounds inducing and accelerating the differentiation of these CD34 positive cells into functional dendritic cells. More in particular, the CD34 positive cells are contacted with anthracyclines and/or anthracenediones. In another aspect, the current invention relates to the cells obtainable by the method according to the invention. In a further aspect the current invention relates to the use of compounds such as anthracyclines and/or anthracenediones that induce and accelerate the differentiation of CD34 positive cells into functional dendritic cells in the manufacture of a medicament for inducing an immune response in human in need thereof.

Abstract: The present invention relates to, inter alia, extracellular drug conjugates (EDC) in which an antibody or other targeting agent (e.g. a targeting moiety) is linked to a drug through a linker (e.g. a non-cleavable linker). These conjugates are useful in the treatment of disease and/or as a tool in the evaluation of biological systems.

Abstract: A liquid composition of an insoluble medicament and a preparation method thereof are disclosed. The composition includes insoluble medicament, oil for injection, phospholipid, and solvent; the percentage by weight of each component is as follows: insoluble medicament 0.01-10%, oil for injection 0%-20%, phospholipid 10-80%, solvent 20-89%. The preparation method for the composition includes the following steps: dissolving an insoluble medicament into solvent or oil for injection or a mixture thereof firstly, and then adding other components, and mixing uniformly; or dissolving an insoluble medicament into a mixture of other components, and mixing uniformly; or dissolving an insoluble medicament into part of solvent firstly, and then adding into a mixed solvent of other components and the remaining solvent, and mixing uniformly.

Abstract: Methods and compositions related to targeting agents to tumor tissue are described.

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: Described herein are compositions and methods for treating or preventing a sexually transmitted infection in a subject.

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 pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. 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 pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.

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.

Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.

Abstract: Disclosed herein are materials and methods for sensitizing multidrug resistant cancer cells that express ABCG2 and related proteins members of a family of ATP-binding transporter superfamily that mediate drug efflux found in some types of multidrug resistant cancer cells. A series of compounds, including (N-(4-chlorophenyl)-2-[(6-{[4,6-di(4-morpholinyl)-1,3,5-tri-azin-2-yl]amino}-1,3-benzothiazol-2-yl)sulfanyl]acetamide), specifically inhibits ABCG2 and can be used to boost the bio-avail-ability of one or more effective cancer killing drugs, making it possible to use certain widely used chemotherapeutic reagent to treat multidrug resistance cancers. Using these compounds in combination with chemotherapeutic drugs that are substrates for ABCG2 and related proteins may also find utility in treating cancer cells that are not currently identified as multi-drug resistant. Additionally, these compounds appear to accelerate the intercellular degradation of ABCG2 and related proteins.

Abstract: Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.

Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.

Abstract: The present invention provides optical agents comprising optically functional cross linked supramolecular structures and assemblies useful for tandem optical imaging and therapy. Supramolecular structures and assemblies of the present invention include optically functional shell-cross linked micelles wherein optical functionality is achieved via incorporation of one or more linking groups that include one or more photoactive moieties. The present invention further includes imaging and therapeutic methods using one or more optical agents of the present invention including optically functional shell cross-linked micelles having an associated therapeutic agent.

Abstract: The present invention relates to a method for effectively delivering an anticancer drug into cancer cells by binding the anticancer drug to pH-sensitive metal nanoparticles so as to be separated from cancer cells. The pH-sensitive metal nanoparticles according to the present invention may be heated by photothermal therapy, thereby effectively killing cancer cells in conjunction with the isolated anticancer drug.

Abstract: A combination therapy is disclosed for treating cancer. The method comprises administering to a cancer patient a therapeutically effective amount of trans-[tetrachlorobis(1H-indazole)ruthenate(III)] or a pharmaceutically acceptable salt thereof, and administering to the patient a therapeutically effective amount of one or more other anti-cancer agents as disclosed herein.

Abstract: Disclosed are compounds represented by formula (I), pharmaceutically acceptable salts thereof, solvates thereof, and solvates of the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, W and are as defined in the present application.

Abstract: The present invention relates to methods of treating pulmonary hypertension in a subject including administering to the subject a therapeutically effective dose of at least one anthracycline.

Abstract: Herein are provided derivatized hyperbranched polyglycerols (“dHPGs”). The dHPG comprises a core comprising a hyperbranched polyglycerol derivatized with C1C20 alkyl chains and a shell comprising at least one hydrophilic substituent bound to hydroxyl groups of the core, wherein the hyperbranched polyglycerol comprises from about 1 to about 200 moles of the at least one hydrophilic substituent. The dHPGs are for use as agents for the delivery of a drug or other biologically active moiety to the urinary tract, the digestive tract, the airways, the vaginal cavity and cervix and the peritoneal cavity to treat indications such as cancer, which may be useful in the treatment of or the manufacture of a medicament, in the preparation, of a pharmaceutical composition for the treatment of cancer, as a pre-treatment or co-treatment to improve drug uptake in a tissue. Furthermore, there are provided methods of making dHPGs.

Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as 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: The present teachings include ratiometric combinatorial drug delivery including nanoparticles, multi-drug conjugates, pharmaceutical compositions, methods of producing such compositions and methods of using such compositions, including in the treatment of diseases and conditions using drug combinations.

Abstract: The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provides methods of making the liposome compositions provided by the present invention.

Abstract: Nanoparticles comprising a prodrug and prodrugs linked to phospholipids, wherein the linkages facilitate release of the prodrugs from the nanoparticles to sites within a target cell or cell membrane by fusion of the particle and the cell membrane are disclosed. Also disclosed are methods for producing and using the nanoparticles and their constituents.

Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors 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 proliferative diseases, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: The invention provides a method of predicting the clearance rate of a carrier-mediated agent and/or the release of an agent from a carrier in a subject comprising measuring the number and/or activity of phagocytic cells and/or the amount and/or activity of opsonins and/or the amount and/or activity of complement within a biological sample obtained from a subject, and predicting the clearance rate of the carrier-mediated agent and/or the release of the agent from the carrier based upon the number and/or activity of the phagocytic cells and/or the amount and/or activity of opsonins and/or the amount and/or activity of complement.

Abstract: This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization from” approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling to” that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal” chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

Abstract: The present application relates to microvesicles derived from a protoplast which is a bacterial, arhaea, fungal or plant cell or the like from which a cell wall is removed. The microvesicles derived from a protoplast enables free loading of a material necessary for diagnosis, treatment, vaccine, target induction, cell membrane fusion with a target cell, reduction of in vivo and in vitro side effects, stability improvement, and the like, and allows the therapeutic material, the diagnostic material and/or the vaccine material to be delivered specifically to a specific tissue or cell.

Abstract: Methods for treating a cancer having a mutant isocitrate dehydrogenase (IDH), including, but not limited to, a malignant low-grade glioma, a secondary glioblastoma, a transforming myeloproliferative disorder (tMPD), and an acute myelogenous leukemia (AML), with a glutaminase inhibitor, including, bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES), are disclosed.

Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula: