Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).

Abstract: An agent for treatment of dry eye comprising a combination of a P2Y2 receptor agonist at a therapeutically effective concentration and hyaluronic acid or a salt thereof at a therapeutically effective concentration, which agent has a dosage form of an ophthalmic agent, can promote the secretion of tear remarkably and can improve corneal epithelial disorders remarkably, and is therefore expected to be a novel agent for treatment of dry eye.

Abstract: This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors 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 an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).

Abstract: The present invention provides therapy and methods for the treatment and prevention of diseases of cell proliferation such as cancer, benign tumors, and viral diseases such as HIV-AIDS, hepatitis B, hepatitis C and cirrhosis. The methods of this invention consist of the administration to a patient of a combination of effective amounts of agents capable of eradicating the neoplastic cells, while sparing the non-neoplastic cells from cytotoxic side-effects. The agents co-administered in therapeutically effective amounts are: chemotherapeutic agents, apoptotic agents, anti-angiogenic agents, cell differentiation agents, immunomodulating agents, antioxidants, vitamins, microelements, enzymes and natural extracts.

Abstract: The compounds are of the class of pyrimidine analogs useful for treating cancer, for example:

Abstract: In one embodiment, the present application discloses synthetic LDL nanoparticles comprising mixtures of components selected from the group consisting of phospholipids, triglycerides, cholesterol ester and free cholesterol; optionally further comprising an agent selected from the group consisting of natural antioxidants, ubiquinol and vitamin E, and methods for preparing the synthetic nanoparticles. The disclosed synthetic LDL nanoparticles are capable of selectively delivering lipophilic drugs and prodrugs to cellular targets expressing LDL receptors after intra venous injection.

Abstract: The present disclosure relates to methods for the treatment of cancer in patients in recognized need of such treatment. The methods comprise administering to such a patient an NAE inhibitor or a pharmaceutically acceptable salt thereof, such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216), and a hypomethylating agent or a pharmaceutically acceptable salt thereof, such as azacitidine or decitabine. Also disclosed are medicaments for use in the treatment of cancer.

Abstract: The invention relates to compositions of nicotinoyl ribosides and nicotinamide riboside derivatives and their methods of use. In some embodiments, the invention relates to methods of making nicotinoyl ribosides. In some embodiments, the invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinoyl riboside. In further embodiments, the invention relates to methods of using nicotinoyl ribosides and nicotinamide riboside derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for improving cell and tissue survival.

Abstract: A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.

Abstract: The present invention uses methylomic analysis and discovers DNA methylation biomarkers for prediction of ovarian cancer prognosis and detection of malignant ovarian cancer. In addition to being independent prognostic factors for patients with current treatment protocols, these DNA methylations are important biomarkers for individualized medicine for future chemotherapy (especially the demethylation agents or other epigenetic drugs).

Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice for treating pancreatic cancer.

Abstract: A first aspect of the invention relates to a combination comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.

Abstract: The present invention is related to a compound conjugating a drug with a glycosaminoglycan, such as hyaluronic acid (HA), where the drug is useful for the treatment of diseases such as inflammation, auto-immune disease, allergy, infection and preferably cancer. The conjugated compound of the present invention can increase the concentration of drug at the specific site of disease by an interaction of the glycosaminoglycan used as target drug delivery carrier and the CD44 cell surface receptor, then enhancing the therapeutic efficacy and reducing the systemic side effect of the site-delivered drug.

Abstract: A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one, is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) with surprisingly superior efficacy and pharmacodynamic properties in vitro and in vivo. Also provided are pharmaceutical compositions including the compound and methods of use of the compound in treating cancer and tumors in vivo, as well as inhibiting glycolytic flux and PFKFB3 enzymatic activity in cells.

Abstract: Use of Neul sialidase inhibitors for the treatment of cancer as a monotherapy or in combination with known chemotherapeutics. Preferably, Neul sialidase inhibitors are oseltamivir phosphate or 2-deoxy-2,3-dehydro-N-acetylneuraminic acid (DANA) or analogues thereof.

Abstract: This application relates to methods of increasing survival or progression-free survival in a patient with a solid tumor, wherein the patient has an elevated serum concentration of C-reactive protein (CRP), by administering a JAK inhibitor or an inhibitor of IL-6 signaling to the patient, as well as methods of predicting survival benefit in these patients from such therapy.

Abstract: The present invention relates to flavone derivatives and to compositions containing one or more of these flavone derivatives. The present invention further relates to flavone derivatives or compositions for use in the treatment and/or prevention of a viral infection, and to a method of preventing or treating these infections.

Abstract: The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom 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: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

Abstract: The present invention provides compounds according to formula I: and pharmaceutically acceptable salts thereof. For compounds of formula I, R1 and R2 are independently selected from the group consisting of H, —C(?O)—(CH2)2-aryl, and —C(?O)—(CH2)n—C(?O)—NH-aryl. The subscript n is from 2 to 6. R3 is selected from the group consisting of H and —C(?O)—O—R4; and R4 is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, arylalkyl, substituted arylalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compounds are provided wherein at least one of R1 and R2 is other than H. Pharmaceutical compositions, methods for inhibiting the growth of cancer cells, and methods for the treatment of cancer are also provided.

Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.

Abstract: The present invention relates to the method of pre-preparing pharmaceutical compositions for therapeutic uses, particularly pre-preparing medications for treating patients (e.g., cancer patients and the like) by intravenous infusion.

Abstract: There is provided a film coated pharmaceutical composition comprising 5?-deoxy-5-fluoro-N-[(pentyloxy)-carbonyl]-cytidine (capecitabine) and at least one disintegrant selected from the group comprising of crospovidone (particle size <15-400?), croscarmellose sodium, sodium starch glycolate, low-substituted hydroxypropylcellulose, Pharmaburst C or any combination of these, together with other pharmaceutically acceptable excipients to form a rapidly disintegrating tablet. This tablet disintegrates in water at 37° C. in a USP Disintegration Apparatus in less than 2 minutes, preferably 1 minute and have a hardness of 8-13 strong Cobb-Units.

Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.

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: Described are methods and compositions for treating cancer that include a dopamine receptor (DR) antagonist such as thioridazine and a chemotherapeutic agent. Optionally, the chemotherapeutic agent is a DNA synthesis inhibitor such as cytarabine or a microtubule inhibitor such as paclitaxel or docetaxel. The methods and compositions are useful for the treatment of cancers such as acute myeloid leukemia.

Abstract: Provided herein are compounds, compositions, and methods for the treatment of viral infections, for example, Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are D-amino acid phosphoramidate halogeno pyrimidine nucleoside analog compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula I: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein: PD, X, R1, R2, RA, and RB are as described herein.

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 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 relates to the use of medium-chain length fatty acids of formula I, triglycerides of formula 2 (wherein n=6-10), salts thereof, or mixtures thereof, in combination with gemcitabine and optionally erlotinib in the treatment of pancreatic cancer in human patients. Exemplary medium-chain length fatty acid/triglyceride compounds include capric acid, sodium caprate, tricaprin, lauric acid, sodium laurate, and trilaurin.

Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Hepatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.

Abstract: The invention provides novel amphiphilic drug-drug conjugates useful as cancer therapeutics, and compositions and methods thereof.

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: The present invention features interferon-free therapies for the treatment of HCV. The therapies comprise administering 2R,6S,13aS,14aR,16aS,Z)-N-(cyclopropylsulfonyl)-6-(5-methylpyrazine-2-carboxamido)-5,16-dioxo-2-(phenanthridin-6-yloxy)-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-exadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a-carboxamide (Compound I), or a pharmaceutically acceptable salt thereof, and another anti-HCV agent. Preferably, the therapies are both interferon- and ribavirin-free. The other anti-HCV agent can be a HCV polymerase inhibitor, an HCV NS5A inhibitor, an HCV entry inhibitor, a cyclophilin inhibitor, or an internal ribosome entry site inhibitor. Preferably, the other anti-HCV agent is an HCV polymerase inhibitor. Also preferably, the other anti-HCV agent is an HCV NS5A inhibitor. Also preferably, the other anti-HCV agent is administered concurrently with Compound I or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.

Abstract: Provided herein are methods, assays and kits for evaluating a sample, e.g., a sample obtained from a cancer patient, to detect one or more hedgehog biomarkers and/or one or more cilium markers. Thus, the invention can be used, inter alia, as a means to identify patients likely to benefit from administration of one or more hedgehog inhibitors, alone or in combination with therapeutic agents; to predict a time course of disease or a probability of a significant event in the disease of a cancer patient; to stratify patient populations; and/or to more effectively treat or prevent a cancer or a tumor associated with hedgehog signaling.

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: Leucine-rich repeat kinase-2 (LRRK2) mutations are a common cause of Parkinson's disease. Inhibitors of LRRK2 kinase that are protective in in vitro and in vivo models of LRRK2-induced neurodegeneration were identified. The presently disclosed subject matter establishes that LRRK2-induced degeneration of neurons in vivo is kinase dependent and that LRRK2 kinase inhibition provides a potential new neuroprotective paradigm for treating Parkinson's disease.

Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.

Abstract: A superior antitumor agent is provided. A salt of 1-(2-deoxy-2-fluoro-4-thio-?-D-arabinofuranosyl)cytosine shows at least one or more of such characteristics as (1) it has superior antitumor activity, (2) it shows superior crystallinity, (3) it shows high water solubility, (4) it does not show deliquescent property, (5) it shows superior flowability, (6) it shows superior tableting property, (7) it can be manufactured with less environmental load, and (8) it can be manufactured in a large scale, and therefore it is useful as a bulk drug for medicaments.

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: 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: Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human pappilomavirus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.

Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.

Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.

Abstract: The present invention provides a combination comprising: a composition comprising at least one non-steroidal anti-inflammatory agent and at least one cytotoxic agent; and a composition comprising at least one ribonucleotide reductase inhibitor. The invention further includes kits comprising a combination of the invention and methods and uses of a combination of the invention for the treatment of cancer treatment of cancer, including solid tumors or tumor metastasis.

Abstract: The present disclosure relates to combinations of N-[2-(2,1,3-benzothiadiazol-5-ylamino)-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N?-(1,1-dimethylethyl)-urea and cytarabine and their use for treating AML or CML.

Abstract: A pharmaceutical composition or combination drug, which contains, as active ingredients, (a) a coordination compound composed of a block copolymer represented by the following formula I or formula II and cisplatin, and (b) gemcitabine hydrochloride. In the formulae I and II, R1, A, R2, R3, m and n are as defined in the description.