Abstract: Embodiments disclosed in the present application relate to a composition that can include a hepatitis C viral nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof, a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof, and a hepatitis C viral non-nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof. Additional embodiments disclosed relate to methods for treating a disease condition such as a hepatitis C virus infection, liver fibrosis and/or impaired liver function with a hepatitis C viral nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof, a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof, and a hepatitis C viral non-nucleoside polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof.

Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.

Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.

Abstract: A compound of the general formula (III): wherein X is O, S, NH or CH2; Y is O, S or NH; Z is O, S or CH2; R1 is C1-8 alkyl, especially C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of R2 and R3 is H—[R4—R5]n—R6—, in which: H—[R4—R5]n— comprises an oligopeptide, R4 being an amino acid and R5 being an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, R6 is a neutral, non-polar amino acid moiety that is bonded to R5 by a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of R3 and R2 is H—[R4—R5]n-R6— or H; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.

Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.

Abstract: The present invention relates to methods for determining whether blood flow is restricted in a blood vessel of an individual suspected of compromised blood flow in the vessel, the method comprising the steps of delivering UTP, a derivative thereof, or a salt thereof to the vessel, assessing blood flow quantitatively in the vessel by obtaining a value that correlates to blood flow in said vessel, comparing the obtained value with a reference value, and determining whether the individual has compromised blood flow based on the results of the comparison. The invention also provides for methods of diagnosing atherosclerotic and ischemic heart diseases using UTP, a derivative thereof, or a salt thereof, as well as methods for inducing maximal hyperemia for diagnostic purposes.

Abstract: Acyclic nucleoside analogs such as acyclovir, ganciclovir, penciclovir and the corresponding pro-drugs, i.e., valacyclovir, valganciclovir and famciclovir, respectively have been identified as inhibitors or antagonists of both telomerase (encoded by TERT) and reverse transcriptase encoded by L-1 (LINE-1) RT, and as useful for treating or preventing cancers induced or mediated by the two enzymes. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase positive and telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing TERT and L1RT are also disclosed.

Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.

Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branchednucleosides, 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: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolised to a biologically active agent; and X is selected from the group consisting of R, or up to three R moieties attached to a linker, Y1, Y2 or Y3, wherein R is selected from a group consisting of alkyl, alkenyl, alkynyl, branched alkyl, branched alkenyl, branched alkynyl, substituted alkyl, substituted alkenyl and substituted alkynyl groups and their analogues; Y1 is a linker group which covalently attached to an R group at one site and is attached to A at a further independent site; Y2 is a linker group which is covalently attached to two R groups at two independent sites and is attached to A at a further independent site; and Y3 is a linker group which is covalently attached to three R groups at three independent sites and is attached to A at a further independent site.

Abstract: The present invention relates to the use of a taste masking agent selected from the group of cellulose; starch; xanthan gum; gellan gum; alginate; galactomannans such as fenugreek, guar gum, tara gum, locust bean gum, and cassia gum; gum karaya; gum tragacanth; carrageenan; and mixture thereof, for improving one or more of mouth feel, taste, aftertaste and smell of a liquid aqueous nutritional composition comprising a nucleotide and/or a nucleoside. It also relates to a nutritional composition comprising an unsavory nucleotide and/or a nucleoside component, having improved sensory characteristics such as improved mouth feel, taste, aftertaste and smell. In particular, it relates to a composition comprising said un-savory nucleotide and/or a nucleoside component, in particular comprising an uridine-containing nucleotide and/or a nucleoside in combination with an unsavory edible oil, such as a fish oil.

Abstract: In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.

Abstract: Provided herein are compositions comprising ningnanmycin or a derivative thereof, as well as their use for controlling or combating a fungal infection in a plant or plant part (e.g., a turfgrass).

Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.

Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R3, R4, R5a, R5b, R6, R7, R8a, R8b, M and W are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.

Abstract: Provided herein are compounds, compositions and methods for the treatment of 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.

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.

Abstract: Provision of a novel combined therapy with ECyd, which therapy exhibits remarkable antitumor effect and gives less adverse effects. The invention provides an antitumor agent containing, in combination, 1-(3-C-ethynyl-?-D-ribopentofuranosyl)cytosine or a salt thereof and carboplatin.

Abstract: The present invention provides methods of treating a cell proliferative disorder, such as lung cancer and breast cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound, such as (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, in combination with a therapeutically effective amount of a second anti-proliferative agent, such as gemcitabine.

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: Induction of telomere shortening, G2 arrest and apoptosis in telomerase positive cancer cells using acyclic nucleoside analogs has been disclosed. In addition, methods for impairment or prevention of tumorigenic telomerase positive cells from having a chance to grow into a tumor and methods for promoting tumor regression (decrease in size of an established tumor) using acyclic nucleoside analogs has been disclosed.

Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.

Abstract: The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional anti-neoplastic compound. In particular, the method relates to a methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional anti-neoplastic compound.

Abstract: Methods for selecting chemotherapeutic agents for treating a cancer are provided that include the steps of providing a cancer cell sample having a population of bulk cancer cells and a population of cancer stem-like cells, culturing a first portion of the cancer cell sample in a hydrodynamic focusing bioreactor under microgravity conditions and for a period of time to selectively enhance the population of cancer stem-like cells and selectively kill the population of bulk cancer cells, contacting the cancer stem-like cells with one or more chemotherapeutic agents, and then selecting the one or more chemotherapeutic agents for treating the cancer if there is an increase in an amount of cytotoxicity. Methods for treating a cancer are also provided in which the identified chemotherapeutic agents are administered to a subject. Further provided are methods for identifying a test compound useful for treating a cancer.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: A large volume infusion dosage form of gemcitabine, comprising a stable large volume solution of gemcitabine or its pharmaceutically acceptable salt in an aqueous vehicle filled in a large volume infusion container, wherein the solution is ready-to-be-infused.

Abstract: The present invention provides administration methods for CDPC for treating stroke. CDPC was delivered via ECS at a concentration of 40 mmol/L-60 mmol/L. In a specific embodiment of the present invention, the concentration of CDPC administered is 50 mmol/L, CDPC is delivered at one time, the flow rate of administration is 0.2 ?L/min, the volume of CDPC is 1.33 ?L/mL of brain tissue, and the CDPC is administered in the caudate nucleus. The method can decrease the concentration of CDPC entering the brain and further decrease the dosage while improving efficacy. Thus, the result is improved and the probability of adverse effects due to the drug is reduced.

Abstract: Compounds represented by the formula 1: wherein each R individually is H, an aliphatic acyl group or an aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, halo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro; are used to treat or prevent arthritis including rheumatoid arthritis.

Abstract: The invention concerns a pharmaceutical composition containing micronized fenofibrate, a surfactant and a binding cellulose derivative, as solubilizing adjuvant, preferably hydroxypropylmethylcellulose. The cellulose derivative represents less than 20 wt. % of the composition. The association of micronized fenofibrate with a binding cellulose derivative, as solubilizing adjuvant and a surfactant enables enhanced bioavailability of the active principle. The invention also concerns a method for preparing said composition without using any organic solvent.

Abstract: Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions. In specific instances, provided herein are intravenous compositions and therapies.

Abstract: Provision of a novel combined therapy with ECyd, which therapy exhibits remarkable antitumor effect and gives less adverse effects. The invention provides an antitumor agent containing, in combination, 1-(3-C-ethynyl-?-D-ribopentofuranosyl) cytosine or a salt thereof and carboplatin.

Abstract: The present invention relates to the use of a tri-substituted glycerol compound for the manufacture of a medicament for the treatment of hematological malignancies. The invention also refers to a kit-of-parts comprising such a medicament. Finally, the invention also relates to a corresponding method for the treatment of such conditions as well as to an in vitro method for determining the susceptibility of such malignant cells to a medicament as defined in the invention.

Abstract: The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.

Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.

Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2. or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.

Abstract: The subject invention concerns materials and methods for treating or preventing a neurodegenerative condition or disease associated with ?-amyloid peptide deposition in neural tissue in a person or animal by administering a therapeutically effective amount of a polyphenol, or an analog, isomer, metabolite, or prodrug thereof, that increases expression or activity of a protein that exhibits ?-secretase activity. The subject invention also provides methods to increase ?-secretase expression and/or activity in cells by administering polyphenol flavonoids like (?)-epigallocatechin-3-gallate (EGCG) and epicatechin (EC), two polyphenols derived from green tea and other plants and that can be produced synthetically. Furthermore, there are provided methods to decrease or inhibit the production of A?1-40 or A?1-42 by administering the EGCG and EC compounds, their analogs, metabolites, and prodrugs.

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: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 4-amino-1-(2-deoxy-2,2-difluoro-?-D-erythro-pentofuranosyl)pyrimidin-2(1H)-on 2?,2?-difluoro-2?-deoxycytidine, or a pharmaceutically acceptable salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR?R? where R? is H and R? is CR5R6CO2R7, where R6 is H, R5 is the side chain, including H and C1, of a naturally occurring alpha amino acid, and R7 is branched or unbranched, substituted or unsubstituted, acyclic or cyclic alkyl, including t-butyl-CH2-, benzyl and C3 to C6 cycloalkyl. Formula (I).

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.

Abstract: Bioactive agents are embedded in a cross-linked dextran and coated with a bioresorbable polymer. When implanted in a mammal, the coated cross-linked dextran composition produces controlled release of the embedded bioactive agent.