Abstract: Analogs or derivatives of nitrobenzylthioinosine corresponding to formula I: in which R represents an unsubstituted or mono- or polysubstituted phenyl, benzyl or heteroaryl group or a phenyl group condensed with heteroaryl, and R? represents an unsubstituted or mono- or polysubstituted NH—C1-6-alkyl, NH-aryl, NH-heteroaryl, NH—C3-8-cycloalkyl, NH—C1-3-alkyl-aryl, NH—C1-3-alkyl-heteroaryl, N(C1-6-alkyl)2, N(C1-3-alkyl-aryl)2, N(C1-3-alkyl-heteroaryl)2, piperidine, piperazine, morpholine or pyrrolidine group; pharmaceutical compositions comprising such analogs or derivatives, and the use of such analogs or derivatives for treating pain and/or various other diseases.

Abstract: Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).

Abstract: A method is provided for reducing weight in a subject by administering an effective amount of a composition comprising omega-3 polyunsaturated fatty acid (PUFA), at least one of L-arginine, L-ornithine, an L-arginine precursor and an L-ornithine precursor, and at least one of a nucleobase, a nucleoside and a nucleic acid. The method can also be used to treat obesity, hyperlipidemia, diabetes and/or hypertension and for improving diathesis, or treating adult disease or disposition to adult disease.

Abstract: The present invention provides a solid composition for oral administration comprising: (i) a drug compound; (ii) chitosan or a derivative thereof or a salt of chitosan or salt of a derivative of chitosan; and (iii) an organic acid. Preferably the drug compound is a polar molecule having a molecular weight of 1 KDa or less, a peptide, a protein or a polysaccharide. The compositions of the invention provide enhance absorption of the drug compound.

Abstract: The invention concerns pharmaceutical formulas designed for the treatment of diseases related to CFTR channel dysfunction, such as cystic fibrosis, asthma or diarrhoea. These formulas contain a molecule, coming in the form of a zwitterion at physiological pH, with the general formula: where X?N or P; and Y?O or S.

Abstract: This invention relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof and an additional therapeutic agent to a patient in need of such treatment.

Abstract: The present invention provides various biomarkers of depression. The present invention also provides various methods of using the biomarkers, including methods for diagnosis of depression, methods of determining predisposition to depression, methods of monitoring progression/regression of depression, methods of assessing efficacy of compositions for treating depression, methods of screening compositions for activity in modulating biomarkers of depression, methods of treating depression, as well as other methods based on biomarkers of depression.

Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.

Abstract: Hyperbranched, water-soluble polymers, obtainable by Michael polyaddition of ?-, ?-, or ?-cyclodextrins and amines to bisacrylamides.

Abstract: 2?-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy; R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5? end.

Abstract: The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and/or pain associated with diseases. The P2X receptor antagonists useful for this invention are non-nucleotide compounds of general Formula I. Compounds of Formula I can be used alone to treat pain. Compounds of Formula I can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the therapeutic effect of pain reduction.

Abstract: The use of squalenic acid or a derivative thereof in formulating at least one polar active principle with a molecular weight of 100 Da or more, in the form of nanoparticles, and pharmaceutical compositions thereof.

Abstract: A nutrient composition comprises an essential nutrient in which at least one exchangeable H atom is 2H and/or at least one C atom is 13C. The nutrient is thus protected from, inter alia, reactive oxygen species.

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: 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: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.

Abstract: Methods of treatment and pharmaceutical combinations are provided for the treatment of acute leukemia, such as acute myelogenous leukemia, and myelodysplastic syndrome. The methods of treatment and pharmaceutical combinations employ an anti-CD33 cytotoxic conjugate in combination with at least one compound selected from the group consisting of an anthracycline and a pyrimidine or purine nucleoside analog. Preferred methods of treatment and pharmaceutical combinations employ gemtuzumab ozogamicin, daunorubicin, and cytarabine.

Abstract: Azole nucleosides represented by the formulae (I) and (II); wherein A=C or N B?C or N X?H; C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br and I; OH, NH2, NH—(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo); Z?H; C1-C6 alkyl, cycloalkyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I; OH NH2, NH—(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo; E=(CH2)HONHR; n is an interger from 0-6 and more typically 0-3; R1= aryl or heterocyclo; each of W, Y, R is individually selected from the group consisting of H; C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, and I; O, OH, Oalkyl, Oaryl, NH2, NH(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo); provided that at least one of W, Y, and R is other than H and wherein both W and Y together can be ?O; and each D individually is OH, Oalkyl, Oaryl, FL and H; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are provided.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: The present invention relates to new dimethylphenoxy inhibitors of viral protease or parasitic enzymes, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention provides compounds capable of treating against hepatitis infections, particularly hepatitis B viral infections. Compounds of the invention are nucleic acid-based and preferably comprise 2, 3, 4, 5 or 6 nucleoside units.

Abstract: Cyclic di-GMP or cyclic dinucleotides thereof can be used to inhibit cancer cell proliferation or to increase cancer cell apoptosis in vitro as well as in vivo in a patient.

Abstract: Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor.

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: The present invention relates to the use of riluzole or pharmaceutically acceptable salts of riluzole in the production of drugs for restoring and amplifying the immune function in the treatment of infectious diseases and cancers.

Abstract: The present invention relates to the field of improving the flavour of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. More particularly, the present invention provides flavour modulating substances selected from the group represented by formula (1): and edible salts thereof and edible esters thereof, which can advantageously be used for modulating the flavour of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. These flavour modulating substances can be used to impart desirable taste attributes in a wide variety of applications and products. In addition, the present flavour modulating substances are capable of modulating the taste and/or aroma impact of other, flavour imparting, substances contained within these same products, thereby improving the overall flavour quality of these products.

Abstract: The present invention relates to methods for treating, killing, and/or inhibiting the growth of Herpes viruses in human subjects comprising topically administering to a human subject in need thereof a nanoemulsion composition having antiviral properties.

Abstract: The invention provides novel mercaptopurine derivatives, e.g., S-allylthio-6-mercaptopurine and S-allylthio-6-mercaptopurine 9-riboside, as well as pharmaceutical compositions thereof. These compounds are highly efficient anti-proliferative agents, thus can be useful for treatment of various diseases or disorders, in particular, proliferative, inflammatory, skin and immune diseases or disorders.

Abstract: Provided are methods of designing a putative inhibitor of a human 5?-methylthioadenosine phosphorylase (MTAP). Also provided are methods of inhibiting a human MTAP.

Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.

Abstract: Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:

Abstract: It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural “riboswitches” (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies.

Abstract: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing agent such as paclitaxel, and a telomerase inhibitory agent such as AZT. The invention also provides methods for identifying other agents with telomere damage-inducing activity and/or telomerase inhibitory activity (as well as and compositions having such activity), for use in the treatment of cancer.

Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.

Abstract: The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs. In particular, the invention provides isoguanosine nucleosides and derivatives thereof as well a method of increasing the mutation rate of a virus such as bovine viral diarrhea virus (BVDV) and hepatitis C virus (HCV).

Abstract: The present invention relates to a compound having inhibitory activity on a Rho-GTPase cell protein, the compound having the formula I (Formula I) wherein A is selected from N and N—H, R1 is selected from H and NHR3, R2 is selected from NHR4, OR4, O and halogen, R3 is selected from H and —COR5, R4 is selected from H, a C1-C6 alkyl and a substituted or unsubstituted phenyl, R5 is selected from a C1-C12 alkyl and a substituted or unsubstituted phenyl, R6 is selected from H, —COR5, —CO2R5, —PR7R8 and —PR7R8OPR7R8R8R7, R7 is selected from O and S, R8 is selected from H, OR4 and OSATE (—OCH2CH2SCOR5), and wherein each represents a single bond or a double bond, provided that when one of them is a double bond the other one is a single bond, and pharmaceutically acceptable salts and derivatives thereof. In particular, the compounds of the invention may be used as antitumor agents the action of which interfere with the signaling pathways normally involved in tumor development processes.

Abstract: In accordance with the present invention, there are provided methods for the treatment of mitochondrial disorders. Invention methods include the administration of a pyrimidine-based nucleoside such as triacetyluridine, or the like. Also provided are methods of reducing or eliminating symptoms associated with mitochondrial disorders. Mitochondrial disorders particularly appropriate for treatment include those attributable to a deficiency of one or more pyrimidines.

Abstract: Novel nucleoside analog compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.

Abstract: Pharmaceutical composition, containing fixed doses of hydroxyurea and didanosine, a method of manufacturing such composition, and to the use of the composition for the treatment of retroviral infections.

Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.

Abstract: The present invention discloses a method for treating HIV that includes administering ?-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using ?-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. ?-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.

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: The present invention provides ribonucleoside 2?,3?-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2?,3?-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection.

Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers and an immunostimulatory oligonucleotides for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers and an immunostimulatory oligonucleotides of the invention preferably comprise novel purines. The immunomers according to the invention further comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunomodulatory oligonucleotide and having an accessible 5? end.

Abstract: Methods of providing pain relief by administering a water-soluble derivative of spicamycin. Methods of using pain mediation agents are also provided.

Abstract: Disclosed are methods for treating hepatitis C viral infections using deaza-purine compounds of Formula I: wherein W, W1, W2, Y, R1, Z, Y? and R are as defined herein.

Abstract: This invention relates to methods of treating or preventing lupus comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate or clathrate thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing lupus comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate or clathrate thereof and an additional therapeutic agent to a patient in need of such treatment.

Abstract: 2? and 3?-Prodrugs of 1?, 2?, 3? or 4?-branched ?-D or ?-L nucleosides, or their pharmaceutically acceptable salts and derivatives are described, which are useful in the prevention and treatment of Flaviviridae infections and other related conditions. These modified nucleosides provide superior results against flaviviruses and pestiviruses, including hepatitis C virus and viruses generally that replicate through an RNA dependent RNA reverse transcriptase. Compounds, compositions, methods and uses are provided for the treatment of Flaviviridae infection, including HCV infection, 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.