Abstract: The present invention provides methods, compositions, formulations, and kits related to acadesine, or a prodrug, analog, or salt thereof, and/or a blood clotting inhibitor for preventing or reducing adverse side effects in a patient. The type of patient that may benefit includes a patient with decreased left ventricular function, a patient with a prior myocardial infarction, a patient undergoing non-vascular surgery, or a fetus during labor and delivery.

Abstract: Provided in the following specification are precursors or synthons that are useful for the synthesis of various arabinose based chemical and radiochemical derivatives of nitroimidazole-containing azomycin arabinosides, such as radioiodinated 1-#-D-(5-deoxy-5-[I*]-iodoarabinofuranosyl)-2-nitroimidazole (*IAZA), and radiofluorinated 1-#-D-(5-deoxy-5-[18F]-iodoarabinofuranosyl)-2-nitroimidazole (18FAZA). Such compounds are useful in imaging, therapy, or radiotherapy. Further, various syntheses of said precursors/synthons and the incorporation of said precursors/synthons into kits is provided. The precursors/synthons provided herein allow for an improved and facile manufacturing process for nitroimidazole-containing azomycin arabinosides.

Abstract: A method of treatment of a human patient suffering from myeloid neoplasias, includes administrating a therapeutically effective amount of 5-aminoimidazole-4-carboxamide (acadesine), acadesine precursors or acadesine derivatives.

Abstract: It is an object of the present invention to provide a growth hormone secretagogue that is excellent in effect of promoting secretion of a growth hormone and is orally available. The growth hormone secretagogue of the present invention contains one or more selected from the group consisting of S-adenosylmethionine and/or a salt thereof, a Siberian larch extract, an olive extract, and a stilbene-based compound as an active ingredient. S-adenosylmethionine and/or the salt thereof may be a form itself of chemically synthesized S-adenosylmethionine and/or the salt thereof, or may be a microbial cell or a culture containing S-adenosylmethionine and/or the salt thereof. The stilbene-based compound may be an extract extracted from a Vitaceae plant or a Gnetaceae plant. The olive extract may be an extract separated from a fruit of olive.

Abstract: We disclose the synthesis and use of chiral ionic liquids based on a substituted pentose, furanose, hexose, or pyranose sugar. The compounds and processes to make or use them are provided.

Abstract: The present invention provides compounds of the formula, wherein A, B, G, R2, R6, and X are defined herein, pharmaceutical compositions of the same, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof.

Abstract: This invention is directed to novel compounds of formula (I) having the structure (I) wherein U, V, W, Z, R1, X1, X2, and Y are defined herein. The compounds of formula (I) and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals mediated, at least in part, by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV).

Abstract: Compounds containing nucleic acid bases or their precursors modified by enrichment at specific sites with heavy stable isotopes of elements naturally present at those sites in minute amount are useful for the treatment of diseases characterized by altered gene expression and altered pattern of epigenomic control. These compounds, when used as nutrients or in other medicinal application methods, can alter the DNA methylation pattern in a simple way through the well-understood mechanism of kinetic isotope effect (KIE). This effect could also be useful for modifying methylation kinetics in stem cell technology, cloning and as disease therapeutics.

Abstract: Provided in the following specification are precursors or synthons that are useful for the synthesis of various arabinose based chemical and radiochemical derivatives of nitroimidazole-containing azomycin arabinosides, such as radioiodinated 1-#-D-(5-deoxy-5-[I*]-iodoarabinofuranosyl)-2-nitroimidazole (*IAZA), and radiofluorinated 1-#-D-(5-deoxy-5-[18F]-iodoarabinofuranosyl)-2-nitroimidazole (18FAZA). Such compounds are useful in imaging, therapy, or radiotherapy. Further, various syntheses of said precursors/synthons and the incorporation of said precursors/synthons into kits is provided. The precursors/synthons provided herein allow for an improved and facile manufacturing process for nitroimidazole-containing azomycin arabinosides.

Abstract: A method for preparing [18F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0˜25 ?L of 40% TBAHCO3 or K2.2.2./K2CO3 (5˜25 mg/0.5˜3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water (1.0/0.2 (v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [18F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CH3CN as a solvent into a reactor and by reacting the same for 5˜35 minutes at 50˜120° C.; and a fourth step for preparing a pure [18F]fallypride by purifying the prepared [18F]fallypride product.

Abstract: The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including for example nuclease resistance.

Abstract: Nucleotide analogues comprising a reactive hydrazide function (formula II) used as initial synthons for preparing compounds (formula I) capable of inducing mutations or capable of inhibiting a DNA polymerase or a kinase provided. Nucleic acids comprising the nucleotide and nucleoside analogues are also provided. Methods of using the compounds are also provided.

Abstract: The invention relates to oligonucleotides including at least one lipophilic substituted nucleotide analog and a pyrimidine-purine dinucleotide. The invention also relates to pharmaceutical compositions and methods of use thereof.

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 disclosure relates to a method of treatment of a human patient suffering from a B-cell lymphoproliferative disorders such as B-cell chronic lymphocytic leukemia (B-CLL), splenic marginal zone lymphoma (SMZL), mantle cell lymphoma (MCL), follicular lymphoma (FL), lymphoplasmacytic lymphoma (LPL), and Waldenström syndrome (WS), by the administration of a therapeutically effective amount of 5-aminoimidazole-4-carboxamide riboside (acadesine) or its precursors (eg. its mono-, di- and tri-5?-phosphates). This makes acadesine and its bioprecursors (eg. its mono-, di- and tri-5?-phosphates) useful as therapeutic agents for B-cell lymphoproliferative disorders in humans. The surprising feature that T cells are virtually not affected means that the side effect (immunosuppression) is minor, what represents a therapeutical advantage of acadesine over cladribine, fludarabine and other nucleosides known in the art.

Abstract: Compounds for use as PET probes and methods for synthesizing and using these, comprising [18F]D-FAC and other cytosine and adenosine analogs.

Abstract: The present invention relates to a 2-nitroimidazole derivative, a diagnostic pharmaceutical composition which contains such 2-nitroimidazole derivative, the use of the 2-nitroimidazole derivative for the detection of hypoxic biological tissue as well a method for the detection of hypoxic biological tissue by the use of the 2-nitroimidazole derivative.

Abstract: To provide an excellent amidite for synthesizing modified nucleic acid, which enables a protective group therein to be removed under a moderate condition, thereby stably producing a hydroxyl group-containing modified nucleic acid, and a method for synthesizing modified nucleic acid using the amidite. Specifically, an amidite for synthesizing modified nucleic acid, expressed by General Formula (I): where X represents a base, Y represents a substituent, Z represents a protective group for protecting a hydroxyl group in the substituent, and Q represents one of a hydrogen atom, a hydroxyl group and a hydroxyl group protected by a protective group, wherein the protective group can be removed in an aprotic solvent, and when the protective group is removed, the hydroxyl group emerges in the substituent, and a method for synthesizing modified nucleic acid using the amidite.

Abstract: A method for the prophylaxis or treatment of an inflammatory bowel disease is provided, comprising administering to a patient having or at risk of developing an inflammatory bowel disease a therapeutically or preventatively effective amount of one or more ribofuranose derivatives having the Formula (I): wherein R is a group selected from a carboxamide, an amidine, and pharmaceutically acceptable acid addition salts thereof, and the configuration at the C2 carbon of the ribofuranose moiety is D or L. The one or more ribofuranose derivatives (I) may be used in combination with further active agents such as antivirals or agents effective against inflammatory bowel disease.

Abstract: Nucleosides, novel nucleoside analog compounds and their novel prodrug forms are disclosed. The novel compounds, prodrugs, 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: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.

Abstract: Novel monocyclic L-Nucleoside compounds have the general formula Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.

Abstract: Novel monocyclic L-Nucleoside compounds have the general formula Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.

Abstract: Nucleosides, novel nucleoside analog compounds and their novel prodrug forms are disclosed. The novel compounds, prodrugs, 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: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.

Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.