Abstract: Disclosed herein are compounds having Formula I, which are non-natural L-adenosine analogs. Also disclosed are their methods of making. Still further, disclosed are the uses of the disclosed compounds to treat cardiovascular disease, ischemia related injuries; and neurodegenerative diseases. The compounds disclosed herein have the formula: wherein R1 and R2 are, independently, H, branched or straight-chain, substituted or unsubstituted alkyl, alkenyl, alkynyl, or aryl; R3 is branched or straight-chain, substituted or unsubstituted alkyl, hydroxy-alkyl, or —C(?O)NR6R7; and R4 and R5 are, independently, H, hydroxy, halogen, and NR8R9, wherein R6, R7, R8, and R9 are, independently, H, branched or straight-chain, substituted or unsubstituted alkyl, alkenyl, alkynyl, or aryl.

Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, an ischemic condition, a reperfusion injury, obesity, a wasting disease, or diabetes, comprising administering an effective amount of a Purine Derivative to an animal in need thereof.

Abstract: The present application discloses methods and compositions for increasing patient tolerability during myocardial imaging comprising the administration of doses of caffeine and one or more adenosine A2A receptor agonists to a mammal undergoing myocardial imaging.

Abstract: A subject-matter of the invention is a cosmetic method for caring for wrinkled skin, for the purpose of softening the wrinkles, comprising the successive stages: (a) of topical application to the wrinkled areas of a first composition including a pulverulent phase comprising porous particles which comprise at least one antiwrinkle active principle at least partially absorbed in the said particles, the said composition being substantially devoid of solvent for the said active principle, and (b) of topical application to the skin of the face comprising at least the said areas of a second composition including a fatty and/or aqueous phase comprising a solvent for the said active principle.

Abstract: Extended release formulations of S-methyladenosylmethionine (SAMe) are provided, as are methods of treating various disorders using extended release SAMe formulations. The extended release formulations may be used to treat a variety of disorders, including liver disorders, psychiatric disorders and joint disorders. Thus, extended release SAMe formulations may be used to treat alcoholic liver disease, fatty liver disease, hepatitis, generalized anxiety disorder, obsessive compulsive disorder, post traumatic stress disorder, panic disorder, and depressive disorders such as depression (e.g. major clinical depression) and dysthymia.

Abstract: The present invention relates to the use of S-adenosyl-L-methionine or its salts for preparing a composition for the regulation of behavioral problems in pets.

Abstract: A conjugate between an anti-thrombotic agent and a bioabsorbable polymer is provided. In addition, a method is provided for applying a coating comprising an anti-thrombotic agent and a bioabsorbable polymer conjugate to at least a portion of an implantable device to prevent or reduce the formation of thrombosis on the surface of the device. A first or sub-layer of the coating is prepared by mixing a polymeric material and a biologically active agent with a solvent, thereby forming a homogeneous solution. A second or outer layer comprises an anti-thrombotic heparin-bioabsorbable polymer conjugate. This coating may be applied over the inner drug-containing layers using, for example, a dip coating or spray coating process. After drying, the anti-thrombotic heparin bioabsorbable polymer conjugate remains in the outer layer of the coating, allowing agent from the inner layer to be eluted there through.

Abstract: The present disclosure relates to diets, compounds, e.g., GCN2 agonists and methods that selectively reduce adipose tissue mass relative to the mass of other tissue types and increase insulin sensitivity. Another aspect of the disclosure relates to methods for identifying GCN2 agonists that will decrease the activity and/or expression of one or more of adipogenic genes thereby selectively inhibiting the cellular mechanisms that lead to fat production. Such agonists have the effect of reducing adipose tissue mass in an individual.

Abstract: Adenosine analogue-type A3 receptor agonists having the formula wherein D is N or CH; E is O; X1 is a group of the formula —CR20R2 1-CYCLE, where R20 and R21 are the same or different and are H, F or CH3; CYCLE is where G is N, CH, CF, CCH3 or CCF3, M is H, Y is —O— or N?, and Z is —N? when Y is O, or is O when Y is —N?; R5 is H, CH3, I, Br, Cl, CF3, OH or NH2; and R8 is —NR9R10, —CHR9R10 or —N?CR9R10, where R9 and R10 are the same and are C1-C4 alkyl, C1-C4 alkenyl or C1-C4 alkoxyalkyl X2 is mono-N— or di-N,N—(C1-C4)alkylaminocarbonyl, mono-N—or di-N,N—(C3-C5)cycloalkyl-aminocarbonyl or N-(C1-C4)alkyl-N-(C3-C5)cycloalkylamino-carbonyl; X3 is OH or NH2; X4 is OH; X5 is H , halogen, (C1-C10)alkyl , (C2-C10)alkenyl , (C2-C10)alkynyl , or either of the latter two groups where terminally substituted by an aryl or heteroaryl group and, when having a terminal methyl group, optionally further terminally substituted by hydroxyl.

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: This document describes compounds, extracts, and pharmaceutical compositions relating to Gastrodia spp., and methods for the treatment subjects having metabolic disorders or medical conditions such as Huntington's disease, a trinucleotide repeat disease or abnormal blood glucose levels.

Abstract: Novel compound having the following formula: wherein W represents a hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C3-6 cycloalkyl, or an optionally substituted C1-6 haloalkyl, Y represents a hydrogen, or a saccharide, Q represents a quinoline or isoquinoline. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same.

Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor.

Abstract: The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, Formula: (1); wherein: R1 is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is an optionally substituted benzoquinone, optionally substituted naphthoquinone or optionally substituted fused heterocycloquinone: R2 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, aryl or heteroaryl; and R3 is selected such that R3NH2 represents a cytotoxic nucleoside analogue or an ester or phosphate ester prodrug of a cytotoxic nucleoside analogue, with the proviso that if R1 is an aryl group then R2 is not H.

Abstract: Stable compositions of S-adenosyl-1-methionine with dextran are described. The compositions according to the invention are stable over time and are valuable for use as active constituents in pharmaceutical and cosmeceutical preparations.

Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists having the structure of Formula I: which are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: The present invention provides a therapeutic method for treating an inflammatory response caused by autoimmune stimulation, comprising the administration to a patient in need thereof of an antiinflammatory amount amount of an A2A adenosine receptor agonist. The autoimmune stimulation can be caused by arthritis, particularly rheumatoid arthritis. Optionally, the method includes administration of a type IV PDE inhibitor.

Abstract: The present invention is directed to the systemic administration of Fosfluridine Tidoxil, (5-fluorouridine)-5?-phosphoric acid (3-dodecylmercapto-2-decyloxy)propylester or a salt thereof, for the treatment of intraepithelial proliferative diseases such as actinic keratosis. The Fosfluridine Tidoxil can be systemically administered alone or in combination with topical treatment agents.

Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formula I and III-XI, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds according to Formula I and III-XI.

Abstract: The invention relates to modulation of the immune system. More particularly, the invention relates to modulating the immune system through the use of oligonucleotide-derived compounds. The invention provides immunostimulatory agents that are less expensive to make than existing immunostimulatory oligonucleotides. The immunostimulatory agents according to the invention can, in preferred embodiments, cause immune stimulation across species lines.

Abstract: Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.

Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. Such derivative is useful as medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

Abstract: The present invention concerns the therapeutic treatment of inflammatory conditions by a combined administration of methotrexate and an agonist of the A3 adenosine receptor. Provided are methods of therapeutic treatment comprising such a combined administration, pharmaceutical compositions useful in such methods comprising either an and use if either an agonist of the A3 adenosine receptor or methotrexate, as well as used of any of these active agents for preparing such a pharmaceutical composition.

Abstract: The present disclosure describes a novel composition for the treatment and/or prevention of neurogenic inflammation. Such composition is also useful in the treatment and/or prevention of disease states and conditions associated with neurogenic inflammation. Such disease states and conditions include, but are not limited to, migraine headache, arthritis and fibromyalgia. The composition comprises nutrient compounds in a novel combination and formulation to treat and/or prevent neurogenic inflammation and disease states and conditions associated therewith. By reducing neurogenic inflammation, the compositions of the present disclosure reduce the symptoms associated with neurogenic inflammation, such as pain and systemic inflammation in general.

Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a compounds useful for this invention include compounds of general Formulae I and III-XII, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and III-XII.

Abstract: A method of prophylaxis or treatment of inflammatory conditions, including, but not limited to, intestinal epithelial inflammation due to intestine-specific conditions (e.g., Crohn's disease or ulcerative colitis) or systemic causes of inflammation (e.g., endotoxemia, sepsis, hemorrhagic shock/resuscitation or pancreatitis) is disclosed. In the method of the invention, an affected patient is administered a therapeutically effective amount of a composition including an NAD-related compound, in a form that is accessible to a receptor molecule, conveyed in a pharmaceutically acceptable carrier vehicle. NAD-related compounds include nicotinamide adenine dinucleotide (NAD+), cyclic adenosine diphosphate ribose (cADPR), or functionally equivalent analogues, derivatives, metabolites or agonists thereof or prodrugs therefor.

Abstract: The production of a purified extracellular bacterial signal called autoinducer-2 is regulated by changes in environmental conditions associated with a shift from a free-living existence to a colonizing or pathogenic existence in a host organism. Autoinducer-2 stimulates LuxQ luminescence genes, and is believed also to stimulate a variety of pathogenesis related genes in the bacterial species that produce it. A new class of bacterial genes is involved in the biosynthesis of autoinducer-2.

Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.

Abstract: The present invention relates to a method for a tailored treatment of mastocytosis comprising a) assessing whether or not a c-kit mutation at position 816 is detected in a sample of a patient and b) administering a specific 816 mutant c-kit inhibitor in case a mutation is detected in step a) or an inhibitor displaying efficacy on c-kit wild in case no mutation is detected in step a). The invention is more particularly suited 10 for treating category II, III and IV mastocytosis.

Abstract: A method for accelerating the process of removing ethanol from the blood through the use of certain additives that accelerate the metabolic oxidation of ethanol, and others which in addition act as catalysts or “pseudo” enzymes for the oxidation. These additives include multivalent transition metal ions, as well as complexes thereof, and NAD+ which enhance the oxidation reaction. The method described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: The present invention provides methods of inhibiting orthopoxvirus replication and/or treating orthopoxvirus infection with certain nucleoside compounds and derivatives thereof. These compounds are particularly useful as inhibitors of vaccinia virus and variola virus replication and/or for the treatment of vaccinia virus and variola virus infection. The nucleoside compounds may be administered alone or in combination with other agents active against orthopoxvirus infection, in particular against vaccinia virus or variola virus infection. Another aspect of the present invention provides for the use of such nucleoside compounds in the manufacture of a medicament for the inhibition of orthopoxvirus replication and/or for the treatment of orthopoxvirus infection. Yet a further aspect of the present invention provides such nucleoside compounds for use as a medicament for the inhibition of orthopoxvirus replication and/or for the treatment of orthopoxvirus infection.

Abstract: Physical forms of beta-L-2?-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2?-deoxythymidine can be used in the manufacture of other forms of beta-L-2?-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.

Abstract: 2-Substituted-5?-O-(1-boranotriphosphate)adenosine derivatives having at position 2 a radical R1 selected from the group consisting of H; halogen; O-hydrocarbyl; S-hydrocarbyl; NR3R4; and hydrocarbyl optionally substituted by halogen, CN, SCN, NO2, OR3, SR3 or NR3R4; wherein R3 and R4 are each independently H or hydrocarbyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring optionally containing 1-2 further heteroatoms selected from oxygen, nitrogen and sulfur, and pharmaceutically acceptable salts or diastereoisomers thereof or a mixture of diastereoisomers, are useful for treatment of type 2 diabetes.

Abstract: The invention relates to a composition for the stabilization of sulphur-containing amino acids and/or for the inhibition of the continuous formation of sulphur-containing amino acids in withdrawn blood, to the use of suitable substances and compositions therefor as well as optionally for the determination of sulphur-containing amino acids in blood, to a process for these purposes, as well as to a blood collecting device applied appropriately to these processes.

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-eythro-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: Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

Abstract: A chromium complex for use in treating metabolic disorders, particularly Type 1 and Type 2 diabetes.

Abstract: There is described a process for the synthesis of a fluoronucleoside compound, said process comprising mixing a substrate and an enzyme from Streptomyces cattelya as catalyst. The process may be used to produce an 18F labelled fluoronucleoside compound. There is also described an enzyme derived from Streptomyces cattelya which has the capacity to catalyse the synthesis of a fluoronucleoside compound.

Abstract: Novel compositions and methods are provided for identifying agents which affect chromosomal stability and aging.

Abstract: The present invention includes compositions and methods for the treatment of animals that are immunosuppressed by preparing a topical composition supplemented with one or more compounds selected from the group consisting of nucleotides, nucleosides, nucleobases and mixtures thereof in an amount effective for promoting wound healing and contacting the wound of the immunosuppressed mammal with the topical composition.

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: Disclosed is a synthesis suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonist having the structure of Formula I: wherein R is optionally substituted phenyl, that are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

Abstract: The present invention relates to compounds according to the general formula (I) wherein X is selected from the group consisting of wherein n and p are independently 0, 1, 2, or 3, provided that n+p is a least 1; and unsubstituted and at least monosubstituted C1-C10-alkylene-Y, C2-C10-alkylene-Y, C3-C10-cycloalkylene-Y and C3-C10-cycloalkenylene-Y; and R1, A, B, Q, T, Y, E and W have the meanings given in the description. These compounds are useful for the manufacture of a medicament for the treatment of insulin resistance, type 2 diabetes, metabolic syndrome, lipid disorders or cardiovasular disease or for providing an anti-lipolytic effect.

Abstract: Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.

Abstract: The present invention provides compositions for oral administration of compounds having A2A adenosine receptor agonist activity. These compositions are useful for treatment of inflammatory conditions.

Abstract: A method of identifying a 5?AMP-activated protein kinase inhibitor for treating a neurodegenerative disease. Disclosed are a method and a packaged product for treating a neurodegenerative disease. Also disclosed is a method for treating a 5?AMP-activated protein kinase-related disease and a related packaged product.

Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.

Abstract: The present invention discloses a method for the prevention of atherosclerosis, its genesis, progression and restenosis in human patients undergoing treatments for arterial lesions such as PTA or atherectomy, and which may be accompanied by stent implantation. Further, the treatment method disclosed has applicability in all stages of atherosclerosis in which monocytes play a role. The compound utilized in the present method as the active agent is a 2-halo-2?-deoxyadenosine such as 2-chloro-deoxyadenosine (2-CdA). The treatment method of the present invention includes the administration of 14 doses of 2-CdA in the amount of 0.12 mg/kg. One dose is given intravenously before the coronary intervention, another is given intravenously after the intervention and the remaining twelve doses are given subcutaneously at weekly intervals over a subsequent three month period.