| Entries |
| Document | Title | Date |
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| 20080200421 | COATING FOR A MEDICAL DEVICE HAVING AN ANTI-THROMBOTIC CONJUGATE - 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. In addition, the outmost layer prevents the formation of thrombosis, and also serves to modulate the release kinetics of the agent(s) contained within an inner layer(s) of the coating. | 08-21-2008 |
| 20080200422 | Methods for reduction of adipose tissue mass - 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. | 08-21-2008 |
| 20080221060 | Therapeutic Compounds - Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X=OH, R | 09-11-2008 |
| 20080274997 | Stable Granulates Containing S-adenosylmethionine and Process for Preparation Thereof - A fluid bed granulation process for manufacturing non-hygroscopic, stable granulates containing a water-soluble salt of S-adenosylmethionine is described. Said process comprises: | 11-06-2008 |
| 20080287390 | Pyrazolidinol compounds - The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient. | 11-20-2008 |
| 20080300213 | Use of A3 Adenosine Receptor Agonist in Osteoarthritis Treatment - The present invention provides the use of an A | 12-04-2008 |
| 20080300214 | Compounds for the Treatment of Marihuana Dependence, Withdrawal, and Usage - The invention provides methods for treating or suppressing marihuana usage, withdrawal, or dependence involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, uridine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal. | 12-04-2008 |
| 20080312180 | Methods to Protect Skeletal Muscle Against Injury - Disclosed herein are compositions and methods for the treatment of skeletal muscle and/or the protection of skeletal muscle against injury. The adenosine A | 12-18-2008 |
| 20090012035 | DENDRIMER CONJUGATES OF AGONISTS AND ANTAGONISTS OF THE GPCR SUPERFAMILY - Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A | 01-08-2009 |
| 20090012036 | Stable S-adenosyl-L-methionine - Stable compositions of defined non-racemic diastereomeric ratios of S-adenosyl-L-methionine, methods for their synthesis and methods for their uses are described. The compositions according to the invention are very stable and are valuable for use as active constituents in pharmaceutical compositions. | 01-08-2009 |
| 20090018101 | S-ADENOSYL-L-METHIONINE ANALOGS WITH EXTENDED ACTIVATED GROUPS FOR TRANSFER BY METHYLTRANSFERASES - S-Adenosyl- | 01-15-2009 |
| 20090042831 | USE OF 5'-METHYLTHIOADENOSINE (MTA) IN THE PREVENTION AND/OR TREATMENT OF AUTOIMMUNE DISEASES AND/OR TRANSPLANT REJECTION - 5′-methylthioadenosine (MTA), its pharmaceutically acceptable salts and/or prodrugs may be used in the prevention and/or treatment of autoimmune diseases, such as, for example, Multiple Sclerosis (MS), as well as in the prevention and/or treatment of transplant rejection. | 02-12-2009 |
| 20090048203 | SUBSTITUTED ADENINES AND THE USES THEREOF - This invention relates to compounds of Formula (I): and their use in the treatment of bacterial infections. | 02-19-2009 |
| 20090069267 | CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS - The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. | 03-12-2009 |
| 20090082304 | Methods of Treating Hematological Malignancies with Nucleoside Analog Drugs - The present invention provides methods of treating hematological malignancies, including multi-drug resistant malignancies, with 8-amino-adenosine and variants thereof. Also encompassed by the present invention is a method of predicting the response of a patient diagnosed with a hematological malignancy to treatment with a nucleoside analog and a method of screening candidate drugs for efficacy in treating hematological malignancies. | 03-26-2009 |
| 20090088403 | A3 ADENOSINE RECEPTORS AS TARGETS FOR THE MODULATION OF CENTRAL SEROTONERGIC SIGNALING - The present invention relates to the use of adenosine type 3 receptor (A3R) modulators to modulate serotonin transporter (SERT) function in vivo. In particular, antagonists of A3R can be used to inhibit A3R-dependent upregulation of SERT, for example, as antidepressants. | 04-02-2009 |
| 20090088404 | Extended Release Pharmaceutical Formulations of S-Adenosylmethionine - 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. | 04-02-2009 |
| 20090118221 | METHOD OF TREATING ARRHYTHMIAS - Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A | 05-07-2009 |
| 20090156544 | A1 ADENOSINE RECEPTOR AGONISTS - Disclosed are novel compounds that are partial and full A | 06-18-2009 |
| 20090170805 | ANTI-MICROBIAL AGENTS AND USES THEREOF - Many pathogens, including | 07-02-2009 |
| 20090197824 | Extended Release Pharmaceutical Formulations of S-Adenosylmethionine - 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. | 08-06-2009 |
| 20090197825 | NOVEL COMPOUNDS AND COMPOSITIONS AND METHODS OF USE - Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of 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. | 08-06-2009 |
| 20090203637 | NOVEL CYTOSTATIC 7-DEAZAPURINE NUCLEOSIDES - The invention provides compounds of formula I: | 08-13-2009 |
| 20090209480 | CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS - The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. | 08-20-2009 |
| 20090221521 | SYSTEMIC PURINE ADMINISTRATION: MODULATING AXONAL OUTGROWTH OF CENTRAL NERVOUS SYSTEM NEURONS - Methods for modulating the axonal outgrowth of central nervous system neurons are provided by means of internalized purine administration such as by intravenous, intraarterial, subcutaneous, intramuscular, intraperitoneal, and intrapleural administration. The methods are noted for stimulating the axonal outgrowth of central nervous system neurons following an injury (e.g., stroke, traumatic brain injury, cerebral aneurism, spinal cord injury and the like). | 09-03-2009 |
| 20090253647 | 2-PROPYNYL ADENOSINE ANALOGS WITH MODIFIED 5'-RIBOSE GROUPS HAVING A2A AGONIST ACTIVITY - The invention provides compounds having the following general formula (I): | 10-08-2009 |
| 20090258836 | EFFECTIVE DELIVERY OF CROSS-SPECIES A3 ADENOSINE-RECEPTOR ANTAGONISTS TO REDUCE INTRAOCULAR PRESSURE - Provided are methods for reducing intraocular pressure in an individual having an ocular disorder causing elevated intraocular pressure, such as glaucoma. The method comprises administering to the individual an effective intraocular pressure-reducing amount of a pharmaceutical composition comprising an A | 10-15-2009 |
| 20090264383 | Inhibitor of Adenylyl Cyclase for Treating a Disorder of the Circadian Rhythm - The invention relates to use of a composition comprising an inhibitor of adenylyl cyclase in the elongation of circadian rhythm, a method of extending the period of circadian rhythm in a subject, said method comprising administering to said subject an inhibitor of adenylyl cyclase, and to adenylyl cyclase inhibitor for use in the treatment of a disorder of the circadian rhythm. Preferably the inhibitor is a P-site inhibitor, preferably 9-(tetrahydrofuryl)-adenine. The composition may further comprise a JNK inhibitor. | 10-22-2009 |
| 20090275529 | METHOD FOR IMPROVING CARDIOVASCULAR RISK PROFILE OF COX INHIBITORS - A method of reducing the increased risk of cardiovascular events attendant with the use of COX or selective COX-2 inhibitors including restoring disrupted cholesterol metabolic function engendered by the use of the COX or selective COX-2 inhibitors and reducing the production of foam cells caused thereby. The disrupted cholesterol metabolic function is restored and the production of foam cells is reduced by the step of administering an adenosine A2A receptor agonist having a threshold level of activity of 0.1 μM to a patient using the COX or COX-2 inhibitor. The adenosine A2A receptor agonist is administered orally in amounts sufficient to saturate the A2A receptor and at time intervals sufficient to maintain the restored cholesterol metabolic function. | 11-05-2009 |
| 20090291909 | AMINOSUGAR, GLYCOSAMINOGLYCAN, AND S-ADENOSYLMETHIONINE COMPOSITION FOR THE TREATMENT AND REPAIR OF CONNECTIVE TISSUE - A composition for the protection, treatment and repair and for reducing the inflammation of connective tissue in mammals and a method for the treatment of connective tissue in mammals by the administration of the composition. The composition includes S-Adenosylmethionine (SAM), and a component selected from an aminosugar or salts thereof (e.g., glucosamine) or glycosaminoglycans (e.g., chondroitin salts) or mixtures or fragments thereof. The composition optionally includes manganese which promotes the production of connective tissue matrix. The composition also optionally includes methyl donors or methyl donor cofactors, such as vitamin B12, vitamin B6, folic acid, dimethylglycine or trimethylglycine. | 11-26-2009 |
| 20090298788 | 2-POLYCYCLIC PROPYNYL ADENOSINE ANALOGS HAVING A2A AGONIST ACTIVITY - The invention provides compounds having the following general formula (I): | 12-03-2009 |
| 20090298789 | ORGAN ARREST, PROTECTION AND PRESERVATION - The present invention relates to a method for arresting, protecting and/or preserving an organ which includes administering effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) local anaesthetic to a subject in need thereof. | 12-03-2009 |
| 20090325896 | PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS - Disclosed are novel compounds that are partial and full A | 12-31-2009 |
| 20100004191 | Compositions of S-adenosyl-L-methionine. - Compositions of S-adenosyl-L-methionine with indole-3-propionic acid and methods to treat conditions associated with DNA hypomethylation are disclosed. | 01-07-2010 |
| 20100048500 | Anti-viral nucleoside analogs and methods for treating viral infections, especially HIV infections - The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: | 02-25-2010 |
| 20100056465 | COMPOUNDS, COMPOSITIONS AND METHODS OF USING SAME FOR MODULATING URIC ACID LEVELS - 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. | 03-04-2010 |
| 20100062993 | Adenosine Nucleotides as Dietary Supplements and as Agents in the Prevention of Cancer and the Metastasis Thereof - It is the embodiment of this invention that Methylthioadenosine and its pharmaceutically acceptable salts as dietary supplements are more efficient, more economical and better tolerated than conventional existing dietary supplements such as S-Adenosylmethionine in the promotion of normal cell growth. It is a further embodiment of this invention that Methylthioadenosine and its pharmaceutically acceptable salts as dietary supplements are more efficient, more economical and better tolerated than conventional existing dietary supplements such as S-Adenosylmethionine in the destruction of aberrant cells that can cause various cancer. It is a further embodiment of this invention that Methylthioadenosine and its pharmaceutically acceptable salts as dietary supplements are more efficient, more economical and better tolerated than conventional existing dietary supplements such as S-Adenosylmethionine in the prevention of cancer cell metastasis | 03-11-2010 |
| 20100062994 | Adenosine Receptor Antagonists - The present application discloses locked nucleoside compounds of the Formula I which act as antagonists of adenosine receptors, in particular the adenosine A3 receptor, and the use of such adenosine A3 receptor compounds in medicine, e.g. for the treatment or alleviation or prophylaxis of selected from the group consisting of pain; inflammatory diseases, arthritis, multiple sclerosis, inflammation, asthma and psoriasis; gastro-intestinal disorders; allergy; disorders associated with mast cell or eosinophil activation and degranulation; cardio-vascular disorders; cutaneous diseases; wound healing; opthalmological disorders; respiratory disorders; kidney diseases; central nervous system disorders; Alzheimer's disease, Creutzfeldt-Jacob disease, Huntington's disease and Parkinson's disease; trauma and seizure; diabetes; osteoporosis; diseases of the immune system; cancers, infections; high blood pressure, locomotor hyperactivity, hypertension and depression; acute hypoxia; neonatal hypoxia, hypoxia and chronic hypoxia; and infertility. | 03-11-2010 |
| 20100099642 | TGF-BETA STIMULANT AND FURTHER AGENT TO REDUCE SIDE EFFECTS - The invention relates to the use of TGF-beta stimulating agents, and in particular members of the triphenylethylene class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of cardiovascular disease, autoimmune diseases or neurodegeneration. In particular, improved compositions consisting of triphenylethylene agents combined with one or more additional active pharmaceutical agents in order to mitigate against side-effects of the triphenylethylene are described and claimed. | 04-22-2010 |
| 20100113379 | cAMP DEPENDENT INDUCTION OF AUTOPHAGY - The present invention relates to the induction of autophagy via mTOR independent pathways which modulated intracytosolic cAMP levels. In some embodiments, autophagy may be induced in a cell by reducing intracytosolic cAMP levels, for example using a cAMP antagonist, such as clonidine. This may be useful, for example in the treatment of neurodegenerative disorders or pathogen infections. | 05-06-2010 |
| 20100152127 | 2-PROPYNYL ADENOSINE ANALOGS HAVING A2A AGONIST ACTIVITY AND COMPOSITIONS THEREOF - The invention provides compounds having the following general formula (I): | 06-17-2010 |
| 20100160250 | METHOD FOR TREATING INFLAMMATORY CONDITIONS - This invention provides a method for inhibiting the release of interleukin-1β in a mammal. This invention also provides a method for preventing or treating pulmonary diseases, ophthalmic diseases, and autoimmune diseases that are associated with inflammation or inflammatory conditions. The invention also provides a method for preventing or treating neurodegenerative diseases, or pain in a mammal. The method comprises administering to a mammal in need thereof a therapeutically effective amount of a mononucleoside compound, which is an antagonist of P2X | 06-24-2010 |
| 20100168048 | Method of Stabilizing S-Adenosyl-L-Methionine and Stabilized Composition - Provided are a process for producing a S-adenosyl-L-methionine-containing composition which is very excellent in a stability by adding at least ascorbic acids or salts thereof to a composition liquid containing S-adenosyl-L-methionine and then drying the above composition liquid or separating and drying a crystallized deposit obtained from the above composition liquid, a S-adenosyl-L-methionine-containing composition obtained by the above production process and a molding obtained from the above composition. | 07-01-2010 |
| 20100168049 | COMBINATION OF MONOSACCHARIDES AND ADENOSINE AND USE THEREOF - The present invention relates to a composition, especially a cosmetic and/or dermatological composition, containing, in a physiologically acceptable medium, a combination of at least one monosaccharide chosen from mannose, rhamnose and a mixture thereof, and of at least one additional compound chosen from adenosine, an analogue thereof and a mixture thereof. | 07-01-2010 |
| 20100184715 | STABLE SALTS OF S-ADENOSYLMETHIONINE AND PROCESS FOR THE PREPARATION THEREOF - The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe. | 07-22-2010 |
| 20100190737 | COMPOSITIONS COMPRISING INOSINE AND OROTIC ACID AND METHODS OF USE THEREOF FOR THE TREATMENT OF CERTAIN HEART CONDITIONS AND ENHANCEMENT OF WORK CAPACITY - The invention comprises a composition of inosine and orotic acid or a salt thereof, and its methods of use in treating, maintaining and enhancing the health of the heart, and specifically the integrity of the myocardium. The effective combination of inosine and orotic acid/orotate effectively improves various medical parameters that are widely used to assess cardiac function and structure. These include EKG and VCG recordings, quantitative assessments of work capacity and athletic performance, clinically relevant observations, and direct biochemical, histological and ultrastructural analyses. The observations and controlled studies in mice, rats, rabbits, cardiology patients and high performance human athletes (cyclists) consistently support the effectiveness of the combination of inosine and orotic acid/orotate in both preventing and reversing damage to the myocardium resulting from physical stress. | 07-29-2010 |
| 20100210579 | PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS - Disclosed are novel compounds a compound of Formula I | 08-19-2010 |
| 20100222292 | METHOD FOR TRANSDIFFERENTIATION OF BODY TISSUES - The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune diseases. | 09-02-2010 |
| 20100249053 | METHOD FOR INDUCING HEPATOCYTE PROLIFERATION AND USES THEREOF - The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A | 09-30-2010 |
| 20100261668 | INHIBITORS OF S-ADENOSYL-L-METHIONINE DECARBOXYLASE - Novel mechanism-based inhibitors of S-adenosyl-L-methionine decarboxylase are provided. These compounds of formula (1) inhibit the life cycle of trypanosomes, and are useful to treat subjects infected with African trypanosomes. The invention includes pharmaceutical compositions and methods of using the compounds of formula (1). | 10-14-2010 |
| 20100279970 | METHOD OF REDUCING INTRAOCULAR PRESSURE IN HUMANS - Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for reducing intraocular pressure comprising administering an effective amount of compounds of Formula I to a subject in need thereof. | 11-04-2010 |
| 20100279971 | ANTIFOLATE COMPOUNDS FOR THE TREATMENT OF MELANOMA - This invention relates to compounds of the formula X) or XI) (X) (XI) wherein: each —R | 11-04-2010 |
| 20100286082 | RIBOSWITCHES AND METHODS AND COMPOSITIONS FOR USE OF AND WITH RIBOSWITCHES - Riboswitches are targets for antibiotics and other small molecule therapies. Riboswitches and portions thereof can be used to regulate the expression or function of RNA molecules and other elements and molecules. Riboswitches and portions thereof can be used in a variety of other methods to, for example, identify or detect compounds. Compounds can be used to stimulate, active, inhibit and/or inactivate the riboswitch. Riboswitches and portions thereof, both alone and in combination with other nucleic acids, can be used in a variety of constructs and RNA molecules and can be encoded by nucleic acids. | 11-11-2010 |
| 20100298254 | ORGAN ARREST, PROTECTION AND PRESERVATION - The present invention relates to a method for arresting, protecting and/or preserving an organ which includes administering effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) local anaesthetic to a subject in need thereof. | 11-25-2010 |
| 20100317610 | Methods and Compositions for Inducing Deregulation of EPHA7 and ERK Phosphorylation in Human Acute Leukemias - Methods for assessing a pathological condition in a subject include measuring one or more markers where a difference is indicative of acute lymphoblastic leukemia (ALL) or a predisposition to ALL, uses and compositions are disclosed. | 12-16-2010 |
| 20100317611 | METHODS, COMPOSITIONS, UNIT DOSAGE FORMS, AND KITS FOR PHARMACOLOGIC STRESS TESTING WITH REDUCED SIDE EFFECTS - Methods are presented that comprise the administration of a pharmaceutical composition comprising adenosine and dipyridamole, as well methods comprising the combined administration of dipyridamole administered as a bolus with adenosine given as an infusion, both at dosages below their respective single agent dosages, for detecting the presence and/or assessing the severity of myocardial ischemia during pharmacologic stress tests. The methods are useful for exploiting the vasodilating abilities of adenosine at doses at which side effects related to adenosine are substantially reduced while optimal coronary artery perfusion is achieved. Also presented are compositions, unit dosage forms, and kits that are useful in performing the methods. | 12-16-2010 |
| 20110003765 | SUBSTITUTED 4--PIPERIDINE-1-CARBOXYLIC ACID ESTERS AS A2AR AGONISTS - The present invention provides substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions containing the same that are selective agonists of A | 01-06-2011 |
| 20110003766 | ALKOXY-CARBONYL-AMINO-ALKYNYL-ADENOSINE COMPOUNDS AND DERIVATIVES THEREOF AS A2AR AGONISTS - Provided herein are alkoxy-carbonyl-amino-alkynyl-adenosine compounds and derivatives thereof and pharmaceutical compositions containing the same that are selective agonists of A | 01-06-2011 |
| 20110009354 | 5',-SUBSTITUTED ADENOSYNES PREPARATION THEREOF AND USE AS INHIBITORS OF S-ADENOSYLMETHIONINE DECARBOXYLASE - The crystal structure of the complex of S-adenosylmethionine methyl ester with hΛdoMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5′-deoxy-5′-[N-methyl-N-[2-(aminooxy)ethyl]amino-8-methyl]adenosine (MAOEMA) and 5′-deoxy-5′-[N-methyl-N-[4-(aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally. | 01-13-2011 |
| 20110009355 | Azapeptide Derivatives - This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir. | 01-13-2011 |
| 20110015145 | CLADRIBINE FORMULATIONS FOR IMPROVED ORAL AND TRANSMUCOSAL DELIVERY - Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral and buccal administration of cladribine. | 01-20-2011 |
| 20110021453 | Methods and compositions for providing cardiac protection - The invention provides a method of treating a cardiac disease by administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to a patient. The compound capable of inhibiting AC5 may be administered singly or in combination with another agent, such as, for instance a β-blocker. In some embodiments, the AC5 inhibiting compound is 9-β-D-arabinofuranosyladenine (AraAde). The compound may be administered in an amount of about 1 to about 200 mg/kg/day, about 1 to about 100 mg/kg/day, about 10 to about 80 mg/kg/day, about 12 to about 40 mg/kg/day or about 15 to about 25 mg/kg/day. In some embodiments, the compound is administered parenterally. The cardiac disease may be, for instance, myocardial infarction (MI) or heart failure (HF). The compound capable of inhibiting AC5 may be administered alone or in conjunction with one or more other active agents. Likewise, the invention provides a method of treating a heart attack, a method of inhibiting myocardial apoptosis, and a method of treating heart failure by administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to a patient in the same manner. | 01-27-2011 |
| 20110028420 | Regression of Established Atherosclerotic Plaques, and Treating Sudden-Onset Asthma Attacks, using PARP Inhibitors - A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms. | 02-03-2011 |
| 20110039798 | SUBSTITUTED NUCLEOSIDE DERIVATIVES WITH ANTIVIRAL AND ANTIMICROBIAL PROPERTIES - The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS. | 02-17-2011 |
| 20110039799 | A1 ADENOSINE RECEPTOR AGONIST POLYMORPHS - Provided are polymorphs of an A | 02-17-2011 |
| 20110059915 | PURINE DERIVATIVES AND METHODS OF USE THEREOF - The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for treating or preventing an ischemic condition, reperfusion injury, a cellular proliferative disorder, a cardiovascular disease, a neurological disorder, a skin disorder, a radiation-induced injury, a wound, or an inflammatory disease comprising administering an effective amount of a Purine Derivative to a subject in need thereof. | 03-10-2011 |
| 20110065663 | ANTI-CANCER COMBINATION THERAPY - The present invention relates to a combination of therapeutic agents comprising: (a) a cytosine-based anti-cancer drug and/or a purine-based anticancer drug and (b) a therapeutic agent selected from the group consisting of thymidine phosphorylase inhibitors, and antibiotics against Mollicutes bacteria. The present invention also relates to the simultaneous, separate or sequential use of said combination for the treatment of cancer in mammals, especially in humans. The present invention also relates to methods of treatment of cancer, preferably in mammals infected with Mollicutes bacteria. | 03-17-2011 |
| 20110077215 | DNA Methylation As A Target For Diagnosis And Treatment Of Chronic Lymphocytic Leukema (CLL) - Global DNA methylation is a predictor of aggressive disease in patients with chronic lymphocytic leukemia. The higher the DNA methylation, the more likely a patient is going to require systemic therapy. Although there is a gradual decline in global DNA methylation with increasing age in normal individuals, the methylation index only decreases by approximately 0.03 per decade. A pilot study was performed in which patients with chronic lymphocytic leukemia were treated with low doses of DNA methylation inhibitors to evaluate if inhibition of DNA methylation can translate into a clinical benefit. Inhibition of DNA methylation was observed to lead to re-expression of tumor suppressors and normal cellular function. At low non-toxic doses of 0.05-0.09 mg per kilogram per day for three days every 28 days, some patients with chronic lymphocytic leukemia were observed to achieve a reduction in circulating leukemia cells. This was observed to correlate with a reduction in global DNA methylation and an alteration in methylation of core histones. | 03-31-2011 |
| 20110086812 | Transition state sturcture of 5'-methylthioadenosine/s-adenosylhomocysteine nucleosidases - Provided are methods of designing a putative inhibitor of a 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidase. The methods comprise designing a chemically stable compound that resembles the charge and geometry of the 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidase transition state. Also provided are methods of inhibiting 5′-methylthioadenosine/S-adenosylhomocysteine nucleosidases using the inhibitors found by the above methods. | 04-14-2011 |
| 20110092451 | NUCLEOTIDE ANALOGUES WITH QUATERNARY CARBON STEREOGENIC CENTERS AND METHODS OF USE - The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3′ position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases. | 04-21-2011 |
| 20110105425 | USE OF ADENOSINE ASPARTATE FOR THE PREPARATION OF PHARMACEUTICAL PRODUCTS FOR THE TREATMENT OF LIVER CANCER - The present invention relates to the novel use of an adenosine aspartate product for the formulation of a drug intended to prevent the development of preneoplastic lesions and to reverse some types of cancer, particularly liver cancer, providing chemoprotection, preventing myelotoxic effects. | 05-05-2011 |
| 20110130358 | METHOD FOR TRANSDIFFERENTIATION OF BODY TISSUES - The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune diseases. | 06-02-2011 |
| 20110136755 | 2-PROPYNYL ADENOSINE ANALOGS WITH MODIFIED 5'-RIBOSE GROUPS HAVING A2A AGONIST ACTIVITY - The invention provides compounds having the following general formula (I): | 06-09-2011 |
| 20110152214 | SILK POLYMER-BASED ADENOSINE RELEASE: THERAPEUTIC POTENTIAL FOR EPILEPSY - This invention relates to sustained release formulations comprising silk fibroin biopolymer and adenosine, that provide for sustained, focal release of adenosine at therapeutic levels for the treatment of epilepsy and/or the prevention of epileptogenesis. An embodiment provides for a silk-based, adeno sine-releasing implant that alleviates seizures or prevents epileptogenesis. Another embodiment provides for a method of treating epilepsy or preventing epileptogenesis comprising focally administering adenosine in a sustained-release, silk-based adenosine delivery system. | 06-23-2011 |
| 20110152215 | RIBOSWITCHES, METHODS FOR THEIR USE, AND COMPOSITIONS FOR USE WITH RIBOSWITCHES - 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. In addition, the architecture of riboswitches allows actual pieces of the natural switches to be used to construct new non-immunogenic genetic control elements, for example the aptamer (molecular recognition) domain can be swapped with other non-natural aptamers (or otherwise modified) such that the new recognition domain causes genetic modulation with user-defined effector compounds. The changed switches become part of a therapy regimen—turning on, or off, or regulating protein synthesis. Newly constructed genetic regulation networks can be applied in such areas as living biosensors, metabolic engineering of organisms, and in advanced forms of gene therapy treatments. | 06-23-2011 |
| 20110166093 | USE OF ADENOSINE RECEPTOR AGONISTS IN THERAPY - Use of compounds of formula: (I) wherein R is C | 07-07-2011 |
| 20110166094 | AGONISTS OF A2A ADENOSINE RECEPTORS FOR TREATING RECURRENT TUMOR GROWTH - The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A | 07-07-2011 |
| 20110172177 | COMBINATION, KIT AND METHOD OF REDUCING INTRAOCULAR PRESSURE - The present invention is directed to a combination or a kit comprising a prostaglandin analog and an adenosine receptor A | 07-14-2011 |
| 20110207689 | THE TREATMENT OF HEARING LOSS - The invention provides a method of treating noise-induced hearing loss, the method including the step of administering an A | 08-25-2011 |
| 20110230434 | USE OF S-ADENOSYLMETHIONINE, VITAMIN E, AND VITAMIN C FOR THE TREATMENT OF OXIDATIVE LIVER INJURY OR INSULIN RESISTANCE - The present invention provides antioxidant compositions comprising S-adenosylmethionine (SAMe), vitamin E and vitamin C and uses thereof for the treatment of liver injury and insulin resistance. | 09-22-2011 |
| 20110230435 | Methods and Compositions for Treating Obesity and Related Disorders - The invention provides methods for, and compositions effective for, treating obesity, inhibiting weight gain, treating diabetes mellitus, inhibiting atherosclerosis and treating related disorders and conditions comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to a patient. The compound capable of inhibiting AC5 may be administered singly or in combination with another agent. In some embodiments, the AC5 inhibiting compound is 9-β-D-arabinofuranosyladenine (AraAde). The compounds may be administered in an amount of about 1 to about 200 mg/kg/day, about 1 to about 100 mg/kg/day, about 10 to about 80 mg/kg/day, about 12 to about 40 mg/kg/day or about 15 to about 25 mg/kg/day. In some embodiments, the compound is administered orally. | 09-22-2011 |
| 20110237537 | METHODS FOR ASSESSMENT AND TREATMENT OF MOOD DISORDERS VIA SINGLE NUCLEOTIDE POLYMORPHISMS ANALYSIS - Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method. | 09-29-2011 |
| 20110245193 | COMBINATION COMPOSITIONS FOR REDUCING INTRAOCULAR PRESSURE - Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog and an adenosine A | 10-06-2011 |
| 20110245194 | ADENOSINE COMPOUNDS AND THEIR USE THEREOF - The present invention is directed to a benzyloxy cyclopentyladenosine (BCPA) compounds and to their use as selective A | 10-06-2011 |
| 20110245195 | METHOD OF REDUCING INTRAOCULAR PRESSURE IN HUMANS - Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT). | 10-06-2011 |
| 20110251151 | COMBINATION COMPOSITIONS FOR REDUCING INTRAOCULAR PRESSURE - Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine A | 10-13-2011 |
| 20110257120 | BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B - 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-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: | 10-20-2011 |
| 20110269707 | Modified nucleosides for the treatment of viral infections and abnormal cellullar proliferation - The disclosed invention is a composition for and a method of treating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug. | 11-03-2011 |
| 20110312908 | SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE - The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers. | 12-22-2011 |
| 20120004191 | Combinational Compositions And Methods For Treatment Of Cancer - The present invention provides methods of treating a cell proliferative disorder, such as a 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 in combination with a therapeutically effective amount of a second anti-proliferative agent. | 01-05-2012 |
| 20120040923 | STABLE S-ADENOSYL-L-METHIONINE - Stable compositions of defined non-racemic diastereomeric ratios of S-adenosyl-L-methionine, methods for their synthesis and methods for their uses are described. The compositions according to the invention are very stable and are valuable for use as active constituents in pharmaceutical compositions. | 02-16-2012 |
| 20120065155 | A3 ADENOSIDE RECEPTOR AGONISTS FOR THE REDUCTION OF INTRAOCULAR PRESSURE - The present disclosure provides the use of an A3R agonist, such as IB-MECA, for reducing in a subject, preferably, human subject, intra ocular pressure (IOP). Similarly, the invention provides a pharmaceutical composition and a method for reducing IOP in a subject making use of the A | 03-15-2012 |
| 20120071432 | CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS - The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-ac-Live agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. | 03-22-2012 |
| 20120071433 | Substituted 6-(Benzylamino) Purine Riboside Derivatives, Use Thereof and Compositions Containing These Derivatives - The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also to the compositions, which contain these derivatives as active ingredients. | 03-22-2012 |
| 20120077770 | Methods of Diagnosing and Treating Multiple Sclerosis - Methods of using a 15-oxysterol, e.g., 15-ketocholestene (15-KE), 15-ketocholestane (15-KA), and/or 15-hydroxy-cholestene (15-HC), as a biomarker to monitor disease progression in multiple sclerosis (MS), and methods of treating secondary progressive MS (SPMS) using inhibitors of poly(ADP ribose) polymerase-1 (PARP-1). | 03-29-2012 |
| 20120077771 | COMPOSITIONS FOR USE IN CARDIOPLEGIA COMPRISING ESMOLOL AND ADENOSINE - The invention related to a composition for use in cardioplegia, said composition comprising (i) esmolol; and (ii) adenosine, wherein in use the concentration of said esmolol is in the range 0.3-1.5 mM, and wherein in use the concentration of said adenosine is in the range 0.1-1.5 mM. The invention also relates to methods of making and using such compositions. | 03-29-2012 |
| 20120083464 | NEUROPROTECTIVE PROPERTIES OF 5'-METHYLTHIOADENOSINE - The present invention relates to the use of MTA, its pharmaceutically acceptable salts and/or prodrugs thereof as active ingredient in the manufacture of a medicament for the prevention or treatment of nerve cell death or damage, a neuroprotective medicament, a medicament for the regeneration of nerve cells, and a medicament for the prevention or treatment of a neurological or psychiatric disease. The present invention also relates to a method of prevention or treatment of nerve cell death or damage, a method of neuroprotection, a method of regenerating nerve cells and a method of prevention or treatment of a neurological or psychiatric disease. | 04-05-2012 |
| 20120094947 | METHOD FOR THE SELECTIVE THERAPY OF DISEASE - Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents. In addition, screening methods for identifying competitive antagonists, protective agents and potentiating agents, for use according to the methods of the invention, are provided. | 04-19-2012 |
| 20120142625 | Substituted Purine And 7-Deazapurine Compounds - The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-07-2012 |
| 20120149657 | 2'-FLUORO ARABINO NUCLEOSIDES AND USE THEREOF - A method of treating cancer using certain 2′-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: (I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions containing these compounds. | 06-14-2012 |
| 20120165285 | COMBINED PREPARATION FOR USE AS A MEDICAMENT - A combined preparation comprising an A | 06-28-2012 |
| 20120172324 | COMPOSITIONS AND METHODS FOR REDUCING THE RISK OF AGENT-INDUCED LIVER TOXICITY - The present disclosure relates generally to a co-formulation or co-administration of acetaminophen with one or more chemicals that are metabolites or their derivatives in the methionine and glutathione biosynthesis pathways, for protection against acetaminophen-induced liver toxicity. The formulation may comprise acetaminophen and diet supplements such as S-methylmethionine (SMM). The present disclosure also encompasses methods of providing pain or fever relief with protection against acetaminophen-induced liver injury with the formulations described herein. Embodiments of the present disclosure also include co-formulation or co-administration of an agent and one or more other chemicals for reducing agent-induced liver toxicity via depletion of glutathione. | 07-05-2012 |
| 20120196825 | COMPOSITIONS AND METHODS FOR MODULATING THE IMMUNE SYSTEM - The present invention provides methods and compositions for the prophylaxis of blood cell disorders such as neutropenia, thrombocytopenia, lymphocytopenia, and anaemia. The invention provides methods wherein compositions comprising at least one cytokinin compound are administered either therapeutically or prophylactically. The invention further has utility in methods of DNA repair. | 08-02-2012 |
| 20120202764 | LOW MOLECULAR WEIGHT PHARMACOLOGICAL ACTIVITY MODULATORS - Claimed are a compound of the general formula (I) and pharmaceutically acceptable salts thereof, where M signifies metal atoms selected independently from the group comprising Pd, Fe, Mn, Co, Ni, Cu, Zn and Mo; R | 08-09-2012 |
| 20120220546 | COMPOSTIONS DESIGNED FOR THE INHIBITION AND/OR BLOCKING OF THE EPITHELIAL/MESENCHYMAL TRANSITION - 5′-methylthioadenosine (MTA) is described as a compound that is susceptible to inhibiting and/or blocking the epithelial-mesenchymal transition (EMT), a process whereby epithelial cells become mesenchymal cells. | 08-30-2012 |
| 20120232029 | 2',4'-SUBSTITUTED NUCLEOSIDES AS ANTIVIRAL AGENTS - 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. | 09-13-2012 |
| 20120238520 | Novel Medical Use - The present invention relates to a compound which is (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol | 09-20-2012 |
| 20120252750 | FORMULATIONS FOR REDUCING NEURONAL DEGENERATION - Nutriceutical and pharmaceutical formulations for treating neurodegenerative disorders such as Alzheimer's disease are provided. Nutriceutical formulations include two or more of folate, vitamin E, and acetyl-L-carnitine (ALCAR). Pharmaceutical formulations include two or more of 3-deaza-adenosine (DZA), N-acetyl-L-cysteine (NAC), and S-adenosylmethionine (SAM). | 10-04-2012 |
| 20120252751 | ANTI-VIRAL NUCLEOSIDE ANALOGS AND METHODS FOR TREATING VIRAL INFECTIONS, ESPECIALLY HIV INFECTIONS - The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: | 10-04-2012 |
| 20120258927 | INHIBITORS OF E1 ACTIVATING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 10-11-2012 |
| 20120264706 | PURINE DERIVATIVES AS ADENOSINE A1 RECEPTOR AGONISTS AND METHODS OF USE THEREOF - 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. | 10-18-2012 |
| 20120264707 | BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B - 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-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: | 10-18-2012 |
| 20120270829 | USE OF ADENOSINE A3 RECEPTOR AGONISTS FOR TREATMENT OF NEUROPATHIC PAIN - A method of treating neuropathic pain in a subject is provided. The method comprises administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of an A | 10-25-2012 |
| 20120295862 | NUCLEOBASE-FUNCTIONALIZED CONFORMATIONALLY RESTRICTED NUCLEOTIDES AND OLIGONUCLEOTIDES FOR TARGETING OF NUCLEIC ACIDS - Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these compounds, wherein the compounds can be formed by coupling of an intermediate with a linker. Certain embodiments disclose the use of these compounds for detecting single nucleotide polymorphisms, and for increasing the thermal affinity of nucleic acid complements as compared to unmodified nucleic acid complements. In addition, the disclosed compounds can decrease enzymatic degradation of nucleic acids. | 11-22-2012 |
| 20120295863 | Dual-Action Compounds Targeting Adenosine A2A Receptor and Adenosine Transporter for Prevention and Treatment of Neurodegenerative Diseases - The present invention provides therapeutic agents for preventing and treating neurodegenerative diseases. These agents synergistically target both the adenosine A | 11-22-2012 |
| 20120329747 | NOVEL HYDRAZONE DERIVATIVES HAVING POTENT ANTITUMOR ACTIVITY TOWARD MULTI-DRUG RESISTANT TUMOR CELLS - A patentable new class of hydrazone derivative compounds is described, as are methods for synthesizing such compounds. The hydrazones of the invention can be used, for example, as potent anti-cancer agents, including to inhibit the growth of cancer cells that exhibit multidrug resistance. | 12-27-2012 |
| 20130005676 | ENHANCING THE THERAPEUTIC EFFECT OF ACUPUNCTURE WITH ADENOSINE - The present invention relates to a method of improving the therapeutic effect of acupuncture in a subject. The method involves administering adenosine, an adenosine mimetric, an adenosine modulator, an adenosine transport inhibitor, enzymes involved in adenosine metabolism, and/or an adenosine receptor agonist to the subject under conditions effective to improve the therapeutic effect of the acupuncture. | 01-03-2013 |
| 20130018010 | POLYMERIC CONJUGATES OF ADENINE NUCLEOSIDE ANALOGS - The present invention relates to polymeric conjugates of adenine nucleoside analogs. In particular, the invention relates to multi-arm polyethylene glycol conjugates of adenine nucleoside analogs and use thereof. The present invention, more specifically, provides polymeric conjugates of toyocamycin and its derivatives. Furthermore, the present invention provides a method for preparing the polymeric conjugates of adenine nucleoside analogs and a method of using the same for treating a cancer, inhibiting the growth or proliferation of cancer cells, treating a viral infection, treating a disease or condition associated with abnormal expression of VEGF. Most polymeric conjugates of toyocamycin was stable in PBS but released toyocamycin in vivo to provided inhibition of cancer cell growth. | 01-17-2013 |
| 20130040906 | Inhibitors of Human EZH2, and Methods of Use Thereof - The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject. | 02-14-2013 |
| 20130040907 | Compounds, Compositions and Methods of Using Same for Modulating Uric Acid Levels - 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. | 02-14-2013 |
| 20130045942 | N6-SUBSTITUTED ADENOSINE DERIVATIVES AND N6-SUBSTITUTED ADENINE DERIVATIVES AND USES THEREOF - The present invention provides N | 02-21-2013 |
| 20130045943 | A3AR AGONISTS FOR THE TREATMENT OF UVEITIS - The present disclosure relates to the use of an A | 02-21-2013 |
| 20130090300 | INHIBITORS OF INFLUENZA ENDONUCLEASE ACTIVITY AND TOOLS FOR THEIR DISCOVERY - The invention provides inhibitors of influenza endonuclease activity and tools for their discovery. | 04-11-2013 |
| 20130109645 | ADENOSINE RECEPTOR AGONISTS FOR THE TREATMENT AND PREVENTION OF VASCULAR OR JOINT CAPSULE CALCIFICATION DISORDERS | 05-02-2013 |
| 20130109646 | METHOD FOR TREATING GLAUCOMA OR OCULAR HYPERTENSION WITH AN ADENOSINE DERIVATIVE | 05-02-2013 |
| 20130123208 | METHOD OF TREATING MULTIPLE SCLEROSIS WITH ADENOSINE RECEPTOR AGONISTS - The present invention includes a composition comprising an A | 05-16-2013 |
| 20130131005 | METHODS AND COMPOSITIONS FOR PROVIDING CARDIAC PROTECTION - The invention provides a method of reducing infarct size and/or limiting, decreasing and/or inhibiting reperfusion injury and/or ameliorating heart failure in a patient comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to the patient. The compound capable of inhibiting AC5 is particularly effective when administered during or after reperfusion in patients suffering from an ischemic injury. | 05-23-2013 |
| 20130131006 | METHOD FOR INHIBITING THE INDUCTION OF CELL DEATH BY INHIBITING THE SYNTHESIS OR SECRETION OF AGE-ALBUMIN IN CELLS OF THE MONONUCLEAR PHAGOCYTE SYSTEM - The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc. | 05-23-2013 |
| 20130143833 | TRANSPLANTS - The present invention relates to a method of reducing injury to cells, a tissue or organ to be explanted from a body and upon implantation into a body by administering a composition to the cell, tissue or organ, including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) an antiarrhythmic agent. The invention also provides a composition for reducing injury to vasculature ex vivo including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) an antiarrhythmic agent. | 06-06-2013 |
| 20130157971 | 2'-FLUORONUCLEOSIDES - 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: | 06-20-2013 |
| 20130172285 | LINKED PURINE PTERIN HPPK INHIBITORS USEFUL AS ANTIBACTERIAL AGENTS - The disclosure provides linked purine pterin compounds and analogues thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I | 07-04-2013 |
| 20130184231 | ORGAN ARREST, PROTECTION AND PRESERVATION - The present invention relates to a method for arresting, protecting and/or preserving an organ which includes administering effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) local anaesthetic to a subject in need thereof. | 07-18-2013 |
| 20130190264 | TRAUMA THERAPY - The invention provides a method of reducing injury to cells, tissues or organs of a body following trauma by administering a composition to the body following trauma, including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) a local anaesthetic. Also provided is a composition for reducing injury to cells, tissues or organs of a body following trauma including: (i) and (ii). The composition may be hypertonic. | 07-25-2013 |
| 20130217643 | METHOD OF REDUCING INTRAOCULAR PRESSURE IN HUMANS - Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for reducing intraocular pressure comprising administering an effective amount of compounds of Formula I to a subject in need thereof. | 08-22-2013 |
| 20130237491 | 4'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AS INHIBITORS OF HCV RNA REPLICATION - The present invention relates to the use of nucleoside derivatives of formula Ia | 09-12-2013 |
| 20130274220 | METHODS, ASSAYS AND COMPOUNDS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING METHYLTHIOINOSINE PHOSPHORYLASE - The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors. | 10-17-2013 |
| 20130281400 | Metabolic Downregulation for Cell Survival - The present provides a system and method of maintaining and/or increasing cell viability by downregulating cellular metabolic rate under hypoxic conditions. The present invention also relates to a system and method of prolonging the survival of implanted cells that are under hypoxic condition until host neovascularization is achieved. | 10-24-2013 |
| 20130324491 | BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B - 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-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: | 12-05-2013 |
| 20130331351 | NOVEL ANTIBACTERIAL COMPOUNDS - The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim | 12-12-2013 |
| 20130338094 | SUBSTITUTED PYRROLO]2,3-D]PYRIMIDINES - The present disclosure relates to compounds of formula (I-A) using the compounds | 12-19-2013 |
| 20130345162 | NOVEL ANTI-VIRAL THERAPEUTIC - Anti-viral therapeutics for use in viral targets having VPg unlinkase activity, including the broad class of picornaviruses, and therapeutic methods directed at suppression of such activity are provided. Such anti-viral therapies for use against human rhinovirus, for example, are particularly desirable as they would lessen both the severity and duration of upper respiratory distress in both normal and asthmatic individuals. Assays and purification protocols for detecting and purifying VPg unlinkase are also provided. | 12-26-2013 |
| 20130345163 | BIOLOGICAL MARKER FOR INFLAMMATION - Inflammatory state in a subject is assayed by determining the level of expression of A | 12-26-2013 |
| 20140005137 | TISSUE MAINTENANCE | 01-02-2014 |
| 20140005138 | Ribofuranosyl Purine Compounds, Methods for Preparing the Same and Use Thereof | 01-02-2014 |
| 20140011763 | 1,2,3-Triazolyl Purine Derivatives - The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections. An example of a 1,2,3-triazolyl purine derivative of the invention is | 01-09-2014 |
| 20140018314 | METHOD OF REDUCING INTRAOCULAR PRESSURE IN HUMANS - Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT). | 01-16-2014 |
| 20140024611 | ANTI-MICROBIAL AGENTS AND USES THEREOF - Many pathogens, including | 01-23-2014 |
| 20140045781 | PROCESSES FOR THE PREPARATION OF REGADENOSON AND A NEW CRYSTALLINE FORM THEREOF - This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described. | 02-13-2014 |
| 20140051654 | Substituted Purine and 7-Deazapurine Compounds - The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 02-20-2014 |
| 20140057863 | MODIFIED NUCLEOSIDES FOR THE TREATMENT OF VIRAL INFECTIONS AND ABNORMAL CELLULAR PROLIFERATION - The disclosed invention is a composition for and a method of treating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug. | 02-27-2014 |
| 20140057864 | COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING A RETROVIRUS INFECTION - The invention provides methods, compositions, and kits featuring a ribonucleoside chain terminator for use in preventing or inhibiting a retrovirus infection. | 02-27-2014 |
| 20140066394 | Substituted 6-(Benzylamino) Purine Riboside Derivatives, Use Thereof and Compositions Containing These Derivatives - A method of treatment using 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. | 03-06-2014 |
| 20140073596 | N-Pyrazole A2A Receptor Agonists - 2-adenosine N-pyrazole compounds having the following formula: | 03-13-2014 |
| 20140100183 | CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS - The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. | 04-10-2014 |
| 20140100184 | SELECTIVE INHIBITORS OF HISTONE METHYLTRANSFERASE DOT1L - Structure and mechanism based design was used to design potent ribose containing inhibitors of DOT1L with IC | 04-10-2014 |
| 20140100185 | UNIT DOSAGE OF APADENOSON - The present invention provides a unit dosage of Apadenoson, a pharmacological stress agent, and use of the same as a pharmacologic agent for myocardial perfusion imaging. | 04-10-2014 |
| 20140107059 | COMPOSITIONS CONTAINING ADENOSINE OR AN ADENOSINE ANALOGUE AND HYDROTROPES FOR COSMETIC USE - The present invention provides aqueous compositions comprising (a) at least one compound selected from the group consisting of adenosine and adenosine analogues, and (b) at least one hydrotrope in an amount effective to solubilize said at least one compound (a) in water, for cosmetic uses. | 04-17-2014 |
| 20140113880 | MODIFIED 2' AND 3'-NUCLEOSIDE PRODRUGS FOR TREATING FLAVIVIRIDAE INFECTIONS - 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. | 04-24-2014 |
| 20140128338 | COMPOUNDS, COMPOSITIONS AND METHODS OF USING SAME FOR MODULATING URIC ACID LEVELS - 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. | 05-08-2014 |
| 20140162970 | Treating Cardiac Arrhythmias, Heart Failure, Peripheral Artery Disease and Stroke With Cyclopentyl-Triazolo-Pyrimidine or Derivative Thereof - The present invention relates to new methods for treating and/or preventing cardiac arrhythmias, heart failure, stroke and/or peripheral artery disease by administering a composition comprising triazolopyrimidine, or derivative or metabolite thereof. In particular, the present invention relates to methods for treating cardiac arrhythmias, heart failure, stroke and/or peripheral artery disease by administering CycloPentyl-TriazoloPyrimidine. | 06-12-2014 |
| 20140171383 | CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS - The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. | 06-19-2014 |
| 20140187509 | USE OF S-ADENOSYLMETHIONINE, VITAMIN E, AND VITAMIN C FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DYSFUNCTION - The present invention provides a method of preventing or treating cardiovascular dysfunction by administering a therapeutically effective amount of (a) one or more of (i) S-adenosylmethionine or a derivative or pharmaceutically acceptable salt thereof and (ii) N-acetylcysteine or a derivative or pharmaceutically acceptable salt thereof; (b) vitamin E or a derivative or pharmaceutically acceptable salt thereof; and (c) vitamin C or a derivative or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. | 07-03-2014 |
| 20140206639 | USES OF DIHYDRO BASES - The present invention provides pharmaceutical compositions comprising a dihydro base described herein (e.g., compound DHdC). The dihydro base may show multiple tautomerism and may increase mutation of an RNA and/or DNA of a virus or cancer cell. The dihydro base may be used to reduce DNA methylation (e.g., in a cancer cell). The present invention also provides kits including the inventive pharmaceutical compositions and methods of treating a viral infection (e.g., influenza, HIV infection, or hepatitis C) or cancer using the pharmaceutical compositions or kits. | 07-24-2014 |
| 20140213541 | AGONISTS OF A2A ADENOSINE RECEPTORS FOR TREATING RECURRENT TUMOR GROWTH - The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A | 07-31-2014 |
| 20140213542 | COMPOSITION CONTAINING S-ADENOSYL-L-METHIONINE WITH EXCELLENT STORAGE STABILITY - The present invention relates to a composition including S-adenosyl-L-methionine; and at least one kind of additive selected from carboxymethylcellulose, hydroxypropylcellulose, soybean polysaccharide, casein sodium, and zein, in which S-adenosyl-L-methionine is extracted from S-adenosyl-L-methionine-containing cells obtained by culturing a microorganism having an ability to produce SAMe, and the content of the additive in the composition falls within the range of 0.05 to 15 times by mass of S-adenosyl-L-methionine in the composition. The present invention provides a composition containing a high concentration of S-adenosyl-L-methionine, which is useful as a water-soluble physiologically active substance, and being excellent in storage stability and bioabsorbability. The present invention also relates to a molded article formed by using the composition and a method of producing the composition. | 07-31-2014 |
| 20140235562 | COMPOUNDS AND METHODS OF TREATING OCULAR DISORDERS - A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS). | 08-21-2014 |
| 20140235563 | 2',4'-SUBSTITUTED NUCLEOSIDES AS ANTIVIRAL AGENTS - 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. | 08-21-2014 |
| 20140256668 | SUBSTITUTED PYRROLO]2,3-D]PYRIMIDINES - The present disclosure relates to compounds of formula (I-A) using the compounds | 09-11-2014 |
| 20140256669 | USE OF N6-(2-HYDROXYETHYL)-ADENOSINE IN PREPARATION OF CROP PESTICIDE - A method for controlling a pest on a crop includes applying a pesticide that comprises N6-(2-hydroxyethyl)-adenosine as an active ingredient for controlling the pest. The pesticide may include 20 wt % N6-(2-hydroxyethyl)-adenosine, 1-3 wt % dispersing agent, and 66.5% wt % water. The pesticide may further include a dispersion agent, a thickening agent, or an antifreeze agent as an auxiliary agent. The dispersing agent may be one or more selected from sodium lignin sulfonate, NNO, Agricultural Emulsifier 500#, Agricultural Emulsifier 700#, Agricultural Emulsifier 600#, Agricultural Emulsifier 1602#, methylene bis-methylnaphthalene sodium sulfonate, sodium salt of alkyl naphthalene sulfonate condensate, or polyoxyethylene castor oil. The thickening agent may be one or more selected from carboxymethyl cellulose, urea, poly vinyl alcohol, aluminum magnesium silicate, or xanthan gum. The antifreeze agent may be one or more selected from ethylene glycol, propylene glycol, glycerol, glycerin-diethylene glycol diethyl ether, methyl-his-propylene glycol, or urea. | 09-11-2014 |
| 20140303106 | METHYLTRANSFERASE INHIBITORS FOR TREATING CANCER - Compounds having methyltransferase inhibitory activity are disclosed. The compounds have the structure | 10-09-2014 |
| 20140309188 | USE OF PHARMACEUTICAL COMPOSITION COMPRISING DEOXYNUCLEOSIDE AND NUCLEOSIDE FOR TREATMENT OF TUMOR - A method for treatment of a tumor including administering to a patient in need thereof a pharmaceutical preparation including a combination of a deoxynucleoside and a nucleoside. The deoxynucleoside is selected from deoxyadenosine, deoxyguanosine, deoxycytidine, thymidine, or a mixture thereof. The nucleoside is selected from adenosine, guanosine, cytidine, uridine, deoxyadenosine, deoxyguanosine, deoxycytidine, thymidine, or a mixture thereof. | 10-16-2014 |
| 20140323424 | METHODS FOR ASSESSMENT AND TREATMENT OF MOOD DISORDERS VIA SINGLE NUCLEOTIDE POLYMORPHISMS ANALYSIS - Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method. | 10-30-2014 |
| 20140323425 | NUCLEOSIDE ANALOGUES FOR THE TREATMENT OF A VIRAL INFECTION, AND METHOD FOR EVALUATING THE SENSITIVITY TO SAID TREATMENT - The present invention describes the use of nucleoside analogues for the treatment of viral infections, in particular of an HIV infection, and also compositions comprising at least one of these analogues, and a method for evaluating the sensitivity to said treatment. | 10-30-2014 |
| 20140336141 | MAO-B INHIBITORS DERIVED FROM THE ONE-CARBON CYCLE - The invention exploits the elucidation of a connection between the S-adenosylmethionine one-carbon cycle and MAO-B levels and describes drug efficacy testing methods and the use of compounds of the S-adenosylmethionine one-carbon cycle as MAO-B inhibitors in disease prevention and treatment. | 11-13-2014 |
| 20150011495 | Methods of Synthesizing Substituted Purine Compounds - The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. | 01-08-2015 |
| 20150011496 | METHODS AND COMPOSITIONS FOR STIMULATING BONE REGENERATION - The invention provides methods and compositions for stimulating or promoting bone regeneration or repairing bone fracture or for stimulating or increasing differentiation or activation of osteoblasts by administering to a subject a therapeutically effective amount of an adenosine receptor agonist, or an analog, derivative or combination thereof, an adenosine receptor antagonist, or an analog, derivative or combination thereof, or adenosine or a compound that upregulates, increases the amount of or increases the biological activity of adenosine. The invention also extends to pharmaceutical compositions such as those comprising an agent that modulates an adenosine receptor such as an adenosine A | 01-08-2015 |
| 20150018298 | POLYCYCLIC-CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE - Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): | 01-15-2015 |
| 20150018299 | TREATMENT OF LIVER CONDITIONS - The present disclosure concerns the A | 01-15-2015 |
| 20150038445 | METHODS AND COMPOSITIONS FOR TREATING PAIN - The disclosure provides a new use of adenosine analogs for the treatment of pain through activation of neurokinin 1 (NK1) receptor signaling pathway, thereby inducing the activation of M-type potassium channel to induce outward currents. A method and pharmaceutical composition for treating pain comprising an adenonsine analog that activates NK1 receptor signaling, thereby inducing outward current are also provided. | 02-05-2015 |
| 20150038446 | COMPOSITIONS AND METHODS FOR TREATING RETINAL DEGRADATION - The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor. | 02-05-2015 |
| 20150038447 | ORGAN PROTECTION, PRESERVATION AND RECOVERY - This application describes compositions, methods of treatment, and methods of manufacturing a medicament for reducing injury or damage to cells, tissues or organs during ischemia, reperfusion, or following ischemia or trauma. The methods for reducing damage to a cell, tissue or organ comprise administering an effective amount of a composition including (i) a potassium channel opener or agonist and/or adenosine receptor agonist; and (ii) an antiarrhythmic agent. The methods may further include postconditioning the cell, tissue or organ. | 02-05-2015 |
| 20150038448 | COMBINATION, KIT AND METHOD OF REDUCING INTRAOCULAR PRESSURE - The present invention is directed to a combination or a kit comprising a prostaglandin analog and an adenosine receptor A | 02-05-2015 |
| 20150051166 | Methods of Treating Neurological Diseases - The present invention is directed to novel treatment of controlling hippocampal neural circuit hyperexcitability occurring in a neurological disease or disorder associated with epileptogenesis in a subject in need of such treatment, comprising the step of contacting the hippocampus in said subject with a compound effective to restore excitatory/inhibitor balance thereby controlling the neural circuit hyperexcitability. Further provided is a method of treating a neurological disease or disorder associated with epileptogenesis in a subject in need of such treatment, comprising the step of administering an amount of an adenosine A1 receptor agonist pharmacologically effective to block epileptogenetic activities without blocking excitatory synaptic transmission. | 02-19-2015 |
| 20150080330 | METHOD OF REDUCING INTRAOCULAR PRESSURE IN HUMANS - Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT). | 03-19-2015 |
| 20150094275 | SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE - The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers. | 04-02-2015 |
| 20150119351 | THERAPY OF TUMORS AND INFECTIOUS AGENTS DEFICIENT IN METHYLTHIOADENOSINE PHOSPHORYLASE - Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents. In addition, screening methods for identifying competitive antagonists, protective agents and potentiating agents, for use according to the methods of the invention, are provided. | 04-30-2015 |
| 20150290236 | PHARMACEUTICAL COMPOSITIONS OF REGADENOSON - The present invention relates to novel pharmaceutical compositions of Regadenoson and its pharmaceutically acceptable salts, solvates or hydrates in the form of solution, wherein the compositions are free from phosphate buffer and EDTA. Further the invention relates to pharmaceutical composition of Regadenoson comprising a tonidty modifier. | 10-15-2015 |
| 20150342979 | DOT1L INHIBITORS FOR USE IN THE TREATMENT OF LEUKEMIA - The present invention relates to DOT1L inhibitors. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 12-03-2015 |
| 20150344517 | STABLE INDOLE-3-PROPIONATE SALTS OF S-ADENOSYL-L-METHIONINE - Stable indole-3-propionic acid salts of S-adenosyl-L-methionine, or a pharmaceutically acceptable salt thereof, are disclosed, as well as pharmaceutical compositions comprising the indole-3-propionic acid salts, methods of using the indole-3-propionic acid salts and processes for making same. | 12-03-2015 |
| 20150352137 | THYMIDINE FOR PREVENTING NEURAL TUBE DEFECTS - The present invention relates to the prevention of neural tube defects. In particular, the invention provides thymidine or dTMP for use in a method of preventing or prophylactically treating a neural tube defect. The method may comprise administering the thymidine or dTMP to a female mammal that is pregnant or that may become pregnant. The thymidine or dTMP may be administered in combination with one or more purine molecules. | 12-10-2015 |
| 20150366893 | SUBSTITUTED PURINE AND 7-DEAZAPURINE COMPOUNDS - The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 12-24-2015 |
| 20150374737 | Dual-Action Compounds Targeting Adenosine A2A Receptor and Adenosine Transporter for Prevention and Treatment of Neurodegenerative Diseases - The present invention provides therapeutic agents for preventing and treating neurodegenerative diseases. These agents synergistically target both the adenosine A | 12-31-2015 |
| 20160000926 | CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS - The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. | 01-07-2016 |
| 20160024135 | Adenosine receptor activation reagent and the uses of thereof - The present invention relates to application of N(6)-(2-hydroxyethyl)-adenosine (HEA) and its derivatives as an adenosine A | 01-28-2016 |
| 20160039860 | ENANTIOMERS OF THE 1',6'-ISOMER OF NEPLANOCIN A - Enantiomers of 1′,6′-isoneplanocin, including derivatives of the enantiomers of 1′,6′-isoneplanocin, are disclosed along with novel synthetic methods. In particular, a substituted cyclopentane epoxide is synthesized into the enantiomers of 1′,6′-isoneplanocin. Enantiomers of carbocyclic nucleoside analogs of 3-deazaneplanocin to provide D- and L-like 1′,6′-iso-3-deazaneplanocin are also disclosed. The small molecule chemotherapeutic compounds beneficially provide DNA and RNA antiviral activity, demonstrating activity towards, for example, human cytomegalovirus, measles, Ebola, norovirus, dengue, vaccinia and HBV. Compounds exhibiting reduced S-adenosylhomocysteine hydrolase inhibitory effects are disclosed and provide improved toxicity profiles in comparison to neplanocin. The invention provides improved prophylactic and/or therapeutic antiviral efficacy. | 02-11-2016 |
| 20160052955 | METHYLTRANSFERASE INHIBITORS FOR TREATING CANCERS - Compounds having methyltransferase inhibitory activity are disclosed. The compounds have the structure | 02-25-2016 |
| 20160067271 | Methods And Compositions For Preventing Or Treating Obesity - The invention includes methods of treating, preventing, or limiting obesity or weight gain, or reducing or suppressing appetite, by the administration of A2A adenosine receptor pathway agonists. The A2AR pathway agonists may be administered in conjunction with a therapeutic agent having a side effect of weight gain, in order to prevent or limit that weight gain. In some instances, the A2AR pathway agonist is administered as a sleeping pill, and in other instances the A2AR pathway agonist is administered in a non-drowsy formulation. | 03-10-2016 |
| 20160082033 | COMPOSITIONS OF SELENOORGANIC COMPOUNDS AND METHODS OF USE THEREOF - The present application relates to compositions comprising selenium compounds, such as 5′-Methylselenoadenosine, a compound of Formula (I), and combinations thereof, and methods of using the same for inhibiting β amyloid aggregation, ApoE4 expression, p38 or Tau protein phosphorylation, or increasing Neprilysin and Insulin Degrading Enzyme expression. | 03-24-2016 |
| 20160120894 | USE OF ADENOSINE ASPARTATE IN THE DIFFERENTIAL ACTIVATION OF MACROPHAGES IN INFLAMMATORY-FIBROGENIC PROCESSES AND ITS REVERSAL - The present invention relates to the use of adenosine aspartate for differential activation of macrophages in inflammatory-fibrogenic processes and its reversal. | 05-05-2016 |
| 20160137686 | ANHYDROUS POLYMORPHS OF [(2R,3S,4R,5R)-5-(6-(CYCLOPENTYLAMINO)-9H-PURIN-9-YL)-3,4-DIHYDROXYTETRAH- YDROFURAN-2-YL)] METHYL NITRATE AND PROCESSES OF PREPARATION THEREOF - The present invention provides novel anhydrous polymorph forms of 2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate (Compound A). The present invention also provides processes for preparation of the anhydrous polymorphic forms of compound A. | 05-19-2016 |
| 20160158266 | 2' FLUORONUCLEOSIDES - 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: | 06-09-2016 |
| 20160158267 | METHODS OF PREVENTING, REDUCING OR TREATING MACULAR DEGENERATION - The present invention is directed to selective adenosine A | 06-09-2016 |
| 20160158268 | METHOD OF REDUCING INTRAOCULAR PRESSURE IN HUMANS - Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT). | 06-09-2016 |
| 20160168185 | NON-RIBOSE CONTAINING INHIBITORS OF HISTONE METHYLTRANSFERASE DOT1L FOR CANCER TREATMENT | 06-16-2016 |
| 20160194348 | SUBSTITUTED PYRROLO[2,3-D]PYRIMIDINES | 07-07-2016 |
| 20180021363 | COMPOUNDS AND METHODS FOR TREATING NEUROLOGICAL AND CARDIOVASCULAR CONDITIONS | 01-25-2018 |
| 20220135573 | SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE - The present disclosure provides novel heteroaryl compounds of formula (VII). Such compounds are useful for the treatment of cancers. | 05-05-2022 |
