Abstract: Compounds provided herein are novel substituted tetrahydropurinones of Formula (I): 1

Abstract: Pharmaceutical compositions are disclosed for the treatment of acute, chronic and/or neuropathic pain. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an analgesic agent and a pharmaceutically acceptable carrier. The analgesic agent is selected from opioid analgesics, NMDA antagonists, substance P antagonists, COX 1 and COX 2 inhibitors, tricyclic antidepressants (TCA), selective serotonin reuptake inhibitors (SSRI), capsaicin receptor agonists, anesthetic agents, benzodiazepines, skeletal muscle relaxants, migraine therapeutic agents, anti-convulsants, anti-hypertensives, anti-arrythmics, antihistamines, steroids, caffeine, and botulinum toxin. The method of using these compounds and a method of treating acute, chronic and/or neuropathic pain and migraine in a mammal including a human is also disclosed.

Abstract: The present invention is directed to methods for readily propagating somatic tissue stem cells ex vivo. The methods comprise enhancing guanine nucleotide (GNP) biosynthesis, thereby expanding guanine nucleotide pools. This in turn conditionally suppresses asymmetric cell kinetics in the explanted tissue cells. The methods of the invention include pharmacological methods and genetic methods. The resulting cultured somatic stem cells can be used for a variety of applications including cell replacement therapies such as bone marrow transplants, gene therapies, tissue engineering, and in vitro organogenesis.

Abstract: A screening method for identifying a drug-like compound or lead compound for the development of a drug-like compound in which (1) a xanthine or related compound is exposed to a histone deacetylase, (2) the binding of the compound to the histone deacetylase is measured or the change in the activity of the histone deacetylase is measured or the change in the binding of the histone deacetylase to activated glucocorticoid receptor (GR) is measured and (3) any compound capable of the required binding to the histone deacetylase or producing the required change in the activity of the histone deacetylase or its binding to activated glucocorticoid receptor is identified. Methods of treatment make use of compounds identifiable by the screening methods.

Abstract: The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediated by a neural cell growth repulsion factor. The activator may comprise a direct or an indirect activator of the protein kinase; the repulsion factor typically comprises one or more natural, endogenous proteins mediating localized repulsion or inhibition of neural cell growth; and the target cells are generally vertebrate neurons, typically injured mammalian neurons. The subject compositions include mixtures comprising a neural cell, an activator of a cyclic nucleotide dependent protein kinase and a neural cell growth repulsion factor.

Abstract: A substantially taste masked liquid pharmaceutical composition containing a pharmaceutically effective amount of an unpleasant tasting drug dissolved or dispersed in an aqueous excipient base, said excipient base comprising polyvinyl pyrrolidone and/or copolyvidone, and high molecular weight polyethylene glycol.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Disclosed is theobromine with an anti-carcinogenic activity which inhibits the suppression of GJIC (gap junctional intercellular communication), a pathological phenomenon occurring during development of various kinds of cancers including liver cancer, as well as DNA synthesis of cancer cells thereby inhibiting proliferation of liver, gastric and colon cancer cells.

Abstract: The invention relates to the combined administration of a PDE4 or PDE3/4 inhibitor and a disease modifying anti-rheumatic drug (DMARDs) or anti-rheumatic or anti-arthritic drug.

Abstract: A compound of the following formula: 1

Abstract: A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients comprising at least 5% crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution; a substantially spherical granule for pharmaceutical use comprising famiciclovir and 5% or more crystalline cellulose, together with an optional coating; and a sachet containing a unit dose of famiciclovir in the form of such granules.

Abstract: The present invention provides compounds having the formula I: X is (C1-C8)alkylene, (C2-C8)alkenylene, (C2-C8)alkynylene, wherein one of the carbon atoms in the alkylene, alkenylene or alkynylene groups is optionally replaced with a group having the formula —O—, —N(R4)C(O)—, —OC(O—, S—, —S(O)—or —SO2—, or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising compounds having the formula I. The compounds of the invention are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents for treatment of diseases that are mediated by A2B adenosine receptors.

Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory drug of low water solubility in a therapeutically effective amount, wherein the drug is present in the form of solid particles, about 25% to 100% by weight of which are smaller than 1 &mgr;m. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders and have particular advantages where rapid onset of therapeutic effect is desired.

Abstract: Selective MMP-13 inhibitors are fused pyrimidinones of the formula 1

Abstract: A pH-dependent sustained release, drug delivery composition capable of being formed into tablets or pellets, wherein the release is controlled by a diffusion barrier formed by the interaction of a pH-dependent gelling material and a pH-independent non-gelling material, comprising a polymer matrix comprising, by weight, (a) 10 to 50% sodium alginate, (b) 2 to 15% propylene glycol alginate and (c) 40 to 80% of a pharmaceutical medicament.

Abstract: This invention relates to novel crystalline H polymorphic forms, Form I, II and IV of Cipamfylline, methods of preparation, and use thereof in the treatment of PDE4 and TNF mediated diseases. Cipamfylline is 1,3-di-cyclopropylmethyl-8-amino xanthine, and represented by formula (I).

Abstract: The present invention concerns the modulation of glycogene synthase kinase 3&bgr; (G3SK-3&bgr;) by an adenosine receptor ligand. Depending on the type of ligand, the modulation may be manifested by down-regulation or up-regulation of the kinase's activity.

Abstract: A skin cream is presented which reduces wrinkles upon topical application to the skin. The main ingredients of the composition include water and a xanthine based compound composition which is mixed together in a first vessel and a glycerin composition heated in a second vessel. The three components of the active ingredient are mixed carefully, making sure that any precipitate produced is remixed into the solution. After heating and mixing the components, the entire composition is cooled with care being taken to push any precipitate back into solution to ensure an even distribution of all of the components. The active ingredient thus produced may be combined with a suitable pharmaceutical vehicle to provide the topical wrinkle reducing moisturizing and protecting composition. The composition is topically applied to the effected area over a period of days or months in order to reduce or entirely eliminate wrinkles and dryness from the skin. The final active ingredient may also be used for other applications.

Abstract: A pressure-liquefied propellant mixture for aerosols, comprising a fluorinated alkane, in particular 1,1,1,2-tetrafluoroethane and/or 1,1,1,2,3,3,3-heptafluoropropane, and carbon dioxide, makes possible an improvement of the wetting properties of pharmaceutically active compounds, with which the formulation problems existing with hydrofluoroalkanes in relation to suspension as well as solution aerosols can be overcome and thus improved medicinal aerosol formulations can be obtained. With the aid of carbon dioxide, it is also possible to specifically influence the pressure and thus the particle size distribution and also by displacement of oxygen from the hydrofluoroalkanes to improve the storage stability of oxidation-sensitive active compounds.

Abstract: A method for a therapeutic treatment, comprising administering to a subject in need an effective amount of an active agent for achieving a therapeutic effect, the therapeutic effect comprises modulating GSK-3B activity in cells and said active agent is selected from the group consisting of an adenosine A1 receptor ligand (A1RL), an A2 adenosine receptor ligand (A2RL), an adenosine A3 receptor ligand (A3RL) and a combination of the same.

Abstract: Novel tricyclic compounds are found to be useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by cytokine intracellular signaling.

Abstract: Benzimidazole derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection 1

Abstract: The present invention is directed to a method of inducing neurogenesis by administering to a mammal an effective quantity of a compound that induces neurogenesis, where neurogenesis includes proliferation of neural stem and progenitor cells, differentiation of these cells into neurons, and/or survival of these new neurons. In general, the compound comprises three moieties, A, L, and B, covalently linked. A can be a purine, tetrahydroindolone, or pyrimidine; L is a linker, while B is a moiety that promotes absorption of the compound. A particularly preferred compound is N4-[[3-(6-oxo-1,6-dihydropurin-9-yl)-1-oxopropyl] amino] benzoic acid (also known as AIT-082 or leteprinim potassium). Another aspect of the invention is pharmaceutical compositions for inducing neurogenesis.

Abstract: Novel purine L-nucleoside compounds are disclosed, in which both the purine rings and the sugar are either modified, functionalized, or both. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Th1 and Th2.

Abstract: A method of decreasing the signs or symptomatology in a patient with a neurologic condition or disease, or in a patient due to effects of exposure to an exogenous substance, such as a pharmaceutical agent, comprising selecting a patient having at least one sign or symptom selected from the group consisting of akinesia, bradykinesia, dyskinesias, gait disturbances, posture disturbances, rigid limbs, speech impairments and tremor and administering to the patient one or more than one effective doses of a phosphodiesterase inhibitor.