Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. wherein A is an optionally substituted aryl or an optionally substituted heteroaryl; B is an optionally substituted aryl or an optionally substituted heteroaryl; R1 is hydrogen, (C1–C4)alkyl, halo-substituted (C1–C4)alkyl, or (C1–C4)alkoxy; and R4 is as described herein.

Abstract: A composition for suppressing appetite and cravings for substances such as nicotine, coffee, sweets or chocolate while improving energy and enhancing mood comprises theobromine or a salt thereof at an effective amount of from about 250 to 4000 mg. Using such relatively high proportions of theobromine, without added caffeine or ephedrine provides an effective method for promoting weight control or to halt substance cravings without the side effects associated with such stimulants. The composition also includes Rhodiola rosea extract to offset stress effects from reduced food or substance intake, and to further improve mood, and clarity of thought and ability to handle stress, and to also increase endurance while reducing muscle pain.

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: 3,7-Dihydro-purine-2,6-dione derivatives of Formula (I) are provided wherein R1, R2, R3 and R4 are herein defined for use as CRF receptor ligands in the treatment of disorders characterized by overexpression of corticotropin releasing factor (CRF), such as anxiety, depression, and irritable bowel syndrome.

Abstract: A tablet for oral administration of nutritional indium comprises about 10–50 mg indium sulfate, about 4–20 mg caffeine, about 2–10% by weight cocoa powder, and about 5–10% by weight ethyl cellulose, in combination with about 50–150 ?g of each of zinc oxide, copper (II) oxide, magnesium oxide, potassium iodide, selenium amino acid chelate, chromium amino acid chelate and manganese amino acid chelate.

Abstract: A composition that will substantially reduce the deleterious effects of alcohol on the body and substantially reduce the side effects associated with hangovers (i.e. headaches, dizziness, nausea, dry mouth, etc) when taken as recommended. The composition includes an effective amount of (I)-glycine, (I)-glutathione, thiamine, magnesium, selenium, molybdenum. Other vitamins, mineral compounds, flavoring, coloring, and solubility agents may also be added.

Abstract: The present invention relates to a pharmaceutical composition, comprising (a) a phosphodiesterase 5 inhibitor or a pharmaceutically acceptable salt thereof and (b) at least one of the active ingredients selected from the group consisting of (i) an anti-diabetic agent; (ii) HMG-Co-A reductase inhibitors; (iii) an anti-hypertensive agent; and (iv) a serotonin reuptake inhibitor (SSRI) or, in each case, or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: The invention pertains to theophylline (1-methyl, 3-methyl xanthine) and IBMX (1-methyl, 3-isobutyl xanthine) derivatives of formulas I and II: where R1 is —CH3 or —CH2CH(CH3)2, and R2 is where R3 and R4 are independently selected from the group consisting of OCH3, CH3, NO2, F, Cl, Br and I.

Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.

Abstract: The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterization and/or treatment (or management) of neuro degenerative diseases, particularly amyotrophic lateral sclerosis.

Abstract: Methods useful for reducing pulmonary vasoconstriction or improving pulmonary hemodynamics in a patient are disclosed. More particularly, this invention relates to administering A1 adenosine receptor antagonists to reduce pulmonary vasoconstriction and improve pulmonary hemodynamics.

Abstract: The invention provides therapeutic methods and compositions comprising adenosine A1 antagonists for treating memory loss produced by reversible transient hypoxia and associated synaptic dysfunction.

Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:

Abstract: The present invention relates to a therapeutic agent for neurodegenerative disorders, comprising a xanthine derivative represented by formula (I): 1

Abstract: A compound having the following formula (I): 1

Abstract: A compound of the following formula: wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The compounds of formula (I) may be used to treat, among other indications, asthma and diarrhea.

Abstract: A compound of the following formula: wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The compounds of formula (I) may be used to treat, among other indications, asthma and diarrhea.

Abstract: A composition for suppressing appetite and cravings for substances such as nicotine, coffee, sweets or chocolate while improving energy and enhancing mood comprises theobromine or a salt thereof at an effective amount of from about 250 to 4000 mg. Using such relatively high proportions of theobromine, without added caffeine or ephedrine provides an effective method for promoting weight control or to halt substance cravings without the side effects associated with such stimulants. The composition also includes Rhodiola rosea extract to offset stress effects from reduced food or substance intake, and to further improve mood, and clarity of thought and ability to handle stress, and to also increase endurance while reducing muscle pain.

Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I 1

Abstract: Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.

Abstract: The present invention relates to novel compounds according to the to the general formulas I, II, III, IV or V: 1

Abstract: The present invention relates to substituted xanthines of general formula 1

Abstract: The invention relates to methods and compositions for measuring the rate of gastric emptying in animals, including humans. The methods of the invention measure the rate of stomach emptying by administration of a marker agent in a delayed-release formulation or food vehicle and blood or serum levels of the marker agent are monitored over time. The blood or serum levels of a marker agent reflect the gastric emptying rate. Incorporating such agents in foods also delays the absorption of such agents and serves as a measure of digestion and gastric emptying. These methods may be used to screen for drugs, herbal substances and other compounds that modulate gastric emptying, such as by increasing prokinetic activity of the gastrointestinal tract.

Abstract: A novel solid pharmaceutical dispersion that improves the bioavailability of poorly water soluble drugs is produced by combining the drug with a polymer carrier such as polyvinylpyrrolidone. The drug is combined with the carrier without the need for using organic solvents or melting temperatures (fusion) through the use of a transition compound such as polyethylene glycol which partially solubilizes the drug and/or plasticizes the polymer.

Abstract: Described herein are respiratory drug condensation aerosols and methods of making and using them. Kits for delivering condensation aerosols are also described. The respiratory drug aerosols typically comprise respiratory drug condensation aerosol particles. In some variations the respiratory drug compound is selected from the group consisting of &bgr;-adrenergics, methylxanthines, anticholinergics, corticosteroids, mediator-release inhibitors, anti-leukotriene drugs, asthma inhibitors, asthma antagonists, anti-endothelin drugs, prostacyclin drugs, ion channel or pump inhibitors, enhancers, or modulators and pharmaceutically acceptable analogs, derivatives, and mixtures thereof. Methods of treating a respiratory ailment using the described aerosols are also described. In general, the methods typically comprise the step of administering a therapeutically effective amount of respiratory drug condensation aerosol to a person with a respiratory ailment.

Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of a 2′-halomethylidene derivative in conjunctive therapy with an effective antineoplastic amount of a S phase or M-phase specific agent.

Abstract: Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.

Abstract: The present invention is a method and composition for suppressing the appetite of a human being using L-theanine. The method comprises the step of orally administering a composition comprising an appetite-suppressing amount of L-theanine. The L-theanine composition used as an appetite suppressant in accordance with the invention can be provided in solid form or liquid form and can be further combined with one or more inert ingredients or one or more additional active ingredients. The appetite suppressant composition of the invention provides a natural way of suppressing the appetite of a human being without causing the side effects associated with conventional appetite suppressants.

Abstract: The present invention relates to a therapeutic agent for neurodegenerative disorders, comprising a xanthine derivative represented by formula (I): or a pharmaceutically acceptable salt thereof as an active ingredient wherein X1, X2, R1, R2, R3 and R4 are herein defined.

Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.

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: The invention is directed to physiologically active compounds of the general formula (Ix) 1

Abstract: Platelet activation is measured by determining Mean Platelet Component (MPC) of suspended blood platelets, using a specific anticoagulant composition. The composition comprises at least one component for effecting platelet sphering (for example EDTA), and at least one platelet antagonist (for example at least one of, and preferably all three of theophylline, adenosine and dipyridamole).

Abstract: Pentoxifylline, pioglitazone and metformin have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging.

Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.

Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.

Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3 is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from:  and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.

Abstract: Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: aqueous polar solvent 30-99.89%, active compound 0.001-60%, optionally containing flavoring agent 0.1-10%. Propellant 2-10%. The non polar composition of the invention comprises formulation II: non-polar solvent 20-85%, active compound 0.005-50%, and optionally flavoring agent 0.1-10% and propellant 50-80%.

Abstract: This invention is a safe and effective composition and method for treating acute migraine attacks using pseudoephedrine, acetaminophen, and other agents in an orally administrated form to alleviate the pain and cluster of symptoms characteristic of migraine attacks such as nausea, photophobia, phonophobia, and functional disabilities as well as the prodrome phase of a migraine attack.

Abstract: 1.

Abstract: A phosphodiesterase antagonist is used to reduce insulin resistance, and to amplify the effect of nitric oxide on skeletal muscle insulin-mediated glucose uptake in a mammal. In some instances, the antagonist is targeted to the liver. In some instances, the insulin resistance is hepatic insulin sensitizing substance (“HISS”) dependant insulin resistance.

Abstract: The present invention relates to a controlled release pharmaceutical composition comprising amounts ranging from about 0.1 to about 4.5% w/w, of one or more of rate controlling cellulosic ether polymers.

Abstract: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.

Abstract: The present invention relates to a therapeutic agent for neurodegenerative disorders, comprising a xanthine derivative represented by formula (I): 1

Abstract: The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally containing one or more heteroatoms selected from 0, N or S; k represents 0 or 1; n represents an integer of 1 to 50; X represents —O—, —N(H)—, —N(C1-6alkyl)-, —N(C3-8cycloalkyl)-, —N(C1-8alkyl)(C3-8 cycloalkyl), —N[(CH2CH2O)m(C1-12 alkyl, aryl, or aralkyl)]-, —CH2O—, —CH2NH—, —CH2N(C1-6alkyl)-, —CH2N(C3-8cycloalkyl)-, or —C1-12alkyl-; Q represents (—CH2)p, (—CH═CH—)p, (—C≡C—)p, (—(O)p1CH2—)p or (—CH2(O)p1)p R6 and R7 independently represent O or S; and all other variables are as defined herein; processes for their preparation, pharmaceutical formulations containing them, and their use in me

Abstract: A multilayer, flexible patch configured for the transdermal treatment of the skin of a human subject with an active ingredient, which ingredient is adapted for reducing the incidence of human cellulite and other fatty tissues comprising a pressure sensitive, skin adherable first layer selected from one of the polymeric materials comprising acrylate copolymer, vinyl ether copolymer, and a silicone adhesive polymer. It contains, by dispersal therethrough, an active ingredient selected from the group consisting of xanthine, hypoxanthine, theophylline, 7-theophylline acetic acid, caffeine, and theobromine. There is an outer backing, second layer comprising a water-soluble, skin conformable fabric adapted to provide moisture vapor permeability so to permit transepidermal moisture escape therethrough. Lastly, there is provided a protective liner, third layer, which is substantially, non-adhesive as to the adjacent, normally skin-adherable first layer and is protective of the active ingredient.

Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: R3 is an optionally substituted group selected from: and wherein X1, X2, Z, R1, R2, and R6 are as described in the specification.