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

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

Abstract: The present invention relates to the use of certain glycol derivatives of xanthines for the treatment of irritable bowel syndrome and functional dyspepsia.

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 a 1,3,8 substituted xanthine derivative of formula I 1

Abstract: The present invention includes a formulation and controlled release dosage form that enable the controlled release of therapeutic agents showing reduced absorption in the lower gastrointestinal tract. The formulation of the present invention includes a therapeutic agent that exhibits greater absorption in the upper GI tract than in the lower GI tract and a permeation enhancer, which serves to increase absorption of the therapeutic agent in the lower GI tract. The formulation of the present invention further includes a carrier that allows the formulation to transition to a bioadhesive gel in-situ after the formulation is dispensed within the GI tract and has had some opportunity to reach the surface of the GI mucosal membrane. The bioadhesive gel formed by the formulation of the present invention works to present effective concentrations of both the therapeutic agent and the permeation enhancer at the surface of the GI mucosal membrane over a period.

Abstract: Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R)-(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS. 5 and 6, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS.

Abstract: There is disclosed a method for preventing tissue injury caused by tissue hypoxia and reoxygenation, comprising administering a compound that inhibits signal transduction by inhibiting cellular accumulation of linoleoyl phosphatidic acid (PA) through an inhibition of the enzyme LPAAT (lysophosphatidic acyltransferase).

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: Disclosed are therapeutic compounds having the formula:

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 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: 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.

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract: Compositions are provided, which comprise at least one nucleoside analogue inhibitor, pharmaceutically acceptable salts, solvates, or prodrugs thereof and fusaric acid, derivatives, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising the above compositions are also provided that optionally further include another therapeutically effective compound, such as a carrier. Systemic and topical preparations comprising the above compositions are also provided as well as methods of treating viral diseases by the administration of the above antiviral agents to a patient.

Abstract: Compounds provided herein are 3,7-dihydro-purine-2,6-dione derivatives of Formula (I): 1

Abstract: A method and compositions for reducing post-surgical adhesion formation/reformation in mammals following surgical injury to a body cavity or organs situated therein. The aqueous compositions comprising pentoxifylline and a polyoxyalkylene block copolymer are applied to the injured areas subsequent to surgical injury.

Abstract: Provided is, among other things, a method of treating in an animal infection or neoplasm of cerebrospinal tissue characterized by a risk of death, the method comprising: (a) injecting a physiologically acceptable fluid for cerebrospinal perfusion into a first catheter into the cerebrospinal pathway, which fluid for cerebrospinal perfusion has an therapeutically effective amount an agent, the agent selected for effectiveness against the infection as identified or diagnosed; (b) withdrawing fluid at a second catheter into the cerebrospinal pathway to create a flow and flow pathway between the first and second catheters; and (c) maintaining the flow for a period of time adapted to perfuse at least 1 CSF volume.

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: 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: 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: A strategy for inducing immune T lymphocytes to respond in such a fashion to their target antigen at first exposure so as to enable them to mount a response of greater magnitude upon any subsequent exposure to the same target is provided. The strategy involves exposure of T cells or animals being immunized to the commonly used phosphodiesterase inhibitor drug, pentoxifylline (POX/PF/Trental), during immune priming. Evidence is provided showing that such exposure leads to enhancement of immune T cells responses upon re-exposure. The strategy is relevant and useful for increasing the efficiency of vaccinations.

Abstract: The present invention provides methods using erythropoietin to improve the tolerance of anti-viral and anti-tumor chemotherapeutic regimens containing interferon. The invention also described improved methods to treat chronic HCV by adjusting the dose of ribavirin to tailor the active dose of the drug while supporting the hemoglobin levels in the patient with EPO. The present invention also provides anti-viral dosing regimens, particularly for chronic HCV comprising administration of an interferon containing anti-viral medicament, EPO, and a compound that reduces the amount of active tumor necrosis factor in the subject.