87 results about "Adenosine a" patented technology

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.

The present invention relates to a compound of formula (I): wherein:R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; andR4 and R5 taken together form a ring having from 5 to 10 carbon atoms.Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.

The present invention relates to methods for producing coronary vasodilation with little peripheral vasodilation by administering doses of a pharmaceutical composition including regadenoson, named (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, — an adenosine A2A receptor agonist — to a human in an amount sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm / sec.

Compounds of formula (I) wherein: X is N; R1 is C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl; R2 is hydrogen, C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl, C6-C14 aryl or C6-C14 aryl(C1-C6) linear or branched alkyl or C6-C14 aryl(C1-C6) linear or branched alkenyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting of halogen, hydroxy, C1-C6 alkoxy linear or branched or C1-C6 alkenyloxy linear or branched, amino, optionally mono- or disubstituted with C1-C6 linear or branched alkyl; R3 is NH2, NHR4; R4 is C1-C6 alkyl or C1-C6 hydroxyalkyl, C1-C3 alkoxyalkyl, amino(C1-C6)alkyl, where the amino group is optionally substituted with one or two C1-C3 linear or branched alkyl groups, or with one or two C2-C3 alkenyl groups C6-C14 aryl or C6-C14 aryl(C1-C6)alkyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting by halogen, hydroxy, C1-C6 alkoxy linear or branched or C1-C6 alkenyloxy linear or branched, amino, mono- or di-substituted with C1-C6 alkyl linear or branched or C1-C6 alkenyl linear or branched; and their pharmaceutically acceptable salts. These compounds are antagonists of the adenosine A2a receptor and useful as medicaments, in particular for the treatment of Parkinson's disease.

The present invention relates generally to compounds of the formula (I):wherein:X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; andG1 and G2 are independently CH or N.The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.

The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and / or a COMT inhibitor and / or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine A2A receptor antagonist singly or together with a dopamine agonist, and / or a COMT inhibitor, and / or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.

A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging.

Provided are therapeutic and / or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and / or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.

A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A2a receptor agonist, at least one liquid carrier, and at least one co-solvent.