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167 results about "Adenosine receptor antagonist" patented technology

An adenosine receptor antagonist is a drug which acts as an antagonist of one or more of the adenosine receptors. Examples include caffeine, theophylline, and theobromine.

Controlled delivery of therapeutic agents from medical articles

The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists. Pharmaceutical compositions comprising an A1 adenosine receptor antagonist disclosed herein and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of the invention are also disclosed. The novel A1 adenosine receptor antagonist compositions find further use in diagnostic and imaging methods.
Owner:BOSTON SCI SCIMED INC

A2B adenosine receptor antagonists

Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
Owner:GILEAD SCI INC

Method of preventing and treating hepatic disease using a2b adenosine receptor antagonists

ActiveUS20070219221A1Decreasing hepatotoxic side effectBiocideOrganic chemistryAlcohol abuseHepatic Diseases
The invention is related to methods of preventing and treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method.
Owner:GILEAD SCI INC

A2a adenosine receptor antagonists

The present invention relates to novel compounds that are A2A adenosine receptor antagonists, and to their use in treating mammals for various disease states, such as obesity, CNS disorders, including the “movement disorders” (Parkinson's disease, Huntington's Chorea, and catelepsy), and cerebral ischemia, excitotoxicity, cognitive and physiological disorders, depression, ADHD, and drug addiction (alcohol, amphetamine, cannabinoids, cocaine, nicotine, and opioids) and to their use in the enhancement of immune response. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
Owner:GILEAD SCI INC

Adenosine A3 receptor antagonists

InactiveUS6436966B1Excellent selective affinityImprove stabilityBiocideOrganic chemistryAdenosine A3 Receptor AntagonistsMedicine
A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.
Owner:TAKEDA PHARMA CO LTD

Methods for the prevention and treatment of fibrosis and sclerosis

Methods of treating or preventing fibrosis and sclerosis by the administration of compositions containing A1 adenosine receptor antagonists and / or P2X purinoceptor antagonists, or combinations thereof.
Owner:ENDACEA

Prodrugs of A2B adenosine receptor antagonists

Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structureand their use in treating mammals for various disease states.
Owner:GILEAD SCI INC

A1 adenosine receptor antagonists

The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists. Pharmaceutical compositions comprising an A1 adenosine receptor antagonist disclosed herein and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of the invention are also disclosed. The novel A1 adenosine receptor antagonist compositions find further use in diagnostic and imaging methods.
Owner:ENDACEA

8-pyrazole substituted xanthine A2B adenosine receptor antagonist and synthesis method and application thereof

The invention relates to a 8-pyrazole substituted xanthine A2B adenosine receptor antagonist and a synthesis method and an application thereof. The structural formula of the A2B adenosine receptor antagonist is shown in the specifications, and the antagonist is synthesized by taking 1,3-dialkyl-5,6-diaminouracil and nitrobenzyl pyrazole-4-formic acid as raw materials and improving a Traube reaction. The synthesis method disclosed by the invention has mild conditions, low cost and high yield, is easy to operate, and is suitable for industrial production. As proved by a pharmacological experiment, the affinity and selectivity of an A2B receptor are enhanced due to substitution of the 8-position of xanthine in 8-pyrazole substituted xanthine with nitrobenzyl pyrazole, the secretion of IL-8 can be suppressed, and the release of inflammatory factors is reduced. The receptor antagonist is suitable for treating bronchial asthma.
Owner:JINZHOU MEDICAL UNIV

A1 adenosine receptor antagonists

Disclosed are A1adenosine receptor antagonists, useful for treating various disease states, in particular disease states for which diuretic treatment is appropriate.
Owner:CV THERAPEUTICS INC

A2B adenosine receptor antagonists

Disclosed are novel compounds that are A2B adenosine receptor antagonists having the following structure: wherein R1 and R2 are independently chosen from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl, and R4 is an optionally substituted heteroaryl moiety. The compounds of the invention are useful for treating various disease states, including asthma, chronic obstructive pulmonary disorder, pulmonary inflammation, emphysema, diabetic disorders, inflammatory gastrointestinal tract disorders, immunological / inflammatory disorders, cardiovascular diseases, neurological disorders, and diseases related to angiogenesis.
Owner:GILEAD SCI INC

A2B adenosine receptor antagonists

Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula IIThe compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
Owner:GILEAD SCI INC

A3 adenosine receptor antagonists and partial agonists

Disclosed are A3 adenosine receptor antagonists and / or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.
Owner:UNITED STATES OF AMERICA

Methods and pharmaceutical compositions for treating sepsis

InactiveUS20060276378A1Promotes therapeutic responseBiocideCarbohydrate active ingredientsAntibiotic AgentsSepsis
Methods and compositions for treating and preventing sepsis are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist in combination with an antibiotic agent. The invention further encompasses pharmaceutical compositions comprising a combination of an A1 adenosine receptor antagonist and an antibiotic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing sepsis.
Owner:ENDACEA

8-Heteroaryl xanthine adenosine A2B receptor antagonists

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.
Owner:KING PHARMA RES & DEV

A1 adenosine receptor antagonists

The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods.wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.
Owner:ENDACEA

8-Heteroaryl xanthine adenosine A2B receptor antagonists

The present invention relates generally to compounds of 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; and G1 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.
Owner:KING PHARMA RES & DEV

Enhancing treatment of cancer and HIF-1 mediated disorders with adenosine A3 receptor antagonists

InactiveUS20060204502A1High activitySustained cellular protection against ischemiaOrganic active ingredientsBiocideDiseaseOncology
The present invention relates to the use of adenosine receptor antagonists, preferably A3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and / or management of diseases or disorders associated with overexpression of HIF-1α and / or increased HIF-1α activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1α (HIF-1α) using the A3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.
Owner:KING PHARMA RES & DEV

Method of treating hepatic disease using A2B adenosine receptor antagonists

ActiveUS7795268B2Decreasing hepatotoxic side effectBiocideOrganic chemistryAlcohol abuseHepatic inflammation
The invention is related to methods of treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases.
Owner:GILEAD SCI INC

A2B adenosine receptor antagonists

Disclosed are methods for making novel A2B adenosine receptor antagonists having the structure of formula I or Formula II:The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
Owner:GILEAD SCI INC

Treatment or prevention of acute renal failure

Adenosine receptor antagonists, especially aminophyllline, are used to treat or prevent acute renal failure. In the preferred embodiment, aminophylline is administered by infusion so that it does not exceed a serum theophylline level of 15-20 micrograms / ml, most preferably the aminophylline is administered to achieve a serum theophylline concentration of 3-10 micrograms / ml, with an infusion rate of 0.1-0.6 mg / kg IBW / hour (IBW=ideal body weight). The adenosine receptor antagonist can also be used to help sustain a kidney for transplant purposes. Preferably, aminophylline is loaded while the kidney is still part of the donor. A dose of aminophylline of 5 mg / kg lean body weight is infused into the donor over a 30-60 min period, with cardiac monitoring. The infusion dose is decreased in the event of supraventricular or ventricular tachycardias. The kidney is removed and placed in the standard “cold” bath, but containing aminophylline at a dose of 5-10 micrograms / ml (5-10 mg / l). The kidney is then transported to the recipient. The recipient is similarly preloaded with 5 mg / kg lean body mass aminophylline intravenously over 30-60 min with cardiac monitoring, with a constant infusion of 0.1-0.3 mg / kg lean body mass / hr continuing during the next 24 hours after the kidney is transplanted into the recipient.
Owner:GENOMED

Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

InactiveUS20060128694A1BiocideNervous disorderPyramidal syndromeAnticonvulsant Agent
There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless legs syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS; also claimed are pharmaceutical compositions consisting of an adenosine A2a receptor antagonist in combination with an antipsychotic agent, an anticonvulsant agent, lithium or an opioid.
Owner:SCHERING CORP
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