163 results about "Adenosine receptor antagonist" patented technology

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.

Disclosed are novel A_2B 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.

The invention is related to methods of preventing and treating hepatic fibrosis using A_2B 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.

The present invention relates to novel compounds that are A_2A 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.

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.

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.

Disclosed are processes for the synthesis of novel compounds that are A_2B adenosine receptor antagonists, having the structure of Formula I or Formula II:

by cyclizing a compound of the formula (3):

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.

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.

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

Disclosed are prodrugs of A_2B adenosine receptor antagonists, and their use in treating mammals for various disease states.

Disclosed are novel compounds that are A_2B 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.

Disclosed are novel compounds that are A_2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

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.

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.

Disclosed are novel A_2B 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.

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 A_2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.

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.

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.

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.