US2008070936A1PendingUtilityA1

Compounds specific to adenosine A1 receptors and uses thereof

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Assignee: OSI PHARM INCPriority: Dec 1, 2000Filed: Sep 20, 2007Published: Mar 20, 2008
Est. expiryDec 1, 2020(expired)· nominal 20-yr term from priority
A61P 9/00A61P 25/00A61K 31/519C07D 487/04A61P 11/00
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Claims

Abstract

This invention pertains to compounds which specifically inhibit the adenosine A 1 receptor and the use of these compounds to treat a disease associated with A 1 adenosine receptors in a subject.

Claims

exact text as granted — not AI-modified
1 - 60 . (canceled)  
     
     
         61 . A method for treating a subject afflicted with a disease associated with an A 1  adenosine receptor in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound having the structure:  
       or  
       
         
           
           
               
               
           
         
       
       or a  
       
         
           
           
               
               
           
         
       
       pharmaceutically acceptable salt thereof so as to thereby treat the subject, wherein the disease is antidiuresis, bradycardia, bronchitis, bronchoconstriction, Alzheimer's disease, cardiac arrythmias, cardiac hypoxia, congestive heart failure, hypertension, inflammation, negative cardiac inotropy and dromotropy, renal failure, sedation or is associated with transmitter release, respiratory epithelia, contraction of smooth muscle underlying respiratory epithelia, vasoconstriction or mast cell degranulation.  
     
     
         62 . The method of  claim 61 , wherein the subject is a mammal.  
     
     
         63 . The method of  claim 62 , wherein the mammal is a human.  
     
     
         64 . The method of  claim 61 , wherein the disease is congestive heart failure.  
     
     
         65 . A method for inhibiting the activity of an A1 adenosine receptor in a cell, which comprises contacting the cell with a compound having the structure:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof.  
     
     
         66 . The method of  claim 65 , wherein the cell is a human cell.  
     
     
         67 . A method for treating a subject having a respiratory disorder associated with the A 1  adenosine receptor in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound having the structure:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, so as to thereby treat the subject.  
     
     
         68 . The method of  claim 67 , wherein the respiratory disorder is asthma, chronic obstructive pulmonary disease, allergic rhinitis, or an upper respiratory disorder.  
     
     
         69 . The method of  claim 67 , wherein the subject is a human.  
     
     
         70 . A pharmaceutical composition comprising a compound having the structure:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.  
     
     
         71 . The pharmaceutical composition of  claim 70 , further comprising at least one of either a steroid, β2 agonist, glucocorticoid, leukotriene antagonist, or an anticolinergic agonist.  
     
     
         72 . The pharmaceutical composition of  claim 70 , wherein the pharmaceutical composition is formulated for administration as a periocular, retrobulbar or intraocular injection.  
     
     
         73 . The pharmaceutical composition of  claim 70 , wherein the pharmaceutical composition is formulated for systemic administration.  
     
     
         74 . The pharmaceutical composition of  claim 70 , wherein the pharmaceutical composition is formulated for administration as a surgical irrigating solution.  
     
     
         75 . A packaged pharmaceutical composition for treating a subject suffering from a disease associated with an A1 adenosine receptor, comprising the pharmaceutical composition of  claim 70  and instructions for using the composition for treating the subject.

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