US2009137802A1PendingUtilityA1

A2b adenosine receptor antagonists

Assignee: ELZEIN ELFATIHPriority: Nov 9, 2001Filed: Jan 28, 2009Published: May 28, 2009
Est. expiryNov 9, 2021(expired)· nominal 20-yr term from priority
A61P 9/00A61P 37/00A61P 43/00A61P 25/00C07D 473/00C07D 239/545C07D 473/06C07D 403/12A61P 11/06A61P 1/00C07D 473/08
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Claims

Abstract

Disclosed are processes for the synthesis of novel compounds that are A 2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Claims

exact text as granted — not AI-modified
1 . An intermediate of the formula: 
       
         
           
           
               
               
           
         
       
       wherein:
 R 1  and R 2  are independently chosen from methyl, ethyl, n-propyl, 2-methylpropyl, and cyclopropylmethyl. 
 
     
     
         2 . The intermediate of  claim 1 , wherein R 1  is n-propyl and R 2  is ethyl: 
       
         
           
           
               
               
           
         
       
       namely 6-[2-(dimethylamino)-1-azavinyl]-1-ethyl-3-propyl-1,3-dihydropyrimidine-2,4-dione. 
     
     
         3 . An intermediate of the formula: 
       
         
           
           
               
               
           
         
       
       wherein R 1  is n-propyl or cyclopropylmethyl. 
     
     
         4 . The intermediate of  claim 3 , wherein R 1  is n-propyl: 
       
         
           
           
               
               
           
         
       
       namely N-(6-amino-2,4-dioxo-3-propyl(1,3-dihydropyrimidin-5-yl))(1-{[3-(trifluoromethyl)-phenyl]methyl}pyrazol-4-yl)carboxamide. 
     
     
         5 . An intermediate of the formula: 
       
         
           
           
               
               
           
         
       
       wherein R 2  is methyl or ethyl. 
     
     
         6 . The intermediate of  claim 5 , wherein R 2  is ethyl: 
       
         
           
           
               
               
           
         
       
       N-(6-amino-1-ethyl-2,4-dioxo(1,3-dihydropyrimidin-5-yl))(1-{{[3-(trifluoromethyl)phenyl]methyl}pyrazol-4-yl)carboxamide. 
     
     
         7 . An intermediate of the formula: 
       
         
           
           
               
               
           
         
       
       wherein R 1  and R 2  are independently chosen from methyl, ethyl, n-propyl, 2-methylpropyl, and cyclopropylmethyl.

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