US2021387997A1PendingUtilityA1

Dihydropyranopyrimidines for the treatment of viral infections

Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COPriority: Jul 1, 2016Filed: Jun 23, 2021Published: Dec 16, 2021
Est. expiryJul 1, 2036(~9.9 yrs left)· nominal 20-yr term from priority
C07D 491/052A61P 31/02A61P 43/00A61P 37/04
62
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Claims

Abstract

This invention relates to dihydropyranopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Claims

exact text as granted — not AI-modified
1 . A compound of formula (I): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, solvate or polymorph thereof, wherein 
         R 1  is C 1-6  alkyl optionally substituted by one or more substituents independently selected from hydroxyl or C 1-3  alkoxy; 
         R 2  is selected from hydrogen, fluorine, C 1-3  alkyl, cyclopropyl, —CF 3 , C 1-3 alkoxy or nitrile. 
       
     
     
         2 - 5 . (canceled) 
     
     
         6 . The compound of  claim 1 , wherein R 1  is C 1-6 alkyl substituted by hydroxyl. 
     
     
         7 . The compound of  claim 6 , wherein R 1  is: 
       
         
           
           
               
               
           
         
       
     
     
         8 . The compound of  claim 1 , wherein R 2  is hydrogen. 
     
     
         9 . The compound of  claim 1 , having the following structure: 
       
         
           
           
               
               
           
         
       
     
     
         10 . A pharmaceutical composition comprising the compound of  claim 1 , or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, solvate or polymorph thereof, together with one or more pharmaceutically acceptable excipients, diluents or carriers. 
     
     
         11 . A compound of formula (II): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, solvate or polymorph thereof, wherein 
         R 1  is C 1-6  alkyl optionally substituted by one or more substituents independently selected from hydroxyl or C 1-3 alkoxy; 
         R 2  is selected from hydrogen, fluorine, C 1-3  alkyl, cyclopropyl, —CF 3 , C 1-3 alkoxy or nitrile. 
       
     
     
         12 . The compound of  claim 11 , wherein R 1  is C 1-6 alkyl substituted by hydroxyl. 
     
     
         13 . The compound of  claim 12 , wherein R 1  is: 
       
         
           
           
               
               
           
         
       
     
     
         14 . The compound of  claim 11 , wherein R 2  is hydrogen. 
     
     
         15 . The compound of  claim 11 , having the following structure: 
       
         
           
           
               
               
           
         
       
     
     
         16 . A pharmaceutical composition comprising the compound of  claim 11 , or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, solvate or polymorph thereof, together with one or more pharmaceutically acceptable excipients, diluents or carriers. 
     
     
         17 . A compound of formula (III): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, solvate or polymorph thereof, wherein 
         R 1  is C 1-6  alkyl optionally substituted by one or more substituents independently selected from hydroxyl or C 1-3 alkoxy; 
         R 2  is selected from hydrogen, fluorine, C 1-3  alkyl, cyclopropyl, —CF 3 , C 1-3 alkoxy or nitrile. 
       
     
     
         18 . The compound of  claim 17 , wherein R 1  is C 1-6 alkyl substituted by hydroxyl. 
     
     
         19 . The compound of  claim 18 , wherein R 1  is: 
       
         
           
           
               
               
           
         
       
     
     
         20 . The compound of  claim 17 , wherein R 2  is hydrogen. 
     
     
         21 . The compound of  claim 17 , having the following structure: 
       
         
           
           
               
               
           
         
       
     
     
         22 . A pharmaceutical composition comprising the compound of  claim 17 , or a pharmaceutically acceptable salt, tautomer(s), stereo-isomeric forms, solvate or polymorph thereof, together with one or more pharmaceutically acceptable excipients, diluents or carriers.

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