US2022008428A1PendingUtilityA1

Fused imidazo-piperidine jak inhibitor compound

Assignee: THERAVANCE BIOPHARMA R&D IP LLCPriority: May 1, 2017Filed: Sep 28, 2021Published: Jan 13, 2022
Est. expiryMay 1, 2037(~10.8 yrs left)· nominal 20-yr term from priority
A61P 27/02A61P 17/04A61P 17/00A61K 9/10A61P 11/08A61K 9/0048A61K 9/0019A61P 11/00A61P 11/06A61K 31/5377A61P 29/00C07D 471/04
70
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Claims

Abstract

The invention provides a compound of formula 1or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides crystalline forms of the compound, pharmaceutical compositions comprising the compound, methods of using the compound to treat diseases amenable to a JAK inhibitor, and processes and intermediates useful for preparing the compound.

Claims

exact text as granted — not AI-modified
1 - 19 . (canceled) 
     
     
         20 . A process for preparing a compound of formula 1 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically-acceptable salt thereof, the process comprising:
 (a) reacting a compound of formula 6: 
 
       
         
           
           
               
               
           
         
       
       with a compound of formula 7: 
       
         
           
           
               
               
           
         
       
       wherein R A  is hydrogen or 2,5-dioxopyrrolidinyl, and
 (b) optionally preparing a pharmaceutically-acceptable salt to provide a compound of formula 1 or a pharmaceutically-acceptable salt thereof. 
 
     
     
         21 - 31 . (canceled) 
     
     
         32 . The process of  claim 20 , wherein R A  is hydrogen. 
     
     
         33 . The process of  claim 20 , wherein R A  is 2,5-dioxopyrrolidinyl. 
     
     
         34 . The process of  claim 32 , wherein step (a) is conducted in the presence of HATU. 
     
     
         35 . The process of  claim 32 , wherein step (a) is conducted in the presence of N,N-diisopropylethylamine. 
     
     
         36 . The process of  claim 32 , wherein step (a) is conducted in DMF. 
     
     
         37 . The process of  claim 33 , wherein step (a) is conducted in the presence of DIPEA. 
     
     
         38 . The process of  claim 33 , wherein step (a) is conducted in DMF.

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