US2020316068A1PendingUtilityA1

Methods for Treating MS Using Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity

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Assignee: MERCK PATENT GMBHPriority: Nov 17, 2015Filed: Jun 8, 2020Published: Oct 8, 2020
Est. expiryNov 17, 2035(~9.3 yrs left)· nominal 20-yr term from priority
Inventors:Tammy Dellovade
C07D 495/04A61K 31/69A61K 31/55A61K 31/5377A61K 31/513A61K 31/506A61K 31/505A61K 31/455A61K 31/445A61K 31/4418C07D 401/14C07D 413/14C07D 405/14C07D 401/04C07D 413/12C07D 403/14C07D 403/12A61P 25/00A61P 43/00A61P 25/28A61P 21/00A61K 31/4545A61K 45/06
45
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Claims

Abstract

The present invention provides methods of treating MS using pyrimidine and pyridine compounds which are inhibitors of Bruton's tyrosine kinase (BTK).

Claims

exact text as granted — not AI-modified
1 - 20 . (canceled) 
     
     
         21 . A method of treating multiple sclerosis (MS), comprising:
 administering to a subject in need thereof a therapeutically effective amount of compound of the following formula:   
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt, a pharmaceutically acceptable tautomer, or a pharmaceutically acceptable stereoisomer thereof, wherein 
       
       R 1 ═H or NH 2 , 
       R 2 ═NH—CH 2 —R 3 , NH—R 4 , or O—CH 2 —R 5 ; 
       R 3 ═N-cyclobutyl, pyrrolidine, or phenyl; 
       R 4 =cyclohexyl, phenyl, or piperidine; and 
       R 5 =pyrrolidine or piperidine. 
     
     
         22 . The method of  claim 21 , wherein the MS is selected from the group consisting of relapsing MS (RMS). relapsing-remitting MS (RRMS), progressive MS (PMS), secondary-progressive MS (SPMS), primary-progressive MS (PPMS), and progressive-relapsing MS (PRMS). 
     
     
         23 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         24 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         25 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         26 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         27 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         28 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         29 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         30 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         31 . The method of  claim 21 , wherein the formula is the following: 
       
         
           
           
               
               
           
         
       
     
     
         32 . The method of  claim 21 , wherein the formula is the following:

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