US2013225812A1PendingUtilityA1

Bruton's tyrosinie kinase activity probe and method of using

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Assignee: PHARMACYCLICS INCPriority: Nov 3, 2006Filed: Apr 3, 2013Published: Aug 29, 2013
Est. expiryNov 3, 2026(~0.3 yrs left)· nominal 20-yr term from priority
Inventors:Zhengying PanShyr Jiann LiHeleen ScheerensLee HonigbergErik Verner
G01N 33/573G01N 2500/00G01N 2333/9121C07D 487/04
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Claims

Abstract

Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use.

Claims

exact text as granted — not AI-modified
1 .- 25 . (canceled) 
     
     
         26 . A compound having the structure: 
       
         
           
           
               
               
           
         
       
     
     
         27 . A process for the preparation of (R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine (4) comprising treatment of (R)-tert-butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate (3) with acid followed by treatment with base to form (R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine (4): 
       
         
           
           
               
               
           
         
       
     
     
         28 . The process of  claim 27 , wherein (R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine is isolated.

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