US2023013862A1PendingUtilityA1

SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AS BRUTON'S TYROSINE KINASE MODULATORS

Assignee: BEIGENE SWITZERLAND GMBHPriority: Apr 25, 2013Filed: Sep 3, 2021Published: Jan 19, 2023
Est. expiryApr 25, 2033(~6.8 yrs left)· nominal 20-yr term from priority
A61K 31/438A61K 31/527A61P 29/00A61K 31/4188C07D 471/14A61K 45/06A61K 31/437C07D 487/20A61K 31/55A61P 43/00C07D 519/00A61P 35/02C07D 487/04A61P 37/02C07D 471/20A61K 31/551A61K 31/5517A61K 31/519A61K 31/435A61P 35/00C07D 487/14A61P 37/00
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Claims

Abstract

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

Claims

exact text as granted — not AI-modified
1 .- 15 . (canceled) 
     
     
         16 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is mantle cell lymphoma (MCL); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         17 . The method of  claim 16 , wherein the subject is an adult patient. 
     
     
         18 . The method of  claim 16 , wherein the subject has received at least one prior therapy. 
     
     
         19 . The method of  claim 16 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy. 
     
     
         20 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is Waldenstrom's macroglobulinemia (WM); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         21 . The method of  claim 20 , wherein the subject is an adult patient. 
     
     
         22 . The method of  claim 20 , wherein the subject has received at least one prior therapy. 
     
     
         23 . The method of  claim 20 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy. 
     
     
         24 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is chronic lymphocytic leukemia (CLL); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         25 . The method of  claim 24 , wherein the subject is an adult patient. 
     
     
         26 . The method of  claim 24 , wherein the subject has received at least one prior therapy. 
     
     
         27 . The method of  claim 24 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy. 
     
     
         28 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is small lymphocytic lymphoma (SLL); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         29 . The method of  claim 28 , wherein the subject is an adult patient. 
     
     
         30 . The method of  claim 28 , wherein the subject has received at least one prior therapy. 
     
     
         31 . The method of  claim 28 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy. 
     
     
         32 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is follicular lymphoma (FL); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         33 . The method of  claim 32 , wherein the subject is an adult patient. 
     
     
         34 . The method of  claim 32 , wherein the subject has received at least one prior therapy. 
     
     
         35 . The method of  claim 32 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy. 
     
     
         36 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is marginal zone lymphoma (MZL); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         37 . The method of  claim 36 , wherein the subject is an adult patient. 
     
     
         38 . The method of  claim 36 , wherein the subject has received at least one prior therapy. 
     
     
         39 . The method of  claim 36 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy. 
     
     
         40 . A method of treating a disease in a subject comprising administering to the subject a compound having the following structure: 
       
         
           
           
               
               
           
         
         wherein the disease is diffuse large B cell lymphoma (DLBCL); and 
         the compound is administered at a dose of 160 mg twice a day (BID) or 320 mg once a day (QD). 
       
     
     
         41 . The method of  claim 40 , wherein the subject is an adult patient. 
     
     
         42 . The method of  claim 40 , wherein the subject has received at least one prior therapy. 
     
     
         43 . The method of  claim 40 , wherein the subject is an adult patient; and the adult patient has received at least one prior therapy.

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