US2018282316A1PendingUtilityA1

Benzimidazole derivatives as bromodomain inhibitors

Assignee: GILEAD SCIENCES INCPriority: May 9, 2013Filed: Jun 6, 2018Published: Oct 4, 2018
Est. expiryMay 9, 2033(~6.8 yrs left)· nominal 20-yr term from priority
A61P 35/00C07D 453/02C07D 413/14C07D 471/04C07D 413/04C07D 417/14
55
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Claims

Abstract

This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4a , R 4b , and R 5 are described herein.

Claims

exact text as granted — not AI-modified
We claim: 
     
         1 . A compound selected from the group consisting of: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         2 . A pharmaceutical composition comprising a compound of  claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 
     
     
         3 . A method of treating a subject having a disease or condition responsive to the inhibition of a bromodomain-containing protein, comprising administering a therapeutically effective amount of a compound of  claim 1 , or a pharmaceutically acceptable salt thereof. 
     
     
         4 . The method of  claim 3 , wherein the bromodomain-containing protein is BRD4. 
     
     
         5 . The method of  claim 3 , wherein the disease or condition is a neoplasm, cancer or tumor of the colon, rectum, prostate, lung, pancreas, liver, kidney, cervix, uterus, stomach, ovary, breast, skin, or the nervous system 
     
     
         6 . The method of  claim 3 , wherein the disease or condition is diffuse large B-cell lymphoma or multiple myeloma.

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