US2017197972A1PendingUtilityA1

Benzodiazepine bromodomain inhibitor

Assignee: GLAXOSMITHKLINE LLCPriority: Nov 5, 2009Filed: Jan 20, 2017Published: Jul 13, 2017
Est. expiryNov 5, 2029(~3.3 yrs left)· nominal 20-yr term from priority
A61P 37/00A61P 35/00A61P 43/00A61P 37/02A61P 29/00A61K 31/5517A61K 45/06C07D 487/04A61K 31/551Y02A50/30
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Claims

Abstract

The present invention relates to a benzodiazepine compound, processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy.

Claims

exact text as granted — not AI-modified
1 . A compound of formula (I) which is 2-[(4S)-6-(4-Chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide 
       
         
           
           
               
               
           
         
       
       or a salt thereof. 
     
     
         2 . A compound of formula (I) which is 2-[(4S)-6-(4-Chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         3 . A compound of formula (I) which is 2-[(4S)-6-(4-Chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide 
       
         
           
           
               
               
           
         
       
     
     
         4 . A pharmaceutical composition which comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2  and one or more pharmaceutically acceptable carriers, diluents or excipients. 
     
     
         5 . A pharmaceutical composition which comprises a compound of formula (I) as defined in  claim 3  and one or more pharmaceutically acceptable carriers, diluents or excipients. 
     
     
         6 . A combination pharmaceutical product comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2  together with one or more other therapeutically active agents. 
     
     
         7 . A compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2  for use in therapy. 
     
     
         8 . A compound of formula (I) as defined in  claim 3  for use in therapy. 
     
     
         9 . A compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2 , for use in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated. 
     
     
         10 . A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to  claim 9 , wherein the disease or condition is a chronic autoimmune and/or inflammatory condition. 
     
     
         11 . A compound of formula (I) or a pharmaceutically acceptable salt thereof for use according to  claim 9 , wherein the disease or condition is cancer. 
     
     
         12 . The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2 , in the manufacture of a medicament for the treatment of diseases or conditions for which a bromodomain inhibitor is indicated. 
     
     
         13 . A method for treatment of a disease or condition, for which a bromodomain inhibitor is indicated, in a subject in need thereof which comprises administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2 . 
     
     
         14 . A method for treatment according to  claim 13 , wherein the disease or condition is a chronic autoimmune and/or inflammatory condition. 
     
     
         15 . A method for treatment according to  claim 13 , wherein the disease or condition is cancer. 
     
     
         16 . A method for treatment according to  claim 13 , wherein the subject is a human. 
     
     
         17 . A method for inhibiting a bromodomain which comprises contacting the bromodomain with a compound of formula (I) or a pharmaceutically acceptable salt thereof as defined in  claim 2 . 
     
     
         18 . A method for treatment according to  claim 13 , further comprising administering a therapeutically effective amount of one or more other therapeutically active agents. 
     
     
         19 . A method for treatment according to  claim 13 , wherein the one or more other therapeutically active agents is selected from antibiotics, anti-virals, glucocorticosteroids, muscarinic antagonists and beta-2 agonists. 
     
     
         20 . A method for treatment according to  claim 13 , wherein the compound of formula (I) and the one or more other therapeutically active agents are administered sequentially.

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