US2016002202A1PendingUtilityA1

2',6'-dioxo-3'-deutero-piperdin-3-yl-isoindoline compounds

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Assignee: DEUTERX LLCPriority: Mar 28, 2011Filed: Jun 19, 2015Published: Jan 7, 2016
Est. expiryMar 28, 2031(~4.7 yrs left)· nominal 20-yr term from priority
Inventors:Sheila Dewitt
A61P 7/00A61P 35/00C07B 59/002C07D 401/04A61P 25/28C07B 2200/05A61P 29/00
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Claims

Abstract

The present application describes 2-(2′,6′-dioxo-3′-deutero-piperidin-3′-yl)isoindoles, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Claims

exact text as granted — not AI-modified
1 - 3 . (canceled) 
     
     
         4 . A deuterium-enriched compound having the following formula or a stereoisomer or pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         wherein: 
         R 8  is selected from H and D; 
         R 8a  is —OR 12a    
         one of X and Y is C═O and the other is selected from CH 2 , CHD, and CD 2 C═O; 
         Z is H or D, provided that the abundance of deuterium in Z is at least 30%; 
         R 1 -R 7  are independently selected from H and D; 
         R 12a  is CH 2 —R a —R b —R c ; 
         R a  is selected from aryl, (C 1 -C 6 )heterocycloalkyl, and (C 2 -C 9 )heteroaryl, wherein R a  is optionally substituted with 1-3 halogen; 
         R b  is selected from (CH 2 ) m , O(CH 2 ) m , and (CH 2 ) m O; 
         m is selected from 0-3; 
         R c  is selected from aryl, (C 1 -C 6 )heterocycloalkyl, and (C 2 -C 9 )heteroaryl; 
         wherein a hydrogen atom present in any of the substituents is optionally replaced by deuterium. 
       
     
     
         5 - 24 . (canceled) 
     
     
         25 . The deuterium-enriched compound of  claim 4 , wherein X is C═O. 
     
     
         26 . The deuterium-enriched compound of  claim 4 , wherein R a  is aryl. 
     
     
         27 . The deuterium-enriched compound of  claim 25 , wherein R a  is aryl. 
     
     
         28 . The deuterium-enriched compound of  claim 26 , wherein said aryl is phenyl. 
     
     
         29 . The deuterium-enriched compound of  claim 27 , wherein said aryl is phenyl. 
     
     
         30 . The deuterium-enriched compound of  claim 27 , wherein R b  is (CH 2 ) m . 
     
     
         31 . The deuterium-enriched compound of  claim 29 , wherein R b  is (CH 2 ) m . 
     
     
         32 . The deuterium-enriched compound of  claim 27 , wherein R c  is (C 1 -C 6 )heterocycloalkyl. 
     
     
         33 . The deuterium-enriched compound of  claim 30 , wherein R c  is (C 1 -C 6 )heterocycloalkyl. 
     
     
         34 . The deuterium-enriched compound of  claim 31 , wherein R c  is (C 1 -C 6 )heterocycloalkyl. 
     
     
         35 . The deuterium-enriched compound of  claim 33 , wherein (C 1 -C 6 )heterocycloalkyl is morpholinyl. 
     
     
         36 . The deuterium-enriched compound of  claim 34 , wherein (C 1 -C 6 )heterocycloalkyl is morpholinyl. 
     
     
         37 . The deuterium-enriched compound of  claim 33 , wherein the abundance of deuterium in Z is at least 90%. 
     
     
         38 . The deuterium-enriched compound of  claim 34 , wherein the abundance of deuterium in Z is at least 90%. 
     
     
         39 . The deuterium-enriched compound of  claim 36 , wherein the abundance of deuterium in Z is at least 90%. 
     
     
         40 . The deuterium-enriched compound of  claim 33 , wherein R 1 -R 7  are H, and R 8  is H. 
     
     
         41 . The deuterium-enriched compound of  claim 34 , wherein R 1 -R 7  are H, and R 8  is H. 
     
     
         42 . The deuterium-enriched compound of  claim 36 , wherein R 1 -R 7  are H, and R 8  is H. 
     
     
         43 . The deuterium-enriched compound of  claim 39 , wherein R 1 -R 7  are H, and R 8  is H. 
     
     
         44 . A pharmaceutical composition comprising a deuterium-enriched compound of claim  1  and one or more excipients. 
     
     
         45 . A pharmaceutical composition comprising a deuterium-enriched compound of  claim 33  and one or more excipients. 
     
     
         46 . A pharmaceutical composition comprising a deuterium-enriched compound of  claim 34  and one or more excipients. 
     
     
         47 . A pharmaceutical composition comprising a deuterium-enriched compound of  claim 43  and one or more excipients. 
     
     
         48 . A method of treating systemic lupus erythematosus, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim  1  to treat systemic lupus erythematosus. 
     
     
         49 . The method of  claim 48 , wherein the compound is a compound of  claim 33 . 
     
     
         50 . The method of  claim 48 , wherein the compound is a compound of  claim 43 . 
     
     
         51 . A method of treating a disorder selected from the group consisting of scleroderma and sarcoidosis, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim  1  to treat the disorder.

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