US2018244680A1PendingUtilityA1

Spiro-lactam nmda receptor modulators and uses thereof

Assignee: APTINYX INCPriority: Jan 29, 2013Filed: May 2, 2018Published: Aug 30, 2018
Est. expiryJan 29, 2033(~6.5 yrs left)· nominal 20-yr term from priority
A61P 9/10A61P 25/18A61P 25/28A61P 25/20A61P 25/24A61P 25/04A61P 25/14A61P 25/02A61P 25/08A61P 25/00A61P 21/00C07D 487/10
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Claims

Abstract

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Claims

exact text as granted — not AI-modified
1 .- 4 . (canceled) 
     
     
         5 . A compound represented by formula I: 
       
         
           
           
               
               
           
         
       
       or a stereoisomer and/or a pharmaceutically acceptable salt thereof, wherein:
 R b  is H; 
 R 1  is H; 
 R 2  is H; 
 R 3  is —C(O)R 32 , wherein R 32  is —CH 3 ; 
 R 5  has the formula —CH(CHR 4 R 6 )—X, wherein X is 1,3,4-oxadiazolyl; 
 R 4  is methyl; and 
 R 6  is hydroxyl. 
 
     
     
         6 . A pharmaceutical composition, the pharmaceutical composition comprising:
 a compound represented by formula I:   
       
         
           
           
               
               
           
         
       
       or a stereoisomer and/or a pharmaceutically acceptable salt thereof, wherein:
 R b  is H; 
 R 1  is H; 
 R 2  is H; 
 R 3  is —C(O)R 32 , wherein R 32  is —CH 3 ; 
 R 5  has the formula —CH(CHR 4 R 6 )—X, wherein X is 1,3,4-oxadiazolyl; 
 R 4  is methyl; and 
 R 6  is hydroxyl; and 
 a pharmaceutically acceptable excipient.

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