US2008033165A1PendingUtilityA1

[Beta]-Lactamyl Vasopressin V1a Antagonists and Methods of Use

61
Individually held — no corporate assignee on recordPriority: Oct 12, 2001Filed: Aug 7, 2007Published: Feb 7, 2008
Est. expiryOct 12, 2021(expired)· nominal 20-yr term from priority
Inventors:Gary A. KoppelRobert F. Bruns, Jr.
A61P 9/08A61P 35/00A61P 9/10A61P 37/02A61P 43/00A61P 31/18A61P 7/00A61P 7/02A61P 9/00A61P 37/06A61P 37/08A61P 9/04A61P 3/10A61P 25/06A61P 25/18A61P 25/04A61P 25/16A61P 25/08A61P 29/02A61P 29/00A61P 25/00A61P 25/32A61P 25/22A61P 25/24A61P 27/02A61P 25/28A61P 25/36A61P 1/12A61P 1/02A61P 19/02A61P 15/00A61P 19/08A61P 11/00A61P 13/02A61P 17/00A61P 11/02A61P 21/00A61P 17/04A61P 19/10A61P 19/04A61P 13/10A61P 15/06A61P 19/00A61P 1/04A61P 11/06A61P 1/08A61P 1/06A61P 1/00A61P 13/08A61P 17/06C07D 403/14C07D 413/04C07D 413/14C07D 409/14C07D 403/04C07D 401/14C07D 417/14
61
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Claims

Abstract

Novel 2-(azetidin-2-on-1-yl) alkanedioic acid derivativies and 2-(azetidin-2-on-1-yl) alkoxyalkanoic acid derivativies are described for use in the treatment of disease states responsive to antagonism of the vasopressin V 1a receptor.

Claims

exact text as granted — not AI-modified
1 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts, hydrates, and solvates thereof.  
     
     
         2 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       wherein X′ is optionally substituted aryl(C 1 -C 4  alkyl); and pharmaceutically acceptable salts, hydrates, and solvates thereof.  
     
     
         3 . The compound of  claim 2  wherein X′ is 3-fluoro-5-trifluoromethylbenzyl.  
     
     
         4 . The compound of  claim 2  wherein X′ is 4-chloro-3-trifluoromethylbenzyl.  
     
     
         5 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       wherein R 5  is H or C 1 -C 6  alkyl; and X is optionally substituted aryl(C 1 -C 4  alkyl); and pharmaceutically acceptable salts, hydrates, and solvates thereof.  
     
     
         6 . The compound of  claim 5  wherein R 5  is H; and X is (R)-α-methylbenzyl.  
     
     
         7 . The compound of  claim 5  wherein R 5  is CH 3 ; and X is 3-trifluoromethylbenzyl.  
     
     
         8 . A compound of the formula  
       
         
           
           
               
               
           
         
       
       wherein X is 1,2,3,4-tetrahydronaphth-1-yl or optionally substituted aryl(C 3 -C 7  cycloalkyl); and pharmaceutically acceptable salts, hydrates, and solvates thereof.  
     
     
         9 . The compound of  claim 8  wherein X is (R)-1,2,3,4-tetrahydronaphth-1-yl.  
     
     
         10 . The compound of  claim 8  wherein X is 1-phenylcyclopent-1-yl.

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