US2018155363A1PendingUtilityA1

Compounds for the treatment of ischemia-reperfusion-related diseases

Assignee: MINERVA PATENTS S APriority: Mar 21, 2012Filed: Dec 12, 2017Published: Jun 7, 2018
Est. expiryMar 21, 2032(~5.7 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 41/00A61P 9/00A61P 9/10A61P 25/00G01N 33/5005C07D 498/08A61K 31/553Y10S435/886
35
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Claims

Abstract

The present invention relates to compounds of formula (I) useful in the treatment of ischemia-reperfusion-related pathologies.

Claims

exact text as granted — not AI-modified
1 - 15 . (canceled) 
     
     
         16 . A compound of formula (I) 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is selected from the group consisting of H, Me, ═CH 2 , CH 2 Ph, CH 2 OH and CH 2 OBn; 
         R 2  is selected from the group consisting of Ph, CH 2 Ph and CHPh 2 ; 
         R 3  is COOH; 
         wherein said phenyl can be substituted by one or more group selected from the group consisting of halogen, CN, NO 2 , NH 2 , OH, COOH, CO and C 1-6 alkyl; 
         or a pharmaceutically acceptable salt thereof; 
         excluding the compound (1R,5S,7R)-3-Benzyl-2-oxo-6,8-dioxa-3-azabicyclo[3.2.1]octan-7-carboxylic acid. 
       
     
     
         17 . The compound according to  claim 16 , of formula (Ia) 
       
         
           
           
               
               
           
         
         wherein 
       
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   R 1   
                   R 2   
                   R 3   
                 
                     
                     
                 
                     
                   H 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   H 
                   CH(Ph) 2   
                   (R)—CO 2 H 
                 
                     
                   H 
                   CH(Ph) 2   
                   (S)—CO 2 H 
                 
                     
                   H 
                   Ph 
                   (R)—CO 2 H 
                 
                     
                   H 
                   Ph 
                   (S)—CO 2 H 
                 
                     
                   (S)—Me 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—Me 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—Me 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (R)—Me 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 Ph 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 Ph 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 Ph 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (S)—CH 2 Ph 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 OBn 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 OBn 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 OBn 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (R)—CH 2 OBn 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (S)—CH 2 OH 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 OH 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 OH 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (R)—CH 2 OH 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   ═CH 2   
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   ═CH 2   
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         18 . The compound according to  claim 16 , of formula (Ib) 
       
         
           
           
               
               
           
         
         wherein 
       
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   R 1   
                   R 2   
                   R 3   
                 
                     
                     
                 
                     
                   H 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   H 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   H 
                   CH(Ph) 2   
                   (R)—CO 2 H 
                 
                     
                   H 
                   CH(Ph) 2   
                   (S)—CO 2 H 
                 
                     
                   H 
                   Ph 
                   (R)—CO 2 H 
                 
                     
                   H 
                   Ph 
                   (S)—CO 2 H 
                 
                     
                   (S)—Me 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—Me 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—Me 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (R)—Me 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 Ph 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 Ph 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 Ph 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (S)—CH 2 Ph 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 OBn 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 OBn 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 OBn 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (R)—CH 2 OBn 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (S)—CH 2 OH 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (S)—CH 2 OH 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   (R)—CH 2 OH 
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   (R)—CH 2 OH 
                   PhCH 2   
                   (S)—CO 2 H 
                 
                     
                   ═CH 2   
                   PhCH 2   
                   (R)—CO 2 H 
                 
                     
                   ═CH 2   
                   PhCH 2   
                   (S)—CO 2 H

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