US2011144197A1PendingUtilityA1

Alcanoic acid amides substituted by saturated o-heterocycles

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Assignee: HEROLD PETERPriority: Sep 17, 2005Filed: Feb 18, 2011Published: Jun 16, 2011
Est. expirySep 17, 2025(expired)· nominal 20-yr term from priority
A61P 9/04A61P 9/12A61P 9/00A61P 9/10A61P 27/06A61P 13/12A61K 31/335
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Claims

Abstract

Compounds of the general formula (formula I) in which the meanings of the substituents R 1 and R 6 are as indicated in claim 1 , have renin-inhibiting properties and can be used as medicines.

Claims

exact text as granted — not AI-modified
1 - 8 . (canceled) 
     
     
         9 . A compound of the formula 
       
         
           
           
               
               
           
         
         or a pharmaceutically useful salt thereof; in which 
         R 1  is an optionally substituted tetrahydrofuranyl, optionally substituted tetrahydrofuranylmethyl, optionally substituted tetrahydropyranyl or optionally substituted tetrahydropyranylmethyl; 
         R 2  and R 3  are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl; 
         R 4  and R 5  are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl; 
         R 6  is a group —CH 2 —R 7 , —CH 2 —CO—R 7 , —CH 2 —CH 2 —R 7 , —CH 2 —NR 8 —CO—R 7 , —CH 2 —CO—NR 8 —CH 2 —R 7 , —CH 2 —CH 2 —NR 8 —R 7 , —CH 2 —CO—NR 8 —R 7  or —CO—NR 8 —CH 2 —R 7 ; 
         R 7  is an optionally substituted cyclic radical; and 
         R 8  is hydrogen, C 1-6 alkyl or C 1-6 alkanoyl. 
       
     
     
         10 . A compound of the formula 
       
         
           
           
               
               
           
         
         or a salt thereof, especially a pharmaceutically useful salt thereof; in which 
         R 1  is an optionally substituted tetrahydrofuranyl, optionally substituted tetrahydrofuranylmethyl, optionally substituted tetrahydropyranyl or optionally substituted tetrahydropyranylmethyl; 
         R 2  and R 3  are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl; 
         R 4  and R 5  are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl; 
         R 6  is a group —CH 2 —R 7 , —CH 2 —CO—R 7 , —CH 2 —CH 2 —R 7 , —CH 2 —NR 8 —CO—R 7 , —CH 2 —CO—NR 8 —CH 2 —R 7 , —CH 2 —CH 2 —NR 8 —R 7 , —CH 2 —CO—NR 8 —R 7  or —CO—NR 8 —CH 2 —R 7 ; 
         R 7  is an optionally substituted cyclic radical; and 
         R 8  is hydrogen, C 1-6 alkyl or C 1-6 alkanoyl. 
       
     
     
         11 . A compound according to  claim 10  of the formula 
       
         
           
           
               
               
           
         
         or a salt thereof; in which 
         R 1 , R 4 , R 5  and R 6  have the meaning as indicated for the compound of the formula (I) according to  claim 10 . 
       
     
     
         12 . A pharmaceutically useful salt of a compound according to  claim 11 . 
     
     
         13 . A method for the prevention, for delaying the progression or for the treatment of high blood pressure, heart failure, glaucoma, myocardial infarction, renal failure or restenoses, which comprises administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically useful salt thereof according to  claim 9 , to a patient in need thereof. 
     
     
         14 . A pharmaceutical composition, comprising a compound of the formula (I) or a pharmaceutically useful salt thereof, according to  claim 9 , and a pharmaceutically inert excipient. 
     
     
         15 . A pharmaceutical combination in the form of a product or of a kit comprising individual components a) of a compound of the formula (I) or a pharmaceutically useful salt thereof, according to  claim 9 , and b) of at least one pharmaceutical form whose active ingredient has a cardiovascular effect. 
     
     
         16 . A compound according to  claim 10 , of the formula 
       
         
           
           
               
               
           
         
         or a pharmaceutically useful salt thereof.

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