US2012238579A1PendingUtilityA1

New Compounds 806

42
Assignee: BESIDKI YEVGENIPriority: Apr 23, 2007Filed: Mar 23, 2012Published: Sep 20, 2012
Est. expiryApr 23, 2027(~0.8 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 29/00A61P 25/04A61P 25/00A61P 25/06A61P 25/08A61P 17/04C07D 405/14C07D 405/04C07D 261/08A61K 31/415
42
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Claims

Abstract

The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.

Claims

exact text as granted — not AI-modified
1 - 15 . (canceled) 
     
     
         16 . A compound of formula I, 
       
         
           
           
               
               
           
         
         wherein: 
         X is O; 
         R 1  is pyrimidinyl or pyrazinyl, wherein R 1  may have 1, 2 or 3 R 11  substituents;
 wherein R 11  at each occurrence is independently selected from the group consisting of C 1-6 alkyl and C 1-6 alkoxy, and 
 
         R 2  is pyridinyl, which may have 1, 2 or 3 R 14  substituents;
 wherein R 14  at each occurrence is independently selected from the group consisting of C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 haloalkoxy, C 1-6 haloalkoxyC 1-6 alkoxy and C 1-6 haloalkoxyC 1-6 alkyl; 
 
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         17 . A compound according to  claim 16 , wherein:
 X is O;   R 1  is pyrazinyl, which may be mono-substituted with R 11  wherein R 11  is C 1-6 alkoxy, and   R 2  is pyridinyl, which may be mono-substituted with R 14  wherein R 14  is selected from C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 haloalkoxy, C 1-6 haloalkoxyC 1-6 alkoxy and C 1-6 haloalkoxyC 1-6 alkyl;   or a pharmaceutically acceptable salt thereof.   
     
     
         18 . A compound according to  claim 16 , wherein R 1  is pyrazine-2-yl,
 or a pharmaceutically acceptable salt thereof.   
     
     
         19 . A compound according to  claim 16 , wherein R 1  is mono-substituted with methyl or methoxy, or a pharmaceutically acceptable salt thereof. 
     
     
         20 . A compound according to  claim 19 , wherein R 1  is mono-substituted with methoxy, 
       or a pharmaceutically acceptable salt thereof. 
     
     
         21 . A compound according to  claim 16 , wherein R 2  is pyridine-4-yl or pyridine-3-yl,
 or a pharmaceutically acceptable salt thereof.   
     
     
         22 . A compound according to  claim 16 , wherein:
 R 2  is mono-substituted with R 14 , wherein R 14  is independently selected from the group consisting of trifluoropropoxy, trifluoromethoxyethoxy, trifluoroethoxyethoxy, trifluoromethoxymethyl, trifluoromethoxyethyl, trifluoroethoxymethyl and trifluoroethoxyethyl,   or a pharmaceutically acceptable salt thereof.   
     
     
         23 . A compound according to  claim 22 , wherein R 2  is mono-substituted with trifluoroethoxymethyl, or a pharmaceutically acceptable salt thereof. 
     
     
         24 . A compound according to  claim 16 , wherein:
 X is O;   R 1  is pyrazine-2-yl, mono-substituted with methoxy;   R 2  is pyridine-3-yl, mono-substituted with trifluoroethoxymethyl,   or a pharmaceutically acceptable salt thereof.   
     
     
         25 . A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to  claim 16  or a pharmaceutically acceptable salt thereof, in association with one or more pharmaceutically acceptable diluents, excipients or inert carriers. 
     
     
         26 . A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to  claim 24  or a pharmaceutically acceptable salt thereof, in association with one or more pharmaceutically acceptable diluents, excipients or inert carriers.

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