(1-azinone)-substituted pyridoindoles

Abstract

Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R 1 is H or optionally substituted alkyl; R 2 , R 3 , R 4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF 3 , and —CN; G is —CR 12 R 13 —NR 5 — or —NR 5 —CR 12 R 13 ; R 5 is H, optionally substituted alkyl, optionally substituted heterocycle, —C(═O)—R 6 , —C(═O)—O—R 7 , or —C(═O)—NR 19 R 20 ; R 6 and R 7 are each optionally substituted alkyl or optionally substituted heterocycle; R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 19 and R 20 are each independently selected from H or optionally substituted alkyl; R 14 and R 15 are each independently H or halogen; L is —CH 2 —O—, —CH 2 CH 2 —, —CH═CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

1 . A compound of formula I: 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is H or optionally substituted alkyl; 
         R 2 , R 3 , R 4  are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF 3 , and —CN; 
         G is —CR 12 R 13 —NR 5 — or —NR 5 —CR 12 R 13 ; 
         R 5  is H, optionally substituted alkyl, optionally substituted heterocycle, —C(═O)—R 6 , —C(═O)—O—R 7 , or —C(═O)—NR 19 R 20 ; 
         R 6  and R 7  are each optionally substituted alkyl or optionally substituted heterocycle; 
         R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 19  and R 20  are each independently selected from H or optionally substituted alkyl; 
         R 14  and R 15  are each independently H or halogen; 
         Y is N; 
         L is —CH 2 —O—, —CH 2 CH 2 —, —CH═CH— or a bond; and 
         B is aryl or heteroaryl or cycloalkyl;
 with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine. 
 
       
     
     
         2 . A method of treating a disease or condition which is susceptible to treatment with an MCH 1  receptor modulator, comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to  claim 1 .