Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof

Abstract

The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R 1 to R 15 , A, B, L, i as well as X 1 -X 4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.

1 . A compound of formula (I): 
       
         
           
           
               
               
           
         
       
       wherein:
 A is aryl or heteroaryl, optionally substituted by one or more fluorine atoms; 
 L are each independently hydrogen, fluorine, chlorine, bromine, iodine, hydroxy, carboxy, formyl, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 1-6 -alkyl-S, C 1-6 -alkyl-S—C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, C 3-7 -cycloalkyl-C 2-6 -alkenyl, C 3-7 -cycloalkyl-C 2-6 -alkynyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, aryl, aryl-C 1-6 -alkyl, aryl-C 2-6 -alkenyl, aryl-C 2-6 -alkynyl, heterocyclyl, heterocyclyl-C 1-6 -alkyl, heterocyclyl-C 2-6 -alkenyl, heterocyclyl-C 2-6 -alkynyl, heteroaryl, heteroaryl-C 1-6 -alkyl, heteroaryl-C 2-6 -alkenyl, heteroaryl-C 2-6 -alkynyl, R 15 —O, R 15 —O—C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—CO, R 14 —CO—(R 14 )N, (R 14 ) 2 N—CO—(R 14 )N, R 14 —SO 2 —(R 14 )N, (R 14 ) 2 N—SO 2  or R 14 —SO 2 , wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F 3 C, HF 2 C, FH 2 C, hydroxy-C 1-6 -alkyl, C 1-3 -alkyl, C 1-6 -alkoxy, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO and HOSO 2 —; 
 i is 0, 1, 2 or 3; 
 B is a C 1-4 -alkylene bridge, optionally substituted by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-4 -alkyl, C 1-6 -alkyl-S—C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl, R 15 —O, (R 14 ) 2 N—SO 2 , (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, R 14 —SO 2 , R 14 —CO—(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N—SO 2 , R 14 —CO— and R 14 —SO—, wherein
 two C 1-4 -alkyl groups bound to the same carbon atom of the C 1-4 -alkylene bridge may be joined together to form a C 3-7 -cycloalkyl group, and 
 each of the above-mentioned groups and the C 3-7 -cycloalkyl group formed from the C 1-4 -alkyl groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl, C 1-3 -alkoxy, R 15 —O—C 1-3 -alkyl, R 14 —CO(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, (R 14 ) 2 N—SO 2 — and HOSO 2 —, and 
 wherein when B is a C 3-4 -alkylene bridge, the CH 2  group of the C 3-4 -alkylene bridge, which is bound to the group A, is optionally replaced by —O—; 
 
 R 1  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, C 3-7 -cycloalkyl-C 2-6 -alkenyl, C 3-7 -cycloalkyl-C 2-6 -alkynyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, aryl, aryl-C 1-6 -alkyl, aryl-C 2-6 -alkenyl, aryl-C 2-6 -alkynyl, heterocyclyl, heterocyclyl-C 1-6 -alkyl, heterocyclyl-C 2-6 -alkenyl, heterocyclyl-C 2-6 -alkynyl, heteroaryl, heteroaryl-C 1-6 -alkyl, heteroaryl-C 2-6 -alkenyl or heteroaryl-C 2-6 -alkynyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl, C 1-3 -alkoxy, hydroxy-C 1-6 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO—(R 14 ) 2 N—SO 2 , R 14 —CO—(R 14 )N, R 14 —SO 2 —(R 14 )N and HOSO 2 —; 
 
 X 1 , is nitrogen or C(R 10 ); 
 X 2 , X 3 , X 4  are each independently nitrogen or C(R 11 ),
 with the proviso that 0, 1, 2 or 3 of the groups X 1 , X 2 , X 3  and X 4  are nitrogen; 
 
 R 2  is C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, R 15 —O—C 1-3 -alkyl, C 1-6 -alkyl-S—C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 2-6 -alkynyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, heterocyclyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl-C 1-3 -alkyl, C 3-7 -cycloalkyl-C 2-3 -alkenyl, heterocyclyl-C 2-3 -alkenyl, heterocyclyl-C 2-3 -alkynyl, aryl, heteroaryl, aryl-C 1-3 -alkyl, heteroaryl-C 1-3 -alkyl, aryl-C 2-3 -alkenyl, aryl-C 2-3 -alkynyl, heteroaryl-C 2-3 -alkenyl or heteroaryl-C 2-3 -alkynyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, F 3 C, HF 2 C, FH 2 C, hydroxy, oxo, carboxy, formyl, cyano, nitro, (R 14 ) 2 N, HOSO 2 —, C 1-3 -alkyl, C 1-6 -alkyl-S—C 1-3 -alkyl, (R 14 ) 2 N—SO 2 —, R 14 —CO—(R 14 )N, R 14 —SO 2 —(R 14 )N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, R 5 —O and R 15 —O—C 1-3 -alkyl; 
 
 R 3 , R 4  are each independently hydrogen, C 1-6 -alkyl, fluorine, F 3 C, HF 2 C or FH 2 C; 
 R 5 , R 7  are each independently hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, heterocyclyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, C 3-7 -cycloalkyl-C 2-6 -alkynyl, heterocyclyl-C 1-3 -alkyl, C 3-7 -cycloalkyl-C 2-4 -alkenyl, heterocyclyl-C 2-4 -alkenyl, heterocyclyl-C 2-4 -alkynyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, aryl, heteroaryl, aryl-C 1-3 -alkyl, heteroaryl-C 1-3 -alkyl, aryl-C 2-3 -alkenyl, heteroaryl-C 2-3 -alkenyl, aryl-C 2-3 -alkynyl or heteroaryl-C 2-3 -alkynyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-3 -alkyl, R 15 —O, C 1-3 -alkyl-S, aryl, heteroaryl, heteroaryl-C 1-3 -alkyl, aryl-C 1-6 -alkyl, R 14 —CO—(R 14 )N, R 14 —SO 2 —(R 14 )N, (R 14 ) 2 N—SO 2 —, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO and HOSO 2 —; 
 
 R 6 , R 9  are each independently hydrogen, C 1-6 -alkyl, C 1-6 -alkoxy-C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, C 2-6 -alkenyl, heterocyclyl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl or C 2-6 -alkynyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, cyano, C 1-3 -alkyl, C 1-6 -alkoxy- and (R 14 ) 2 N; 
 
 R 8  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, C 3-7 -cycloalkyl-C 2-4 -alkenyl, C 3-7 -cycloalkyl-C 2-4 -alkynyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, heterocyclyl-C 2-4 -alkenyl, heterocyclyl-C 2-4 -alkynyl, aryl, aryl-C 1-3 -alkyl, aryl-C 2-4 -alkenyl, aryl-C 2-4 -alkynyl, heteroaryl, heteroaryl-C 1-3 -alkyl, heteroaryl-C 2-4 -alkenyl or heteroaryl-C 2-4 -alkynyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, R 15 —O, R 15 —O—C 1-3 -alkyl, R 15 —S, R 15 —S—C 1-3 -alkyl, aryl, heteroaryl, heteroaryl-C 1-3 -alkyl, aryl-C 1-6 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, (R 14 ) 2 N—CO—N(R 14 )—, (R 14 ) 2 N—SO 2 — and HOSO 2 —; 
 
 R 10  is hydrogen, fluorine, chlorine, bromine, iodine, cyano, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, C 3-7 -cycloalkyl-C 2-6 -alkynyl, heterocyclyl, heterocyclyl-C 1-6 -alkyl, heterocyclyl-C 2-6 -alkenyl, heterocyclyl-C 2-6 -alkynyl, C 3-7 -cycloalkyl-C 2-6 -alkenyl, heterocyclyl-C 2-4 -alkenyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, aryl, aryl-C 1-6 -alkyl, heteroaryl, heteroaryl-C 1-6 -alkyl, aryl-C 2-6 -alkenyl, heteroaryl-C 2-6 -alkenyl, aryl-C 2-6 -alkynyl or heteroaryl-C 2-6 -alkynyl, R 15 —O, R 15 —O—C 1-3 -alkyl, R 12 —SO 2 —(R 13 )N or R 12 —CO—(R 13 )N
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 1-6 -alkyl-S, C 1-6 -alkyl-S—C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, aryl, aryl-C 1-6 -alkyl, heterocyclyl, heterocyclyl-C 1-6 -alkyl, heteroaryl, heteroaryl-C 1-6 -alkyl, R 15 —O, R 15 —O—CO, R 15 —CO, R 15 —O—CO— 
 
 (R 14 )N, (R 14 ) 2 N—CO—O, R 15 —O—C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—CO, R 14 —CO—(R 14 )N, (R 14 ) 2 N—CO—(R 14 )N, (R 14 ) 2 N—SO 2 —, (R 14 ) 2 N—SO 2 —(R 14 )N, R 14 —SO 2 —, F 3 C, HF 2 C, FH 2 C, F 3 C—O, HF 2 C—O, FH 2 C—O and R 14 —SO 2 —(R 14 )N; 
 R 11  are each independently hydrogen, fluorine, chlorine, bromine, iodine, R 15 —O, (R 14 ) 2 N or C 1-3 -alkyl,
 wherein the C 1-3 -alkyl group is optionally substituted by one or more fluorine atoms; 
 
 R 12  is C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl-C 2-6 -alkenyl, aryl-C 2-3 -alkenyl, heteroaryl-C 2-4 -alkenyl, heterocyclyl-C 2-4 -alkenyl, aryl-C 2-3 -alkynyl, C 3-7 -cycloalkyl-C 2-4 -alkynyl, heterocyclyl-C 2-4 -alkynyl-heteroaryl-C 2-3 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, heterocyclyl, heterocyclyl-C 1-4 -alkyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl-C 2-6 -alkenyl, C 3-7 -cycloalkenyl-C 2-6 -alkynyl, aryl, aryl-C 1-4 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl or (R 14 ) 2 N,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, R 15 —O, R 15 —O—C 1-3 -alkyl, R 14 —CO(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N—SO 2 —, R 14 —SO 2 —, R 14 —SO, R 14 —S, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl and (R 14 ) 2 N—CO; 
 
 R 13  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, heterocyclyl-C 2-3 -alkenyl, heterocyclyl-C 2-3 -alkynyl, heteroaryl, heteroaryl-C 2-3 -alkenyl, heteroaryl-C 2-3 -alkynyl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, R 15 —O, R 15 —O—C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl and R 14 CO; 
 
 or 
 R 12  and R 13  together form a C 2-6 -alkylene bridge, so that with the inclusion of the nitrogen atom linked to R 13  and the SO 2 — or CO group linked to R 12 , a heterocyclic ring is formed,
 wherein one or two CH 2  groups of the C 2-6 -alkylene bridge are optionally replaced independently of one another by O, S, SO, SO 2  or N(R 14 ) in such a way that in each case two O or S atoms or an 0 and an S atom are not joined together directly, and 
 the C atoms of the above-mentioned C 2-6 -alkylene bridge are optionally substituted by one or more groups selected from fluorine, chlorine, bromine, hydroxy, carboxy, formyl, cyano, F 3 C, HF 2 C, FH 2 C, C 1-6 -alkyl, C 1-6 -alkoxy, oxo and nitro; 
 
 R 14  are each independently hydrogen, C 1-6 -alkyl, C 1-6 -alkoxy-C 1-3 -alkyl, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-C 1-3 -alkyl, aryl or aryl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl, wherein two C 1-6 -alkyl groups bound to the same nitrogen atom together may form a C 2-6 -alkylene bridge, so that with the inclusion of the nitrogen atom bound to the groups R 14  a heterocyclic ring is formed,
 wherein a CH 2  group of the C 2-6 -alkylene bridge may be replaced by O, S or N(R 14 ), and 
 the above-mentioned groups and the heterocyclic ring are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-3 -alkyl, hydroxy-C 1-3 -alkyl, C 1-3 -alkoxy, (R 15 ) 2 N—CO or (R 15 ) 2 N, and 
 
 R 15  are each independently hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 1-3 -alkyl- and C 1-3 -alkoxy; 
 
 
       and tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof. 
     
     
         2 . The compound according to  claim 1 , wherein
 A is phenyl, biphenyl, naphthyl or a 5-, 6-, 7-, 8-, 9- or 10-membered aromatic mono- or bicyclic heteroaryl group which contains 1-4 heteroatoms selected from the group consisting of N, O and S.   
     
     
         3 . The compound according to  claim 1 , wherein the group 
       
         
           
           
               
               
           
         
       
       is selected from the group consisting of: 
       
         
           
           
               
               
           
         
       
     
     
         4 . The compound according to  claim 1 , wherein
 A is phenyl, thienyl, thiazolyl or pyridyl.   
     
     
         5 . The compound according to  claim 1 , wherein
 L are each independently hydrogen, fluorine, chlorine, bromine, iodine, hydroxy, carboxy, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl, R 15 —O, R 15 —O—C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—CO, R 14 —CO—(R 14 )N, (R 14 ) 2 N—CO—(R 14 )N, (R 14 ) 2 N—SO 2 —, R 14 —SO 2 —(R 14 )N or C 1-3 -alkyl-SO 2 —,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, hydroxy, oxo, carboxy, cyano, nitro, F 3 C, HF 2 C, FH 2 C, hydroxy-C 1-3 -alkyl, C 1-3 -alkyl, C 1-3 -alkoxy, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl and (R 14 ) 2 N—CO; and 
   i is 0, 1 or 2.   
     
     
         6 . The compound according to  claim 1 , wherein
 L are each independently hydrogen, fluorine, chlorine, bromine, iodine, cyano, hydroxy, C 1-6 -alkyl, C 1-6 -alkoxy, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, phenyl, (R 14 ) 2 N, (R 14 ) 2 N—CO, R 14 —CO—(R 14 )N, (R 14 ) 2 N—CO—(R 14 )N, R 14 —SO 2 —(R 14 )N or (R 14 ) 2 N—SO 2 —,
 wherein the above-mentioned groups are optionally substituted by one or more fluorine atoms, and 
   i is 0, 1 or 2.   
     
     
         7 . The compound according to  claim 1 , wherein
 L are each independently hydrogen, fluorine, chlorine, bromine, hydroxy, C 1-4 -alkyl or C 1-4 -alkoxy,
 wherein the above-mentioned groups are optionally substituted by one or more fluorine atoms, and 
   i is 0, 1 or 2.   
     
     
         8 . The compound according to  claim 1 , wherein
 B is a C 1-4 -alkylene bridge,
 wherein the C 1-4 -alkylene bridge is optionally substituted by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-4 -alkyl, C 1-6 -alkyl-S—C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl, R 15 —O, (R 14 ) 2 N—SO 2 —, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, R 14 —SO 2 —, R 14 —CO—(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N—SO 2 —, R 14 —CO and R 14 —SO, and 
 wherein two C 1-4 -alkyl groups bound to the same carbon atom of the C 1-4 -alkylene bridge are optionally joined together forming a C 3-7 -cycloalkyl group, and 
 wherein the above-mentioned groups and the C 3-7 -cycloalkyl group formed from the C 1-4 -alkyl groups are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl, C 1-3 -alkoxy, R 15 —O—C 1-3 -alkyl, R 14 —CO(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, (R 14 ) 2 N—SO 2 — and HOSO 2 —. 
   
     
     
         9 . The compound according to  claim 1 , wherein
 B is a C 1-4 -alkylene bridge,
 wherein the C 1-4 -alkylene bridge is optionally substituted independently of one another by one or more groups selected from among fluorine, hydroxy, carboxy, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-4 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl, R 15 —O, (R 14 ) 2 N—SO 2 — and (R 14 ) 2 N, and 
 wherein two C 1-4 -alkyl groups bound to the same carbon atom of the C 1-4 -alkylene bridge are optionally joined together forming a C 3-7 -cycloalkyl group, and 
 wherein the above-mentioned groups and the C 3-7 -cycloalkyl group formed from the C 1-4 -alkyl groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, hydroxy, carboxy, cyano, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl, C 1-3 -alkoxy and R 15 —O—C 1-3 -alkyl. 
   
     
     
         10 . The compound according to  claim 1 , wherein
 B is a C 1-4 -alkylene bridge,
 wherein the C 1-4 -alkylene bridge is optionally substituted independently of one another by one or more groups selected from among C 1-4 -alkyl, phenyl or benzyl, and 
 wherein two C 1-4 -alkyl groups bound to the same carbon atom of the C 1-4 -alkylene bridge are optionally joined together forming a C 3-6 -cycloalkyl group, and 
 wherein the above-mentioned groups and the C 3-6 -cycloalkyl group formed from the C 1-4 -alkyl groups are optionally substituted independently of one another by one or more groups selected from fluorine, hydroxy and C 1-3 -alkoxy. 
   
     
     
         11 . The compound according to  claim 1 , wherein
 B is selected from the group consisting of:   
       
         
           
           
               
               
           
         
         wherein one or more hydrogen atoms are optionally replaced by fluorine. 
       
     
     
         12 . The compound according to  claim 1 , wherein
 B is a C 1-2 -alkylene bridge,
 wherein the C 1-2 -alkylene bridge is optionally substituted by one or more C 1-4 -alkyl groups, and 
 wherein two C 1-4 -alkyl groups bound to the same carbon atom of the C 1-2 -alkylene bridge may be joined together forming a cyclopropyl group, and 
 wherein one or more hydrogen atoms of the above-mentioned C 1-2 -alkylene bridge and/or the C 1-4 -alkyl groups and/or the cyclopropyl group formed therefrom are optionally replaced by one or more fluorine atoms. 
   
     
     
         13 . The compound according to  claim 1 , wherein partial formula (II) 
       
         
           
           
               
               
           
         
         is selected from the group consisting of: 
       
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         14 . The compound according to  claim 1 , wherein
 R 1  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, hydroxy, carboxy, cyano, nitro, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl, C 1-3 -alkoxy and hydroxy-C 1-3 -alkyl. 
   
     
     
         15 . The compound according to  claim 1 , wherein
 R 1  is hydrogen, C 1-4 -alkyl, C 3-4 -alkenyl, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from among fluorine, hydroxy and C 1-3 -alkoxy. 
   
     
     
         16 . The compound according to  claim 1 , wherein
 R 2  is C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 1-6 -alkoxy-C 1-3 -alkyl, C 1-6 -alkyl-S—C 1-3 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkenyl-C 1-3 -alkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, F 3 C, HF 2 C, FH 2 C, hydroxy, carboxy, cyano, nitro, C 1-3 -alkyl, (R 14 ) 2 N—SO 2 —, (R 14 ) 2 N, R 14 —CO—(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, R 15 —O and R 15 —O—C 1-3 -alkyl. 
   
     
     
         17 . The compound according to  claim 1 , wherein
 R 2  is C 1-6 -alkyl, C 2-6 -alkynyl, C 3-6 -cycloalkyl-C 1-3 -alkyl, heterocyclyl-C 1-3 -alkyl, phenyl, phenyl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the heteroaryl groups are 5- or 6-membered aromatic heteroaryl groups which contain 1, 2 or 3 heteroatoms selected from N, O and S, and 
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, cyano, hydroxy, C 1-3 -alkyl, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkoxy and (R 14 ) 2 N. 
   
     
     
         18 . The compound according to  claim 1 , wherein
 R 2  is n-propyl, n-butyl, 2-propynyl, 2-butynyl, benzyl, 2-phenylethyl, pyridylmethyl, furanylmethyl, thienylmethyl or thiazolylmethyl,
 wherein the above-mentioned propyl, butyl, propynyl and butynyl groups are optionally substituted by one or more fluorine atoms and the benzyl, and 2-phenylethyl, furanylmethyl, thienylmethyl or thiazolylmethyl are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, methyl, F 3 C, HF 2 C, FH 2 C and H 2 N. 
   
     
     
         19 . The compound according to  claim 1 , wherein
 R 3  is hydrogen, C 1-6 -alkyl, fluorine, F 3 C, HF 2 C or FH 2 C; and   R 4  is hydrogen.   
     
     
         20 . The compound according to  claim 1 , wherein
 R 8  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, carboxy, cyano, nitro, C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO, (R 14 ) 2 N—CO—N(R 14 )—, (R 14 ) 2 N—SO 2 —, R 15 —O, R 15 —O—C 1-3 -alkyl, R 15 —S and R 15 —S—C 1-3 -alkyl. 
   
     
     
         21 . The compound according to  claim 1 , wherein
 R 8  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, phenyl, phenyl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the heteroaryl groups are 5- or 6-membered aromatic heteroaryl groups which contain 1, 2 or 3 heteroatoms selected from the group consisting of N, O and S, and 
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, carboxy, hydroxy, cyano, C 1-3 -alkyl, C 1-3 -alkoxy, C 1-3 -alkoxy-C 1-3 -alkyl, C 1-3 -alkyl-S, C 1-3 -alkyl-S—C 1-3 -alkyl, hydroxy-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO—N(R 14 )— and (R 14 ) 2 N—SO 2 —. 
   
     
     
         22 . The compound according to  claim 1 , wherein
 R 8  is hydrogen, C 1-6 -alkyl, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-C 1-3 -alkyl, phenyl-C 1-3 -alkyl or tetrahydropyranyl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, pyrrolidin-1-ylmethyl, hydroxy, cyano, C 1-3 -alkyl, C 1-3 -alkoxy, C 1-3 -alkyl-S, hydroxy-C 1-3 -alkyl, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl, (R 14 ) 2 N—CO—N(R 14 )— and (R 14 ) 2 N—SO 2 —. 
   
     
     
         23 . The compound according to  claim 1 , wherein
 R 5 , R 7  are each independently hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, heterocyclyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl-C 1-3 -alkyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-3 -alkyl, aryl, heteroaryl, aryl-C 1-3 -alkyl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, carboxy, cyano, nitro, C 1-3 -alkyl, C 1-3 -alkoxy, C 1-3 -alkyl-S, aryl, heteroaryl, heteroaryl-C 1-3 -alkyl, aryl-C 1-3 -alkyl, (R 14 ) 2 N—SO 2 —, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl and (R 14 ) 2 N—CO. 
   
     
     
         24 . The compound according to  claim 1 , wherein
 R 5  is C 1-6 -alkyl, cyclopropyl, C 3-6 -cycloalkyl-C 1-3 -alkyl or phenyl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, cyano, hydroxy, carboxy, C 1-3 -alkyl, C 1-3 -alkoxy and (R 14 ) 2 N, and 
   R 7  is C 1-6 -alkyl, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-C 1-3 -alkyl, phenyl or phenyl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, cyano, hydroxy, carboxy, C 1-3 -alkyl, C 1-3 -alkoxy and (R 14 ) 2 N. 
   
     
     
         25 . The compound according to  claim 1 , wherein
 R 5 , R 7  are each independently C 1-4 -alkyl or cyclopropyl,
 wherein one or more hydrogen atoms of the above-mentioned groups are optionally replaced by fluorine atoms. 
   
     
     
         26 . The compound according to  claim 1 , wherein
 R 6  is hydrogen, and   R 9  is hydrogen or C 1-4 -alkyl,
 wherein one or more hydrogen atoms of the C 1-4 -alkyl group are optionally replaced by fluorine. 
   
     
     
         27 . The compound according to  claim 1 , wherein
 R 10  is hydrogen, fluorine, chlorine, bromine, cyano, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-6 -alkyl, heterocyclyl, heterocyclyl-C 1-6 -alkyl, C 3-7 -cycloalkenyl, aryl, aryl-C 1-6 -alkyl, heteroaryl, heteroaryl-C 1-6 -alkyl, R 15 —O, R 15 —O—C 1-3 -alkyl, R 12 —SO 2 —(R 13 )N or R 12 —CO—(R 13 )N,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C 3-7 -cycloalkyl, heterocyclyl, (R 14 ) 2 N, (R 14 ) 2 N—CO, R 15 —CO, R 15 —O—CO, R 14 —CO—(R 14 )N, (R 14 ) 2 N—CO—(R 14 )N, (R 14 ) 2 N—SO 2 —, (R 14 ) 2 N—SO 2 —(R 14 )N, R 14 —SO 2 —, C 1-4 -alkyl, R 15 —O, C 1-4 -alkyl-S, F 3 C, HF 2 C, FH 2 C, F 3 C—O, HF 2 C—O, FH 2 C—O and R 14 —SO 2 —(R 14 )N; and 
   R 11  each independently denotes hydrogen, fluorine, chlorine, bromine, iodine, methyl or F 3 C.   
     
     
         28 . The compound according to  claim 1 , wherein
 R 10  is hydrogen, fluorine, chlorine, bromine, cyano, C 1-4 -alkyl, C 1-4 -alkoxy, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-oxy, C 3-6 -cycloalkyl-C 1-3 -alkoxy, 1,3-diazacyclohexan-2-on-1-yl, 2-oxo-1,3-oxazinan-3-yl, 3-oxomorpholino, 1,1-dioxo-[1,2,6]thiadiazinan-2-yl, phenyl, pyridyl, thienyl, furyl, R 12 —CO—(R 13 )N or R 12 —SO 2 —(R 13 )N,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, carboxy, cyano, C 1-4 -alkyl, C 1-4 -alkoxy, C 1-4 -alkyl-S, R 15 —CO, R 15 —O—CO, R 14 —SO 2 —, F 3 C, HF 2 C, FH 2 C, F 3 C—O, HF 2 C—O, FH 2 C—O and (R 14 ) 2 N—CO; and 
   R 11  are each independently hydrogen, fluorine, chlorine, or bromine.   
     
     
         29 . The compound according to  claim 1 , wherein
 R 10  is R 12 —CO—(R 13 )N, R 12 —SO 2 —(R 13 )N, cyanophenyl or cyanothienyl,
 wherein the above-mentioned cyanophenyl and cyanothienyl groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, C 1-4 -alkyl, C 1-4 -alkoxy, F 3 C, HF 2 C, FH 2 C, F 3 C—O, HF 2 C—O and FH 2 C—O; and 
   R 11  are each independently hydrogen, fluorine, chlorine, or bromine.   
     
     
         30 . The compound according to  claim 1 , wherein
 R 12  is C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, C 3-7 -cycloalkenyl, C 3-7 -cycloalkenyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl or (R 14 ) 2 N,
 wherein the above-mentioned groups are optionally substituted by one or more groups selected from fluorine, chlorine, bromine, hydroxy, carboxy, cyano, nitro, C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, C 1-3 -alkoxy, hydroxy-C 1-3 -alkyl, R 14 —CO(R 14 )N, R 14 —SO 2 (R 14 )N, (R 14 ) 2 N—SO 2 —, R 14 —SO 2 —R 14 —SO, R 14 —S, (R 14 ) 2 N, (R 14 ) 2 N—C 1-3 -alkyl and (R 14 ) 2 N—CO; and 
   R 13  is hydrogen, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-3 -alkyl, aryl, aryl-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, hydroxy, cyano, C 1-3 -alkyl, C 1-3 -alkoxy, hydroxy-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, (R 14 ) 2 N— and (R 14 ) 2 N—C 1-3 -alkyl, 
   or   R 12  and R 13  together form a C 2-6 -alkylene bridge, so that with the inclusion of the nitrogen atom attached to R 13  and the SO 2  or CO group attached to R 12  a heterocyclic ring is formed,
 wherein one or two CH 2  groups of the C 2-6 -alkylene bridge are optionally replaced independently of one another by O, S, SO, SO 2  or N(R 14 ) in such a way that in each case two O or S atoms or one O atom and an S atom are not directly joined together, and 
 wherein the C atoms of the above-mentioned C 2-6 -alkylene bridge are optionally substituted independently of one another by one or more groups selected from among fluorine, hydroxy, carboxy, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl and C 1-3 -alkoxy. 
   
     
     
         31 . The compound according to  claim 1 , wherein
 R 12  is C 1-6 -alkyl, heterocyclyl, phenyl, phenyl-C 1-3 -alkyl, heteroaryl, heteroaryl-C 1-3 -alkyl or (R 14 ) 2 N,
 wherein the heteroaryl groups are 5- or 6-membered aromatic heteroaryl groups which contain 1 or 2 heteroatoms selected from the group consisting of N, O and S, wherein a maximum of one O or S atom may be present, and 
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine, bromine, hydroxy, cyano, C 1-3 -alkyl, C 1-3 -alkoxy, heterocyclyl, heterocyclyl-C 1-3 -alkyl, hydroxy-C 1-3 -alkyl, (R 14 ) 2 N and (R 14 ) 2 N—C 1-3 -alkyl; and 
   R 13  is hydrogen, C 1-6 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, C 3-6 -cycloalkyl, C 3-6 -cycloalkyl-C 1-3 -alkyl, phenyl, phenyl-C 1-3 -alkyl, heteroaryl or heteroaryl-C 1-3 -alkyl,
 wherein the heteroaryl groups are 5- or 6-membered aromatic heteroaryl groups which contain 1 or 2 heteroatoms selected from the group consisting of N, O and S, wherein a maximum of one O or S atom may be present, and 
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from a fluorine, chlorine, bromine, hydroxy, cyano, C 1-3 -alkyl, C 1-3 -alkoxy, hydroxy-C 1-3 -alkyl, heterocyclyl, heterocyclyl-C 1-3 -alkyl, (R 14 ) 2 N— and (R 14 ) 2 N—C 1-3 -alkyl; 
   or   R 12  and R 13  together form a C 2-6 -alkylene bridge, so that with the inclusion of the nitrogen atom attached to R 13  and the SO 2  or CO group attached to R 12  a heterocyclic ring is formed,
 wherein one or two CH 2  groups of the C 2-6 -alkylene bridge may be replaced independently of one another by O, S, SO, SO 2  or N(R 14 ) in such a way that in each case two O or S atoms or an O atom and an S atom are not directly joined together, and 
 wherein the C atoms of the above-mentioned C 2-6 -alkylene bridge are optionally substituted independently of one another by one or more groups selected from among fluorine, hydroxy, carboxy, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl and C 1-3 -alkoxy. 
   
     
     
         32 . The compound according to  claim 1 , wherein
 R 12  is C 1-4 -alkyl, morpholinyl, phenyl, benzyl, pyridyl or (CH 3 ) 2 N,
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine and bromine; 
   R 13  is hydrogen, methyl, ethyl, phenyl or 4-fluorophenyl
 wherein the above-mentioned groups are optionally substituted independently of one another by one or more groups selected from fluorine, chlorine and bromine; 
   or   R 12  and R 13  with the inclusion of the nitrogen atom attached to R 13  and the SO 2  or CO group attached to R 12  together form a heterocyclic ring of formulae (IIa), (IIb), (IIc) or (IId)   
       
         
           
           
               
               
           
         
       
     
     
         33 . The compound according to  claim 1 , wherein
 R 12  and R 13  together form a C 2-6 -alkylene bridge, so that with the inclusion of the nitrogen atom attached to R 13  and the SO 2  or CO group attached to R 12  a heterocyclic ring is formed,
 wherein one or two CH 2  groups of the C 2-6 -alkylene bridge are optionally replaced independently of one another by O, S, SO, SO 2  or N(R 14 ) in such a way that in each case two O or S atoms or an O atom and an S atom are not directly joined together, and 
 wherein the C atoms of the above-mentioned C 2-6 -alkylene bridge are optionally substituted independently of one another by one or more groups selected from fluorine, hydroxy, carboxy, F 3 C, HF 2 C, FH 2 C, C 1-3 -alkyl and C 1-3 -alkoxy. 
   
     
     
         34 . The compound according to  claim 1 , wherein
 R 12  and R 13  with the inclusion of the nitrogen atom attached to R 13  and the SO 2  or CO group attached to R 12  together form a heterocyclic ring of formulae (IIa), (IIb), (IIc) or (IId)   
       
         
           
           
               
               
           
         
       
     
     
         35 . The compound according to  claim 1 , wherein
 R 14  is hydrogen or C 1-6 -alkyl,
 wherein one or more hydrogen atoms of the C 1-6 -alkyl group are optionally replaced by fluorine. 
   
     
     
         36 . The compound according to  claim 1 , wherein
 R 15  is hydrogen or C 1-3 -alkyl.   
     
     
         37 . The compound according to  claim 1 , wherein compound is of formula (Ia), (Ib), (Ic), (Id) or (Ie): 
       
         
           
           
               
               
           
         
       
       wherein
 A, B, L, x 2 , x 3 , x 4 , i, R 1 , R 2 , R 3 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14  and R 15  are as defined in  claim 1 . 
 
     
     
         38 . A physiologically acceptable salt of the compound according to  claim 1 . 
     
     
         39 . A pharmaceutical composition comprising a compound according to  claim 1  and one or more inert carriers and/or diluents. 
     
     
         40 . The pharmaceutical composition according to  claim 39 , further comprising one or more medicinally effective active substances selected from beta-secretase inhibitors, gamma-secretase inhibitors, amyloid aggregation inhibitors, directly or indirectly acting neuroprotective substances, anti-oxidants, Cox inhibitors, NSAIDs additionally or exclusively having Aβ lowering properties, HMG-CoA reductase inhibitors, acetylcholinesterase inhibitors, NMDA receptor antagonists, AMPA agonists, substances modulating the concentration or release of neurotransmitters, substances inducing the secretion of growth hormone, CB-1 receptor antagonists or inverse agonists, antibiotics, PDE-IV inhibitors, PDE-IX inhibitors, GABA A  inverse agonists, nicotinic agonists, histamine H3 antagonists, 5 HAT-4 agonists or partial agonists, 5HT-6 antagonists, a2-adrenoreceptor antagonists, muscarinic M1 agonists, muscarinic M2 antagonists and metabotropic glutamate-receptor 5 positive modulators. 
     
     
         41 . The pharmaceutical composition according to  claim 39 , further comprising one or more medicinally effective active substances selected from alzhemed, vitamin E, ginkolide, donepezil, rivastigmine, tacrine, galantamine, memantine, NS-2330, ibutamoren mesylate, capromorelin, minocyclin and rifampicin. 
     
     
         42 . A method for treating or preventing a disease or condition associated with an abnormal processing of Amyloid Precursor Protein (APP) or aggregation of Abeta peptide, comprising administering to a patient in need thereof a compound according to  claim 1 . 
     
     
         43 . A method for treating or preventing diseases or conditions influenced by inhibiting the β-secretase activity, comprising administering to a patient in need thereof a compound according to  claim 1 , wherein the compound acts as a β-secretase Inhibitor. 
     
     
         44 . A method for treating or preventing diseases or conditions influenced by inhibiting the aspartylprotease cathepsin D, comprising administering to a patient in need thereof a compound according to  claim 1 . 
     
     
         45 . A method for preventing the metastasisation of tumour cells, comprising administering to a patient in need thereof a compound according to  claim 1 . 
     
     
         46 . A method for treating or preventing a disease or condition selected from the group consisting of: Alzheimer's disease (AD), MCI (“mild cognitive impairment”), trisomy 21 (Down's syndrome), cerebral amyloid angiopathy, degenerative dementias, hereditary cerebral haemorrhage with amyloidosis, Dutch type (HCHWA-D), Alzheimer's dementia with Lewy bodies, trauma, stroke, pancreatitis, Inclusion Body Myositis (IBM), and other peripheral amyloidoses, diabetes or arteriosclerosis, comprising administering to a patient in need thereof a compound according to  claim 1 . 
     
     
         47 . A method for treating or preventing Alzheimer's disease (AD), comprising administering to a patient in need thereof a compound according to  claim 1 . 
     
     
         48 . A method for inhibiting β-secretase activity, comprising contacting β-secretase with an effective inhibitory amount of a compound according to  claim 1 .