Steroid derivatives

Abstract

Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.

What is claimed is:  
     
         1 . A compound of the following formula:  
       
         
           
           
               
               
           
         
       
       wherein 
 R 3  is hydrogen, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 1 , R 2 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —S—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino;  
 R is —X—Y-Z, in which X is a bond, or alkyl or alkenyl, optionally inserted with —NH—, —N(alkyl)-, —O—, or —S—, and further optionally forming a cyclic moiety with R 16  and the 2 ring carbon atoms to which R 16  and R 17  are bonded; Y is —CO—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, —N(alkyl)-CO—, or a bond; and Z is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio; or is —CH(A)-B with A being a side chain of an amino acid, and B being hydrogen, —NR a R b , or —COOR c  wherein each of R a , R b , and R c , independently, is hydrogen or alkyl; and  
 n is 0, 1, or 2;  
 provided that when Z is substituted with carboxyl or alkyloxycarbonyl, Y is a bond and either X or Z contains at least one double bond, and that when Y is a bond, either X is —NH-alkyl-, —NH-alkenyl-, —N(alkyl)-alkyl-, —N(alkyl)-alkenyl-, —O-alkyl-, —O-alkenyl-, —S-alkyl-, or —S-alkenyl-; or Z is substituted with halo, sulfonic acid, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl, or is alkenyl;  
 or a salt thereof.  
 
     
     
         2 . The compound of  claim 1 , wherein n is 0.  
     
     
         3 . The compound of  claim 1 , wherein R 3  is amino, carboxyl, halo, sulfonic acid, —O-sulfonic acid, or alkyl; R 6  is hydroxy, amino, carboxyl, halo, sulfonic acid, —O-sulfonic acid, or alkyl; and each of R 3  and R 6 , independently, is in the α-configuration.  
     
     
         4 . The compound of  claim 1 , wherein R 5  is hydrogen and is in the β-configuration.  
     
     
         5 . The compound of  claim 1 , wherein R 3  is oxo; each of R 1 , R 2 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl.  
     
     
         6 . The compound of  claim 5 , wherein each of R 1 , R 2 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, or oxo; and each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen or hydroxy; or a salt thereof.  
     
     
         7 . The compound of  claim 6 , wherein X is a bond or alkyl.  
     
     
         8 . The compound of  claim 7 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —NR a R b  or —COOR c    
     
     
         9 . The compound of  claim 1 , wherein X is a bond or alkyl.  
     
     
         10 . The compound of  claim 9 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —N a R b  or —COOR c    
     
     
         11 . The compound of  claim 6 , wherein Y is —CO—, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—NH—, —NH—CO—, or a bond.  
     
     
         12 . The compound of  claim 11 , wherein Z is alkyl, alkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, halo, sulfonic acid, carboxyl, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl; or is —CH(A)-B.  
     
     
         13 . The compound of  claim 1 , wherein Z is alkyl or aryl, each of which being optionally substituted with hydroxy; or is —CH(A)-B with A being an amino acid side chain having an aromatic moiety, and B being —NR a R b , or —COOR c .  
     
     
         14 . The compound of  claim 1 , wherein R 17  contains a straight chain having 6-20 chain atoms.  
     
     
         15 . The compound of  claim 14 , wherein R 17  contains a straight chain having 8-16 chain atoms.  
     
     
         16 . The compound of  claim 1 , wherein X is —CH(CH 3 )—CH 2 —, Y is a bond, and Z is —CH 2 —CH═C(R′)(CH 3 ) with R′ being hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio.  
     
     
         17 . The compound of  claim 1 , wherein said compound is:  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         18 . A compound of the following formula:  
       
         
           
           
               
               
           
         
       
       wherein 
 each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino;  
 R 17  is —X—Y-Z, in which X is a bond, or alkyl or alkenyl, optionally inserted with —NH—, —N(alkyl)-, —O—, or —S—, and further optionally forming a cyclic moiety with R 16  and the 2 ring carbon atoms to which R 16  and R 17  are bonded; Y is —CO—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, —N(alkyl)-CO—, or a bond; and Z is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio; or is —CH(A)-B with A being an amino acid side chain containing an aromatic moiety, and B being hydrogen, —NR a R b , or —COOR c  wherein each of R a , R b , and R c , independently, is hydrogen or alkyl; and  
 n is 0, 1, or 2;  
 provided that when Z is substituted with carboxyl or alkyloxycarbonyl, Y is a bond and either X or Z contains at least one double bond, and that when Y is a bond, either X is —NH-alkyl-, —NH-alkenyl-, —N(alkyl)-alkyl-, —N(alkyl)-alkenyl-, —O-alkyl-, —O-alkenyl-, —S-alkyl-, or —S-alkenyl-; or Z is substituted with halo, sulfonic acid, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl, or is alkenyl;  
 or a salt thereof.  
 
     
     
         19 . The compound of  claim 18 , wherein n is 0.  
     
     
         20 . The compound of  claim 18 , wherein each of R 3  and R 6 , independently, is hydroxy, amino, carboxyl, halo, sulfonic acid, —O-sulfonic acid, or alkyl, and is in the α-configuration.  
     
     
         21 . The compound of  claim 18 , wherein R 5  is hydrogen and is in the β-configuration.  
     
     
         22 . The compound of  claim 18 , wherein each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl.  
     
     
         23 . The compound of  claim 22 , wherein each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, or oxo; and each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen or hydroxy.  
     
     
         24 . The compound of  claim 23 , wherein X is a bond or alkyl.  
     
     
         25 . The compound of  claim 24 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —NR a R b  or —COOR c    
     
     
         26 . The compound of  claim 18 , wherein X is a bond or alkyl.  
     
     
         27 . The compound of  claim 26 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —NR a R b  or —COOR c    
     
     
         28 . The compound of  claim 18 , wherein Y is —CO—, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—NH—, —NH—CO—, or a bond.  
     
     
         29 . The compound of  claim 28 , wherein Z is alkyl, alkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, halo, sulfonic acid, carboxyl, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl; or is —CH(A)-B.  
     
     
         30 . The compound of  claim 18 , wherein Z is alkyl or aryl, each of which being optionally substituted with hydroxy; or is —CH(A)-B with A being an amino acid side chain having an aromatic moiety, and B being —NR a R b , or —COOR c .  
     
     
         31 . The compound of  claim 18 , wherein R 17  contains a straight chain having 6-20 chain atoms.  
     
     
         32 . The compound of  claim 31 , wherein R 17  contains a straight chain having 8-16 chain atoms.  
     
     
         33 . The compound of  claim 18 , wherein X is —CH(CH 3 )—CH 2 —, Y is a bond, and Z is —CH 2 —CH═C(R′)(CH 3 ) with R′ being hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio.  
     
     
         34 . The compound of  claim 18 , wherein said compound is:  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         35 . A compound of the following formula:  
       
         
           
           
               
               
           
         
       
       wherein 
 each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino;  
 R 17  is —X—Y-Z, in which X is a bond, or alkyl or alkenyl, optionally inserted with —NH—, —N(alkyl)-, —O—, or —S—, and further optionally forming a cyclic moiety with R 16  and the 2 ring carbon atoms to which R 16  and R 17  are bonded; Y is —CO—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, —N(alkyl)-CO—, or a bond; and Z is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio; or is —CH(A)-B with A being a side chain of an amino acid, and B being hydrogen, —NR a R b , or —COOR c  wherein each of R a , R b , and R c , independently, is hydrogen or alkyl; and  
 n is 0, 1, or 2;  
 provided that when Z is substituted with carboxyl or alkyloxycarbonyl, Y is a bond and either X or Z contains at least one double bond, and that when Y is a bond, either X is —NH-alkyl-, —NH-alkenyl-, —N(alkyl)-alkyl-, —N(alkyl)-alkenyl-, —O-alkyl-, —O-alkenyl-, —S-alkyl-, or —S-alkenyl-; or Z is substituted with halo, sulfonic acid, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl, or is alkenyl; and  
 further provided that at least one of R 3  and R 4 , R 4  and R 5 , R 5  and R 6 , R 7  and R 8 , R 12  and R 13 , and R 15  and R 16 , independently, is deleted to form a double bond;  
 or a salt thereof.  
 
     
     
         36 . The compound of  claim 35 , wherein at least one of R 3  and R 4 , R 4  and R 5 , R 12  and R 13 , and R 15  and R 16 , independently, is deleted to form a double bond.  
     
     
         37 . The compound of  claim 35 , wherein n is 0.  
     
     
         38 . The compound of  claim 35 , wherein R 3  is hydroxy, amino, carboxyl, halo, sulfonic acid, —O-sulfonic acid, or alkyl, and is in the α-configuration.  
     
     
         39 . The compound of  claim 35 , wherein each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl.  
     
     
         40 . The compound of  claim 39 , wherein each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, or oxo; and each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen or hydroxy.  
     
     
         41 . The compound of  claim 40 , wherein X is a bond or alkyl.  
     
     
         42 . The compound of  claim 41 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —NR a R b  or —COOR c    
     
     
         43 . The compound of  claim 35 , wherein X is a bond or alkyl.  
     
     
         44 . The compound of  claim 35 , wherein Y is —CO—, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—NH—, —NH—CO—, or a bond.  
     
     
         45 . The compound of  claim 35 , wherein Z is alkyl or aryl, each of which being optionally substituted with hydroxy; or is —CH(A)-B with A being an amino acid side chain having an aromatic moiety, and B being —N a R b , or —COOR c .  
     
     
         46 . The compound of  claim 35 , wherein R 17  contains a straight chain having 6-20 chain atoms.  
     
     
         47 . The compound of  claim 46 , wherein R 17  contains a straight chain having 8-16 chain atoms.  
     
     
         48 . The compound of  claim 35 , wherein X is —CH(CH 3 )—CH 2 —, Y is a bond, and Z is —CH 2 —CH═C(R′)(CH 3 ) with R′ being hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio.  
     
     
         49 . The compound of  claim 35 , wherein Z is alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl.  
     
     
         50 . The compound of  claim 49 , wherein n is 0.  
     
     
         51 . The compound of  claim 49 , wherein R 3  is hydroxy, amino, carboxyl, halo, sulfonic acid, —O-sulfonic acid, or alkyl, and is in the α-configuration.  
     
     
         52 . The compound of  claim 49 , wherein each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl.  
     
     
         53 . The compound of  claim 52 , wherein each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, or oxo; and each of R 5 , R 8 , R 9 , R 10 , R 13  and R 14 , independently, is hydrogen or hydroxy.  
     
     
         54 . The compound of  claim 53 , wherein X is a bond or alkyl.  
     
     
         55 . The compound of  claim 54 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —NR a R b  or —COOR c    
     
     
         56 . The compound of  claim 49 , wherein X is a bond or alkyl.  
     
     
         57 . The compound of  claim 56 , wherein Y is —C(═O)—NH— or —NH—C(═O)—; and Z is —CH(A)-B with A being a side chain of Tyr or Phe, and B being —NR a R b  or —COOR c    
     
     
         58 . The compound of  claim 49 , wherein Y is —CO—, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—NH—, —NH—CO—, or a bond.  
     
     
         59 . The compound of  claim 49 , wherein R 17  contains a straight chain having 6-20 chain atoms.  
     
     
         60 . The compound of  claim 59 , wherein R 17  contains a straight chain having 8-16 chain atoms.  
     
     
         61 . The compound of  claim 49 , wherein X is —CH(CH 3 )—CH 2 —, Y is a bond, and Z is —CH 2 —CH═C(R′)(CH 3 ) with R′ being hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio.  
     
     
         62 . The compound of  claim 49 , wherein said compound is:  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         63 . A pharmaceutical composition for treating a UR- or a LXR-mediated disorder, said composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound of the following formula:  
       
         
           
           
               
               
           
         
       
       wherein 
 R 3  is hydrogen, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 1 , R 2 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino;  
 R 17  is —X—Y-Z, in which X is a bond, or alkyl or alkenyl, optionally inserted with —NH—, —N(alkyl)-, —O—, or —S—, and further optionally forming a cyclic moiety with R 16  and the 2 ring carbon atoms to which R 16  and R 17  are bonded; Y is —CO—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, —N(alkyl)-CO—, or a bond; and Z is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio; or is —CH(A)-B with A being a side chain of an amino acid, and B being hydrogen, —NR a R b , or —COOR c  wherein each of R a , R b , and R c , independently, is hydrogen or alkyl; and  
 n is 0, 1, or 2;  
 provided that when Z is substituted with carboxyl or alkyloxycarbonyl, Y is a bond and either X or Z contains at least one double bond, and that when Y is a bond, either X is —NH-alkyl-, —NH-alkenyl-, —N(alkyl)-alkyl-, —N(alkyl)-alkenyl-, —O-alkyl-, —O-alkenyl-, —S-alkyl-, or —S-alkenyl-; or Z is substituted with halo, sulfonic acid, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl, or is alkenyl;  
 or a salt thereof.  
 
     
     
         64 . The composition of  claim 63 , wherein said compound is:  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         65 . A pharmaceutical composition for treating a UR- or a LXR-mediated disorder, said composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound of the following formula:  
       
         
           
           
               
               
           
         
       
       wherein 
 each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino;  
 R 17  is —X—Y-Z, in which X is a bond, or alkyl or alkenyl, optionally inserted with —NH—, —N(alkyl)-, —O—, or —S—, and further optionally forming a cyclic moiety with R 6 and the 2 ring carbon atoms to which R 16  and R 17  are bonded; Y is —CO—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, —N(alkyl)-CO—, or a bond; and Z is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is substituted with hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio; or is —CH(A)-B with A being an amino acid side chain containing an aromatic moiety, and B being hydrogen, —NR a R b , or —COOR c  wherein each of R a , R b , and R c , independently, is hydrogen or alkyl; and  
 n is 0, 1, or 2;  
 provided that when Z is substituted with carboxyl or alkyloxycarbonyl, Y is a bond and either X or Z contains at least one double bond, and that when Y is a bond, either X is —NH-alkyl-, —NH-alkenyl-, —N(alkyl)-alkyl-, —N(alkyl)-alkenyl-, —O-alkyl-, —O-alkenyl-, —S-alkyl-, or —S-alkenyl-; or Z is substituted with halo, sulfonic acid, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl, or is alkenyl;  
 or a salt thereof.  
 
     
     
         66 . The composition of  claim 65 , wherein said compound is:  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         67 . A pharmaceutical composition for treating a UR- or a LXR-mediated disorder, said composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound of the following formula:  
       
         
           
           
               
               
           
         
       
       wherein 
 each of R 1 , R 2 , R 3 , R 4 , R 4′ , R 6 , R 7 , R 11 , R 12 , R 15 , R 16 , and R 17′ , independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, —O-sulfonic acid, or alkyl optionally inserted with —NH—, —N(alkyl)-, —O—, —S—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, or —N(alkyl)-CO—, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or —O-sulfonic acid;  
 each of R 5 , R 8 , R 9 , R 10 , R 13 , and R 14 , independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino;  
 R 17  is —X—Y-Z, in which X is a bond, or alkyl or alkenyl, optionally inserted with —NH—, —N(alkyl)-, —O—, or —S—, and further optionally forming a cyclic moiety with R 16  and the 2 ring carbon atoms to which R 16  and R 17  are bonded; Y is —CO—, —SO—, —SO 2 —, —O—SO 2 —, —SO 2 —O—, —O—SO 3 —, —SO 3 —O—, —CO—O—, —O—CO—, —CO—NH—, —CO—N(alkyl)-, —NH—CO—, —N(alkyl)-CO—, or a bond; and Z is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, and is optionally substituted with hydroxy, alkoxy, amino, halo, sulfonic acid, —O-sulfonic acid, carboxyl, oxo, alkyloxycarbonyl, alkylcarbonyloxy, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl, alkylsulfinyl, alkylsulfonyl, or alkylthio; or is —CH(A)-B with A being a side chain of an amino acid, and B being hydrogen, —NR a R b , or —COOR c  wherein each of R a , R b , and R c , independently, is hydrogen or alkyl; and  
 n is 0, 1, or 2;  
 provided that when Z is substituted with carboxyl or alkyloxycarbonyl, Y is a bond and either X or Z contains at least one double bond, and that when Y is a bond, either X is —NH-alkyl-, —NH-alkenyl-, —N(alkyl)-alkyl-, —N(alkyl)-alkenyl-, —O-alkyl-, —O-alkenyl-, —S-alkyl-, or —S-alkenyl-; or Z is substituted with halo, sulfonic acid, —O-sulfonic acid, alkylsulfinyl, or alkylsulfonyl, or is alkenyl; and further provided that at least one of R 3  and R 4 , R 4  and R 5 , R 5  and R 6 , R 7  and R 8 , R 12  and R 13 , and R 15  and R 16 , independently, is deleted to form a double bond;  
 or a salt thereof.  
 
     
     
         68 . The composition of  claim 67 , wherein said compound is: