Anti-cancer agents and uses thereof

Abstract

The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A 1 is N or CR 1 ; A 3 is N or CR 3 ; A 5 is N or CR 5 ; R 1 , R 3 -R 6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.

1 . A compound of Formula I: 
     
       
         
         
             
             
         
       
     
     or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 A 1  is N or CR 1 , wherein R 1  is hydrogen, halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, alkoxycarbonylamino, aminocarbonylamino, monoalkylaminocarbonylamino, dialkylaminocarbonylamino, N-alkyl-N-alkoxycarbonyl-amino, N-alkyl-N-aminocarbonyl-amino, N-alkyl-N-monoalkylaminocarbonyl-amino or N-alkyl-N-dialkylaminocarbonyl-amino; 
 A 3  is N or CR 3 , wherein R 3  is hydrogen, halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, alkoxycarbonylamino, aminocarbonylamino, monoalkylaminocarbonylamino, dialkylaminocarbonylamino, N-alkyl-N-alkoxycarbonyl-amino, N-alkyl-N-aminocarbonyl-amino, N-alkyl-N-monoalkylaminocarbonyl-amino or N-alkyl-N-dialkylaminocarbonyl-amino; 
 A 5  is N or CR 5 ; 
 R 4  is 1-indolyl or 1-indazolyl, each of which is optionally substituted by one or two substituents independently selected from the group consisting of halo, hydroxy, nitro, cyano, alkyl, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl and dialkylaminocarbonylalkyl, 
 or R 4  is adamantyl, 
 or R 4  is selected from the group consisting of 
 
     
       
         
         
             
             
         
       
     
     wherein R 7 , R 8 , R 10  and R 11  are independently selected from the group consisting of hydrogen, halogen, hydroxy, alkyl, haloalkyl, hydroxyalkyl, alkoxy, cyano, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, sulfonylamino, alkylsulfonylamino and phenyl,
 or any two adjacent groups selected from R 7 , R 8 , R 9 , R 10  and R 11 , together with the carbon atoms to which they are attached, form a 5- or 6-membered aromatic, heteroaromatic or fully or partially unsaturated non-aromatic ring, which ring has 0-2 oxygen atoms, 0-2 sulfur atoms, 0-3 nitrogen atoms and 2-6 carbon atoms, and which ring, together with the phenyl or pyridyl ring to which it is fused, forms a bicyclic moiety, wherein said bicyclic moiety is optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, haloalkanoyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl and dialkylaminosulfonyl; 
 R 5  and R 6  are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, benzyloxycarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, alkoxycarbonylamino, ureido, N-alkylureido, N′-alkylureido, N,N′-dialkylureido, N,N′,N′-trialkylureido, N′,N′-dialkylureido, N′-alkoxy-N′-alkylureido, tetrazolyl, 2-oxo-pyrrolidin-1-yl, 2-oxo-piperidin-1-yl, benzyl and benzyloxy, wherein said benzyl and benzyloxy are optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkoxy, amino, monoalkylamino, dialkylamino, nitro and cyano; 
 n is 0 or 1, and L is a linker selected from the group consisting of —R a —N(R x )—R b —, —N(C(O)—CH 3 )—, —R a —OR b —, —R a —S—R b , —S(O)—, —S(O) 2 —, C 1-4  alkylene, —C(O)—, —C(═N—OH)—, —CH(OH)—, —C(R x )(OH)—, —CH(OR x )—, —C(R x )(OR y )—, —NH—C(O)—, —N(R x )—C(O)—, —C(O)—NH—, —C(O)—N(R x )—, —S(O) 2 —NH—, —S(O) 2 —N(R x )—, —NH—S(O) 2 —, —N(R x )—S(O) 2 — and —NH—S(O) 2 —CH 2 —, wherein R x  and R y  are independently alkyl, and R a  and R b  are independently CO 4  alkylene; and 
 X is Ar, HetAr or BiHetAr, wherein Ar is an aryl group having 6-10 carbons in the ring portion, HetAr is a 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, or HetAr is a 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, and BiHetAr is a heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur; 
 wherein Ar, HetAr and BiHetAr are each optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, alkoxyalkyl, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, morpholinyl and formyloxyalkoxyalkyl; 
 provided that: 
 (1) A 1 , A 3  and A 5  are not all nitrogen; 
 (2) when A 1  is CR 1 , A 3  is CR 3 , A 5  is CR 5  and X is optionally-substituted phenyl:
 at least one of R 1 , R 5  or R 6  is other than hydrogen, halo, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl or amino; and 
 R 4  is selected from the group consisting of 
 
 
     
       
         
         
             
             
         
       
       wherein any two adjacent groups selected from R 7 , R 8 , R 9 , R 10  and R 11 , together with the carbon atoms to which they are attached, form a 5- or 6-membered aromatic, heteroaromatic or fully or partially unsaturated non-aromatic ring, which ring has 0-2 oxygen atoms, 0-2 sulfur atoms, 0-3 nitrogen atoms and 2-6 carbon atoms, and which ring, together with the phenyl or pyridyl ring to which it is fused, forms a bicyclic moiety, wherein said bicyclic moiety is optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, haloalkanoyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl and dialkylaminosulfonyl; 
       (3) when each of R 1 , R 5  and R 6  is independently hydrogen, halo, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl or amino:
 X is HetAr or BiHetAr; and 
 R 4  is selected from the group consisting of 
 
     
     
       
         
         
             
             
         
       
       wherein any two adjacent groups selected from R 7 , R 8 , R 9 , R 10  and R 11 , together with the carbon atoms to which they are attached, form a 5- or 6-membered aromatic, heteroaromatic or fully or partially unsaturated non-aromatic ring, which ring has 0-2 oxygen atoms, 0-2 sulfur atoms, 0-3 nitrogen atoms and 2-6 carbon atoms, and which ring, together with the phenyl or pyridyl ring to which it is fused, forms a bicyclic moiety, wherein said bicyclic moiety is optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, haloalkanoyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl and dialkylaminosulfonyl; and 
       (4) when one of A 1 , A 3  or A 5  is nitrogen, and the other two are not nitrogen:
 at least one of R 5  or R 6  is other than hydrogen, halo, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl or amino. 
 
     
   
   
       2 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 A 1  is CR 1 ;   A 3  is CR 3 , and R 3  is hydrogen;   A 5  is CR 5 ; and   at least one of R 1 , R 5  or R 6  is other than hydrogen.   
   
   
       3 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 A 1  is CR 1 , and R 1  is hydrogen;   A 3  is CR 3 , and R 3  is hydrogen;   A 5  is CR 5 , and R 5  is hydrogen; and   R 6  is other than hydrogen.   
   
   
       4 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, having Formula II: 
     
       
         
         
             
             
         
       
     
     wherein three of R 7 , R 8 , R 9 , R 10  and R 11  are hydrogen, and the other two are independently selected from the group consisting of hydrogen, halogen, hydroxy, alkyl, haloalkyl, hydroxyalkyl, alkoxy, cyano, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, sulfonylamino, alkylsulfonylamino and phenyl;
 X is HetAr; 
 n is 1; and 
 R 1 , R 3 , R 5 , R 6  and L are defined as in  claim 1 . 
 
   
   
       5 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1  is hydrogen or hydroxy;   R 3  is hydrogen;   R 5  is selected from the group consisting of hydrogen, benzyl and (C 1-4  alkoxy)benzyl;   R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, ureido, N—(C 1-4  alkyl)ureido, N′—(C 1-4  alkyl)ureido, N,N′-di(C 1-4  alkyl)ureido, N,N′,N′-tri(C 1-4  alkyl)ureido, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl;   L is selected from the group consisting of —NH—, —N(R x )—, —N(C(O)—CH 3 )—, —C(O)—, —C(═N—OH)—, —R a —S—R b —, —S(O) 2 —, —R a —O—R b — and —C(CH 3 )(OH)—, wherein R x  is C 1-4  alkyl, and R a  and R b  are independently C 0-4  alkylene; and   X is selected from the group consisting of pyridinyl, 1-oxy-pyridinyl and pyrazinyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, C 1-4  alkoxy(C 1-4 )alkyl, amino, mono(C 1-4  alkyl)amino, di(C 1-4  alkyl)amino, cyano, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, morpholin-1-yl and formyloxy(C 1-4 )alkoxy(C 1-4 )alkyl.   
   
   
       6 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen; and   R 6  is other than hydrogen.   
   
   
       7 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein three of R 7 , R 8 , R 9 , R 10  and R 11  are hydrogen, and the other two are independently selected from the group consisting of hydrogen, halo, phenyl, CIA alkyl, halo(C 1-4 )alkyl, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino and C 1-4  alkylsulfonylamino. 
   
   
       8 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein four of R 7 , R 8 , R 9 , R 10  and R 11  are hydrogen, and the other is selected from the group consisting of hydrogen, chloro, trifluoromethyl, dimethylamino, methylsulfonylamino and phenyl. 
   
   
       9 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 7 , R 8 , R 9 , R 10  and R 11 , together with the phenyl ring to which they are attached, form a moiety selected from the group consisting of phenyl, 2-chlorophenyl, 3-phenylphenyl, 2-trifluoromethylphenyl, 3-dimethylaminophenyl and 3-methanesulfonylaminophenyl. 
   
   
       10 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino or (C 1-4  alkyl)sulfonylamino. 
   
   
       11 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl. 
   
   
       12 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—, or —N(R x )— or —C(O)—. 
   
   
       13 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH— or —C(O)—. 
   
   
       14 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—. 
   
   
       15 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl. 
   
   
       16 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       17 . The compound according to  claim 4 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is 3-pyridyl. 
   
   
       18 . The compound according to  claim 7 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen;   R 6  is hydroxyl, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino or (C 1-4  alkyl)sulfonylamino;   L is —NH— or —C(O)—; and   X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl.   
   
   
       19 . The compound according to  claim 18 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl. 
   
   
       20 . The compound according to  claim 18 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—. 
   
   
       21 . The compound according to  claim 18 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       22 . A compound selected from the group consisting of 
     5-(pyridin-3-ylamino)-biphenyl-3-ol; 
     2′-chloro-5-(pyridin-3-ylamino)-biphenyl-3-ol; 
     5-(pyridin-3-ylamino)-2′-trifluoromethyl-biphenyl-3-ol; 
     3′-dimethylamino-5-(pyridin-3-ylamino)-biphenyl-3-ol; 
     5-(pyridin-3-ylamino)-[1,1′;3′,1″]terphenyl-3-ol; and 
     N-[5′-hydroxy-3′-(pyridin-3-ylamino)-biphenyl-3-yl]-methanesulfonamide;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       23 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, having Formula II: 
     
       
         
         
             
             
         
       
       wherein any two adjacent groups selected from R 7 , R 8 , R 9 , R 10  and R 11 , together with the carbon atoms to which they are attached, form a 5- or 6-membered aromatic, heteroaromatic or fully or partially unsaturated non-aromatic ring, which ring has 0-2 oxygen atoms, 0-2 sulfur atoms, 0-3 nitrogen atoms and 2-6 carbon atoms, and which ring, together with the phenyl ring to which it is fused, forms a bicyclic moiety, wherein said bicyclic moiety is optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, haloalkanoyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl and dialkylaminosulfonyl;
 n is 1; and 
 R 1 , R 3 , R 5 , R 6 , L and X are defined as in  claim 1 . 
 
     
   
   
       24 . The compound according to  claim 23 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is HetAr. 
   
   
       25 . The compound according to  claim 23 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1  is hydrogen or hydroxy;   R 3  is hydrogen;   R 5  is selected from the group consisting of hydrogen, benzyl and (CIA alkoxy)benzyl;   R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, ureido, N—(C 1-4  alkyl)ureido, N′—(C 1-4  alkyl)ureido, N,N′-di(C 1-4  alkyl)ureido, N,N′,N′-tri(C 1-4  alkyl)ureido, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl;   L is selected from the group consisting of —NH—, —N(R x )—, —N(C(O)—CH 3 )—, —C(O)—, —C(═N—OH)—, —R a —S—R b —, —S(O) 2 —, —R a —O—R b —, and —C(CH 3 )(OH)—, wherein R x  is C 1-4  alkyl, and R a  and R b  are independently C 0-4  alkylene; and   X is selected from the group consisting of pyridinyl, 1-oxy-pyridinyl and pyrazinyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, C 1-4  alkoxy(C 1-4 )alkyl, amino, mono(C 1-4  alkyl)amino, di(C 1-4  alkyl)amino, cyano, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, morpholin-1-yl and formyloxy(C 1-4 )alkoxy(C 1-4 )alkyl.   
   
   
       26 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen; and   R 6  is other than hydrogen.   
   
   
       27 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is selected from the group consisting of indanyl, benzo[1,3]dioxolyl, 1,3-dihydro-indol-2-onyl, quinolinyl, benzofuranyl, indazolyl, benzothienyl and indolyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, cyano, C 2-5  alkanoyl and halo(C 2-5 )alkanoyl. 
   
   
       28 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is selected from the group consisting of indan-5-yl, indan-4-yl, benzo[1,3]dioxol-5-yl, benzo[1,3]dioxol-4-yl, 1,3-dihydro-indol-2-on-4-yl, quinolin-8-yl, benzofuran-4-yl, indazol-4-yl, indazol-7-yl, benzo[b]thiophen-4-yl, indol-7-yl, indol-5-yl, indol-6-yl and indol-4-yl, each of which is optionally substituted with one substitutent selected from the group consisting of fluoro, chloro, methyl, cyano and trifluoroacetyl. 
   
   
       29 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is selected from the group consisting of indan-5-yl, indan-4-yl, benzo[1,3]dioxol-5-yl, benzo[1,3]dioxol-4-yl, 1,3-dihydro-indol-2-on-4-yl, quinolin-8-yl, benzofuran-4-yl, indazol-4-yl, indazol-7-yl, benzo[b]thiophen-4-yl, 1-methyl-indol-7-yl, indol-5-yl, indol-6-yl, indol-4-yl, 7-fluoro-indol-4-yl, 2-cyano-indol-4-yl, 2-methyl-indol-4-yl, 3-trifluoroacetyl-indol-4-yl, 1-methyl-indol-4-yl and 3-chloro-indol-4-yl. 
   
   
       30 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicylic moiety is indol-4-yl optionally substituted with one substitutent selected from the group consisting of halo, C 1-4  alkyl, cyano, C 2-5  alkanoyl and halo(C 2-5 )alkanoyl. 
   
   
       31 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicylic moiety is indol-4-yl optionally substituted once with chloro, fluoro, methyl or trifluoroacetyl. 
   
   
       32 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicylic moiety is indol-4-yl. 
   
   
       33 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 1  is selected from the group consisting of hydrogen and hydroxy. 
   
   
       34 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 1  is hydrogen. 
   
   
       35 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 3  is hydrogen. 
   
   
       36 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 5  is selected from the group consisting of hydrogen, benzyl and (C 1-4  alkoxy)benzyl. 
   
   
       37 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 5  is hydrogen. 
   
   
       38 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, ureido, N—(C 1-4  alkyl)ureido, N′—(C 1-4  alkyl)ureido, N,N′-di(C 1-4  alkyl)ureido, N,N′,N′-tri(C 1-4  alkyl)ureido, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl. 
   
   
       39 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl. 
   
   
       40 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is selected from the group consisting of hydrogen, chloro, hydroxyl, methyl, methoxy, 4-methoxybenzyloxy, amino, acetylamino, propanoylamino, methoxycarbonylamino, benzyloxycarbonylamino, methylsulfonylamino, N′,N′-dimethylureido, carbamoyl, methoxycarbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl. 
   
   
       41 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino or (C 1-4  alkyl)sulfonylamino. 
   
   
       42 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is selected from the group consisting of —NH—, —N(R x )—, —N(C(O)—CH 3 )—, —C(O)—, —C(═N—OH)—, —R a —S—R b —, —S(O) 2 —, —R a —O—R b — and —C(CH 3 )(OH)—, wherein R x  is C 1-4  alkyl, and R a  and R b  are independently C 0-4  alkylene. 
   
   
       43 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is selected from the group consisting of —NH—, —N(CH 3 )—, —C(O)—, —C(═N—OH)—, —S—CH 2 —, —S(O) 2 —, —O— and —C(CH 3 )(OH)—. 
   
   
       44 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—, —N(R x )— or —C(O)—. 
   
   
       45 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH— or —C(O)—. 
   
   
       46 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridinyl, 1-oxy-pyridinyl and pyrazinyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, C 1-4  alkoxy(C 1-4 )alkyl, amino, mono(C 1-4  alkyl)amino, di(C 1-4  alkyl)amino, cyano, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, morpholin-1-yl and formyloxy(C 1-4 )alkoxy(C 1-4 )alkyl. 
   
   
       47 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridin-2-yl, pyridin-3-yl, 1-oxy-pyridin-3-yl, pyridin-4-yl and pyrazinyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of chloro, methyl, ethyl, hydroxy, hydroxymethyl, methoxy, amino, dimethylamino, cyano, carbamoyl, morpholin-1-yl and (2-formyloxyethoxy)methyl. 
   
   
       48 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridin-2-yl, pyridin-3-yl, 6-cyano-pyridin-3-yl, 6-chloro-pyridin-3-yl, 2-chloro-pyridin-3-yl, 6-hydroxy-pyridin-3-yl, 6-methyl-pyridin-3-yl, 5-methyl-pyridin-3-yl, 2-ethyl-pyridin-3-yl, 6-hydroxymethyl-pyridin-3-yl, 6-amino-pyridin-3-yl, 2-dimethylamino-pyridin-3-yl, 6-carbamoyl-pyridin-3-yl, 6-methoxy-pyridin-3-yl, 2-((2-formyloxyethoxy)methyl)-pyridin-3-yl, 1-oxy-pyridin-3-yl, pyridin-4-yl, 2-chloro-pyridin-4-yl, 2-chloro-6-methyl-pyridin-4-yl, 2,6-dimethyl-pyridin-4-yl, 2-cyano-6-methyl-pyridin-4-yl, 2-methoxy-pyridin-4-yl, 3-methoxy-pyridin-4-yl, 2-(morpholin-1-yl)-pyridin-4-yl, pyrazinyl and 5-cyano-pyrazin-2-yl. 
   
   
       49 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl optionally substituted by one substituent selected from the group consisting of methyl, cyano, chloro, hydroxy, hydroxymethyl, amino, methoxy and carbamoyl. 
   
   
       50 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       51 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen;   the bicylic moiety is indol-4-yl optionally substituted with one substitutent selected from the group consisting of halo, C 1-4  alkyl, cyano, C 2-5  alkanoyl and halo(C 2-5 )alkanoyl;   R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, ureido, N—(C 1-4  alkyl)ureido, N′—(C 1-4  alkyl)ureido, N,N′-di(C 1-4  alkyl)ureido, N,N′,N′-tri(C 1-4  alkyl)ureido, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl;   L is selected from the group consisting of —NH—, —N(CH 3 )—, —C(O)—, —C(═N—OH)—, —S—CH 2 —, —S(O) 2 —, —O— and —C(CH 3 )(OH)—; and   X is selected from the group consisting of pyridinyl, 1-oxy-pyridinyl and pyrazinyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, C 1-4  alkoxy(C 1-4 )alkyl, amino, mono(C 1-4  alkyl)amino, di(C 1-4  alkyl)amino, cyano, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, morpholin-1-yl and formyloxy(C 1-4 )alkoxy(C 1-4 )alkyl.   
   
   
       52 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicylic moiety is indol-4-yl. 
   
   
       53 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino or (C 1-4  alkyl)sulfonylamino. 
   
   
       54 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl, acetylamino, methoxycarbonylamino or methylsulfonylamino. 
   
   
       55 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH— or —C(O)—. 
   
   
       56 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl, carbamoyl and morpholin-1-yl. 
   
   
       57 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, chloro, methoxy, methyl, ethyl, carbamoyl and morpholin-1-yl. 
   
   
       58 . The compound according to  claim 51 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       59 . A compound selected from the group consisting of: 
     3-(1H-indazol-7-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-benzo[b]thiophen-4-yl-5-(pyridin-3-ylamino)-phenol; 
     3-(1H-indazol-4-yl)-5-(pyridin-3-ylamino)-phenol; 
     [3-benzo[b]thiophen-4-yl-5-(4-methoxybenzyloxy)-phenyl]-pyridin-3-yl-amine; 
     3-(indan-5-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-(indan-4-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-(pyridin-3-ylamino)-5-quinolin-8-yl-phenol; 
     3-(1-methyl-1H-indol-7-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-benzo[1,3]dioxol-5-yl-5-(pyridin-3-ylamino)-phenol; 
     4-[3-hydroxy-5-(pyridin-3-ylamino)-phenyl]-1,3-dihydro-indol-2-one; 
     3-(1H-indol-5-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-(1H-indol-7-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-(1H-indol-6-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-benzo[1,3]dioxol-4-yl-5-(pyridin-3-ylamino)-phenol; and 
     [3-benzo[t]ran-4-yl-5-(2-methoxy-pyridin-4-ylamino)-phenyl]-carbamic acid methyl ester;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       60 . A compound selected from the group consisting of: 
     3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-(2-methyl-1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenol; 
     3-(1H-indol-4-yl)-5-(pyridin-2-ylamino)-phenol; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-pyridin-3-yl-methanone; 
     2,2,2-trifluoro-1-{4-[3-hydroxy-5-(pyridine-3-carbonyl)-phenyl]-1H-indol-3-yl-ethanone; 
     3-(1H-indol-4-yl)-5-(1-oxypyridin-3-ylamino)-phenol; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-pyridin-3-yl-methanone oxime;
 (6-chloropyridin-3-yl)-[3-hydroxy-5-(1H-indol-4-yl)-phenyl]-methanone; 
 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-(6-hydroxypyridin-3-yl)-methanone; 
     5-[3-hydroxy-5-(1H-indol-4-yl)-phenylamino]-pyridin-2-ol; 
     3-(1H-indol-4-yl)-5-(pyridin-3-yloxy)-phenol; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-pyrazin-2-yl-methanone; 
     3-(1-methyl-1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenol; 
     [3-(1H-indol-4-yl)-5-methoxyphenyl]-pyridin-3-yl-amine; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-(6-hydroxymethyl-pyridin-3-yl)-methanone; 
     3-(1-hydroxy-1-pyridin-3-yl-ethyl)-5-(1H-indol-4-yl)-phenol; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-(6-methyl-pyridin-3-yl)-methanone; 
     [3-(1H-indol-4-yl)-5-nitrophenyl]-pyridin-3-yl-amine; 
     3-(1H-indol-4-yl)-5-(pyridin-4-ylamino)-phenol; 
     3-(1H-indol-4-yl)-5-(pyrazin-2-ylamino)-phenol; 
     3-(1H-indol-4-yl)-5-(methyl-pyridin-3-yl-amino)-phenol; 
     3-(3-chloro-1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenol; 
     (6-amino-pyridin-3-yl)-[3-hydroxy-5-(1H-indol-4-yl)-phenyl]-methanone; 
     [3-(1H-indol-4-yl)-5-methyl-phenyl]-pyridin-3-yl-amine; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-(5-methyl-pyridin-3-yl)-methanone;
 (2-chloro-pyridin-3-yl)-[3-hydroxy-5-(1H-indol-4-yl)-phenyl]-methanone; 
 
     5-[3-hydroxy-5-(1H-indol-4-yl)-phenylamino]-pyrazine-2-carbonitrile; 
     [3-chloro-5-(1H-indol-4-yl)-phenyl]-pyridin-3-yl-amine; 
     [3-hydroxy-5-(1H-indol-4-yl)-phenyl]-(6-methoxy-pyridin-3-yl)-methanone; 
     [3-(1H-indol-4-yl)-5-(pyridin-3-carbonyl)-phenyl]-carbamic acid benzyl ester; 
     [3-amino-5-(1H-indol-4-yl)-phenyl]-pyridin-3-yl-methanone; 
     [3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenyl]-benzoic acid methyl ester; 
     3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-benzonitrile; 
     5-[3-hydroxy-5-(1H-indol-4-yl)-phenylamino]-pyridin-2-carboxylic acid amide; 
     N-[3-(1H-indol-4-yl)-5-(pyridin-3-carbonyl)-phenyl]-acetamide; 
     N-[3-(1H-indol-4-yl)-5-(pyridin-3-carbonyl)-phenyl]-methanesulfonamide; 
     [3-(1H-indol-4-yl)-5-(pyridin-3-carbonyl)-phenyl]-carbamic acid methyl ester; 
     N-[3-(1H-indol-4-yl)-5-(pyridin-3-carbonyl)-phenyl]-propionamide; 
     5-[3-hydroxy-5-(1H-indol-4-yl)-phenylamino]-pyridine-2-carbonitrile; 
     3-[3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenyl]-1,1-dimethyl-urea; 
     3-(1H-indol-4-yl)-5-(pyrazin-2-ylamino)-benzamide; 
     N-[3-(1H-indol-4-yl)-5-(pyridine-3-sulfonyl)-phenyl]-acetamide; 
     N-[3-(1H-indol-4-yl)-5-(pyridine-4-carbonyl)-phenyl]-acetamide; 
     3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-benzamide; 
     N-[3-(1H-indol-4-yl)-5-(pyridin-3-ylmethylsulfanyl)-phenyl]-acetamide; 
     formic acid 2-{3-[3-hydroxy-5-(1H-indol-4-yl)-phenylamino]-pyridin-2-ylmethoxy}-ethyl ester; 
     [3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenyl]-carbamic acid methyl ester; 
     N-[3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenyl]-methanesulfonamide; 
     N-[3-(1H-indol-4-yl)-5-(2-methoxy-pyridine-4-carbonyl)-phenyl]-acetamide; 
     [3-amino-5-(1H-indol-4-yl)-phenyl]-(2-methoxy-pyridin-4-yl)-methanone; 
     N-[3-(2-chloro-pyridine-4-carbonyl)-5-(1H-indol-4-yl)-phenyl]-acetamide; 
     1-[3-(1H-indol-4-yl)-5-(pyridine-3-carbonyl)-phenyl]-pyrrolidin-2-one; 
     4-[3-hydroxy-5-(pyridin-3-ylamino)-phenyl]-1H-indole-2-carbonitrile; 
     N-[3-(2-cyano-1H-indol-4-yl)-5-(pyridine-3-carbonyl)-phenyl]-methanesulfonamide; 
     N-[3-(1H-indol-4-yl)-5-(pyridine-4-carbonyl)-phenyl]-methanesulfonamide; 
     N-[3-(2-chloro-pyridine-4-carbonyl)-5-(1H-indol-4-yl)-phenyl]-methanesulfonamide; 
     N-[3-(2-chloro-6-methyl-pyridine-4-carbonyl)-5-(1H-indol-4-yl)-phenyl]-methanesulfonamide; 
     methyl 3-(6-cyanopyridin-3-ylamino)-5-(1H-indol-4-yl)phenylcarbamate; 
     3-(2-ethylpyridin-3-ylamino)-5-(1H-indol-4-yl)phenol; 
     [3-(1H-indol-4-yl)-5-oxazolo[4,5-b]pyridin-2-yl-phenyl]carbamic acid methyl ester; 
     3-(2-(dimethylamino)pyridin-3-ylamino)-5-(1H-indol-4-yl)phenol; 
     N-[3-(2-Methoxy-pyridine-4-carbonyl)-5-(1H-indol-4-yl)-phenyl]-methanesulfonamide; 
     [3-(1H-indol-4-yl)-5-(2-methoxy-pyridin-4-ylamino)-phenyl]-carbamic acid methyl ester; 
     [3-(2-chloro-6-methyl-pyridin-4-ylamino)-5-(1H-indol-4-yl)-phenyl]-carbamic acid methyl ester; 
     3-(2-cyano-6-methyl-pyridin-4-ylamino)-5-(1H-indol-4-yl)-phenyl]-carbamic acid methyl ester; 
     [3-(2,6-dimethyl-pyridin-4-ylamino)-5-(1H-indol-4-yl)-phenyl]-carbamic acid methyl ester; 
     3-(2-chloro-pyridin-4-ylamino)-5-(1H-indol-4-yl)-phenyl]-carbamic acid methyl ester; 
     [3-(1H-indol-4-yl)-5-(2-morpholin-4-yl-pyridin-4-ylamino)-phenyl]-carbamic acid methyl ester; and 
     [3-(7-fluoro-1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenyl]-carbamic acid methyl ester;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       61 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1  and R 3  are each hydrogen; and   R 5  and R 6  are each other than hydrogen.   
   
   
       62 . The compound according to  claim 61 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 the bicyclic moiety is indol-4-yl or benzo[b]thiophen-4-yl;   R 5  and R 6  are independently selected from the group consisting of (C 1-4  alkyl)sulfonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)carbonylamino, hydroxyl, benzyl and (C 1-4  alkoxy)benzyl;   L is —NH— or —C(O)—; and   X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl.   
   
   
       63 . The compound according to  claim 62 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is indol-4-yl. 
   
   
       64 . The compound according to  claim 62 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 5  and R 6  are independently selected from the group consisting of hydroxyl, benzyl and (C 1-4  alkoxy)benzyl. 
   
   
       65 . The compound according to  claim 62 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 5  is benzyl or methoxybenzyl. 
   
   
       66 . The compound according to  claim 62 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl. 
   
   
       67 . The compound according to  claim 62 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—. 
   
   
       68 . The compound according to  claim 62 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       69 . A compound selected from the group consisting of: 
     2-benzyl-3-(1H-indol-4-yl)-5-(pyridin-3-ylamino)-phenol; and 
     3-benzo[b]thiophen-4-yl-2-(4-methoxybenzyl)-5-(pyridin-3-ylamino)-phenol;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       70 . The compound according to  claim 24 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 3 , R 5  and R 6  are each hydrogen; and   R 1  is other than hydrogen.   
   
   
       71 . The compound according to  claim 70 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 the bicyclic moiety is indol-4-yl;   R 1  is selected from the group consisting of (C 1-4  alkyl)sulfonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)carbonylamino, hydroxyl and amino;   L is —NH— or —C(O)—; and   X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl.   
   
   
       72 . The compound according to  claim 71 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 1  is hydroxyl or amino. 
   
   
       73 . The compound according to  claim 71 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —C(O)—. 
   
   
       74 . The compound according to  claim 71 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       75 . A compound selected from the group consisting of: 
     [2-hydroxy-5-(1H-indol-4-yl)-phenyl]-pyridin-3-yl-methanone; and 
     (2-amino-5-(1H-indol-4-yl)phenyl)-(pyridin-3-yl)methanone.
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       76 . The compound according to  claim 23 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is Ar. 
   
   
       77 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen; and   R 6  is other than hydrogen.   
   
   
       78 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1  is hydrogen or hydroxy;   R 3  is hydrogen;   R 5  is selected from the group consisting of hydrogen, benzyl and (C 1-4  alkoxy)benzyl;   the bicylic moiety is indol-4-yl optionally substituted with one substitutent selected from the group consisting of halo, C 1-4  alkyl, cyano, C 2-5  alkanoyl and halo(C 2-5 )alkanoyl;   R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, ureido, N—(C 1-4  alkyl)ureido, N′—(C 1-4  alkyl)ureido, N,N′-di(C 1-4  alkyl)ureido, N,N′,N′-tri(C 1-4  alkyl)ureido, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl;   L is selected from the group consisting of —NH—, —N(R x )—, —N(C(O)—CH 3 )—, —C(O)—, —C(═N—OH)—, —R a —S—R b —, —S(O) 2 —, —R a —O—R b — and —C(CH 3 )(OH)—, wherein R x  is C 1-4  alkyl, and R a  and R b  are independently C 0-4  alkylene; and   X is phenyl optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, C 1-4  alkoxy(C 1-4 )alkyl, amino, mono(C 1-4  alkyl)amino, di(C 1-4  alkyl)amino, cyano, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, morpholin-1-yl and formyloxy(C 1-4 )alkoxy(C 1-4 )alkyl.   
   
   
       79 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is indol-4-yl. 
   
   
       80 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is (C 1-4  alkyl)sulfonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)carbonylamino or hydroxyl. 
   
   
       81 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH— or —C(O)—. 
   
   
       82 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is phenyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl. 
   
   
       83 . The compound according to  claim 76 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen;   the bicyclic moiety is indol-4-yl;   R 6  is (C 1-4  alkyl)sulfonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)carbonylamino or hydroxyl;   L is —NH— or —C(O)—; and   X is phenyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl.   
   
   
       84 . The compound according to  claim 83 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl. 
   
   
       85 . The compound according to  claim 83 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—. 
   
   
       86 . The compound according to  claim 83 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is phenyl or cyanophenyl. 
   
   
       87 . A compound selected from the group consisting of: 
     3-(1H-indol-4-yl)-5-phenylamino-phenol; and 
     4-(3-hydroxy-5-(1H-indol-4-yl)phenylamino)benzonitrile;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       88 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, having Formula V: 
     
       
         
         
             
             
         
       
       wherein any two adjacent groups selected from R 7 , R 8 , R 9 , R 10  and R 11 , together with the carbon atoms to which they are attached, form a 5- or 6-membered aromatic, heteroaromatic or fully or partially unsaturated non-aromatic ring, which ring has 0-2 oxygen atoms, 0-2 sulfur atoms, 0-3 nitrogen atoms and 2-6 carbon atoms, and which ring, together with the phenyl ring to which it is fused, forms a bicyclic moiety, wherein said bicyclic moiety is optionally substituted with one or two substituents independently selected from the group consisting of halo, hydroxy, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, nitro, cyano, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, amino, monoalkylamino, dialkylamino, formylamino, alkylcarbonylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, haloalkanoyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, monoalkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, sulfonylamino, alkylsulfonylamino, aminosulfonyl, monoalkylaminosulfonyl and dialkylaminosulfonyl; 
       X is HetAr or BiHetAr; and 
       R 1 , R 3 , R 5  and R 6  are defined as in  claim 1 . 
     
   
   
       89 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen; and   R 6  is other than hydrogen.   
   
   
       90 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is indol-4-yl. 
   
   
       91 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)sulfonylamino or hydroxyl. 
   
   
       92 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is acetylamino, methoxycarbonylamino, methylsulfonylamino or hydroxyl. 
   
   
       93 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridinyl, pyrazinyl, benzoxazol-2-yl and oxazolo[4,5-b]pyridin-2-yl, each of which is optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl. 
   
   
       94 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridin-3-yl, pyridin-4-yl, benzoxazol-2-yl and oxazolo[4,5-b]pyridin-2-yl, each of which is optionally substituted once with C 1-4  alkoxy. 
   
   
       95 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridin-3-yl, 6-methoxy-pyridin-3-yl, pyridin-4-yl, benzoxazol-2-yl and oxazolo[4,5-b]pyridin-2-yl. 
   
   
       96 . The compound according to  claim 88 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 1 , R 3  and R 5  are each hydrogen;   the bicyclic moiety is indol-4-yl;   R 6  is (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)sulfonylamino or hydroxyl; and   X is selected from the group consisting of pyridinyl, pyrazinyl, benzoxazol-2-yl and oxazolo[4,5-b]pyridin-2-yl, each of which is optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl.   
   
   
       97 . The compound according to  claim 96 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is acetylamino, methoxycarbonylamino, methylsulfonylamino or hydroxyl. 
   
   
       98 . The compound according to  claim 96 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridin-3-yl, pyridin-4-yl, benzoxazol-2-yl and oxazolo[4,5-b]pyridin-2-yl, each of which is optionally substituted once with C 1-4  alkoxy. 
   
   
       99 . The compound according to  claim 96 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is selected from the group consisting of pyridin-3-yl, pyridin-4-yl and benzoxazol-2-yl. 
   
   
       100 . A compound selected from the group consisting of: 
     N-[3-(1H-indol-4-yl)-5-oxazolo[4,5-b]pyridin-2-yl-phenyl]-acetamide; 
     3-(1H-indol-4-yl)-5-pyridin-3-yl-phenol; 
     [3-(1H-indol-4-yl)-5-oxazolo[4,5-b]pyridin-2-yl-phenyl]carbamic acid methyl ester; 
     N-[3-benzoxazol-2-yl-5-(1H-indol-4-yl)-phenyl]-acetamide; 
     [3-benzoxazol-2-yl-5-(1H-indol-4-yl)-phenyl]-carbamic acid methyl ester; 
     N-[3-benzoxazol-2-yl-5-(1H-indol-4-yl)-phenyl]-methanesulfonamide; 
     [3-(1H-indol-4-yl)-5-pyridin-3-yl-phenyl]-carbamic acid methyl ester; 
     N-[3-(1H-indol-4-yl)-5-pyridin-3-yl-phenyl]-acetamide; 
     [3-(1H-indol-4-yl)-5-pyridin-4-yl-phenyl]-carbamic acid methyl ester; 
     N-[3-(1H-indol-4-yl)-5-pyridin-4-yl-phenyl]-methanesulfonamide; 
     N-[3-(1H-indol-4-yl)-5-pyridin-4-yl-phenyl]-acetamide; and 
     N-[3-(1H-indol-4-yl)-5-(6-methoxy-pyridin-3-yl)-phenyl]-acetamide;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       101 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, having Formula III: 
     
       
         
         
             
             
         
       
       wherein X is HetAr;
 n is 1; and 
 R 5 -R 11  and L are defined as in  claim 1 . 
 
     
   
   
       102 . The compound according to  claim 101 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 5  is selected from the group consisting of hydrogen, benzyl and (C 1-4  alkoxy)benzyl;   the bicylic moiety is indol-4-yl optionally substituted with one substitutent selected from the group consisting of halo, C 1-4  alkyl, cyano, C 2-5  alkanoyl and halo(C 2-5 )alkanoyl;   R 6  is selected from the group consisting of hydrogen, halo, hydroxyl, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, benzyloxy, (C 1-4  alkoxy)benzyloxy, amino, mono(C 1-4 )alkylamino, di(C 1-4 )alkylamino, (C 1-4  alkyl)carbonylamino, (C 1-4  alkoxy)carbonylamino, benzyloxycarbonylamino, (C 1-4  alkyl)sulfonylamino, ureido, N—(C 1-4  alkyl)ureido, N′—(C 1-4  alkyl)ureido, N,N′-di(C 1-4  alkyl)ureido, N,N′,N′-tri(C 1-4  alkyl)ureido, N′,N′-di(C 1-4  alkyl)ureido, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, (C 1-4  alkoxy)carbonyl, cyano, nitro and 2-oxo-pyrrolidin-1-yl;   L is selected from the group consisting of —NH—, —N(R x )—, —N(C(O)—CH 3 )—, —C(O)—, —C(═N—OH)—, —R a —S—R b —, —S(O) 2 —, —R a —O—R b — and —C(CH 3 )(OH)—, wherein R x  is C 1-4  alkyl, and R a  and R b  are independently C 0-4  alkylene; and   X is selected from the group consisting of pyridinyl, 1-oxy-pyridinyl and pyrazinyl, each of which is optionally substituted with one or two substitutents selected from the group consisting of halo, C 1-4  alkyl, halo(C 1-4 )alkyl, hydroxy, hydroxy(C 1-4 )alkyl, C 1-4  alkoxy, C 1-4  alkoxy(C 1-4 )alkyl, amino, mono(C 1-4  alkyl)amino, di(C 1-4  alkyl)amino, cyano, carbamoyl, mono(C 1-4  alkyl)aminocarbonyl, di(C 1-4  alkyl)aminocarbonyl, morpholin-1-yl and formyloxy(C 1-4 )alkoxy(C 1-4 )alkyl.   
   
   
       103 . The compound according to  claim 101 , or a pharmaceutically-acceptable salt or solvate thereof, wherein the bicyclic moiety is indol-4-yl. 
   
   
       104 . The compound according to  claim 101 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is (C 1-4  alkyl)sulfonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)carbonylamino, C 1-4  alkoxy or hydroxyl. 
   
   
       105 . The compound according to  claim 101 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH— or —C(O)—. 
   
   
       106 . The compound according to  claim 101 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl. 
   
   
       107 . The compound according to  claim 101 , or a pharmaceutically-acceptable salt or solvate thereof, wherein:
 R 5  is hydrogen;   the bicyclic moiety is indol-4-yl;   R 6  is (C 1-4  alkyl)sulfonylamino, (C 1-4  alkoxy)carbonylamino, (C 1-4  alkyl)carbonylamino, C 1-4  alkoxy or hydroxyl;   L is —NH— or —C(O)—; and   X is pyridyl optionally substituted once with a substituent selected from the group consisting of cyano, halo, C 1-4  alkoxy, C 1-4  alkyl and carbamoyl.   
   
   
       108 . The compound according to  claim 107 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl or C 1-4  alkoxy. 
   
   
       109 . The compound according to  claim 107 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxyl or methoxy. 
   
   
       110 . The compound according to  claim 107 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH—. 
   
   
       111 . The compound according to  claim 107 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       112 . A compound selected from the group consisting of: 
     [4-(1H-indol-4-yl)-6-methoxypyrimidin-2-yl]-pyridin-3-ylamine; and 
     6-(1H-indol-4-yl)-2-(pyridin-3-ylamino)-pyrimidin-4-ol;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       113 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, having Formula IV: 
     
       
         
         
             
             
         
       
       wherein R 4  is adamantyl;
 X is HetAr; 
 n is 1; and 
 R 1 , R 3 , R 5 , R 6  and L are defined as in  claim 1 . 
 
     
   
   
       114 . The compound according to  claim 113 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 5  is hydroxyl. 
   
   
       115 . The compound according to  claim 113 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydrogen. 
   
   
       116 . The compound according to  claim 113 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is selected from the group consisting of —C(H)(OH)— and —C(O)—. 
   
   
       117 . The compound according to  claim 113 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl. 
   
   
       118 . A compound selected from the group consisting of: 
     2-adamant-2-yl-4-(hydroxypyridin-3-ylmethyl)-phenol; and 
     (3-adamant-2-yl-4-hydroxyphenyl)-pyridin-3-yl-methanone;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       119 . The compound according to  claim 1 , or a pharmaceutically-acceptable salt or solvate thereof, having Formula IV: 
     
       
         
         
             
             
         
       
       wherein R 4  is 2-, 3- or 4-quinolinyl or 1-indolyl, each of which is optionally substituted by one or two substituents independently selected from the group consisting of halo, nitro and cyano;
 X is HetAr; 
 n is 1; and 
 R 1 , R 3 , R 5 , R 6  and L are defined as in  claim 1 . 
 
     
   
   
       120 . The compound according to  claim 119 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 5  is hydrogen. 
   
   
       121 . The compound according to  claim 119 , or a pharmaceutically-acceptable salt or solvate thereof, wherein R 6  is hydroxy. 
   
   
       122 . The compound according to  claim 119 , or a pharmaceutically-acceptable salt or solvate thereof, wherein L is —NH— or —C(O)—. 
   
   
       123 . The compound according to  claim 119 , or a pharmaceutically-acceptable salt or solvate thereof, wherein X is pyridyl or quinolin-3-yl. 
   
   
       124 . A compound selected from the group consisting of: 
     3-(6-nitroindol-1-yl)-5-(pyridin-3-ylamino)-phenol; 
     1-[3-hydroxy-5-(pyridin-3-ylamino)-phenyl-1H-indole-5-carbonitrile; 
     3-(pyridin-3-ylamino)-5-quinolin-3-yl-phenol; and 
     [3-(5-fluoro-indol-1-yl)-5-hydroxy-phenyl]-pyridin-3-yl-methanone;
 or a pharmaceutically-acceptable salt or solvate thereof. 
 
   
   
       125 . A compound, or a pharmaceutically-acceptable salt or solvate thereof, of Formula VI: 
     
       
         
         
             
             
         
       
     
     wherein R 12  is halo. 
   
   
       126 . The compound N-[3-bromo-5-(pyridine-3-carbonyl)-phenyl-acetamide, or a pharmaceutically-acceptable salt or solvate thereof. 
   
   
       127 . A pharmaceutical composition comprising the compound according to any one of  claims 1 - 126 , or a pharmaceutically-acceptable salt or solvate thereof, and a pharmaceutically-acceptable carrier or diluent. 
   
   
       128 . The composition of  claim 127 , wherein said compound is present in a concentration of about 0.01 μM to about 100 μM. 
   
   
       129 . The composition of  claim 127 , wherein said compound is present in a concentration of about 0.03 μg/mL to about 30 μg/mL. 
   
   
       130 . The composition of  claim 127 , suitable for administration by a subcutaneous, intravenous, intramuscular, intraperitoneal, buccal or ocular route, rectally, parenterally, instrasystemically, intravaginally, topically, orally, or as an oral or nasal spray. 
   
   
       131 . The composition of  claim 127 , suitable for oral administration, wherein said compound is present in a concentration of about 0.01 μM to about 100 μM. 
   
   
       132 . The composition of  claim 127 , suitable for oral administration, wherein said compound is present in a concentration of about 0.03 μg/mL to about 30 μg/mL. 
   
   
       133 . A method of treating a condition that results from abnormal cell growth, cellular differentiation, tumor growth or invasion, comprising administering to a patient in need of such treatment a pharmaceutically-effective amount of a compound of any one of  claims 1 - 126 , or a pharmaceutically-acceptable salt or solvate thereof. 
   
   
       134 . A method of treating cancer, comprising administering to a patient in need of such treatment a pharmaceutically-effective amount of a compound of any one of  claims 1 - 126 , or a pharmaceutically-acceptable salt or solvate thereof. 
   
   
       135 . The method according to  claim 134 , wherein the cancer is leukemia, non-small cell lung, myeloma, colon, CNS, melanoma, ovarian, renal, prostate, breast, cervical, soft-tissue sarcomas or pancreatic cancer. 
   
   
       136 . The method according to  claim 134 , wherein the cancer is leukemia, colon or non-small cell lung. 
   
   
       137 . The method according to  claim 133 , wherein said pharmaceutically-effective amount is between about 0.1 and about 200 milligrams per kilogram per day. 
   
   
       138 . The method according to  claim 133 , wherein said pharmaceutically-effective amount is between about 1.0 and about 100 milligrams per kilogram per day. 
   
   
       139 . The method according to  claim 134 , wherein said pharmaceutically-effective amount is between about 0.1 and about 200 milligrams per kilogram per day. 
   
   
       140 . The method according to  claim 134 , wherein said pharmaceutically-effective amount is between about 1.0 and about 100 milligrams per kilogram per day. 
   
   
       141 . A method of hindering or blocking cell cycle progression, comprising contacting one or more cells with a compound of any one of  claims 1 - 126 , or a pharmaceutically-acceptable salt or solvate thereof. 
   
   
       142 . The method according to  claim 141 , wherein the cells are cancerous cells. 
   
   
       143 . The method according to  claim 141 , wherein the cells are leukemia cells, soft-tissue sarcoma cells, or non-small cell lung, myeloma, colon, CNS, melanoma, ovarian, renal, prostate, breast, cervical or pancreatic cancer cells. 
   
   
       144 . The method according to  claim 141 , wherein the cells are leukemia, non-small cell lung or colon cancer cells.