Derivatives of quinoline as inhibitors of DYRK1A and/or DYRK1B kinases

1. A compound of formula (I)

or a salt, stereoisomer, tautomer or N-oxide thereof,

wherein

R 1 , R 3 are independently selected from the group consisting of

(i) H, CN, NO 2 , C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl;

wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 7 ;

(ii) C(═O)R 5 , C(═O)OR 6 , C(═O)SR 6 , C(═O)N(R 6a )(R 6b ), OR 6 , S(═O) n R 6 , S(═O) n N(R 6a )(R 6b ), S(═O) n OR 6 , N(R 6a )(R 6b ), N(R 6 )C(═O)R 5 , N(R 6 )C(═O)OR 6 , N(R 6 )C(═O)N(R 6a )(R 6b ), N(R 6 )S(═O) n R 6 , N(R 6 )S(═O) n N(R 6a )(R 6b ), N(R 6 )S(═O) n OR 6 ;

(iii) a 3- to 9-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring and a 6- to 14-membered saturated, partially unsaturated or fully unsaturated carbobicyclic or heterobicyclic ring, wherein said heterocyclic or heterobicyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic or bicyclic moieties is independently unsubstituted or substituted with one or more, same or different substituents R 8 ;

R 2 is selected from the group consisting of H, halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkoxy and C 1 -C 6 -haloalkoxy;

R 4 is independently selected from the group consisting of

(i) H, CN, NO 2 , C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl;

wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 7 ;

(ii) C(═O)R 5 , C(═O)OR 6 , C(═O)SR 6 , C(═O)N(R 6a )(R 6b ), OR 6 , S(═O) n R 6 , S(═O) n N(R 6a )(R 6b ), S(═O) n OR 6 , N(R 6 )C(═O)R 5 , N(R 6 )C(═O)OR 6 , N(R 6 )C(═O)N(R 6a )(R 6b ), N(R 6 )S(═O) n R 6 , N(R 6 )S(═O) n N(R 6a )(R 6b ), N(R 6 )S(═O) n OR 6 ;

(iii) a 3- to 9-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring and a 6- to 14-membered saturated, partially unsaturated or fully unsaturated carbobicyclic or heterobicyclic ring, wherein said heterocyclic or heterobicyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic or bicyclic moieties is independently unsubstituted or substituted with one or more, same or different substituents R 8 ;

R 5 , R 6 , R 6a , R 6b are independently selected from the group consisting of H, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkylcarbonyl, wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 9 ; and

a 3- to 9-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring, wherein said heterocyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic moieties is independently unsubstituted or substituted with one or more, same or different substituents R 10 ;

R 7 is selected from the group consisting of halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -alkynyl, C 2 -C 6 -haloalkynyl, C(═O)R 5 , C(═O)OR 6 , C(═O)SR 6 , C(═O)N(R 6a )(R 6b ), OR 6 , S(═O) n R 6 , S(═O) n N(R 6a )(R 6b ), S(═O) n OR 6 , N(R 6a )(R 6b ), N(R 6 )C(═O)R 5 , N(R 6 )C(═O)OR 6 , N(R 6 )C(═O)N(R 6a )(R 6b ), N(R 6 )S(═O) n (R 6 ), N(R 6 )S(═O) n N(R 6a )(R 6b ), N(R 6 )S(═O) n OR 6 ; and

a 3- to 9-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring and a 6- to 14-membered saturated, partially unsaturated or fully unsaturated carbobicyclic or heterobicyclic ring, wherein said heterocyclic or heterobicyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or hetero-atom in the aforementioned cyclic or bicyclic moieties is unsubstituted or substituted with one or more, same or different substituents R 8 ;

R 8 is selected from the group consisting of halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -alkynyl, C 2 -C 6 -haloalkynyl, C 1 -C 6 -alkylcarbonyl, N(R 6a )(R 6b ), OR 6 and S(═O) n R 6 ;

R 9 is selected from the group consisting of halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -alkynyl, C 2 -C 6 -haloalkynyl, C 1 -C 6 -alkylcarbonyl, N(R 11a )(R 11b ), OR 11 and S(═O) n R 11 ;

and a 3- to 9-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring, wherein said heterocyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic moieties is unsubstituted or substituted with one or more, same or different substituents R 10 ;

R 10 is selected from halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -alkynyl, C 2 -C 6 -haloalkynyl, C 1 -C 6 -alkylcarbonyl, N(R 11a )(R 11b ), OR 11 and S(═O) n R 11 ;

R 11 , R 11a , R 11b are independently selected from the group consisting of H, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl and C 2 -C 6 -alkynyl;

and wherein

n is 0, 1 or 2.

2. The compound according to claim 1 , wherein R 1 is selected from the group consisting of

(i) H, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -alkynyl, C 2 -C 6 -haloalkynyl;

wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 7 ;

(ii) C(═O)R 5 , C(═O)OR 6 , C(═O)SR 6 , C(═O)N(R 6a )(R 6b ), OR 6 , S(═O) n R 6 , S(═O) n N(R 6a )(R 6b ), S(═O) n OR 6 , N(R 6a )(R 6b ), N(R 6 )C(═O)R 5 , N(R 6 )C(═O)OR 6 , N(R 6 )C(═O)N(R 6a )(R 6b ), N(R 6 )S(═O) n R 6 , N(R 6 )S(═O) n N(R 6a )(R 6b ), N(R 6 )S(═O) n OR 6 ;

(iii) C 1 -C 3 -alkyl, C 2 -C 3 -alkenyl, and C 2 -C 3 ;

wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 7 ;

wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 7 ;

and wherein all other substituents have the meaning as defined in claim 1 .

3. The compound according to claim 1 , wherein R 2 is selected from the group consisting of H, halogen, CN, NO 2 , C 1 -C 2 -alkyl, vinyl, C 1 -C 2 -alkoxy and C 1 -C 2 -haloalkoxy;

and wherein all other substituents have the meaning as defined in claim 1 .

4. The compound according to claim 1 , wherein R 3 is selected from the group consisting of

(i) H, halogen, CN, NO 2 , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -alkynyl, C 2 -C 6 -haloalkynyl;

wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 7 ;

(ii) C(═O)R 5 , C(═O)OR 6 , C(═O)SR 6 , C(═O)N(R 6a )(R 6b ), OR 6 , S(═O) n R 6 , S(═O) n N(R 6a )(R 6b ), S(═O) n OR 6 , N(R 6a )(R 6b ), N(R 6 )C(═O)R 5 , N(R 6 )C(═O)OR 6 , N(R 6 )C(═O)N(R 6a )(R 6b ), N(R 6 )S(═O) n R 6 , N(R 6 )S(═O) n N(R 6a )(R 6b ), N(R 6 )S(═O) n OR 6 ;

and wherein all other substituents have the meaning as defined in claim 1 .

5. The compound according to claim 1 , wherein R 4 is selected from the group consisting of H, halogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different R 7 ;

and a 5- to 6-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring, wherein said heterocyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic or bicyclic moieties is independently unsubstituted or substituted with one or more, same or different substituents R 8 ;

and wherein all other substituents have the meaning as defined in claim 1 .

6. The compound according to claim 1 , wherein R 5 , R 6 , R 6a and R 6b are independently from each other selected from the group consisting of H, C 1 -C 5 -alkyl, C 2 -C 5 -alkenyl, C 2 -C 5 -alkynyl, wherein each substitutable carbon atom in the aforementioned moieties is independently unsubstituted or substituted with one or more, same or different substituents R 9 ; and a 5- to 6-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring, wherein said heterocyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic moieties is independently unsubstituted or substituted with one or more, same or different substituents R 10 .

7. The compound according to claim 1 , wherein R 7 is selected from the group consisting of halogen, CN, NO 2 , C 1 -C 5 -alkyl, C 1 -C 5 -haloalkyl, C 2 -C 5 -alkenyl, C 2 -C 5 -haloalkenyl, C 2 -C 5 -alkynyl, C 2 -C 5 -haloalkynyl, OR 6 , N(R 6a )(R 6b ); and a 5- to 6-membered saturated, partially unsaturated or full unsaturated carbocyclic or heterocyclic ring and a 8- to 9-membered saturated, partially unsaturated or fully unsaturated carbobicyclic or heterobicyclic ring, wherein said heterocyclic or heterobicyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic or bicyclic moieties is independently unsubstituted or substituted with one or more, same or different substituents R 8 .

8. The compound according to claim 1 , wherein R 8 is selected from the group consisting of C 1 -C 3 -alkyl, C 2 -C 3 -alkenyl, C 1 -C 3 -alkylcarbonyl, C 2 -C 3 -alkynyl and N(R 6a )(R 6b ).

9. The compound according to claim 1 , wherein R 9 is selected from the group consisting of halogen, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, N(R 11a )(R 11b ) and a 5- to 6-membered saturated, partially unsaturated or fully unsaturated carbocyclic or heterocyclic ring, wherein said heterocyclic ring comprises one or more, same or different heteroatoms selected from O, N or S, wherein said N- and/or S-atoms are independently oxidized or non-oxidized, and wherein each substitutable carbon or heteroatom in the aforementioned cyclic moiety is independently unsubstituted or substituted with one or more, same or different substituents R 10 .

10. The compound according to claim 1 , wherein R 10 is selected from the group consisting of halogen, C 1 -C 3 -alkyl, C 2 -C 3 -alkenyl, C 1 -C 3 -alkylcarbonyl, C 2 -C 3 -alkynyl and N(R 11a )(R 11b ).

11. The compound according to claim 1 , wherein R 11 , R 11a and R 11b are independently selected from the group consisting of H, C 1 -C 3 -alkyl, C 2 -C 3 -alkenyl and C 2 -C 3 -alkynyl.

12. The compound according to claim 1 , wherein said compound is selected from the group consisting of 4-chloro-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; (3S)-1-(6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinolin-4-yl)piperidin-3-amine; 1-N-(6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinolin-4-yl)cyclohexane-1,4-diamine; (3S)-1-(6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinolin-4-yl)pyrrolidin-3-amine; 4-(pyridin-3-yl)-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 4-(pyridin-4-yl)-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 4-phenyl-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; {5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl}(6-{1H-pyrrolo[2,3-b]pyridin-3-yl)}quinolin-4-yl)methanol; N-(1-methylpiperidin-4-yl)-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinolin-4-amine; 8-chloro-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline hydrochloride; 8-methyl-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline hydrochloride; 8-fluoro-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 6-{1H-pyrrolo[2,3-b]pyridin-3-yl}-8-(trifluoromethoxy)quinoline; 8-methoxy-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; N-(furan-3-ylmethyl)-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinolin-3-amine; 8-methyl-4-phenyl-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 8-methyl-4-(pyridin-3-yl)-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 8-fluoro-4-(pyridin-3-yl)-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline; 3-(4-chloroquinolin-6-yl)-N-methyl-N-(prop-2-en-1-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; methyl({3-[4-(pent-4-en-1-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl}methyl)(prop-2-en-1-yl)amine; N-methyl-3-[4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-methyl-3-[4-(morpholin-4-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(4-chloroquinolin-6-yl)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-methyl-3-(quinolin-6-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(8-methoxyquinolin-6-yl)-N-methyl-N-(prop-2-en-1-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(8-fluoroquinolin-6-yl)-N-methyl-N-(prop-2-en-1-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(8-chloroquinolin-6-yl)-N-methyl-N-(prop-2-en-1-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(8-methoxyquinolin-6-yl)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(8-fluoroquinolin-6-yl)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carb oxamide; N-benzyl-3-(8-fluoroquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-benzyl-3-(8-chloroquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-(8-fluoroquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-(3-aminopropyl)-3-(8-chloroquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; N-benzyl-3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-(3-aminopropyl)-3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-N-methyl-N-(prop-2-en-1-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-[8-fluoro-4-(2-phenylethyl)quinolin-6-yl]-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-{4-[(3R)-3-aminopiperidin-1-yl]-8-fluoroquinolin-6-yl}-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; N-methyl-3-[8-methyl-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-{4-[(3S)-3-aminopiperidin-1-yl]-8-fluoroquinolin-6-yl}-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; N-methyl-3-[8-fluoro-4-(4-methylpyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-[8-methoxy-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-{3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl}acetamide; 3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-{4-[(3R)-3-aminopiperidin-1-yl]-8-fluoroquinolin-6-yl}-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-{4-[(3R)-3-aminopiperidin-1-yl]-8-fluoroquinolin-6-yl}-N-(pyrimidin-5-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; benzyl({3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl}methyl)amine; (3R)-1-(6-{5-[(benzylamino)methyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-8-fluoroquinolin-4-yl)piperidin-3-amine; ({3-[8-fluoro-4-(pyridin-3-yl)quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl}methyl)(methyl)(prop-2-en-1-yl)amine; 3-{4-[(3S)-3-aminopiperidin-1-yl]-3-nitroquinolin-6-yl}-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-{3-amino-4-[(3S)-3-aminopiperidin-1-yl]quinolin-6-yl)}-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-{4-[(3S)-3-aminopiperidin-1-yl]-3-{[(3-chlorophenyl)methyl]amino}quinolin-6-yl}-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-(3-{[(3-chlorophenyl)methyl]amino}-4-(morpholin-4-yl)quinolin-6-yl)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-[3-acetamido-4-(morpholin-4-yl)quinolin-6-yl]-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; N-methyl-3-[4-(morpholin-4-yl)-3-[(oxan-4-ylmethyl)amino]quinolin-6-yl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-{4-[(4-aminocyclohexyl)amino]-3-nitroquinolin-6-yl}-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-{4-[(4-aminocyclohexyl)amino]-3-[(oxan-4-ylmethyl)amino]quinolin-6-yl}-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride; 3-(3-aminoquinolin-6-yl)-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 3-{3-[(oxan-4-ylmethyl)amino]quinolin-6-yl}-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 4-[(1-methylpiperidin-4-yl)amino]-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinoline-3-carbonitrile; N-methyl-N-(1-methylpiperidin-4-yl)-3-nitro-6-{1H-pyrrolo[2,3-b]pyridin-3-yl}quinolin-4-amine; 1-{4-[(3-amino-6-{1H-pyrrolo[2,3-b]pyridin-3-yl)}quinolin-4-yl)amino]piperidin-1-yl}ethan-1-one; N-(3-aminopropyl)-3-(8-fluoroquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride and 3-(3-acetamidoquinolin-6-yl)-N-(pyridin-3-ylmethyl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide.

13. A pharmaceutical composition comprising a pharmaceutically effective amount of the compound of claim 1 , optionally further comprising a pharmaceutically acceptable carrier, diluent or excipient.

14. The compound of claim 1 , wherein R 4 is N(R 6a )(R 6b ), and wherein when R 4 is N(R 6a )(R 6b ), R 6a is independently selected from the group consisting of C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkylcarbonyl, wherein each substitutable carbon atom in the aforementioned moieties of C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkylcarbonyl is independently unsubstituted or substituted with one or more, same or different substituents R 9 , and R 6b is independently selected from the group consisting of H, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkylcarbonyl, wherein each substitutable carbon atom in the aforementioned moieties of C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkylcarbonyl is independently unsubstituted or substituted with one or more, same or different substituents R 9 .