Substituted pyrazolo[1,5-A]pyridines, their preparation and use as medicaments

1. A compound of general formula (I):

wherein

R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 ; or an heteroarylalkyl radical C 1-10 ;

or R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted by one or more substituents selected from the group consisting of a C 1-6 alkyl group, a linear or branched C 1-6 alkoxy group, —F, —Cl, —I, —Br, —CF 3 , —CH 2 F, —CHF 2 , —CN, —OH, —SH, —NH 2 , oxo, —(C═O)R′, —SR′, —SOR′, —SO 2 R′, —NHR′, —NR′R″,

wherein R′ and R″ at each occurrence independently represents a linear or branched C 1-6 -alkyl group;

or R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C 3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group;

R 3 represents hydrogen or halogen;

n is 0, 1 or 2;

m is 1, 2, 3 or 4;

and - - - - - represents an optional double bond,

with the proviso that when R 1 and R 2 together with the bridging nitrogen form a piperidine, R 3 is hydrogen, n is 0, and m is not 3;

or a pharmaceutically acceptable salt, stereoisomer, or solvate thereof.

2. The compound according to claim 1 , wherein R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally having at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 ; or a heteroarylalkyl radical C 1-10 .

3. The compound according to claim 1 , wherein R 1 and R 2 independently represent hydrogen, methyl, ethyl, propyl or a group selected from:

wherein p is 1 or 2.

4. The compound according to claim 1 , wherein R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted by methyl, ethyl, isopropyl, tertbutyl or a group selected from:

wherein R′ is C 1-6 alkyl.

5. The compound according to claim 1 , wherein R 1 and R 2 together with the bridging nitrogen represents one of the following structures:

6. The compound according to claim 4 , wherein R 1 and R 2 together with the bridging nitrogen represents one of the following structures:

7. The compound according to claim 1 , wherein R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl which is condensed or spirofused to another ring or ring system to form one of the following structures:

8. The compound according to claim 1 , which is selected from:

2-((4-(4-tert-butylpiperidin-1-yl)butoxy)methyl)pyrazolo[1,5-a] pyridine maleate;

2-((2-(azepan-1-yl)ethoxy)methyl)pyrazolo[1,5-a]pyridine maleate;

N-(cyclopropylmethyl)-N-propyl-4-(pyrazolo[1,5-a]pyridin-2-ylmethylpyrazolo[1,5-a]pyridin-2-ylmethoxy)butan-1-amine maleate;

2-(4-(pyrazolo[1,5-a]pyridin-2-ylmethylpyrazolo[1,5-a]pyridin-2-ylmethoxy)butyl)-1,2,3,4-tetrahydroisoquinoline maleate;

N-adamantyl-4-(pyrazolo[1,5-a]pyridin-2-ylmethylpyrazolo[1,5-a]pyridin-2-ylmethoxy)butan-1-amine maleate;

1′-(4-(pyrazolo[1,5-a]pyridin-2-ylmethylpyrazolo[1,5-a]pyridin-2-ylmethoxy)butyl)-3H-spiro[isobenzofuran-1,4′-piperidine] maleate;

2-((2-(pyrrolidin-1-yl)ethoxy)methyl)pyrazolo[1,5-a]pyridine maleate;

2-((4-(azepan-1-yl)butoxy)methyl)pyrazolo[1,5-a]pyridine maleate;

2-((4-(4-methylpiperazin-1-yl)butoxy)methyl)pyrazolo[1,5-a]pyridine maleate;

2-((4-(4-cyclohexylpiperazin-1-yl)butoxy)methyl)pyrazolo[1,5-a]pyridine maleate;

1-(4-(4-(pyrazolo[1,5-a]pyridin-2-ylmethylpyrazolo[1,5-a]pyridin-2-ylmethoxy)butyl)piperazin-1-yl)ethanone;

1-benzyl-N-methyl-N-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)piperidin-4-amine difumarate;

4-(2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethyl)morpholine;

2-(2-(piperidin-1-yl)ethoxy)pyrazolo[1,5-a]pyridine oxalate;

2-(2-(pyrrolidin-1-yl)ethoxy)pyrazolo[1,5-a]pyridine oxalate;

N,N-diethyl-2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethanamine oxalate;

4-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)morpholine oxalate;

2-(4-(piperidin-1-yl)butoxy)pyrazolo[1,5-a]pyridine oxalate;

N,N-diethyl-4-(pyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine oxalate;

2-(4-(pyrrolidin-1-yl)butoxy)pyrazolo[1,5-a]pyridine oxalate;

N-benzyl-N-methyl-4-(pyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine oxalate;

N-benzyl-N-methyl-2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethanamine oxalate;

2-(4-(4-(naphthalen-2-yl)piperidin-1-yl)butoxy)pyrazolo[1,5-a]pyridine;

1′-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)-3H-spiro[isobenzofuran-1,4′-piperidine] oxalate;

2-(4-(4-cyclohexylpiperazin-1-yl)butoxy)pyrazolo[1,5-a]pyridine2-(4-(4-cyclohexylpiperazin-1-yl)butoxy)pyrazolo[1,5-a]pyridine dimaleate;

2-(4-(4-tert-butylpiperidin-1-yl)butoxy)pyrazolo[1,5-a]pyridine hydrochloride;

N-methyl-N-phenethyl-4-(pyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine hydrochloride;

N-methyl-4-(pyrazolo[1,5-a]pyridin-2-yloxy)-N-(pyridin-4-ylmethyl)butan-1-amine dihydrochloride;

2-(4-(1,4′-bipiperidin-1′-yl)butoxy)pyrazolo[1,5-a]pyridine difumarate;

2-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)decahydroisoquinoline fumarate;

N-(cyclopropylmethyl)-N-propyl-4-(pyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine maleate;

2-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)-1,2,3,4-tetrahydroisoquinoline maleate;

N-adamantyl-4-(pyrazolo[1,5-a]pyridin-2-yloxy)-butan-1-amine maleate;

2-(4-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)butoxy)pyrazolo[1,5-a]pyridine dimaleate;

2-(2-(4-tert-butylpiperidin-1-yl)ethoxy)pyrazolo[1,5-a]pyridine maleate;

N-methyl-N-phenethyl-2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethanamine maleate;

1-benzyl-N-methyl-N-(2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethyl)piperidin-4-amine dimaleate;

2-(2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethyl)decahydroisoquinoline maleate;

N-(cyclopropylmethyl)-N-(2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethyl)propan-1-amine maleate;

2-(2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethyl)-1,2,3,4-tetrahydroisoquinoline maleate;

2-(2-(1,4′-bipiperidin-1′-yl)ethoxy)pyrazolo[1,5-a]pyridine dimaleate;

2-(2-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)ethoxy)pyrazolo[1,5-a]pyridine dimaleate;

2-(2-(4-cyclohexylpiperazin-1-yl)ethoxy)pyrazolo[1,5-a]pyridine dimaleate;

1′-(2-(pyrazolo[1,5-a]pyridin-2-yloxy)ethyl)-3H-spiro[isobenzofuran-1,4′-piperidine] dimaleate;

2-(4-(azepan-1-yl)butoxy)pyrazolo[1,5-a]pyridine maleate;

N-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)cyclohexanamine maleate;

(4aR,8aS)-2-(4-(pyrazolo[1,5-a]pyridin-2-yloxy)butyl)decahydroisoquinoline maleate;

2-(2-(4-ethylpiperazin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo [1,5-a]pyridine maleate;

2-(2-(azepan-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a] pyridine maleate;

2-(2-(piperidin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine oxalate;

N,N-diethyl-2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethanamine oxalate;

4-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)morpholine oxalate;

4-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)morpholine oxalate;

2-(2-(pyrrolidin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine oxalate;

2-(4-(pyrrolidin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine oxalate;

2-(4-(piperidin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine oxalate;

2-(4-(piperidin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

N,N-diethyl-4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine oxalate;

N-benzyl-N-methyl-2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethanamine oxalate;

2-(4-(4-tert-butylpiperdin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(2-(4-tert-butylpiperidin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

1-benzyl-N-methyl-N-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)piperidin-4-amine dimaleate;

2-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)decahydroisoquinoline maleate;

2-(4-(4-cyclohexylpiperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate:

1′-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)-3H-spiro[isobenzofuran-1,4′-piperidine] maleate;

2-(2-(4-cyclohexylpiperazin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

1-benzyl-N-methyl-N-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)piperidin-4-amine maleate;

2-(2-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

1′-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)-3H-spiro[isobenzofuran-1,4′-piperidine] maleate;

N-adamantyl-2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethanamine maleate;

2-(2-(1,4′-bipiperidin-1′-yl)ethoxy)-4,5,67-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)-1,2,3,4-tetrahydroisoquinoline maleate;

2-(4-(azepan-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate

2-(4-(1,4′-bipiperidin-1′-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

N-(cyclopropylmethyl)-N-propyl-4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine maleate;

(4aR,8aS)-2-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)decahydroisoquinoline maleate;

N-benzyl-N-methyl-4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine maleate;

N-adamantyl-4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butan-1-amine maleate;

2-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)-1,2,3,4-tetrahydroisoquinoline maleate;

N-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)cyclohexanamine maleate;

4-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)thiomorpholine maleate;

(4aR,8aS)-2-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)decahydroisoquinoline maleate;

4-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)-1,4-oxazepane maleate;

4-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)-1,4-oxazepane maleate;

N-(cyclopropylmethyl)-N-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)propan-1-amine maleate;

2-(2-(4-isopropylpiperazin-1-yl)ethoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(4-(4-isopropylpiperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(4-(4-methylpiperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(4-((3S,5R)-3,5-dimethylpiperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

1-(4-(4-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)butyl)piperazin-1-yl)ethanone maleate;

2-(4-(4-methyl-1,4-diazepan-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(3-(4-methylpiperazin-1-yl)propoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(4-(4-ethylpiperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(3-(piperidin-1-yl)propoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

2-(3-(4-cyclohexylpiperazin-1-yl)propoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

4-(3-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)propyl)-1,4-oxazepane;

2-(4-(4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl)butyltetrahydro-2H-pyran-4-yl)piperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

1-(4-(3-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)propyl)piperazin-1-yl)ethanone maleate;

4-(2-(4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)ethyl)thiomorpholine maleate;

2-(4-(4-tert-butylpiperidin-1-yl)butoxy)-3-chloro-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

3-chloro-2-(4-chlorobutoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine from 3-chloro-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-ol;

2-(4-(4-tert-butylpiperidin-1-yl)butoxy)-3-chloro-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine maleate;

N-benzyl-2-(3-iodopyrazolo[1,5-a]pyridin-2-yloxy)-N-methylethanamine oxalate;

N-benzyl-2-(3-iodo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-2-yloxy)-N-methylethanamine oxalate; and

3-chloro-2-(4-(4-cyclohexylpiperazin-1-yl)butoxy)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine.

9. A process for the preparation of a compound of general formula (Ia) or (Ib):

comprising reaction of respectively compounds of formula (IIa) or (IIb):

with a compound of formula (III):

in an organic solvent, in the presence of an organic or inorganic base and optionally in the presence of an activating agent,

wherein

R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 ; or an heteroarylalkyl radical C 1-10 ;

or R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted; by one or more substituents selected from the group consisting of a C 3-6 alkyl group, a linear or branched C 1-6 alkoxy group, —F, —Cl, —I, —Br, —CF 3 , —CH 2 F, —CHF 2 , —CN, —OH, —SH, —NH 2 , oxo, —(C═O)R′, —SR′, —SOR′, —SO 2 R′, —NHR′, —NR′R″,

wherein R′ and R″ at each occurrence independently represents a linear or branched C 1-6 -alkyl group;

or R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C 3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group;

n is 0, 1 or 2;

m is 1, 2, 3 or 4;

and Y is a leaving group.

10. A process for the preparation of a compound of general formula (Ia) or (Ib):

comprising reaction of respectively a compound of formula (IVa) and (IVb):

with a compound of formula (V):

in an organic solvent, in the presence of an organic or inorganic base and optionally in the presence of an activating agent,

wherein

R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 ; or an heteroarylalkyl radical C 1-10 ;

or R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted; by one or more substituents selected from the group consisting of a C 1-6 alkyl group, a linear or branched C 1-6 alkoxy group, —F, —Cl, —I, —Br, —CF 3 , —CH 2 F, —CHF 2 , —CN, —OH, —SH, —NH 2 , oxo, —(C═O)R′, —SR′, —SOR′, —SO 2 R′, —NHR′, —NR′R″,

wherein R′ and R″ at each occurrence independently represents a linear or branched C 1-6 -alkyl group;

or R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C 3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group;

n is 0, 1 or 2;

m is 1, 2, 3 or 4;

and X is a leaving group.

11. A process for the preparation of compounds of general formula (Ic) or (Id):

comprising reaction of respectively a compound of formula (IIc) or (IId):

with a compound of formula (III):

in water or an organic solvent, in the presence of an organic or inorganic base and optionally in the presence of an activating agent,

wherein

R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 ; or an heteroarylalkyl radical C 1-10 ;

or R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted by one or more substituents selected from the group consisting of a C 1-6 alkyl group, a linear or branched C 1-6 alkoxy group, —F, —Cl, —I, —Br, —CF 3 , —CH 2 F, —CHF 2 , —CN, —OH, —SH, —NH 2 , oxo, —(C═)R′, —SR′, —SO 2 R′, —NHR′, —NR′R″,

wherein R′ and R″ at each occurrence independently represents a linear or branched C 1-6 -alkyl group;

or R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C 3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group;

n is 0, 1 or 2;

m is 1, 2, 3 or 4;

and Y is a leaving group.

12. A process for the preparation of a compound of general formula (Ic) or (Id):

comprising reaction of respectively a compound of formula (IVc) or (IVd):

with a compound of formula (V):

in an organic solvent, in the presence of an organic or inorganic base and optionally in the presence of an activating agent,

wherein

R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 ; or an heteroarylalkyl radical C 1-10 ;

or R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted; by one or more substituents selected from the group consisting of a C 1-6 alkyl group, a linear or branched C 1-6 alkoxy group, —F, —Cl, —I, —Br, —CF 3 , —CH 2 F, —CHF 2 , —CN, —OH, —SH, —NH 2 , oxo, —(C═O)R′, —SR′, —SOR′, —SO 2 R′, —NHR′, —NR′R″,

wherein R′ and R″ at each occurrence independently represents a linear or branched C 1-6 -alkyl group;

or R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C 3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group;

n is 0, 1 or 2;

m is 1, 2, 3 or 4;

and X is a leaving group.

13. A process for the preparation of a compound of general formula (Ie):

wherein

R 1 and R 2 independently represent hydrogen; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, aliphatic radical C 1-10 ; a substituted or unsubstituted aryl radical; a substituted or unsubstituted heteroaryl radical; a substituted or unsubstituted C 3-9 cycloalkyl radical optionally containing at least one heteroatom as ring member selected from N, O or S; a cycloalkylalkyl radical C 1-10 ; an arylalkyl radical C 1-10 : or an heteroarylalkyl radical C 1-10 ;

or R 1 and R 2 together with the bridging nitrogen form a C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S and optionally substituted by one or more substituents selected from the group consisting of a C 1-6 alkyl group, a linear or branched C 1-6 alkoxy group, —F, —Cl, —I, —BR, —CF 3 , —CH 2 F, —CHF 2 , —CN, —OH, —SH, —NH 2 , oxo, —(C═O)R′, —SR′, —SOR′, —SO 2 R′, —NHR′, —NR′R″,

wherein R′ and R″ at each occurrence independently represents a linear or branched C 1-6 -alkyl group;

or R 1 and R 2 together with the bridging nitrogen form C 3-9 cycloalkyl optionally having at least one additional heteroatom as a ring member selected from N, O or S, which may be condensed to form a ring system with another C 3-9 cycloalkyl optionally having at least one heteroatom as a ring member selected from N, O or S; or which may be condensed to form a ring system with an aryl radical; or which may be spirofused to an aryl or heteroaryl group;

n is 0, 1 or 2;

m is 1, 2, 3 or 4;

and X is a halogen,

the process comprising the direct halogenation with X 2 or halosuccinimide of a compound of formula (VII):

14. A pharmaceutical composition comprising a compound of general formula (I) according to claim 1 , or a pharmaceutically acceptable salt, stereoisomer, or solvate thereof, and at least a pharmaceutically acceptable carrier, additive, adjuvant or vehicle.