Patent

1. A compound having formula (I)

and the salts and stereoisomers thereof, wherein

R 1 is hydrogen, nitro, cyano, azido, polyhaloC 1-6 alkyl, and polyhaloC 1-6 alkoxy;

R 2 is C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; C 2-6 alkenyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; aryl; Het; or —NR 4a R 4b , wherein R 4a and R 4b are, each independently, C 1-6 alkyl, or R 4a and R 4b together with the nitrogen to which they are attached form a 5- or 6-membered saturated heterocyclic ring;

R 3 is hydrogen, C 1-6 alkylcarbonyl, C 1-6 alkyl optionally substituted with aryl, C 1-6 alkoxy -C 1-6 alkyl, or C 3-7 cycloalkyl, C 1-6 alkyl optionally substituted with Het;

R 4 is hydrogen, hydroxy, halo, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxy -C 1-6 alkyl or C 3-7 cycloalkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1-6 alkylamino, azido, mercapto, polyhaloC 1-6 alkyl, and polyhaloC 1-6 alkoxy, C 1-6 alkyl optionally substituted with aryl or Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; C 2-6 alkenyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; aryl; Het; or —NR 4a R 4b ,wherein R 4a and R 4b are, each independently, C 1-6 alkyl, or R 4a and R 4b together with the nitrogen to which they are attached form a 5- or 6-membered saturated heterocyclic ring;

n is one, two, three, four or five;

p is one, two, three, four or five, independently of n;

each aryl as a group or part of a group is phenyl or naphthalenyl, each optionally substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1-6 alkylamino, azido, mercapto, polyhaloC 1-6 alkyl, and polyhaloC 1-6 alkoxy; and

each Het as a group or part of a group is a monocyclic ring with 5 or 6 ring atoms or a bicyclic ring structure comprising a 6 membered ring fused to a 4, 5, or 6 membered ring; each of the rings being saturated, partially unsaturated, or completely unsaturated; at least one of the rings containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulphur; and any one of the rings being optionally substituted with one, two or three substituents each independently selected from the group consisting of halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1-6 alkylamino, azido, mercapto, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkoxy, and C 3-7 cycloalkyl.

2. A compound according to claim 1 , wherein

R 1 is hydrogen, nitro, cyano, azido, polyhaloC 1-6 alkyl, and polyhaloC 1-6 alkoxy;

R 2 is C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; C 2-6 alkenyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; aryl; Het; or —NR 4a R 4b ,wherein R 4a and R 4b are, each independently, C 1-6 alkyl, or R 4a and R 4b together with the nitrogen to which they are attached form a 5- or 6-membered saturated heterocyclic ring;

R 3 is hydrogen, C 1-6 alkylcarbonyl, C 1-6 alkyl optionally substituted with aryl, C 1-6 alkoxy -C 1-6 alkyl, or C 3-7 cycloalkyl, C 1-6 alkyl optionally substituted with Het;

R 4 is hydrogen;

n is one, two, three, four or five;

p is one;

each aryl as a group or part of a group is phenyl or naphthalenyl, each optionally substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1-6 alkylamino, azido, mercapto, polyhaloC 1-6 alkyl, and polyhaloC 1-6 alkoxy; and

each Het as a group or part of a group is a monocyclic ring with 5 or 6 ring atoms or a bicyclic ring structure comprising a 6 membered ring fused to a 4, 5, or 6 membered ring; each of the rings being saturated, partially unsaturated, or completely unsaturated; at least one of the rings containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulphur; and any one of the rings being optionally substituted with one, two or three substituents each independently selected from the group consisting of halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1-6 alkylamino, azido, mercapto, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkoxy, and C 3-7 cycloalkyl.

3. A compound according to claim 1 , wherein R 1 is hydrogen;

R 2 is C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; C 2-6 alkenyl optionally substituted with C 3-7 cycloalkyl, aryl or Het; aryl and Het;

R 3 is hydrogen, C 1-6 alkyl and C 1-6 alkylcarbonyl;

R 4 is hydrogen;

n is one or two;

p is one;

each aryl as a group or part of a group is phenyl or naphthalenyl, each optionally substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1-6 alkylamino, azido, mercapto, polyhaloC 1-6 alkyl, and polyhaloC 1-6 alkoxy; and

each Het as a group or part of a group is a monocyclic ring with 5 or 6 ring atoms or a bicyclic ring structure comprising a 6 membered ring fused to a 4, 5, or 6 membered ring; each of the rings being saturated, partially unsaturated, or completely unsaturated; at least one of the rings containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulphur; and any one of the rings being optionally substituted with one, two or three substituents each independently selected from the group consisting of halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, amino, mono- or diC 1- 6 alkylamino, azido, mercapto, polyhalo C 1-6 alkyl, polyhaloC 1-6 alkoxy, and C 3-7 cycloalkyl.

4. A compound according to any one of claims 1 - 3 , wherein

R 1 is hydrogen;

R 2 is C 2-6 alkenyl optionally substituted with aryl or Het; aryl; or Het;

R 3 is hydrogen;

R 4 is hydrogen;

n is one or two;

p is one;

each aryl as a group or part of a group is phenyl or naphthalenyl, each optionally substituted with one or two substituents selected from halo, amino, mono- or diC 1-6 alkylamino, and polyhaloC 1-6 alkyl; and

each Het as a group or part of a group is a monocyclic ring with 5 or 6 ring atoms or a bicyclic ring structure comprising a 6 membered ring fused to a 4, 5, or 6 membered ring; each of the rings being saturated, partially unsaturated, or completely unsaturated; at least one of the rings containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulphur; and any one of the rings being optionally substituted with one or two substituents each independently selected from the group consisting of halo and polyhaloC 1-6 alkyl.

5. A process for preparing a compound having formula (I)

as claimed in claim 1 , said process comprising the step of

a) reacting in a suitable medium a compound of formula (II) with a compound of formula (III)

and

b) optionally further comprising the step of reacting in a suitable medium the product of step

a) with R 3 —Y;

wherein

R 1 , R 2 , R 3 , R 4 , n and p have the same definition as provided in of claim 1 ;

LG is an halogen atom;

Y is an activating group in coupling reactions or a leaving group in substitution reactions, wherein, in substitution reactions Y is an halogen atom;

wherein in coupling reactions Y is an activated carboxyl derivative, or an active ester,

wherein the suitable medium of the reaction in step a) is anhydrous or non anhydrous chlorinated solvent, or a hydrous or anhydrous polar aprotic solvent, at a temperature between 0° C. and 40° C.,

wherein the suitable medium of the reaction in step b) is in the presence of an inorganic or organic base, at a temperature between −78° C. and 60° C., and wherein the reaction solvent is a polar aprotic solvent.