Substituted 3 (5) -ureido-pyrazole, process for their preparation and their use as antitumor agents.

A 3-ureido-pyrazole derivative represented by formula (I): wherein R is a C1-C6 alkyl, aryl or arylalkyl being optionally substituted with one or more hydroxy, halogen, nitro, cyano, oxo , carboxy, amino, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonylamino, alkoxycarbonylalkylamino, aminocarbonylalkylamino, N-alkyl-N-carbonylamino, N-cycloalkyl-N-alkylaminoalkyl, aminoalkyl, aminocarbonyl, alkyl, cycloalkyl, alkylthio, alkoxy, alkylcarbonyl, alkylsulfonyl, alkylsulfonylamino , aminosulfonyl, alkoxycarbonyl, aryl, aryl, aryloxy, arylthio, arylsulfonyl, arylamino, arylcarbonyl, N-alkyl-piperazinyl, 4-morpholinyl, C1-C4 perfluorinated C2-C4, C2-C4, aminoalkynyl C2-C4 or hydroxyalkynyl C2-C4; R1 is - (CH2) n-R3; n is 0 or an integer of 1 to 4; R3 is hydrogen, hydroxy, amino, or a group selected from the group consisting of cycloalkyl, aryl and heterocyclyl, which is optionally substituted by one or more hydroxy, halogen, nitro, cyano, oxo, carboxy, amino, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonylamino, alkoxycarbonylalkylamino, aminocarbonylalkylamino, N-alkyl-N-carbonylamino, N-cycloalkyl-N-alkylaminoalkyl, aminoalkyl, aminocarbonyl, alkyl, cycloalkyl, alkylthio, alkoxy, alkylcarbonyl, alkylsulfonyl, alkylsulfonylamino, aminosulfonyl, alkoxycarbonyl, aryl, arylalkyl, aryloxy, arylthio, arylsulphonyl, arylamino, arylcarbonyl, N-alkyl-piperazinyl, 4-morpholinyl, C1-C4 perfluorinated alkyl, C2-C4 alkenyl, C2-C4 alkyl, aminoalkynyl C2-C4 or hydroxyalkynyl C2-C4; R2 is hydrogen, or R2 and R1, together with the nitrogen atom to which they are attached form a heterocyclyl or heteroaryl group which is optionally substituted with one or more hydroxy, halogen, nitro, cyano, oxo, carboxy, amino, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonylamino, alkoxycarbonylalkylamino, aminocarbonylalkylamino, N-alkyl-N-carbonylamino, N-cycloalkyl-N-alkylaminoalkyl, aminoalkyl, aminocarbonyl, alkyl, cycloalkyl, alkylthio, alkoxy, alkylcarbonyl, alkylsulfonyl, alkylsulfonylamino, aminosulfonyl, alkoxycarbonyl, aryl, arylalkyl, aryloxy, arylthio, arylsulphonyl, arylamino, arylcarbonyl, N-alkyl-piperazinyl, 4-morpholinyl, C1-C4 perfluorinated alkyl, C2-C4 alkenyl, C2-C4 alkyl, aminoalkynyl C2-C4 or hydroxyalkynyl C2-C4; or a pharmaceutically acceptable salt thereof; with the proviso that when n is 0 and R2 is hydrogen, R is a C3-C6 optionally substituted with an alkyl group linear or branched C1-C6.