Aminomethylene pyrazolones with therapeutic activity

摘要

The invention provides for a compound having the structure according to formula I
wherein:
X is NH or S; R 1 is H or (1C-4C)alkyl; R 2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O- or S- atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy , phenylthio, halogen, or nitro; R 3 and R 4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S- atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S- atoms in the ring, each optionally further substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1 C-4C)alkyl, (1 C-4C)alkyloxy, halo(1 C-4C)alkyl, halo(1 C-4C)alkyloxy, halogen, nitro or (1 C-2C)dioxol forming a ring; or R 3 and R 4 form together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1 C-6C)alkyl, phenyl(1 C-4C)alkyl, phenylketo(1C-4C)alkyl; R 5 is H or CF 3 ; R 6 is (1 C-4C)alkyl, (1 C-4C)alkyloxy, halo(1 C-4C)alkyl, halo(1 C-4C)alkyloxy, nitro or halogen; for use in treatments of carcinoma, in particular to delay, prevent or reverse metastasis in prostate cancer.