Stichting Katholieke Universiteit

Compound Handling B.v.

Sirik Deerenberg

Jacobus Antonius Schalken

Dennis Patrick Piet

Petrus Emmanuel Marie Maas

Siu Ha Tang

Johann Heinrich Tijhuis

Onno Van Hooij

Hendrik Engelbertus Vietor

Nanda Elisabeth Sprenkels

Petrus Emmanuel Maas

Van Onno Hooij

Hendrik Engelbertus VIËTOR

A compound having the structure according to formula III wherein:

Aminomethylene pyrazolones with therapeutic activity

A compound having the structure according to formula III wherein: X is NH or S; Ris H or (1C-4C)alkyl; Ris (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N&#x2014;, O&#x2014; or S&#x2014; 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; Rand Rare 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&#x2014;, O&#x2014; or S&#x2014; atoms in the ring, a monocyclic non-aromatic ring having one or more N&#x2014;, O&#x2014; or S&#x2014; atoms in the ring, each optionally 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&#x2014;, O&#x2014; or S&#x2014; atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, halogen, nitro or (1C-2C)dioxol forming a ring; or Rand Rform together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1C-6C)alkyl, phenyl(1C-4C)alkyl, phenylketo(1C-4C)alkyl; Ris H, Cl, F, Br, Me, NO, t-butyl, OCF, OCH, CF; Ris H, (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, nitro or halogen; Ris H, F, Cl, Br, Me, NO, t-butyl, OCF, OCH, CF; or pharmaceutically acceptable addition salts thereof for use in treatments of carcinoma, in particular to delay, prevent or reverse metastasis in prostate cancer. 

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Delft, Netherlands

Sirik Deerenberg