Politechnika Gdanska

Zaklady Farmaceutyczne Polpharma S.a.

Janusz Rachon

Robert Rynkiewicz

Roman Szramka

Leszek Dembkowski

Slawomir Makowiec

Mariusz Krzyzanowski

Zdzislaw Roznerski

Daniel Zyla

Mateusz Dasko

Sebastian Demkowicz

The present invention relates to 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives and derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol as new compounds. The subject of the invention is the medical use of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives and the medical use of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol derivatives. The subject of the invention is the use of new compounds as an agent with the properties of a steroid sulfatase inhibitor and/or an estrogen receptor modulator. The present invention relates to the medical use of novel compounds for use as an antimicrobial medicament and/or estrogen receptor modulator. In particular, 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives are for use as medicament in cancer therapy. The invention also relates to a process for the preparation of these new compounds, wherein the derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol are the intermediate product from which the sulfamate derivatives are obtained.

Sulfamate derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol, derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol, their medical use and the method of obtaining 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives

A process for the preparation of [1-hydroxy-2-(1-imidazol-1-yl)-ethylidene]bisphosphonic acid consists of the reaction of aqueous solution of 1H-imidazole-1-acetic acid hydrochloride with phosphorus trichloride followed by removal of the excess of phosphorus trichloride, addition of water and hydrolysis of the reaction products. In order to isolate the product the post-reaction mixture is filtered and the anti-solvent is added to the aqueous filtrate in order to crystallize out [1-hydroxy-2-(1-imidazol-1-yl)-ethylidene]bisphosphonic acid monohydrate.

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Janusz Rachon