Treeway Tw001 B.v.

Galapagos Nv

Ronald Van Der Geest

Sytske Hyke Moolenaar

Reginald Christophe Xavier Brys

Katja Conrath

Ana Fernandez Casares

Thierry Jean-Claude Marie Christophe

Katja Els Conrath

The present invention discloses compounds according to Formula I: Wherein Ris as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of that may be useful in the prophylaxis and/or treatment of polycystic kidney disease (PKD), by administering the compound of the invention.

Methods for the treatment of polycystic kidney disease

The present invention relates to the use of a liquid aqueous solution of edaravone in the treatment of an oxidative stress-mediated neurodegenerative disorder in a human patient, said treatment comprising at least once daily oral administration of the liquid edaravone solution to the human patient, to provide a daily dose of 40-120 mg edaravone during an uninterrupted period of at least 10 days. Examples of oxidative stress-mediated neurodegenerative disorders that can be treated in this way include amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), cerebral amyloid angiopathy (CAA), Alzheimer's disease and Parkinson's disease.

Use of edaravone in oral treatment of oxidative-stress mediated neurodegenerative disorders

The invention relates to a salt of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone), wherein the salt is 3-methyl-1-phenyl-2-pyrazolin-5-one napadisylate or 3-methyl-1-phenyl-2-pyrazolin-5-one hemi-napadisylate. These napadisylate salts of edaravone are easy to manufacture and dissolve more rapidly in water than the free edaravone base. In addition, the edaravone salts of the present invention are very stable and easy to handle. The invention also relates to a pharmaceutical composition comprising the aforementioned edaravone salt and to a method of preparing such edaravone salt.

Edaravone salt

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Rotterdam, Netherlands

Ronald Van Der Geest