Bicyclic-compounds for use as a medicament, in particular for treatment of parkinson's disease

US11008282B2 · kind B2 · utility

Inventors

• Hubert Koester · Morcote, CH
• Lisa Von Kleist · Berlin, DE
• Simon MICHAELIS · Berlin, DE
• Kathrin Bartho · Dreieich, DE
• Marén Schlief · Berlin, DE
• Mathias Dreger · Berlin, DE
• Anna K. Schrey · Berlin, DE
• Michael Sefkow · Potsdam, DE
• Friedrich Kroll · Schneverdingen, DE
• Daniel Ohlendorf · Berlin, DE
• Yan Luo · Taipei, TW

Key dates

• Filing date: Dec 19, 2016
• Grant date: May 18, 2021
• Expiry date: Dec 19, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2602/10
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to novel small molecule compounds having a basic structure as depicted by formula (A), where in particular exemplary embodiments R1 is —OH, R2 is —NO2 and R3 is H, R4 and R5 are H, one of R6 and R7 is selected from H, —CONH2, and —CONR92, and the other one is selected from —CONR92 and —CONR11R9, wherein R9 and R11 are (possibly multiply) substituted alkyl and H or alkyl, respectively. The compounds of the invention inhibit the enzyme Catechol-O-methyltransferase (COMT) and exhibit a low off-target profile. The compounds are provided for use as a medicament, in particular for use in prevention or treatment of Parkinson's disease.