Fused tricyclic benzimidazoles derivatives as modulators of TNF activity

US9932343B2 · kind B2 · utility

Assignee

• UCB BIOPHARMA SRL · BE

Inventors

• Rikki Peter Alexander · Slough, GB
• Mark Daniel Calmiano · Slough, GB
• Sabine Defays · Brussels, BE
• Veronique Durieu · Brussels, BE
• Michael Deligny · Brussels, BE
• Jag Paul Heer · Brussels, BE
• Victoria Elizabeth Jackson · Slough, GB
• Jean Keyaerts · Brussels, BE
• Boris Kroeplien · Slough, GB
• Malcolm Mac Coss · Seabrook Island, US
• Yogesh Anil Sabnis · Sandwich, GB
• Matthew Duncan Selby · Sandwich, GB
• Dominique Swinnen · Braine-l'Alleud, BE
• Nathalie Van Houtvin · Brussels, BE
• Zhaoning Zhu · Plainsboro, US
• Uwe Heinelt · Wiesbaden, DE
• Volkmar Wehner · Bischofsheim a.d.Rhön, DE

Key dates

• Filing date: Dec 8, 2014
• Grant date: Apr 3, 2018
• Expiry date: Dec 8, 2034

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D519/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A series of tricyclic benzimidazole derivatives, in particular dihydro-1H-imidazo [1,2-a]benzimidazole, dihydro-1H-pyrrolo [1,2-a]benzimidazole, dihydro-1H-pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.