Sulfoximine substituted quinazolines for pharmaceutical compositions US 20150005278 (A1): a patent evaluation. (2nd August 2016)

• Record Type: Journal Article
• Authors: Gopaul, Kaalin; Koorbanally, Neil A.
• Is Part Of: Expert opinion on therapeutic patents. Volume 26:Number 8(2016:Aug.)
• Page Start: 861
• Page End: 869
• Publication Date: 2016-08-02
• Subjects: Mnk inhibitors -- Mnk1 -- Mnk2 -- quinazoline -- sulfoximine; Drugs -- Patents -- Periodicals; 615.10272
• DOI: 10.1080/13543776.2016.1180366
• Languages: English
• ISSNs: 1354-3776

Abstract

ABSTRACT: Mnk1 and Mnk2 are protein kinases responsible for phosphorylating eIF4E, a eukaryotic initiation factor responsible for initiating translation. Inhibiting Mnk1 and Mnk2 could therefore play a role in treating metabolic diseases such as cancer, diabetes, and hyperlipidemia. A wide range of sulfoximine substituted quinazolines were synthesised and evaluated for their Mnk1 and Mnk2 inhibitory activity. Amongst these compounds, 26 quinazolines showed activity against Mnk1 at <100 nM and 54 showed activity against Mnk2 at 1 nM. The results indicate that this scaffold is much more active against Mnk2 than Mnk1. The synthesised compounds may be future drugs in the treatment of metabolic diseases.