4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections

US12049461B2 · kind B2 · utility

Assignee

• Gilead Sciences, Inc. · US

Inventors

• Ling-Jie Gao · Bierbeek, BE
• Piet Herdewijn · Heverlee, BE
• Steven De Jonghe · Brussels, BE
• William J. Watkins · Saratoga, US
• Lee S. Chong · Newark, US

Key dates

• Filing date: Nov 17, 2020
• Grant date: Jul 30, 2024
• Expiry date: Mar 27, 2041

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.