Triterpenoids with HIV maturation inhibitory activity

US10780102B2 · kind B2 · utility

Assignee

• ViiV Healthcare UK (No.5) Limited · GB

Inventors

• Sing-Yuen Sit · Meriden, US
• Yan Chen · Foster City, US
• Jie Chen · Houston, US
• Jacob Swidorski · Wallingford, US
• Brian Lee Venables · Durham, US
• Ny Sin · East Hampton, US
• Nicholas A. Meanwell · East Hampton, US
• Alicia Regueiro-Ren · Wallingford, US
• Richard A. Hartz · Kennett Square, US
• Li Xu · Middletown, US
• Zheng Liu · Beacon Falls, US

Key dates

• Filing date: Jan 22, 2019
• Grant date: Sep 22, 2020
• Expiry date: Jan 22, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/16
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.