Heterocycle-bisamide inhibitors of scavenger receptor BI

US9884851B2 · kind B2 · utility

Assignees

• Massachusetts Institute of Technology · US
• The Broad Institute, Inc. · US

Inventors

• Chris Dockendorff · Milwaukee, US
• Andrew Germain · Somerville, US
• Partha P. Nag · Somerville, US
• Willmen Youngsaye · Boston, US
• Sivaraman Dandapani · Malden, US
• Benito Munoz · San Diego, US
• Patrick Faloon · Cambridge, US
• Thomas Nieland · Somerville, US
• Monty Krieger · Needham, US
• Miao Yu · Quincy, US

Key dates

• Filing date: Oct 21, 2013
• Grant date: Feb 6, 2018
• Expiry date: Oct 21, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This application describes compounds and methods that can inhibit Scavenger receptor class B, type I (SR-BI) activity, which compounds and methods can be used, for example, to mediate high-density lipoprotein (HDL) lipid uptake and treat hepatitis C viral infections. The compounds have the formula: wherein R1 and R2 are independently H, halogen, cyano, haloalkyl, haloalkyloxy or OMe; or R1 and R2 together are —O—CH2— or —O—CF2—O—; R3 is H, halogen, cyano, haloalkyl or haloalkyloxy; R4 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylmethyl or C3-6cycloheteroalkyl, wherein the heteroatom is N or O; R5 is H or CH3; R6 is C1-6alkyl or C3-6cycloalkyl; and A, B, D and E are each, independently, CH, N, O or S, wherein at least one of A, B, D and E is N, and another of A, B, D and E is N, O or S.