Invention Grant
- Patent Title: Heterocycle-bisamide inhibitors of scavenger receptor BI
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Application No.: US14436610Application Date: 2013-10-21
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Publication No.: US09884851B2Publication Date: 2018-02-06
- Inventor: Chris Dockendorff , Andrew Germain , Partha Pratim Nag , Willmen Youngsaye , Sivaraman Dandapani , Benito Munoz , Patrick Faloon , Thomas Nieland , Monty Krieger , Miao Yu
- Applicant: THE BROAD INSTITUTE, INC. , MASSACHUSETTS INSTITUTE OF TECHNOLOGY
- Applicant Address: US MA Cambridge US MA Cambridge
- Assignee: Massachusetts Institute Of Technology,The Broad Institute, Inc.
- Current Assignee: Massachusetts Institute Of Technology,The Broad Institute, Inc.
- Current Assignee Address: US MA Cambridge US MA Cambridge
- Agency: Pepper Hamilton LLP
- Agent Thomas J. Engellenner; Reza Mollaaghababa
- International Application: PCT/US2013/065991 WO 20131021
- International Announcement: WO2014/063168 WO 20140424
- Main IPC: C07D257/04
- IPC: C07D257/04 ; C07D261/08 ; C07D263/32 ; C07D277/30 ; C07D405/04 ; C07D405/14

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.
Public/Granted literature
- US20150284371A1 HETEROCYCLE-BISAMIDE INHIBITORS OF SCAVENGER RECEPTOR BI Public/Granted day:2015-10-08
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