IP Library Granted Patent US 9,951,055
Granted Patent B2
US 9,951,055 · App. 14/436,626 · Granted Apr 24, 2018

Thiazole-based inhibitors of scavenger receptor BI

Inventors: Chris Dockendorff (Milwaukee, WI); Willmen Youngsaye (Cumberland, RI); Partha Pratim Nag (Somerville, MA); Timothy A. Lewis (Marlborough, MA); Sivaraman Dandapani (Malden, MA); Benito Munoz (Newtonville, MA); Patrick Faloon (Cambridge, MA); Thomas Nieland (Somerville, MA); Monty Krieger (Needham, MA); Miao Yu (Quincy, MA)
Assignees: Massachusetts Institute of Technology; The Broad Institute, Inc.
C07D417/04C07D277/44C07D417/12C07D417/14C07D491/048
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Quick Facts
Patent No.
US 9,951,055
App. No.
14/436,626
Granted
Apr 24, 2018
Kind
B2
Abstract

This application describes compounds and methods that can inhibit Scavenger receptor class B, type I (SR-BI) activity, which compounds and methods can used, for example, to mediate high-density lipoprotein (HDL) lipid uptake and treat hepatitis C viral infections.

Claims (16)

1. A compound of the formula:

or a salt or solvate thereof.

2. A compound of the formula:

or a salt or solvate thereof.

3. A method of inhibiting Scavenger receptor class B, type I (SR-BI) lipid transport activity comprising exposing said receptor to a compound of the formula

or a salt or solvate thereof.

4. A method of inhibiting Scavenger receptor class B, type I (SR-BI) lipid transport activity comprising exposing said receptor to a compound of the formula:

or a salt or solvate thereof.

5. The method of claim 3 or 4 , wherein said lipid transport activity is determined by measuring the binding of 125 I-HDL or Alexa-labeled HDL to cells.

6. The method of claim 3 or 4 , wherein said method comprises increasing the strength of binding of high-density lipoprotein (HDL) to cells.

7. The method of claim 3 or 4 , wherein said method comprises inhibiting SR-BI transport of cholesteryl ester or other lipids from high-density lipoprotein (HDL) into cells expressing SR-BI.

8. The method of claim 3 or 4 , wherein said method comprises inhibiting transport of cholesterol or other lipids from cells expressing SR-BI into high-density lipoprotein (HDL).

9. A method of treating a hepatitis C viral infection, comprising administering to a subject in need thereof an effective amount of a compound of the formula:

or a salt or solvate thereof.

10. A method of treating a hepatitis C viral infection, comprising administering to a subject in need thereof an effective amount of a compound of the formula:

or a salt or solvate thereof.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2017
From: DOCKENDORFF, CHRIS; YOUNGSAYE, WILLMEN; NAG, PARTHA PRATIM; LEWIS, TIMOTHY A.; DANDAPANI, SIVARAMAN; MUNOZ, BENITO; FALOON, PATRICK; NIELAND, THOMAS
To: THE BROAD INSTITUTE, INC.
Reel/Frame 044390/0588 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 4, 2017
From: DOCKENDORFF, CHRIS; YOUNGSAYE, WILLIAM; NAG, PARTHA PRATIM; LEWIS, TIMOTHY A.; DANDAPANI, SIVARAMAN; MUNOZ, BENITO; FALOON, PATRICK; NIELAND, THOMAS
To: THE BROAD INSTITUTE, INC.
Reel/Frame 044291/0500 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 16, 2017
From: KRIEGER, MONTY; YU, MIAO
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 044156/0708 →
CONFIRMATORY LICENSE Recorded Nov 2, 2015
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 037022/0629 →
Continuity (2)
Provisional Application 61716136 · Oct 19, 2012
Related Publication 20160060254A1 · Mar 3, 2016