IP Library Granted Patent US 10,398,681
Granted Patent B2
US 10,398,681 · App. 15/883,750 · Granted Sep 3, 2019

Compounds and compositions that bind and stabilize transthyretin and their use for inhibiting transthyretin amyloidosis and protein-protein interactions

Inventors: Isabella A. Graef (Woodside, CA); Mamoun M. Alhamadsheh (Fremont, CA)
Assignee: The Board of Trustees of the Leland Stanford Junior University
A61K31/415C07D231/12C07D237/08
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Quick Facts
Patent No.
US 10,398,681
App. No.
15/883,750
Granted
Sep 3, 2019
Kind
B2
Abstract

Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.

Claims (9)

1. A kit comprising a unit dose of Compound VIIa:

wherein

R a is selected from the group consisting of OH, CHO, COOH, CONH 2 , CONH(OH), COOR 6 , and CONHR 6 ; and

R 6 is straight or branched alkyl of 1-3 carbon atoms;

or a pharmaceutically acceptable salt thereof.

2. The kit of claim 1 , further comprising a package insert describing the use of Compound VIIa.

3. The kit of claim 1 , wherein R a is selected from the group consisting of COOH CONH 2 , CONH(OH), COOR 6 , and CONHR 6 .

4. The kit of claim 1 , wherein Compound VIIa has a structure of Compound VIIc

or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 5, 2018
From: GRAEF, ISABELLA A.; ALHAMADSHEH, MAMOUN M.
To: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Reel/Frame 046789/0566 →
Continuity (5)
Continuation 15480139 · Apr 5, 2017
Continuation 14876447 · Oct 6, 2015
Continuation 13830731 · Mar 14, 2013
Provisional Application 61745089 · Dec 21, 2012
Related Publication 20190000805A1 · Jan 3, 2019
Cited By (1)
US 12,539,290