IP Library Granted Patent US 10,189,830
Granted Patent B2
US 10,189,830 · App. 14/776,678 · Granted Jan 29, 2019

Alkyl-heteroaryl substituted quinone derivatives for treatment of oxidative stress disorders

Inventors: Andrew W. Hinman (San Francisco, CA); Kieron E. Wesson (Burlingame, CA); Christopher R. Cornell (Mountain View, CA)
Assignee: BIOELECTRON TECHNOLOGY CORPORATION
C07D471/04C07D233/60C07D233/64C07D235/06C07D235/12C07D249/08C07D263/32C07D263/56C07D263/57C07D277/24C07D277/64C07D403/10
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Quick Facts
Patent No.
US 10,189,830
App. No.
14/776,678
Granted
Jan 29, 2019
Kind
B2
Abstract

Disclosed herein are alkyl-heteroaryl substituted quinone derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.

Claims (23)

1. A compound of Formula I or Formula II:

wherein:

R 1 , R 3 and R 4 are independently C 1 -C 6 alkyl or O—C 1 -C 6 alkyl;

R 2 is heteroaryl selected from the group consisting of benzoimidazole, benzothiazole, and benzoxazole, optionally substituted with one or two substituents independently selected from the group consisting of halo, —CH 3 , —CF 3 , —OCH 3 , and —C(O)—N(R 5 )(R 6 ), wherein the substituents are independently linked to the heteroaryl by either a —C— or —N—within the heteroaryl; where the attachment point of the heteroaryl group to the rest of the molecule is either through a C or N in the rings;

R 5 and R 6 are independently selected from the group consisting of —H, —C 1 -C 6 alkyl, and —C 1 -C 6 alkyl-hydroxy, or wherein R 5 and R 6 together with the N to which they are attached form a saturated or unsaturated 3-8 membered ring, optionally incorporating one, two, or three additional heteroatoms each independently selected from the group consisting of N, O, and S, and wherein the ring is optionally substituted with —C 1 -C 6 alkyl; and

z is 3;

or a stereoisomer, mixture of stereoisomers, solvate, hydrate, pharmaceutically acceptable salt or prodrug ester thereof.

2. The compound of claim 1 , wherein:

R 2 is heteroaryl optionally substituted with one or two substituents independently selected from the group consisting of halo, —CH 3 , —CF 3 , and —OCH 3 , wherein the substituents are independently linked to the heteroaryl by either a —C— or —N— within the heteroaryl.

3. The compound of claim 1 , wherein R 1 , R 3 and R 4 are independently C 1 -C 4 alkyl.

4. The compound of claim 1 , wherein R 1 , R 3 and R 4 are independently C 1 -C 2 alkyl.

5. The compound of claim 1 , wherein R 1 , R 3 and R 4 are —CH 3 .

6. The compound of claim 1 , wherein R 1 and R 4 are independently —O—C 1 -C 2 alkyl, and R 3 is C 1 -C 4 alkyl.

7. The compound of claim 1 , wherein R 1 and R 4 are —OCH 3 , and R 3 is —CH 3 .

8. The compound of claim 1 , wherein the compound is a compound of Formula I, or a stereoisomer, mixture of stereoisomers, solvate, hydrate, or pharmaceutically acceptable salt thereof.

9. The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug ester thereof.

10. The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug ester thereof.

11. A pharmaceutical formulation comprising a compound according to claim 1 and a pharmaceutically acceptable excipient.

12. The compound of claim 1 , wherein R 2 is benzoimidazole optionally substituted with one or two substituents independently selected from the group consisting of halo, —CH 3 , —CF 3 , —OCH 3 , and —C(O)—N(R 5 )(R 6 ), wherein the substituents are independently linked to the benzoimidazole by either a —C— or —N— within the benzoimidazole.

13. The compound of claim 1 , wherein R 2 is benzothiazole optionally substituted with one or two substituents independently selected from the group consisting of halo, —CH 3 , —CF 3 , —OCH 3 , and —C(O)—N(R 5 )(R 6 ), wherein the substituents are independently linked to the benzothiazole by either a —C— or —N— within the benzothiazole.

14. The compound of claim 1 , wherein R 2 is benzoxazole optionally substituted with one or two substituents independently selected from the group consisting of halo, —CH 3 , —CF 3 , —OCH 3 , and —C(O)—N(R 5 )(R 6 ), wherein the substituents are independently linked to the benzoxazole by either a —C— or —N— within the benzoxazole.

Assignments (4)
TERMINATION AND RELEASE OF PATENT SECURITY AGREEMENT @ REEL 061803 AND FRAME 0878 Recorded Oct 20, 2023
From: WILMINGTON TRUST, NATIONAL ASSOCIATION, AS ADMINISTRATIVE AGENT
To: PTC THERAPEUTICS, INC.
Reel/Frame 065303/0163 →
SECURITY INTEREST Recorded Oct 28, 2022
From: PTC THERAPEUTICS, INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 061803/0878 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 15, 2019
From: BIOELECTRON TECHNOLOGY CORPORATION
To: PTC THERAPEUTICS, INC.
Reel/Frame 051041/0478 →
CHANGE OF NAME Recorded Feb 8, 2017
From: EDISON PHARMACEUTICALS, INC.
To: BIOELECTRON TECHNOLOGY CORPORATION
Reel/Frame 041660/0644 →
Continuity (2)
Provisional Application 61798937 · Mar 15, 2013
Related Publication 20160024085A1 · Jan 28, 2016