IP Library Granted Patent US 11,312,703
Granted Patent B2
US 11,312,703 · App. 17/096,713 · Granted Apr 26, 2022

Reactive oxygen species scavengers and use for treating diseases

Inventors: Jia-Ning Xiang (Wuhan, CN); Zude Qi (Wuhan, CN); Dezheng Ning (Wuhan, CN); Xianbo Liu (Wuhan, CN)
Assignee: XWPHARMA LTD.
C07D403/12C07D403/14
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Quick Facts
Patent No.
US 11,312,703
App. No.
17/096,713
Granted
Apr 26, 2022
Kind
B2
Abstract

A compound of Formula (I), pharmaceutically acceptable salts thereof, and individual enantiomers or diastereomers thereof. Compositions and methods useful for treatment or suppression of diseases, developmental delays and symptoms related to oxidative stress.

Claims (37)

1. A method of treating ischemia in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound selected from:

or a pharmaceutically acceptable salt of any of the foregoing.

2. The method of claim 1 , wherein the compound is selected from:

methyl (2S)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-5-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)pentanoate (III):

tert-butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-1-carbamoyl-4-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino-)butyl] carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXVIII):

(2S)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-5-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)pentanoate (XXIX):

propan-2-yl (2S)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-5-({[(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)pentanoate (XXX):

propan-2-yl (2S)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-6-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)hexanoate (XXXI):

propan-2-yl (2S)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-6-[(1-oxyl-2,2,5,5-tetramethylpyrrolidin-3-yl)formamido]-hexanoate (XXXII):

(2R)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-6-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)hexanoate (XXXIII):

(2R)-2-{[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy)carbonyl]amino}-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-6-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)hexanoic acid (XXXIV):

or a pharmaceutically acceptable salt of any of the foregoing.

3. The compound of claim 1 , wherein the compound is selected from:

(tert-butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-1-(diethylcarbamoyl)-4-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)-butyl]carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXXV):

(tert-butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-1-(tert-butylcarbamoyl)-5-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)pentyl]-carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXXVI):

butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-5-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)-1-[(propan-2-yl)carbamoyl]pentyl]carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXXVII):

((S)-methyl 2-((S)-2-((S)-1-((2S,5S,E)-2-benzyl-5-((tert-butoxycarbonyl)amino)-7-methyloct-3-enoyl)pyrrolidine-2-carboxamido)-3-methylbutanamido)-5-((((1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy)carbonyl)amino)pentanoate (XXXVIII):

((S)-methyl 2-((S)-2-((S)-1-((2S,5S,E)-2-benzyl-5-((tert-butoxycarbonyl)amino)-7-methyloct-3-enoyl)pyrrolidine-2-carboxamido)-3-methylbutanamido)-5-((((1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy)carbonyl)amino)pentanoate (XXXIX):

(tert-butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-4-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)-1-[(propan-2-yl) carbamoyl]butyl]carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXXXIV):

(tert-butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-4-({[(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)-1-[(propan-2-yl) carbamoyl]butyl]carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXXXV):

((S)-cyclohexyl 2-((R)-1-((2S,5S,E)-2-benzyl-5-((tert-butoxycarbonyl)amino)-7-methyloct-3-enoyl)pyrrolidine-2-carboxamido)-6-((((1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy)carbonyl)amino)hexanoate (XXXXVI):

tert-butyl N-[(4S,5E,7S)-7-benzyl-8-[(2S)-2-{[(1S)-1-{[(1S)-4-({[(1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)-1-[(propan-2-yl)carbamoyl]butyl]carbamoyl}-2-methylpropyl]carbamoyl}pyrrolidin-1-yl]-2-methyl-8-oxooct-5-en-4-yl]carbamate (XXXXVII):

or a pharmaceutically acceptable salt of any of the foregoing.

4. The method of claim 1 , wherein the ischemia is associated with acute kidney injury.

5. The method of claim 1 , wherein the ischemia is associated with stroke.

6. The method of claim 1 , wherein the ischemia is associated with atherosclerosis.

7. The method of claim 1 , wherein the ischemia is associated with hypertensive cardiomyopathy.

8. The method of claim 1 , wherein the ischemia is associated with congestive heart failure.

9. The method of claim 1 , wherein the method comprises administering a pharmaceutical composition comprising the compound.

10. A method of treating ischemia in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound selected from:

or a pharmaceutically acceptable salt of any of the foregoing.

11. The method of claim 10 , wherein the ischemia is associated with acute kidney injury.

12. The method of claim 10 , wherein the ischemia is associated with stroke.

13. The method of claim 10 , wherein the ischemia is associated with atherosclerosis.

14. The method of claim 10 , wherein the ischemia is associated with hypertensive cardiomyopathy.

15. The method of claim 10 , wherein the ischemia is associated with congestive heart failure.

16. The method of claim 10 , wherein the method comprises administering a pharmaceutical composition comprising the compound.

Assignments (2)
CHANGE OF NAME Recorded May 4, 2021
From: XW LABORATORIES INC.
To: XWPHARMA LTD.
Reel/Frame 056177/0619 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2020
From: XIANG, JIA-NING; QI, ZUDE; NING, DEZHENG; LIU, XIANBO
To: XW LABORATORIES INC.
Reel/Frame 054353/0828 →
Continuity (3)
Division 16801286 · Feb 26, 2020
Continuation PCTCN2017100431 · Sep 4, 2017
Related Publication 20210061791A1 · Mar 4, 2021