IP Library Granted Patent US 10,889,572
Granted Patent B2
US 10,889,572 · App. 16/801,286 · Granted Jan 12, 2021

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: XW LABORATORIES INC.
C07D403/12C07D403/14
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Quick Facts
Patent No.
US 10,889,572
App. No.
16/801,286
Granted
Jan 12, 2021
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 (44)

1. A compound selected from:

or a pharmaceutically acceptable salt of any of the foregoing.

2. The compound of claim 1 , wherein the compound has the structure of Formula (III) (methyl (2S)—2-{[(2S)-1-1-[(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):

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound has the structure of Formula (XXVIII) (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);

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , wherein the compound has the structure of Formula (XXIX) ((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):

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 , wherein the compound has the structure of Formula (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}-5-({[(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)pentanoate):

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , wherein the compound has the structure of Formula (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-2,2,6,6-tetramethylpiperidin-4-yl)oxy]carbonyl}amino)hexanoate):

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 1 , wherein the compound has the structure of Formula (XXXII) (propan-2-yl (2S)-2-1[(2S)-1-[(2S,3E,5S)-2-benzyl-5-{[(tert-butoxy) carbonyl]amino 1-7-methyloct-3-enoyl]pyrrolidin-2-yl]formamido}-6-[(1-oxyl-2,2,5,5-tetramethylpyrrolidin-3-yl)formamido]-hexanoate):

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 1 , wherein the compound has the structure of Formula (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)hexanoate):

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 1 , wherein the compound has the structure of Formula (XXXIV) ((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):

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 , wherein the compound has the structure of Formula (XXXV) (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):

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , wherein the compound has the structure of Formula (XXXVI) (tert-butyl N-{(4S,5E,7S)-7-benzyl-8-[(2S)—2-{[(1 S)-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):

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 1 , wherein the compound has the structure of Formula (XXXVII) (tert-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):

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 , wherein the compound has the structure of Formula (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-((((l-oxyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy)carbonyl)amino)pentanoate):

or a pharmaceutically acceptable salt thereof.

14. The compound of claim 1 , wherein the compound has the structure of Formula (XXXIX) ((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-((((l-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy)carbonyl)amino)pentanoate):

or a pharmaceutically acceptable salt thereof.

15. The compound of claim 1 , wherein the compound has the structure of Formula (XXXXIV) (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):

or a pharmaceutically acceptable salt thereof.

16. The compound of claim 1 , wherein the compound has the structure of Formula (XXXXV) (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):

or a pharmaceutically acceptable salt thereof.

17. The compound of claim 1 , wherein the compound has the structure of Formula (XXXXVI) ((S)—cyclohexyl 2-((R)-1-((2S,5S,E)-2-benzyl-5-((tert-butoxycarbonyl)amino)-7-methyloct-3-enoyl)pyrrolidine-2-carboxamido)-6-((((l-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)oxy)carbonyl)amino)hexanoate):

or a pharmaceutically acceptable salt thereof.

18. The compound of claim 1 , wherein the compound has the structure of Formula (XXXXVII) (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):

or a pharmaceutically acceptable salt thereof.

19. A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof.

20. A method of treating acute kidney injury in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.

21. A method of treating acute kidney injury in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical composition of claim 19 .

22. A compound selected from:

or a pharmaceutically acceptable salt of any of the foregoing.

23. A pharmaceutical composition comprising the compound of claim 22 or a pharmaceutically acceptable salt thereof.

24. A method of treating acute kidney injury in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the compound of claim 22 or a pharmaceutically acceptable salt thereof.

25. A method of treating acute kidney injury in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical composition of claim 23 .

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 Mar 25, 2020
From: XIANG, JIA-NING; QI, ZUDE; NING, DEZHENG; LIU, XIANBO
To: XW LABORATORIES INC.
Reel/Frame 052219/0600 →
Continuity (2)
Continuation PCTCN2017100431 · Sep 4, 2017
Related Publication 20200199108A1 · Jun 25, 2020
Cited By (13)
US 12,186,296 US 12,186,298 US 12,226,377 US 12,226,388 US 12,226,389 US 12,239,625 US 12,257,223 US 12,263,150 US 12,263,151 US 12,295,926 US 12,303,478 US 12,478,604 US 12,551,457