IP Library Granted Patent US 9,944,628
Granted Patent B2
US 9,944,628 · App. 14/966,968 · Granted Apr 17, 2018

Inhibitors of cellular necrosis and related methods

Inventors: Junying Yuan (Newton, MA); Yijun Zhou (Shanghai, CN); Shan Qian (Shanghai, CN); Dawei Ma (Shanghai, CN)
Assignees: President and Fellows of Harvard College; Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
C07D403/06C07D233/78
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Quick Facts
Patent No.
US 9,944,628
App. No.
14/966,968
Granted
Apr 17, 2018
Kind
B2
Abstract

A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.

Claims (13)

1. A compound having the following structure (II):

or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, wherein one or two of R 7 , R 8 or R 9 is F, and each remaining R 7 , R 8 or R 9 is H; and R 10 is H or F.

2. The compound of claim 1 , wherein R 10 is H.

3. The compound of claim 1 , wherein R 10 is F.

4. The compound of claim 1 , wherein R 7 is F.

5. The compound of claim 1 , wherein R 8 is F.

6. The compound of claim 1 , wherein R 9 is F.

7. The compound of claim 1 , wherein R 7 and R 8 are F.

8. The compound of claim 1 , wherein R 8 and R 9 are F.

9. The compound of claim 1 , wherein the compound has one of the following structures:

10. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt, or tautomer thereof, and a pharmaceutically acceptable carrier, diluent or excipient.

11. A method of inhibiting a receptor interacting protein kinase 1 (RIP1 kinase) in a subject, the method comprising administering an effective amount of the composition of claim 10 to the subject in need thereof.

12. A method for inhibiting, relieving, or relieving symptoms of an inflammatory disorder selected from the group consisting of ischemia, Crohn's disease, ulcerative colitis, rheumatoid arthritis, psoriasis or psoriatic arthritis, the method comprising administering an effective amount of the composition of claim 10 to a subject in need thereof.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY DATA AND RECEIVING PARTY DATA PREVIOUSLY RECORDED AT REEL: 039041 FRAME: 0910. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Oct 12, 2016
From: ZHOU, YIJUN; QIAN, SHAN; MA, DAWEI
To: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
Reel/Frame 040332/0393 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2016
From: YUAN, JUNYING
To: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
Reel/Frame 039996/0759 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2016
From: YUAN, JUNYING; ZHOU, YIJUN; QIAN, SHAN; MA, DAWEI
To: PRESIDENT AND FELLOWS OF HARVARD COLLEGE; SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY
Reel/Frame 039041/0910 →
Priority Claims (2)
CN 2014 1 0764426 · Dec 11, 2014 · national
CN 2014 1 0767595 · Dec 11, 2014 · national
Continuity (3)
Provisional Application 62105475 · Jan 20, 2015
Provisional Application 62105462 · Jan 20, 2015
Related Publication 20160168128A1 · Jun 16, 2016