IP Library Granted Patent US 9,499,521
Granted Patent B2
US 9,499,521 · App. 15/194,413 · Granted Nov 22, 2016

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
C07D403/06
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Quick Facts
Patent No.
US 9,499,521
App. No.
15/194,413
Granted
Nov 22, 2016
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 (10)

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

or a pharmaceutically acceptable salt or tautomer thereof.

2. A pharmaceutical composition comprising a compound having the following structure (Ia):

or a pharmaceutically acceptable salt or tautomer thereof, and a pharmaceutically acceptable carrier, diluent or excipient.

3. A method of inhibiting receptor interacting protein kinase 1 (RIP1 kinase) in a subject, the method comprising administering an effective amount of a pharmaceutical composition to the subject, wherein the pharmaceutical composition comprises a compound having the following structure (Ia):

or a pharmaceutically acceptable salt or tautomer thereof, and a pharmaceutically acceptable carrier, diluent or excipient.

4. The compound of claim 1 having the following structure (Ia):

or a pharmaceutically acceptable salt thereof.

5. A method of inhibiting receptor interacting protein kinase 1 (RIP1 kinase) in a subject, the method comprising delivering an effective amount of the compound of claim 1 .

6. The compound of claim 1 , (R)-5-((7-chloro-6-fluoro-1H-indol-3-yl)methyl)-3-methylimidazolidine-2,4-dione.

Assignments (3)
CONFIRMATORY LICENSE Recorded Jul 2, 2018
From: HARVARD UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 046464/0219 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2016
From: ZHOU, YIJUN; QIAN, SHAN; MA, DAWEI
To: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
Reel/Frame 039996/0580 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2016
From: YUAN, JUNYING
To: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
Reel/Frame 039996/0607 →
Priority Claims (2)
CN 2014 1 0764426 · Dec 11, 2014 · national
CN 2014 1 0767595 · Dec 11, 2014 · national
Continuity (4)
Division 14966968 · Dec 11, 2015
Provisional Application 62105475 · Jan 20, 2015
Provisional Application 62105462 · Jan 20, 2015
Related Publication 20160304498A1 · Oct 20, 2016