IP Library Granted Patent US 8,765,761
Granted Patent B2
US 8,765,761 · App. 13/868,967 · Granted Jul 1, 2014

6-(1H-indazol-6-yl)-N-{4-[2-methyl-1-(morpholin-4-yl)propan-2-yl]phenyl}imidazo[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a syk inhibitor

Inventors: Scott A. Mitchell (East Haven, CT); Kevin S. Currie (North Branford, CT)
Assignee: Gilead Connecticut, Inc.
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Quick Facts
Patent No.
US 8,765,761
App. No.
13/868,967
Granted
Jul 1, 2014
Kind
B2
Abstract

An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Claims (8)

1. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable vehicle selected from the group consisting of carriers, adjuvants, and excipients.

3. A method for inhibiting spleen tyrosine kinase activity in a human in need thereof, comprising administering to the human an effective amount of the compound according to claim 1 or a pharmaceutically acceptable salt thereof.

4. The method according to claim 3 , wherein an effective amount of said compound or a pharmaceutically acceptable salt thereof is administered to the human intravenously, intramuscularly, parenterally, or orally.

5. A method for determining the presence or absence of spleen tyrosine kinase in a sample, comprising contacting the sample with the compound of claim 1 or a pharmaceutically acceptable salt thereof, and determining the presence or absence of spleen tyrosine kinase in the sample.

6. A method for inhibiting B-cell activity comprising contacting cells expressing spleen tyrosine kinase with the compound of claim 1 or a pharmaceutically acceptable salt thereof.

7. A method for inhibiting adenosine triphosphate hydrolysis, the method comprising contacting cells expressing spleen tyrosine kinase with the compound of claim 1 or a pharmaceutically acceptable salt thereof.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 30, 2020
From: GILEAD CONNECTICUT, INC.
To: KRONOS BIO, INC.
Reel/Frame 053927/0969 →
MERGER AND CHANGE OF NAME Recorded Sep 17, 2020
From: COUGAR MERGER SUB, INC.; CGI PHARMACEUTICALS, INC.; CGI PHARMACEUTICALS, INC.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 053799/0190 →
MERGER Recorded Mar 11, 2014
From: CGI PHARMACEUTICALS, INC.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 032409/0581 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2014
From: ARMISTEAD, DAVID M.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 032409/0684 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2014
From: MITRA, SOUMYA
To: GILEAD CONNECTICUT, INC.
Reel/Frame 032409/0691 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2014
From: BARBOSA, ANTONIO J., JR.; ZHAO, ZHONGDONG
To: CGI PHARMACEUTICALS, INC.
Reel/Frame 032409/0546 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2014
From: MITCHELL, SCOTT A.; CURRIE, KEVIN S.; BLOMGREN, PETER A.; KROPF, JEFFREY E.; LEE, SEUNG H.; XU, JIANJUN; STAFFORD, DOUGLAS G.; HARDING, JAMES P.
To: CGI PHARMACEUTICALS, INC.
Reel/Frame 032409/0530 →
Continuity (5)
Continuation 12632140 · Dec 7, 2009
Provisional Application 61120587 · Dec 8, 2008
Provisional Application 61140514 · Dec 23, 2008
Provisional Application 61240979 · Sep 9, 2009
Related Publication 20130237520A1 · Sep 12, 2013