IP Library Granted Patent US 9,212,191
Granted Patent B2
US 9,212,191 · App. 14/300,189 · Granted Dec 15, 2015

6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a] pyrazin-8-amine as a spleen tyrosine kinase inhibitor

Inventors: Scott A. Mitchell (East Haven, CT); Kevin S. Currie (North Branford, CT)
Assignee: GILEAD CONNECTICUT, INC.
C07D498/04A61K31/495C07D471/04C07D487/04C07D491/107C07D519/00C12Q1/485G01N33/573
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Quick Facts
Patent No.
US 9,212,191
App. No.
14/300,189
Granted
Dec 15, 2015
Kind
B2
Abstract

Provided are imidazopyrazine compounds, particularly including 6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazine-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions:

Claims (8)

1. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

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

3. A method for inhibiting spleen tyrosine kinase activity in a human, 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 the compound 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.

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

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

Assignments (10)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 9, 2014
From: ARMISTEAD, DAVID M.; MITRA, SOUMYA
To: GILEAD CONNECTICUT, INC.
Reel/Frame 033704/0314 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 9, 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.; BARBOSA, ANTONIO J, JR.; ZHAO, ZHONGDONG
To: CGI PHARMACEUTICALS, INC.
Reel/Frame 033703/0939 →
MERGER Recorded Sep 9, 2014
From: CGI PHARMACEUTICALS, INC.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 033704/0052 →
MERGER Recorded Aug 20, 2014
From: CGI-PHARMACEUTICALS, INC.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 033570/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2014
From: ARMISTEAD, DAVID M.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 033570/0118 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2014
From: MITRA, SOUMYA
To: GILEAD CONNECTICUT, INC.
Reel/Frame 033569/0426 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 19, 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 033566/0297 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 19, 2014
From: BARBOSA, ANTONIO J., JR; ZHAO, ZHONGDONG
To: CGI PHARMACEUTICALS, INC.
Reel/Frame 033566/0374 →
Continuity (6)
Continuation 13868967 · Apr 23, 2013
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 20140357627A1 · Dec 4, 2014