IP Library Granted Patent US 9,567,348
Granted Patent B2
US 9,567,348 · App. 14/629,390 · Granted Feb 14, 2017

Substituted pyrazolo[1,5-a]pyrimidines as Syk inhibitors

Inventors: Scott A. Mitchell (East Haven, CT); Kevin S. Currie (North Branford, CT); Peter A. Blomgren (North Branford, CT); Jeffrey E. Kropf (Branford, CT); Seung H. Lee (Branford, CT); Jianjun Xu (Branford, CT); Douglas G. Stafford (Niskayuna, NY)
Assignee: Gilead Connecticut, Inc.
C07D519/00C07D471/04C07D487/04G01N2333/9121
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Quick Facts
Patent No.
US 9,567,348
App. No.
14/629,390
Granted
Feb 14, 2017
Kind
B2
Abstract

Certain pyrazolo[1,5-a]pyrimidines: or pharmaceutically acceptable salts 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 (10)

1. A compound selected from the group consisting of:

N-[5-(3,4-dihydro-2H-1,4-benzoxazin-6-yl)pyrazolo[1,5-a]pyrimidin-7-yl]-5-(morpholin-4-yl)pyridin-2-amine;

N-[5-(1-methyl-1H-1,3-benzodiazol-6-yl)pyrazolo[1,5-a]pyrimidin-7-yl]-5-(morpholin-4-yl)pyridin-2-amine;

6-(7-{[5-(morpholin-4-yl)pyridin-2-yl]amino}pyrazolo[1,5-a]pyrimidin-5-yl)-2,3-dihydro-1H-indol-2-one;

2-[(6-{[5-(1H-indazol-6-yl)pyrazolo[1,5-a]pyrimidin-7-yl]amino}pyridin-3-yl)(methyl)amino]ethan-1-ol;

6-(7-{[5-(morpholin-4-yl)pyridin-2-yl]amino}pyrazolo[1,5-a]pyrimidin-5-yl)-3,4-dihydro-2H-1,4-benzoxazin-3-one;

N-[5-(1H-indol-6-yl)pyrazolo[1,5-a]pyrimidin-7-yl]-5-(morpholin-4-yl)pyridin-2-amine;

N-[5-(1H-1,3-benzodiazol-6-yl)pyrazolo[1,5-a]pyrimidin-7-yl]-5-(morpholin-4-yl)pyridin-2-amine;

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.

Assignments (4)
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 Apr 23, 2015
From: MITCHELL, SCOTT A.; CURRIE, KEVIN S.; BLOMGREN, PETER A.; KROPF, JEFFREY E.; LEE, SEUNG H.; XU, JIANJUN; STAFFORD, DOUGLAS G.
To: CGI PHARMACEUTICALS, INC.
Reel/Frame 035478/0682 →
MERGER Recorded Apr 23, 2015
From: CGI PHARMACEUTICALS, INC.
To: GILEAD CONNECTICUT, INC.
Reel/Frame 035478/0713 →
Continuity (6)
Division 13862194 · Apr 12, 2013
Division 12632151 · Dec 7, 2009
Provisional Application 61120590 · Dec 8, 2008
Provisional Application 61140535 · Dec 23, 2008
Provisional Application 61240983 · Sep 9, 2009
Related Publication 20150266902A1 · Sep 24, 2015