IP Library Granted Patent US 8,198,276
Granted Patent B2
US 8,198,276 · App. 12/451,833 · Granted Jun 12, 2012

Kinase inhibitor compounds

Assignee: Xcovery Holding Company LLC
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Quick Facts
Patent No.
US 8,198,276
App. No.
12/451,833
Granted
Jun 12, 2012
Kind
B2
Abstract

Pyrimidinone derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as inflammatory diseases and certain types of cancer.

Claims (13)

1. A compound of formula I:

or a salt thereof; wherein:

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 are each independently hydrogen, halo, (C1-C3) alkyl, (C1-C3) alkoxy, and (C1-C3) alkylamino;

R 7 is hydrogen, halo, (C1-C6) alkyl, (C1-C6) alkoxy, and (C1-C6) alkylamino wherein the alkyl is optionally substituted by one or two groups that are independently hydroxyl, (C1-C3) alkoxy, and (C1-C3) alkylamino;

R 8 is C(O)NR 9 R 10 or NHR 11 ;

R 9 and R 10 are each independently hydrogen, (C1-C6) alkyl, (C3-C8) cycloalkyl, (C3-C8) heterocyclyl, or R 9 and R 10 together with the nitrogen they are attached to form a (C3-C8) heterocycle;

R 11 is a (C3-C8) cycloalkyl substituted by 1, 2, 3, or 4 groups that are independently oxo, hydroxyl, (C1-C6)alkyl, (C1-C3) alkoxy, (C1-C3) alkylamino, heterocycle, amide, hydroxyl(C1-C6) alkyl, or (C1-C3)alkoxy(C1-C3)alkyl; or R 11 is a (C3-C8) heterocycle substituted by 2, 3, or 4 groups that are independently oxo, hydroxyl, (C1-C6 ) alkyl, (C1-C3) alkylamino, heterocycle, amide, hydroxyl(C1-C6)alkyl, or (C1-C3)alkoxy(C1-C3) alkyl;

X 1 , X 2 are each independently N or CR 4 .

2. The compound of claim 1 , wherein R 11 is a substituted (C3-C8) heterocycle exemplified by one of

3. The compound of claim 1 , wherein R 11 is a substituted (C3-C8) heterocycle exemplified by one of

4. The compound of claim 1 , wherein R 11 is a substituted (C3-C8) cycloalkyl exemplified by one of

5. The compound of claim 1 , wherein R 8 is C(O)NR 9 R 10 exemplified by one of

6. The compound of claim 1 , wherein X 1 and X 2 are independently CR 4 .

Assignments (2)
SECURITY INTEREST Recorded Oct 21, 2010
From: XCOVERY HOLDING COMPANY LLC
To: COMPASS HORIZON FUNDING COMPANY LLC
Reel/Frame 025177/0731 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 2, 2010
From: LIANG, CONGXIN, MR.
To: TYROGENEX, INC.
Reel/Frame 024011/0015 →
Continuity (2)
Provisional Application 60933385 · Jun 6, 2007
Related Publication 20100144768A1 · Jun 10, 2010