IP Library › Granted Patent US 8,263,596
Granted Patent B2
US 8,263,596 · App. 13/081,254 · Granted Sep 11, 2012

Kinase inhibitors and method of treating cancer

Assignee: University Health Network
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Quick Facts
Patent No.
US 8,263,596
App. No.
13/081,254
Granted
Sep 11, 2012
Kind
B2
Abstract

The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.

Claims (22)

1. A compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof, wherein:

R a is —F, methoxy, methyl or ethyl;

R 4 is —H, methyl, ethyl, 2-methoxyethyl or —CH 2 CONH 2 ; and

R 6 is —C═C-(optionally substituted phenyl).

2. The compound of claim 1 , wherein the compound is represented by the following structural formula:

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 wherein:

the phenyl in —CH═CH-(phenyl) is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C 1-6 alkyl, C 1-6 haloalkyl, (C 1-6 aminoalkyl), (C 1-6 alkylamino)C 1-6 alkyl, (C 1-6 dialkylamino)C 1-6 alkyl, (phenyl)C 1-6 alkyl, amino, C 1-6 alkylamino, C 1-6 dialkylamino, —(CH 2 ) 0-3 —N-piperidinyl, —(CH 2 ) 0-3 —N-morpholinyl, —(CH 2 ) 0-3 —N-pyrrolidinyl, —(CH 2 ) 0-3 —N-piperazinyl and —(CH 2 ) 0-3 —N-oxazepanyl, wherein the N-piperazinyl is optionally N′-substituted with C 1-6 alkyl or C 1-6 acyl; and

R 4 is —H or methyl.

4. A compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof.

5. A compound of represented by the following structural formula:

or a pharmaceutically acceptable salt thereof.

6. A compound represented by the following structural formula:

or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, and a compound of claim 1 or a pharmaceutically acceptable salt thereof.

8. The pharmaceutical composition of claim 7 , further comprising a therapeutic agent.

9. The pharmaceutical composition of claim 8 , wherein the therapeutic agent is an anti-cancer drug.

10. The compound of claim 2 wherein:

the phenyl in —CH═CH-(phenyl) is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C 1-6 alkyl, C 1-6 haloalkyl, (C 1-6 aminoalkyl), (C 1-6 alkylamino) C 1-6 alkyl, (C 1-6 dialkylamino)C 1-6 alkyl, (phenyl)C 1-6 alkyl, amino, C 1-6 alkylamino, C 1-6 dialkylamino, —(CH 2 ) 0-3 —N-piperidinyl, —(CH 2 ) 0-3 —N-morpholinyl, —(CH 2 ) 0-3 —N-pyrrolidinyl, —(CH 2 ) 0-3 —N-piperazinyl and —(CH 2 ) 0-3 —N-oxazepanyl, wherein the N-piperazinyl is optionally N′-substituted with C 1-6 alkyl or C 1-6 acyl; and

R 4 is —H or methyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2011
From: SAMPSON, PETER B.; LIU, YONG; LI, SZE-WAN; FORREST, BRYAN T.; PAULS, HEINZ W.; EDWARDS, LOUISE G.; FEHER, MIKLOS; PATEL, NARENDRA KUMAR B.; LAUFER, RADOSLAW; PAN, GUOHUA
To: UNIVERSITY HEALTH NETWORK
Reel/Frame 026573/0313 →
Priority Claims (1)
CA 2010/000518 · Apr 6, 2010 · national
Continuity (3)
Provisional Application 61321332 · Apr 6, 2010
Provisional Application 61321329 · Apr 6, 2010
Related Publication 20110263598A1 · Oct 27, 2011