IP Library Granted Patent US 9,896,446
Granted Patent B2
US 9,896,446 · App. 14/975,605 · Granted Feb 20, 2018

Azaquinazoline inhibitors of atypical protein kinase C

Inventors: Henry J. Breslin (Lansdale, PA); Bruce D. Dorsey (Ambler, PA); Benjamin J. Dugan (Glen Mills, PA); Robert L. Hudkins (Chester Springs, PA); Eugen F. Mesaros (Wallingford, PA); Gregory R. Ott (Media, PA); Craig A. Zificsak (Dowingtown, PA); Allison L. Zulli (Wayne, PA); Ming Tao (Maple Glen, PA); Katherine M. Fowler (Caversham, GB); Emma L. Morris (Biggleswade, GB); Gregoire A. Pave (London, GB); Jonathan R. A. Roffey (Reading, GB); Nathaniel J. T. Monck (Ascot, GB); Christelle N. Soudy (London, GB); Ikeoluwa Olowoye (Hemel Hempstead, GB)
Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
C07D471/04C07D493/08C07D498/04C07D519/00C07F9/6584
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Quick Facts
Patent No.
US 9,896,446
App. No.
14/975,605
Granted
Feb 20, 2018
Kind
B2
Abstract

The present application provides a compound of formula (I) or a salt thereof, wherein R 7 , R 8 , R 9 , G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative diseases.

Claims (21)

1. A compound selected from the group consisting of:

(5-Cyclobutyl-3-fluoro-pyridin-2-yl)-[4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-amine;

{5-Cyclopropyl-2-[2-(3,5,6-trifluoro-pyridin-2-ylamino)-pyridin-4-yl]-pyrido[3,4-d]pyrimidin-4-yl}-methyl-piperidin-4-yl-amine;

(4-Chloro-1-ethyl-1H-pyrazol-3-yl)-[4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-amine;

[4-(5-Cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-amine;

{4-[5-Cyclopropyl-4-(3,3-dimethyl-piperazin-1-yl)-pyrido[3,4-d]pyrimidin-2-yl]-pyridin-2-yl}-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-amine; and

{4-[5-Cyclopropyl-4-(3,3-dimethyl-piperazin-1-yl)-pyrido[3,4-d]pyrimidin-2-yl]-pyridin-2-yl}-(1-isopropyl-1H-pyrazol-3-yl)-amine;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is (5-(Cyclobutyl-3-fluoro-pyridin-2-yl)-[4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-amine or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 , wherein the compound is {5-Cyclopropyl-2-[2-(3,5,6-trifluoro-pyridin-2-ylamino)-pyridin-4-yl]-pyrido[3,4-d]pyrimidin-4-yl}-methyl-piperidin-4-yl-amine or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 , wherein the compound is (4-Chloro-1-ethyl-1H-pyrazol-3-yl)-[4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-amine or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 , wherein the compound is [4-(5-Cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-amine or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , wherein the compound is {4-[5-Cyclopropyl-4-(3,3-dimethyl-piperazin-1-yl)-pyrido[3,4-d]pyrimidin-2-yl]-pyridin-2-yl}-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-amine or a pharmaceutically acceptable salt thereof.

7. The compound of claim 1 , wherein the compound is {4-[5-Cyclopropyl-4-(3,3-dimethyl-piperazin-1-yl)-pyrido[3,4-d]pyrimidin-2-yl]-pyridin-2-yl}-(1-isopropyl-1H-pyrazol-3-yl)-amine or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

9. The pharmaceutical composition of claim 8 , wherein the compound of claim 1 is (5-Cyclobutyl-3-fluoro-pyridin-2-yl)-[4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-amine or a pharmaceutically acceptable salt thereof.

10. The pharmaceutical composition of claim 8 , wherein the compound of claim 1 is {5-Cyclopropyl-2-[2-(3,5,6-trifluoro-pyridin-2-ylamino)-pyridin-4-yl]-pyrido[3,4-d]pyrimidin-4-yl}-methyl-piperidin-4-yl-amine or a pharmaceutically acceptable salt thereof.

11. The pharmaceutical composition of claim 8 , wherein the compound of claim 1 is (4-Chloro-1-ethyl-1H-pyrazol-3-yl)-[4-(5-cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-amine or a pharmaceutically acceptable salt thereof.

12. The pharmaceutical composition of claim 8 , wherein the compound of claim 1 is [4-(5-Cyclopropyl-4-piperazin-1-yl-pyrido[3,4-d]pyrimidin-2-yl)-pyridin-2-yl]-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-amine or a pharmaceutically acceptable salt thereof.

13. The pharmaceutical composition of claim 8 , wherein the compound of claim 1 is {4-[5-Cyclopropyl-4-(3,3-dimethyl-piperazin-1-yl)-pyrido[3,4-d]pyrimidin-2-yl]-pyridin-2-yl}-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-amine or a pharmaceutically acceptable salt thereof.

14. The pharmaceutical composition of claim 8 , wherein the compound of claim 1 is {4-[5-Cyclopropyl-4-(3,3-dimethyl-piperazin-1-yl)-pyrido[3,4-d]pyrimidin-2-yl]-pyridin-2-yl}-(1-isopropyl-1H-pyrazol-3-yl)-amine or a pharmaceutically acceptable salt thereof.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 15, 2024
From: VARIAN BIOPHARMACEUTICALS, INC.
To: WINDTREE THERAPEUTICS, INC.
Reel/Frame 069171/0875 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 13, 2017
From: IGNYTA, INC.
To: CANCER RESEARCH TECHNOLOGY LIMITED
Reel/Frame 040964/0825 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2016
From: CEPHALON, INC.
To: IGNYTA, INC.
Reel/Frame 037529/0079 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2016
From: BRESLIN, HENRY J.; DORSEY, BRUCE D.; DUGAN, BENJAMIN J.; HUDKINS, ROBERT L.; MESAROS, EUGEN F.; OTT, GREGORY R.; ZIFICSAK, CRAIG A.; ZULLI, ALLISON L.; TAO, MING; FOWLER, KATHERINE M.; MORRIS, EMMA L.; PAVE, GREGOIRE A.; ROFFEY, JONATHAN R.A.; MONCK, NATHANIEL J.T.; SOUDY, CHRISTELLE N.; OLOWOYE, IKEOLUWA
To: CEPHALON, INC.; CANCER RESEARCH TECHNOLOGY LIMITED
Reel/Frame 037529/0187 →
Continuity (4)
Continuation 14038915 · Sep 27, 2013
Provisional Application 61707340 · Sep 28, 2012
Provisional Application 61781364 · Mar 14, 2013
Related Publication 20160102094A1 · Apr 14, 2016