IP Library Granted Patent US 9,693,989
Granted Patent B2
US 9,693,989 · App. 14/034,361 · Granted Jul 4, 2017

N4-phenyl-quinazoline-4-amine derivatives and related compounds as ErbB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases

Inventors: Joseph P. Lyssikatos (Piedmont, CA); Julie Marie Hicks (Erie, CO); Fredrik P. Marmsater (Boulder, CO); Qian Zhao (Superior, CO)
Assignee: Array Biopharma, Inc.
A61K31/337A61K31/513A61K31/517A61K39/3955C07D403/12C07D403/14C07D405/14C07D413/12C07D413/14C07D417/12C07D417/14C07D471/04C07D495/04C07D519/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,693,989
App. No.
14/034,361
Granted
Jul 4, 2017
Kind
B2
Abstract

This invention provides compounds of Formula I wherein B, G, A, E, R 1 , R 2 , R 3 , m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

Claims (35)

1. A pharmaceutical composition comprising a compound having the Formula:

or a pharmaceutically acceptable salt thereof;

and a pharmaceutically acceptable diluent or carrier.

2. The pharmaceutical composition of claim 1 , wherein the compound has the Formula:

or a pharmaceutically acceptable salt thereof.

3. The pharmaceutical composition of claim 1 , wherein the compound has the Formula:

or a pharmaceutically acceptable salt thereof.

4. The composition of claim 1 , wherein an anti-tumor agent is administered in combination.

5. The composition of claim 4 , wherein the anti-tumor agent is an anti-metabolite.

6. The composition of claim 5 , wherein the anti-metabolite is 5-fluorouracil.

7. The composition of claim 4 , wherein the anti-tumor agent is an antimitotic agent.

8. The composition of claim 7 , wherein the antimitotic agent is selected from the group consisting of taxol and taxotere.

9. The composition of claim 4 , wherein the anti-tumor agent is an inhibitor of growth factor function.

10. The composition of claim 9 , wherein the inhibitor of growth factor function is trastuzumab.

11. The composition of claim 4 , wherein the anti-tumor agent is an antiangiogenic agent.

12. The composition of claim 11 , wherein the antiangiogenic agent is bevacizumab.

13. A method of treating a cancer that over-expresses HER2 in a mammal, comprising administering to the mammal a therapeutically effective amount of a compound having the Formula:

or a pharmaceutically acceptable salt thereof; wherein the cancer is breast cancer.

14. The method of claim 13 , wherein the compound has the Formula:

or a pharmaceutically acceptable salt thereof.

15. The method of claim 13 , wherein the compound has the Formula:

or a pharmaceutically acceptable salt thereof.

16. The method of claim 13 , wherein the compound has the Formula:

17. The method of claim 13 , wherein the compound has the Formula:

18. The method of claim 13 , wherein an anti-tumor agent is administered in combination.

19. The method of claim 18 , wherein the anti-tumor agent is an anti-metabolite.

20. The method of claim 19 , wherein the anti-metabolite is 5-fluorouracil.

21. The method of claim 18 , wherein the anti-tumor agent is an antimitotic agent.

22. The method of claim 21 , wherein the antimitotic agent is selected from the group consisting of taxol and taxotere.

23. The method of claim 18 , wherein the anti-tumor agent is an inhibitor of growth factor function.

24. The method of claim 23 , wherein the inhibitor of growth factor function is trastuzumab.

25. The method of claim 18 , wherein the anti-tumor agent is an antiangiogenic agent.

26. The method of claim 25 , wherein the antiangiogenic agent is bevacizumab.

27. The pharmaceutical composition of claim 1 , wherein the compound has the Formula:

28. The pharmaceutical composition of claim 1 , wherein the compound has the Formula:

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 27, 2017
From: LYSSIKATOS, JOSEPH P.; MARMSATER, FREDRIK; ZHAO, QIAN; GRESCHUK, JULIE MARIE
To: ARRAY BIOPHARMA, INC.
Reel/Frame 042821/0512 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 27, 2017
From: LYSSIKATOS, JOSEPH P.; GRESCHUK, JULIE MARIE; HENNINGS, D. DAVID; LIU, WEIDONG; MARMSATER, FREDRIK P.; ZHANG, QIAN
To: ARRAY BIOPHARMA, INC.
Reel/Frame 042821/0566 →
Continuity (4)
Division 12085048
Provisional Application 60736289 · Nov 15, 2005
Provisional Application 60817019 · Jun 28, 2006
Related Publication 20140023643A1 · Jan 23, 2014