IP Library › Granted Patent US 9,925,188
Granted Patent B2
US 9,925,188 · App. 15/056,137 · Granted Mar 27, 2018

DNA-PK inhibitors and uses thereof

Inventors: Paul S. Charifson (Framingham, MA); Kevin Michael Cottrell (Cambridge, MA); Hongbo Deng (Southborough, MA); John P. Duffy (Northborough, MA); Huai Gao (Arlington, MA); Simon Giroux (Cambridge, MA); Jeremy Green (Waltham, MA); Katrina Lee Jackson (Cambridge, MA); Joseph M. Kennedy (Charlestown, MA); David J. Lauffer (Stow, MA); Mark Willem Ledeboer (Acton, MA); Pan Li (Lexington, MA); John Patrick Maxwell (Hingham, MA); Mark A. Morris (Somerville, MA); Albert Charles Pierce (Cambridge, MA); Nathan D. Waal (Cambridge, MA); Jinwang Xu (Framingham, MA)
Assignee: Vertex Pharmaceuticals Incorporated
A61K31/506A61K9/20A61K9/48A61K31/5377A61K41/0038A61K47/481C07D239/42C07D401/04C07D401/14C07D403/04C07D403/10C07D405/14C07D409/04C07D409/14C07D413/04C07D413/10C07D413/14C07D417/04C07D417/10C07D417/14C07D471/04C07D491/048C07D491/056C07D495/04C07D521/00
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Quick Facts
Patent No.
US 9,925,188
App. No.
15/056,137
Granted
Mar 27, 2018
Kind
B2
Abstract

The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Claims (28)

1. A method of potentiating a therapeutic regimen for the treatment of breast cancer, colorectal cancer, gastric-esophageal cancer, fibrosarcoma, glioblastoma, hepatocellular carcinoma, head and neck squamous cell carcinoma, melanoma, lung cancer, pancreatic cancer, or prostate cancer in a patient comprising the step of administering to said patient an effective amount of a compound or a pharmaceutical composition comprising said compound, wherein the compound is

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 , wherein the compound is represented by the following formula:

6. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

9. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

10. The method of claim 9 , wherein the compound is represented by the following formula:

11. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

12. The method of claim 1 , wherein the compound is represented by the following formula:

or a pharmaceutically acceptable salt thereof.

13. The method of claim 1 , wherein the pharmaceutical composition is orally administered to the patient.

14. The method of claim 1 , wherein the pharmaceutical composition is a capsule, tablet, or aqueous suspension.

15. The method of claim 14 , wherein the pharmaceutical composition is a capsule.

16. The method of claim 14 , wherein the pharmaceutical composition is a tablet.

17. The method of claim 1 , wherein the therapeutic regimen comprises radiation therapy.

18. The method of claim 1 , wherein the therapeutic regimen comprises an anti-cancer therapeutic agent.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2016
From: CHARIFSON, PAUL S.; COTTRELL, KEVIN MICHAEL; DENG, HONGBO; DUFFY, JOHN P.; GAO, HUAI; GIROUX, SIMON; GREEN, JEREMY; JACKSON, KATRINA LEE; KENNEDY, JOSEPH M.; LAUFFER, DAVID J.; LEDEBOER, MARK WILLEM; LI, PAN; MAXWELL, JOHN PATRICK; MORRIS, MARK A.; PIERCE, ALBERT CHARLES; WAAL, NATHAN D.; XU, JINWANG
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 040486/0103 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2016
From: CHARIFSON, PAUL S.; COTTRELL, KEVIN MICHAEL; DENG, HONGBO; DUFFY, JOHN P.; GAO, HUAI; GIROUX, SIMON; GREEN, JEREMY; JACKSON, KATRINA LEE; KENNEDY, JOSEPH M.; LAUFFER, DAVID J.; LEDEBOER, MARK WILLEM; LI, PAN; MAXWELL, JOHN PATRICK; MORRIS, MARK A.; PIERCE, ALBERT CHARLES; WAAL, NATHAN D.; XU, JINWANG
To: VERTEX PHARMACEUTICALS INCORPORATED
Reel/Frame 039131/0386 →
Continuity (5)
Division 13868703 · Apr 23, 2013
Provisional Application 61777806 · Mar 12, 2013
Provisional Application 61725652 · Nov 13, 2012
Provisional Application 61637512 · Apr 24, 2012
Related Publication 20160250212A1 · Sep 1, 2016