IP Library › Granted Patent US 9,949,981
Granted Patent B2
US 9,949,981 · App. 14/845,795 · Granted Apr 24, 2018

Compositions and methods for treating proliferation disorders

Inventors: Daniel T. Dransfield (Burlington, MA); Sudharshan Eathiraj (Shrewsbury, MA); Jean-Marc Lapierre (Pelham, NH); Brian Schwartz (Woodbridge, CT); Yi Yu (North Easton, MA)
Assignee: ArQule, Inc.
A61K31/5377A61K31/444A61K31/4545A61K31/517A61K45/06
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Quick Facts
Patent No.
US 9,949,981
App. No.
14/845,795
Granted
Apr 24, 2018
Kind
B2
Abstract

The present invention relates to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-(3-morpholinophenyl)-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or N-(1-(3-(3-(4-(1-aminocyclobutyl)phenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-5-yl)phenyl)piperidin-4-yl)-N-methylacetamide. The methods of the present invention can also relate to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing the above compounds in combination with ((R)-6-(2-fluorophenyl)-N-(3-(2-((2-methoxyethyl)amino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine).

Claims (26)

1. A method of treating Proteus syndrome, comprising administering, to said subject, a therapeutically effective amount of a composition comprising at least one of

or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein said Proteus syndrome is treated.

2. The method of claim 1 , wherein said subject is a human.

3. The method of claim 1 , wherein the composition is administered intravenously, orally or intraperitoneally.

4. The method of claim 1 , wherein the compositions further comprise one or more pharmaceutically acceptable carriers or excipients.

5. The method of claim 1 , wherein the composition is administered daily.

6. The method of claim 5 , wherein the composition is administered at about 50 mg to about 100 mg daily.

7. The method of claim 6 , wherein the composition is administered at about 60 mg daily.

8. The method of claim 1 , wherein the composition is administered in an intermittent dosing regimen, wherein the composition is administered at least once in 24 hours, not administered for at least six days, and administered at least once in 24 hours following the at least six days.

9. The method of claim 8 , wherein the composition is administered once a week.

10. The method of claim 8 , wherein the composition is administered once at about 250 mg to about 350 mg.

11. The method of claim 10 , wherein the composition is administered at about 200 mg daily.

12. The method of claim 10 , wherein the composition is administered once at about 300 mg.

13. The method of claim 1 , wherein the composition is administered in an intermittent dosing regimen, wherein the composition is administered at least once daily for at least a week, not administered for at least a second week, and administered daily for at least a third week following the at least second week.

14. The method of claim 13 , wherein the composition is administered at about 150 mg to about 250 mg daily.

15. The method of claim 1 , further comprising administering a therapeutically effective amount of an additional anti-proliferative agent, administering radiation therapy or both.

16. The method of claim 15 , wherein the additional anti-proliferative agent is a kinase inhibitor, an alkylating agent, an antibiotic, an anti-metabolite, a detoxifying agent, an interferon, a polyclonal or monoclonal antibody, a HER2 inhibitor, a histone deacetylase inhibitor, a hormone, a mitotic inhibitor, an MTOR inhibitor, a taxane or taxane derivative, an aromatase inhibitor, an anthracycline, a microtubule targeting drug, a topoisomerase poison drug, or a cytidine analogue drug.

17. The method of claim 15 , wherein the additional anti-proliferative agent is a fibroblast growth factor receptor inhibitor.

18. The method of claim 15 , wherein the additional anti-proliferative agent is a composition comprising

or a pharmaceutically acceptable salt, solvate, or hydrate thereof.

19. The method of claim 18 , wherein the composition comprising

or a pharmaceutically acceptable salt, solvate, or hydrate thereof is administered simultaneously with, preceding administration of, or following administration of the composition comprising

or a pharmaceutically acceptable salt, solvate, or hydrate, or prodrug thereof.

20. The method of claim 18 , wherein the composition comprising

or a pharmaceutically acceptable salt, solvate, or hydrate is administered within 24 hours of administration of the composition comprising

or a pharmaceutically acceptable salt, solvate, or hydrate thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 24, 2015
From: DRANSFIELD, DANIEL T.; EATHIRAJ, SUDHARSHAN; LAPIERRE, JEAN-MARC; SCHWARTZ, BRIAN; YU, YI
To: ARQULE, INC.
Reel/Frame 037130/0160 →
Continuity (3)
Provisional Application 62046502 · Sep 5, 2014
Provisional Application 62082236 · Nov 20, 2014
Related Publication 20160067260A1 · Mar 10, 2016