IP Library › Granted Patent US 10,245,268
Granted Patent B2
US 10,245,268 · App. 15/671,978 · Granted Apr 2, 2019

Treatment of ACVR1-mediated diseases

Inventors: Brian Koh (Foster City, CA); Igor Theurl (Innsbruck, AT); Matthew Robert Warr (Issaquah, WA); James Andrew Whitney (Mercer Island, WA)
Assignee: Sierra Oncology, Inc.
A61K31/5377A61K31/7064
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Quick Facts
Patent No.
US 10,245,268
App. No.
15/671,978
Granted
Apr 2, 2019
Kind
B2
Abstract

Provided herein are methods, compositions, and kits for treating ACVR-1-mediated diseases using N-(cyanomethyl)-4-[2-4-morpholinoanilino)pyrimidin-4-yl]benzamide.

Claims (18)

1. A method of treating an ACVR1-mediated disease comprising administering momelotinib or a pharmaceutically acceptable salt or solvate thereof to a patient in need thereof, wherein the ACVR1-mediated disease is selected from the group consisting of fibrodysplasia ossificans progressive (FOP) and diffuse intrapontine glioma (DIPG).

2. The method of claim 1 , wherein the ACVR1-mediated disease is mediated by a mutant ACVR1 polypeptide.

3. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a substitution mutation.

4. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises an activating mutation in the glycine-serine rich (GS) domain or in the kinase domain.

5. The method of claim 4 , wherein the activating mutation is in the GS domain.

6. The method of claim 5 , wherein the activating mutation is an R206H substitution.

7. The method of claim 4 , wherein the activating mutation is in the kinase domain.

8. The method of claim 7 , wherein the activating mutation is a R258G/S, G328E/V/W/R, or G356D substitution.

9. The method of claim 8 , wherein the activating mutation is a R258G/S substitution.

10. The method of claim 8 , wherein the activating mutation is a G328EN/W/R substitution.

11. The method of claim 8 , wherein the activating mutation is a G356D substitution.

12. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a R206H, Q207E, R258G/S, G328E/V/W/R, or G356D mutation.

13. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a R206H mutation.

14. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a Q207E mutation.

15. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a R258G/S mutation.

16. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a G328E/V/W/R mutation.

17. The method of claim 2 , wherein the mutant ACVR1 polypeptide comprises a G356D mutation.

18. The method of claim 1 , wherein the ACVR1-mediated disease is not anemia.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 7, 2023
From: SIERRA ONCOLOGY LLC
To: GLAXOSMITHKLINE LLC
Reel/Frame 063879/0821 →
CHANGE OF NAME Recorded May 26, 2023
From: SIERRA ONCOLOGY, INC.
To: SIERRA ONCOLOGY LLC
Reel/Frame 063790/0568 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 15, 2018
From: GILEAD SCIENCES, INC.
To: SIERRA ONCOLOGY, INC.
Reel/Frame 047517/0972 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 3, 2018
From: YM BIOSCIENCES AUSTRALIA PTY LTD
To: SIERRA ONCOLOGY, INC.
Reel/Frame 047059/0834 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 9, 2017
From: WHITNEY, JAMES ANDREW; WARR, MATTHEW ROBERT; KOH, BRIAN; THEURL, IGOR
To: GILEAD SCIENCES, INC.
Reel/Frame 043241/0598 →
Continuity (2)
Provisional Application 62373161 · Aug 10, 2016
Related Publication 20180042933A1 · Feb 15, 2018
Cited By (5)
US 12,365,729 US 12,497,452 US 12,655,210 US 12,715,916 US 12,715,917