IP Library Granted Patent US 10,736,875
Granted Patent B2
US 10,736,875 · App. 16/126,199 · Granted Aug 11, 2020

Methods and compositions associated with the granulocyte colony-stimulating factor receptor

Inventors: Lin Zhi (San Diego, CA); Keith Marschke (San Diego, CA); Virginia H. Grant (San Diego, CA); Steven L. Roach (San Diego, CA); Yixing Shen (Encinitas, CA); Jason C. Pickens (San Diego, CA); Bijan Pedram (San Diego, CA); Cornelis Arjan van Oeveren (San Diego, CA); Lino J. Valdez (San Diego, CA); Andrew R. Hudson (San Diego, CA)
Assignee: LIGAND PHARMACEUTICALS, INC.
A61K31/404A61K31/41A61K31/4152A61K31/4155A61K31/454A61K45/06A61N5/10C07D209/34C07D231/46C07D231/52C07D401/12C07D403/12C07D405/06C12Q1/18C12Q1/66
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Quick Facts
Patent No.
US 10,736,875
App. No.
16/126,199
Granted
Aug 11, 2020
Kind
B2
Abstract

Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.

Claims (24)

1. A method of treating a disorder selected from the group consisting of granulocytopenia, neutropenia, amyotrophic lateral sclerosis, multiple sclerosis, multiple dystrophy, and spinal cord injury, the method comprising administering an effective amount of a compound to a subject in need thereof, wherein the compound has the structure of Formula (IV):

a tautomer thereof, or a pharmaceutically acceptable salt thereof, wherein:

R 4 is a 3,5-dimethyl phenyl;

R 5 is CF 3 ;

R 9 is selected from an optionally substituted C 1 -C 6 alkyl, and a C 2 -C 6 alkenyl substituted with —COOH or halogen;

W is NH;

X is N (nitrogen);

Y is C 4 alkenyl.

2. The method of claim 1 , wherein R 9 is an optionally substituted C 1 -C 6 alkyl.

3. The method of claim 2 , wherein R 9 is an optionally substituted C 1 -C 3 alkyl.

4. The method of claim 3 , wherein R 9 is C 1 -C 3 alkyl.

5. The method of claim 1 , wherein the disorder is selected from the group consisting of granulocytopenia, neutropenia, amyotrophic lateral sclerosis, multiple sclerosis, and multiple dystrophy.

6. The method of claim 1 , wherein the compound is administered in combination with an additional therapeutic regimen selected from the group consisting of chemotherapy, bone marrow transplantation, and radiation therapy.

7. The method of claim 1 having the structure:

a tautomer thereof, or pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the compound is:

9. The method of claim 1 , wherein R 9 is C 2 -C 6 alkenyl substituted with —COOH.

10. The method of claim 1 , wherein R 9 is C 2 -C 6 alkenyl substituted with halogen.

11. The method of claim 1 , wherein the disorder is granulocytopenia.

12. The method of claim 1 , wherein the disorder is neutropenia.

13. The method of claim 1 , wherein the disorder is amyotrophic lateral sclerosis.

14. The method of claim 1 , wherein the disorder is multiple sclerosis.

15. The method of claim 1 , wherein the disorder is multiple dystrophy.

16. The method of claim 1 , wherein the disorder is a spinal cord injury.

Assignments (2)
SECURITY INTEREST Recorded Oct 18, 2023
From: CYDEX PHARMACEUTICALS, INC.; LIGAND PHARMACEUTICALS INCORPORATED; METABASIS THERAPEUTICS, INC.; PFENEX INC.
To: CITIBANK, N.A., AS ADMINISTRATIVE AGENT
Reel/Frame 065271/0025 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 10, 2020
From: ZHI, LIN; MARSCHKE, KEITH; GRANT, VIRGINIA H.; ROACH, STEVEN L.; SHEN, YIXING; PICKENS, JASON C.; PEDRAM, BIJAN; VAN OEVEREN, CORNELIS ARJAN; VALDEZ, LINO J.; HUDSON, ANDREW R.
To: LIGAND PHARMACEUTICALS, INC.
Reel/Frame 052068/0835 →