Granted Patent B2

US 12,564,617 · App. 17/478,042 · Granted Mar 3, 2026

Inventors: Jesse Jaynes (Auburn, AL); Henry Wilfred Lopez (Napa, CA); George R. Martin (Rockville, MD); Clayton Yates (Auburn, AL); Balasubramanyam Karanam (Auburn, AL)

Assignee: Riptide Bioscience, Inc.

A61K38/08A61P35/00C12N5/0645

Abstract

Claims (26)

1 . A method of treating a subject for a condition, the method comprising:

administering a therapeutically effective amount of a CD206-binding agent that converts a macrophage M2 phenotype to M1 to a subject to treat the subject for the condition;

wherein:

the condition is a condition associated with chronic inflammation selected from the group consisting of scleroderma, Crohn's disease, fibrosis, idiopathic pulmonary fibrosis, asthma, arthritis, osteoarthritis, rheumatoid arthritis, breast cancer, colon cancer, pancreatic cancer, melanoma, prostate cancer, graft-versus-host disease (GVHD), diabetes, diabetic wounds, Alzheimer's disease, and macular degeneration, and

the CD206-binding agent is described by formula (Ia):

wherein:

R 1 -R 4 are each independently selected from hydrogen, and alkyl;

R 5 and R 6 are each independently selected from optionally substituted aryl;

X 2 is selected from optionally substituted alkyl, optionally substituted heteroaryl, and NR 2a R 2b , where R 2a and R 2b are independently selected from hydrogen, and optionally substituted aryl;

X 3 is selected from optionally substituted aryl; and

n is an integer from 1 to 6;

m is an integer of 3 or less,

or a pharmaceutically acceptable salt or solvate thereof.

2 . The method of claim 1 , wherein the condition is pancreatic cancer or melanoma.

3 . The method of claim 1 , wherein the small molecule active agent is a compound selected from the group consisting of:

4 . The method of claim 1 , wherein R 1 -R 4 are each hydrogen.

5 . The method of claim 1 , wherein R 4 is alkyl, and each of R 1 -R 3 are hydrogen.

6 . The method of claim 1 , wherein R 5 and R 6 are each phenyl.

7 . The method of claim 1 , wherein X 2 is C 1 -C 6 alkyl.

8 . The method of claim 1 , wherein X 2 is C 1 -C 6 alkyl substituted with one or more groups selected from hydroxyl, amino, carboxamide, guanidine, acyl and halogen.

9 . The method of claim 1 , wherein X 2 is optionally substituted heteroaryl.

10 . The method of claim 1 , wherein X 2 is optionally substituted heteroaryl substituted with one or more groups selected from carbonyl and hydroxyl.

11 . The method of claim 1 , wherein X 2 is NR 2a R 2b , where R 2a is an optionally substituted aryl group and R 2b is H.

12 . The method of claim 1 , wherein X 3 is an optionally substituted carbazole.

13 . The method of claim 1 , wherein X 3 is an optionally substituted napthyl.

14 . The method of claim 1 , wherein m is 1 or 2.

Assignments (2)

Continuity (4)

References Cited (133)