Granted Patent B2

US 12,617,810 · App. 18/741,674 · Granted May 5, 2026

Inventors: Imran Alibhai (Sugar Land, TX); Sofia de Achaval (Missouri City, TX); Jeffrey Larson (Seabrook, TX); Brad Henke (Cary, NC)

Assignee: Tvardi Operating Company, Inc.

C07F9/12C07C311/29

Abstract

Claims (18)

1 . A compound of Formula I-B:

or a pharmaceutically acceptable salt or a solvate thereof, wherein

A is halo, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 haloalkyl, or C 1-4 haloalkoxy;

R C is hydroxy; and

n is 0 or 1.

2 . The compound of claim 1 , wherein A is C 1-4 alkoxy.

3 . A pharmaceutical composition comprising: a) a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof, and b) a pharmaceutically acceptable carrier.

4 . A method of treating cancer by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof.

5 . The method of claim 4 , wherein the cancer is head and neck cancer, lung cancer, liver cancer, breast cancer, skin cancer, kidney cancer, testicular cancer, colon cancer, rectal cancer, gastric cancer, metastatic melanoma, prostate cancer, ovarian cancer, cervical cancer, bone cancer, spleen cancer, gall bladder cancer, brain cancer, pancreatic cancer, stomach cancer, anal cancer, multiple myeloma, post-transplant lymphoproliferative disease, restenosis, myelodysplastic syndrome, leukemia, or lymphoma.

6 . A method of treating fibrosis by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof.

7 . The method of claim 6 , wherein the fibrosis is pulmonary fibrosis, bone marrow fibrosis, intestine fibrosis, pancreatic fibrosis, joint fibrosis, liver fibrosis, retroperitoneum fibrosis, renal fibrosis, myelofibrosis, dermal fibrosis, or systemic sclerosis.

8 . A method of treating an inflammatory disease or disorder by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof.

9 . The method of claim 8 , wherein the inflammatory disease or disorder is inflammatory bowel disease, ulcerative colitis, psoriasis, uveitis, scleritis, multiple sclerosis, pancreatitis, or asthma.

10 . A method of treating a neurodegenerative disease or disorder by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof.

11 . The method of claim 10 , wherein the neurodegenerative disease or disorder is chemotherapy-induced peripheral neuropathy, diabetic neuropathy, or familial amyloid polyneuropathy.

12 . A method of treating non-alcoholic fatty liver disease or steatohepatitis by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual an effective amount of a compound of claim 1 .

13 . A method of treating cachexia by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof.

14 . A method of treating anaphylaxis by inhibiting signal transducer and activator of transcription 3 (STAT3) in an individual in need thereof, comprising administering to the individual and effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a solvate thereof.

Assignments (4)

Continuity (4)

References Cited (190)