IP Library Granted Patent US 10,689,369
Granted Patent B2
US 10,689,369 · App. 16/356,172 · Granted Jun 23, 2020

Substituted indazole compounds as RORgammaT inhibitors and uses thereof

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Quick Facts
Patent No.
US 10,689,369
App. No.
16/356,172
Granted
Jun 23, 2020
Kind
B2
Abstract

The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

Claims (31)

1. A compound that is a sodium salt of

2. The compound of claim 1 , wherein the compound is a sodium salt of

3. A method of treating a disorder selected from the group consisting of rheumatoid arthritis, psoriasis, Crohn's disease, inflammatory bowel disease, multiple sclerosis, ankylosing spondylitis, systemic lupus erythematosus, chronic graft-versus-host disease, acute graft-versus-host disease, Celiac Sprue, idiopathic thrombocytopenic thrombotic purpura, myasthenia gravis, Sjogren's syndrome, scleroderma, ulcerative colitis, and epidermal hyperplasia, comprising administering to a subject in need thereof a therapeutically effective amount of the following compound to treat the disorder:

or a pharmaceutically acceptable salt thereof.

4. The method of claim 3 , wherein the compound is

5. The method of claim 3 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

6. The method of claim 3 , wherein the compound is

7. The method of claim 3 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

8. The method of claim 3 , wherein the compound is

9. The method of claim 3 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

10. The method of claim 3 , wherein the compound is

11. The method of claim 3 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

12. The method of claim 3 , wherein the compound is

13. The method of claim 3 , wherein the disorder is psoriasis.

14. The method of claim 4 , wherein the disorder is psoriasis.

15. The method of claim 5 , wherein the disorder is psoriasis.

16. The method of claim 6 , wherein the disorder is psoriasis.

17. The method of claim 3 , wherein the disorder is ankylosing spondylitis.

18. The method of claim 4 , wherein the disorder is ankylosing spondylitis.

19. The method of claim 5 , wherein the disorder is ankylosing spondylitis.

20. The method of claim 6 , wherein the disorder is ankylosing spondylitis.

21. A method of inhibiting the activity of a RORγ, comprising exposing a RORγ to an effective amount of the following compound to inhibit the activity of said RORγ:

or a pharmaceutically acceptable salt thereof.

22. The method of claim 21 , wherein the compound is

23. A method of treating cancer in a subject, comprising administering to the subject an amount of the following compound that is effective to treat the cancer:

or a pharmaceutically acceptable salt thereof; wherein the cancer is a B-cell lymphoma, non-Hodgkin lymphoma, colon cancer, pancreatic cancer, breast cancer, ovarian cancer, prostate cancer, squamous cell carcinoma, basal cell carcinoma, adenocarcinoma, sweat gland carcinoma, sebaceous gland carcinoma, lung cancer, leukemia, bladder cancer, stomach cancer, cervical cancer, testicular cancer, skin cancer, rectal cancer, thyroid cancer, kidney cancer, uterus cancer, esophagus cancer, liver cancer, an acoustic neuroma, oligodendroglioma, meningioma, neuroblastoma, or retinoblastoma.

24. The method of claim 23 , wherein the compound is

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 10, 2020
From: LAPOINTE, BLAIR T.; FULLER, PETER H.; GUNAYDIN, HAKAN; LIU, KUN; SCOTT, MARK E.; TROTTER, B. WESLEY; ZHANG, HONGJUN
To: MERCK SHARP & DOHME CORP.
Reel/Frame 051474/0588 →