IP Library › Granted Patent US 12,390,451
Granted Patent B2
US 12,390,451 · App. 17/690,380 · Granted Aug 19, 2025

Small molecule inhibitor of the JAK family of kinases

Inventors: Edward F. Attiyeh (Villanova, PA); Kurtis E. Bachman (Chester Springs, PA); Gerald C. Chu (Philadelphia, PA); Tatiana Koudriakova (Poway, CA); David C. Polidori (Rancho Santa Fe, CA); Gary V. Borzillo (Upper Gwynedd, PA)
Assignee: Janssen Pharmaceutica NV
A61K31/437A61K45/06A61P1/00A61P35/00C12Q1/6886C12Q2600/106C12Q2600/156C12Q2600/158
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Quick Facts
Patent No.
US 12,390,451
App. No.
17/690,380
Granted
Aug 19, 2025
Kind
B2
Abstract

Disclosed herein are JAK inhibitors that have low systemic toxicity. In some aspects, the disclosure includes methods for treating disease states, disorders, and conditions mediated by JAK, such as stomacho-intestinal system cancers, including colorectal cancers and familial adenomatous polyposis.

Claims (12)

1. A method of treating familial adenomatous polyposis in a subject in need thereof comprising administering to the subject a composition comprising about 75 mg of compound of Formula I or a pharmaceutically acceptable salt thereof twice daily

2. A method of treating stomacho-intestinal system cancer in a subject in need thereof comprising administering to the subject a composition comprising about 75 mg of compound of Formula I or a pharmaceutically acceptable salt thereof twice daily

3. A method of treating colorectal cancer in a subject in need thereof comprising administering to the subject a composition comprising about 75 mg of compound of Formula I or a pharmaceutically acceptable salt twice daily

4. The method of claim 1 , wherein the subject has previously received a therapy or is currently receiving a therapy.

5. The method of claim 4 , wherein the therapy is selected from surgery, radiation therapy, chemotherapy, NSAIDs, Cox-2 inhibitors, EGFR inhibitors, VEGF inhibitors, and checkpoint inhibitors.

6. The method of claim 1 , further comprising administering a second active agent in combination with the compound of Formula I, wherein the second active agent is selected from NSAIDs, Cox-2 inhibitors, cetuximab, panitumumab, bevacizumab, Ziv-aflibercept, regorafenib, ramucirumab, ipilimumab, nivolumab, and pembrolizumab.

7. The method of claim 2 , wherein the subject has previously received a therapy or is currently receiving a therapy.

8. The method of claim 7 , wherein the therapy is selected from surgery, radiation therapy, chemotherapy, NSAIDs, Cox-2 inhibitors, EGFR inhibitors, VEGF inhibitors, and checkpoint inhibitors.

9. The method of claim 2 , further comprising administering a second active agent in combination with the compound of Formula I, wherein the second active agent is selected from NSAIDs, Cox-2 inhibitors, cetuximab, panitumumab, bevacizumab, Ziv-aflibercept, regorafenib, ramucirumab, ipilimumab, nivolumab, and pembrolizumab.

10. The method of claim 3 , wherein the subject has previously received a therapy or is currently receiving a therapy.

11. The method of claim 10 , wherein the therapy is selected from surgery, radiation therapy, chemotherapy, NSAIDs, Cox-2 inhibitors, EGFR inhibitors, VEGF inhibitors, and checkpoint inhibitors.

12. The method of claim 3 , further comprising administering a second active agent in combination with the compound of Formula I, wherein the second active agent is selected from NSAIDs, Cox-2 inhibitors, cetuximab, panitumumab, bevacizumab, Ziv-aflibercept, regorafenib, ramucirumab, ipilimumab, nivolumab, and pembrolizumab.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2022
From: ATTIYEH, EDWARD F.; BACHMAN, KURTIS E.; CHU, GERALD C.; KOUDRIAKOVA, TATIANA; POLIDORI, DAVID C.; BORZILLO, GARY V.
To: JANSSEN RESEARCH & DEVELOPMENT, LLC
Reel/Frame 059584/0775 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2022
From: JANSSEN RESEARCH & DEVELOPMENT, LLC
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 059584/0887 →
Continuity (4)
Provisional Application 63232356 · Aug 12, 2021
Provisional Application 63167287 · Mar 29, 2021
Provisional Application 63159726 · Mar 11, 2021
Related Publication 20220288041A1 · Sep 15, 2022
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