IP Library Granted Patent US 12,263,180
Granted Patent B2
US 12,263,180 · App. 17/323,901 · Granted Apr 1, 2025

Method for treatment of COVID-19-associated conditions

Inventors: Esteban Masuda (Menlo Park, CA); Vadim Markovtsov (San Mateo, CA)
Assignee: Rigel Pharmaceuticals, Inc.
A61K31/675A61K31/155A61K31/245A61K31/427A61K31/4706A61K31/4748A61K31/519A61K31/573A61K31/7048A61K39/42A61P31/14C07K16/1003
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,263,180
App. No.
17/323,901
Granted
Apr 1, 2025
Kind
B2
Abstract

Provided herein are a variety of methods that involve administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having or suspected of having a COVID-19 infection. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having, suspected of having or expected to develop acute respiratory distress syndrome, acute kidney injury, and/or thrombosis. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having, suspected of having or expected to develop symptoms associated with a cytokine response. Aspects of the methods may further include identifying a patient with kidney malfunction, e.g., acute kidney injury, and/or thrombosis.

Claims (52)

1. A method of treatment of a COVID-19 infection, comprising:

administering to a patient having or suspected of having the COVID-19 infection, a compound, wherein the compound is of the formula:

or a pharmaceutically acceptable salt thereof, or

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the patient has or is expected to develop acute respiratory distress syndrome.

3. The method of claim 1 , wherein the patient has a cough but does not have acute respiratory distress syndrome.

4. The method of claim 1 , wherein the patient is over the age of 60 and/or has one or more other lung diseases.

5. The method of claim 4 , wherein the patient has or has a history of having asthma, pneumothorax, atelectasis, bronchitis, chronic obstructive pulmonary disease, lung cancer or pneumonia.

6. The method of claim 1 , wherein the patient has or is expected to develop acute kidney injury.

7. The method of claim 1 , wherein the patient has reduced kidney function but does not have acute kidney injury.

8. The method of claim 1 , wherein the patient is over the age of 60 and/or has one or more other kidney diseases.

9. The method of claim 1 , wherein the patient has or has a history of having dialysis treatments and/or has had a kidney transplant.

10. The method of claim 1 , wherein the patient has or is expected to develop thrombosis.

11. The method of claim 1 , wherein the patient has a prothrombotic coagulation profile but does not have thrombosis.

12. The method of claim 11 , wherein the patient has increased levels of D-dimer.

13. The method of claim 1 , wherein the patient is over the age of 60 and/or has one or more risk factors for developing thrombosis.

14. The method of claim 1 , wherein the patient has or has had a thrombotic event.

15. The method of claim 1 , wherein the administering is systemically administering.

16. The method of claim 15 , wherein the administering is done orally or intravenously.

17. The method of claim 1 , wherein the administering is done by pulmonary administration.

18. The method of claim 17 , wherein the administering is done using an inhaler or nebulizer.

19. The method of claim 1 , wherein the patient is in intensive care.

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

21. A method for treating acute respiratory distress syndrome, comprising:

administering to a patient having, suspected of having or expected to develop acute respiratory distress syndrome, a compound, wherein the compound is of the formula:

or a pharmaceutically acceptable salt thereof, or

or a pharmaceutically acceptable salt thereof.

22. The method of claim 21 , wherein the patient has a COVID-19 infection.

23. The method of claim 21 , wherein the patient has or is expected to develop acute respiratory distress syndrome.

24. The method of claim 21 , wherein the patient has a cough but does not have acute respiratory distress syndrome.

25. The method of claim 21 , wherein the patient is over the age of 60 and/or has one or more other lung diseases.

26. The method of claim 25 , wherein the patient has or has a history of having asthma, pneumothorax, atelectasis, bronchitis, chronic obstructive pulmonary disease, lung cancer or pneumonia.

27. The method of claim 21 , wherein the administering is systemically administering.

28. The method of claim 27 , wherein the administering is done orally or intravenously.

29. The method of claim 21 , wherein the administering is done by pulmonary administration.

30. The method of claim 29 , wherein the administering is done using an inhaler or nebulizer.

31. The method of claim 21 , wherein the patient is in intensive care.

32. The method of claim 21 , wherein the compound is of the formula:

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

or a pharmaceutically acceptable salt thereof.

34. The method of claim 21 , wherein the compound is of the formula:

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

36. The method of claim 21 , wherein the compound is of the formula:

or a pharmaceutically acceptable salt thereof.

37. A method for treating sepsis, comprising:

administering to a patient having, suspected of having or expected to develop sepsis, a compound, wherein the compound is of the formula:

or a pharmaceutically acceptable salt thereof, or

or a pharmaceutically acceptable salt thereof.

38. The method of claim 37 , wherein the patient has a COVID-19 infection.

39. The method of claim 37 , wherein the patient has acute respiratory distress syndrome.

Assignments (3)
SECURITY INTEREST Recorded May 8, 2026
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FUNDING IV TRUST
Reel/Frame 075576/0880 →
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 19, 2021
From: MASUDA, ESTEBAN; MARKOVTSOV, VADIM
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 057232/0469 →
Continuity (4)
Continuation PCTUS2021021951 · Mar 11, 2021
Provisional Application 62988876 · Mar 12, 2020
Provisional Application 63038570 · Jun 12, 2020
Related Publication 20210283152A1 · Sep 16, 2021
References Cited (22)
US 8372415B2 · Sun et al. · 2013 [cited by applicant]
US 20070060603A1 · Singh et al. · 2007 [cited by applicant]
US 20110144059A1 · Bhamidipati et al. · 2011 [cited by applicant]
US 20160060260A1 · Palmer et al. · 2016 [cited by applicant]
WO WO2003063794A2 · 2003 [cited by applicant]
WO WO2003063794A3 · 2015 [cited by applicant]
WO WO2015116729A2 · 2015 [cited by applicant]
Altomare et al., “Potential Anti-Thrombotic Effect without Accompanying Hemorrhage with Fostamatinib Use in Patients with Immune Thrombocytopenia”, Blood, 2019; 134 (Supplement_ 1): 4889. [cited by applicant]
Astrazeneca, “A Study of Fostamatinib in Subjects With Impaired Kidney Function”, https://clinicaltrials.gov/ct2/show/NCT01245790, 2011. [cited by applicant]
Price et al., “Thrombosis and COVID-19 pneumonia: the clot thickens!”, European Respiratory Journal, Jul. 30, 2020; 56(1): 2001608. [cited by applicant]
Rudnick et al., “Acute Kidney Injury in COVID-19: Another Challenge for Nephrology”, American Journal of Nephrology, Oct. 15, 2020; 51(10): 761-763. [cited by applicant]
Anonymous DOD Supports Phase III Clinical Trial Using Fostamatinib (Tavalisse) Against Covid-19, JPEO-CBRND, Jan. 29, 2021. [cited by applicant]
Martin et al., Pharmacokinetic Properties of Fostamatinib in Patients With Renal or Hepatic Impairment: Results From 2 Phase | Clinical Studies, Clinical Therapeutics, 37(12):2823-2836, Dec. 2015. [cited by applicant]
Nadeem et al., Inhibition of spleen tyrosine kinase signaling protects against acute lung injury through blockade of NADPH oxidase and IL-17A in neutrophils and γδ T cells respectively in mice, Int. Immunopharmacol, 68:… [cited by applicant]
Saha et al., Is Fostamatinib a possible drug for covid-19 ?—A computational study, pp. 1-28, May 1, 2020. [cited by applicant]
Sanderson et al., Syk: A Novel Target for Treatment of Inflammation in Lung Disease, Inflammation & Allergy—Drug Targets, 8(2):87-95, 2009. [cited by applicant]
Strich et al., Fostamatinib Inhibits Neutrophils Extracellular Traps Induced by COVID-19 Patient Plasma: A Potential Therapeutic, Journal of Infectious Diseases, 223(6):981-984, Dec. 24, 2020. [cited by applicant]
Van Eeuwijk et al., The Novel Oral Syk Inhibitor, BI1002494, Protects Mice From Arterial Thrombosis and Thromboinflammatory Brain Infarction, Arterioscler Thromb Vasc Biol., 36(6):1247-1253, Jun. 1, 2016. [cited by applicant]
Zhao et al., Activation of C-Type Lectin Receptor and (RIG)-I-Like Receptors Contributes to Proinflammatory Response in Middle East Respiratory Syndrome Coronavirus-Infected Macrophages, Journal of Infectious Diseases, … [cited by applicant]
Al-Harbi et al., “Amelioration of sepsis-induced acute kidney injury through inhibition of inflammatory cytokines and oxidative stress in dendritic cells and neutrophils respectively in mice: Role of spleen tyrosine kin… [cited by applicant]
Kost-Alimova et al., “A High-Content Screen for Mucin-1-Reducing Compounds Identifies Fostamatinib as a Candidate for Rapid Repurposing for Acute Lung Injury”, Cell Reports Medicine, 2020, 1:100137. [cited by applicant]
Weinblatt et al., “Treatment of Rheumatoid Arthritis With a Syk Kinase Inhibitor: A Twelve-Week, Randomized, Placebo-Controlled Trial”, Arthritis & Rheumatism, 2008, 58(11): 3309-3318. [cited by applicant]