IP Library Granted Patent US 8,642,593
Granted Patent B2
US 8,642,593 · App. 13/759,457 · Granted Feb 4, 2014

2,4-pyrimidinediamine compounds and prodrugs and their uses

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Quick Facts
Patent No.
US 8,642,593
App. No.
13/759,457
Granted
Feb 4, 2014
Kind
B2
Abstract

The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

Claims (29)

1. A method of treating a disease in a subject, where the disease is selected from an allergic disease, low grade scarring and scarring, comprising administering to the subject a pharmaceutically effective amount of a compound of any of formulae (I)-(III):

or a pharmaceutically acceptable salt thereof, effective to inhibit the Fc receptor signal transduction cascade.

2. The method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (I):

or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (II):

or a pharmaceutically acceptable salt thereof.

4. The method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (III):

or a pharmaceutically acceptable salt thereof.

5. A method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of a pharmaceutically acceptable salt of a compound of any of formulae (I)-(III).

6. A method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of a mono- or di-sodium salt, a mono- or di-potassium salt, a mono- or di-lithium salt, a calcium salt, a magnesium salt, or an ammonium salt of a compound of any of formulae (I)-(III).

7. A method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of a mono- or di-trifluoroacetic acid salt, a p-toluenesulfonic acid salt, a hydrochloride salt, a benzenesulfonic acid salt, or an ethanesulfonic acid salt of a compound of any of formulae (I)-(III).

8. A method according to claim 1 , comprising administering to the subject a pharmaceutically effective amount of a pharmaceutical composition comprising a compound of any of formulae (I)-(III) or a pharmaceutically acceptable salt thereof, and an acceptable carrier, excipient and/or diluent.

9. A method of treating an autoimmune disease in a subject, the autoimmune disease being selected from Hashimoto's thyroiditis, autoimmune hemolytic anemia, autoimmune atrophic gastritis of pernicious anemia, autoimmune encephalomyelitis, autoimmune orchitis, Goodpasture's disease, autoimmune thrombocytopenia, sympathetic ophthalmia, myasthenia gravis, Graves' disease, primary biliary cirrhosis, chronic aggressive hepatitis, ulcerative colitis, membranous glomerulopathy, systemic lupus erythematosis, rheumatoid arthritis, Sjogren's syndrome, Reiter's syndrome, polymyositis-dermatomyositis, systemic sclerosis, polyarteritis nodosa, multiple sclerosis and bullous pemphigoid, the method comprising administering to the subject a pharmaceutically effective amount of a compound of any of formulae (I)-(III):

or a pharmaceutically acceptable salt thereof, effective to treat the autoimmune disease.

10. The method according to claim 9 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (I):

or a pharmaceutically acceptable salt thereof.

11. The method according to claim 9 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (II):

or a pharmaceutically acceptable salt thereof.

12. The method according to claim 9 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (III):

or a pharmaceutically acceptable salt thereof.

13. A method of treating rheumatoid arthritis in a subject, comprising administering to a subject suffering from rheumatoid arthritis a pharmaceutically effective amount of a compound of any of formulae (I)-(III):

or a pharmaceutically acceptable salt thereof.

14. The method according to claim 13 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (I):

or a pharmaceutically acceptable salt thereof.

15. The method according to claim 13 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (II):

or a pharmaceutically acceptable salt thereof.

16. The method according to claim 13 , comprising administering to the subject a pharmaceutically effective amount of the compound of formula (III):

or a pharmaceutically acceptable salt thereof.

17. The method according to claim 13 in which the amount of the compound or salt administered is effective to achieve a serum concentration of the corresponding drug that is at or above the IC 50 of Syk inhibition of the drug, as measured in an in vitro assay.

Assignments (2)
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 23, 2013
From: SINGH, RAJINDER; SOMASEKHAR, BHAMIDIPATI; CLOUGH, JEFFREY
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 031841/0577 →