IP Library Granted Patent US 8,389,515
Granted Patent B2
US 8,389,515 · App. 12/950,612 · Granted Mar 5, 2013

2,4-pyrimidinediamine compounds and prodrugs and their uses

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Quick Facts
Patent No.
US 8,389,515
App. No.
12/950,612
Granted
Mar 5, 2013
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 (20)

1. A compound of any of formulae (I)-(III):

or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 , having formula (I):

or a pharmaceutically acceptable salt thereof.

3. The compound according to claim 1 , having formula (II):

or a pharmaceutically acceptable salt thereof.

4. The compound according to claim 1 , having formula (III):

or a pharmaceutically acceptable salt thereof.

5. A pharmaceutically acceptable salt of a compound according to claim 1 .

6. A mono- or di-sodium salt, mono- or di-potassium salt, mono- or di-lithium salt, calcium salt, magnesium salt, ammonium salt of a compound according to claim 1 .

7. A mono- or di-trifluoroacetic acid salt, p-toluenesulfonic acid salt, hydrochloride salt, benzenesulfonic acid salt, or ethanesulfonic acid salt of a compound according to claim 1 .

8. A pharmaceutical composition comprising a compound or salt according to claim 1 and an acceptable carrier, excipient and/or diluent.

9. A method of inhibiting cell degranulation in a subject, comprising administering to the subject a pharmaceutically effective amount of a compound or salt according to claim 1 effective to inhibit degranulation.

10. A method of inhibiting an activity of a Syk kinase in a subject, comprising administering to the subject a pharmaceutically effective amount of a compound or salt according to claim 1 effective to inhibit the Syk kinase activity.

11. A method of inhibiting an Fc receptor signal transduction cascade in a subject, comprising administering to the subject a pharmaceutically effective amount of a compound or salt according to claim 1 effective to inhibit the Fc receptor signal transduction cascade.

12. The method according to claim 11 in which the Fc receptor is selected from FcαRI, FcγRI, FcγRIII and FIεRI.

13. A method of inhibiting Syk kinase in a cell comprising contacting a Syk kinase or a cell comprising a Syk kinase with a compound or salt according to claim 1 .

14. A method of inhibiting degranulation of a cell comprising contacting a cell that degranulates with a compound or salt according to claim 1 .

15. A method of inhibiting the Fc receptor signaling cascade comprising contacting a cell expressing an Fc receptor with a compound or salt according to claim 1 .

16. A method of inhibiting the Syk-dependent signal transduction cascade comprising contacting a Syk-dependent receptor or a cell expressing a Syk-dependent receptor with a compound or salt according to claim 1 .

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 Jan 28, 2011
From: SINGH, RAJINDER; SOMASEKHAR, BHAMIDIPATI; CLOUGH, JEFFREY
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 025716/0503 →