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Last Updated: September 26, 2022

Claims for Patent: 7,449,458

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Summary for Patent: 7,449,458
Title:Prodrugs of 2,4-pyrimidinediamine compounds and their uses
Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds of structural formula shown below, compositions comprising these compounds, intermediates and methods for synthesizing these compounds, and methods for using these compounds in a variety of applications including treatment of autoimmune diseases. ##STR00001##
Inventor(s): Bhamidipati; Somasekhar (Foster City, CA), Singh; Rajinder (Belmont, CA), Stella; Valentino J. (Lawrence, KS), Sun; Thomas (Fremont, CA)
Assignee: Rigel Pharmaceuticals, Inc. (South San Francisco, CA)
Application Number:11/337,049
Patent Claims: 1. A compound according to structural formula (IIIa): ##STR00038## or a pharmaceutically acceptable salt wherein R.sup.p is --CH.sub.2--O--P(O)(OH).sub.2.

2. The compound of claim 1 which is a pharmaceutically acceptable salt.

3. The compound of claim 2 which is an alkali metal salt.

4. The compound of claim 3 which is a sodium salt.

5. The compound of claim 4 which is a disodium salt.

6. The compound of claim 3 which is a potassium salt.

7. The compound of claim 6 which is a dipotassium salt.

8. The compound of claim 2 which is an alkaline earth metal salt.

9. The compound of claim 8 which is a calcium salt.

10. The compound of claim 8 which is a magnesium salt.

11. The compound of claim 2 which is an alkylamino salt.

12. The compound of claim 2 which is an ammonium salt.

13. N4-(2,2-dimethyl-4-[(dihydrogen phosphonoxy)methyl]-3-oxo-5-pyrido [1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediam- ine disodium salt hexahydrate.

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Serving leading biopharmaceutical companies globally:

Harvard Business School
Johnson and Johnson
Boehringer Ingelheim
Express Scripts

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