Claims for Patent: 9,737,554

Summary for Patent: 9,737,554

Title:	Prodrugs of 2,4-pyrimidinediamine compounds and their uses
Abstract:	The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
Inventor(s):	Bhamidipati; Somasekhar (Foster City, CA), Singh; Rajinder (Belmont, CA), Sun; Thomas (Palo Alto, CA), Masuda; Esteban (Menlo Park, CA)
Assignee:	Rigel Pharmaceuticals, Inc. (South San Francisco, CA)
Application Number:	15/005,771
Patent Claims:	1. An oral dosage formulation comprising a hydrate of the prodrug salt: ##STR00077## or a pharmaceutically-acceptable carrier, excipient, and/or diluent; wherein: M is Na; the prodrug salt hydrate present in the oral dosage formulation is substantially crystalline prodrug salt hydrate; and the powder X-ray diffraction data of the crystalline prodrug salt hydrate comprises a characteristic peak at a two theta value of 9.9.+-.0.1.degree. in response to radiation of wavelength 1.54059 .ANG.. 2. The oral dosage formulation of claim 1, the formulation comprising from about 50 mg to about 400 mg of the crystalline prodrug salt hydrate. 3. The oral dosage formulation of claim 1, wherein the powder X-ray diffraction data of the crystalline prodrug salt hydrate comprises a characteristic peak at a two theta value of 11.8.+-.0.1.degree.. 4. The oral dosage formulation of claim 1, wherein the powder X-ray diffraction data of the crystalline prodrug salt hydrate comprises a characteristic peak at a two theta value of 21.8.+-.0.1.degree.. 5. The oral dosage formulation of claim 1, wherein the powder X-ray diffraction data of the crystalline prodrug salt hydrate comprises a characteristic peak at a two theta value of 13.2.degree..+-.0.1.degree.. 6. The oral dosage formulation of claim 1, wherein the hydrate of the prodrug salt has the formula: ##STR00078## wherein x is from about 1 to about 15. 7. The oral dosage formulation of claim 6, wherein x is from about 5 to about 10. 8. The oral dosage formulation of claim 6, wherein x is from about 5 to about 8. 9. The oral dosage formulation of claim 6, wherein x is 6. 10. The oral dosage formulation of claim 8, wherein the powder X-ray diffraction data of the crystalline prodrug salt hydrate comprises a characteristic peak at a two theta value of 3.4.degree..+-.0.1.degree.. 11. The oral dosage formulation of claim 1, wherein the hydrate is: ##STR00079##