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US 8,912,170 B2Granted
Prodrugs of 2,4-pyrimidinediamine compounds and their uses
AssigneeRigel Pharmaceuticals, Inc.
InventorsSomasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
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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.
Claims28
A method of treating an autoimmune disease in a mammal afflicted with the disease, the method comprising administering to the mammal an effective amount of an oral dosage formulation comprising a hydrate of the prodrug salt:
- and a pharmaceutically-acceptable carrier, excipient, and/or diluent;
- wherein:
- M is Na;
- the prodrug salt hydrate present in the oral dosage formulation comprises 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 17.2 ±0.1° in response to radiation of wavelength 1.54059±Å, wherein the autoimmune disease is associated with nonanaphylactic hypersensitivity reactions (Type II, Type III and/or Type IV hypersensitivity reactions) or mediated, at least in part, by activation of the FcyR signaling cascade in monocyte cells.
3 more elements
Dependencies are inferred from the claim text.