Rigel Pharmaceuticals, Incorporated

Syntex (u.s.a.) Inc.

Roche Palo Alto LLC

Thomas Weitao Sun

Rajinder Paul Singh

Somasekhar Bhamidipati

Esteban Masuda

Valentino J Stella

Robin D Clark

Counde O'Yang

Francisco Javier Lopez-Tapia

Alam Jahangir

Alexander Victor Muehldorf

Bruce Andrew Kowalczyk

Keith Roger Bley

Ray J Lo

Dane A Goff

Henry Lu

Matt Duan

Sarkiz D Issakani

Hong Ren

Sarkiz D Issankani

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.

Prodrugs of 2,4-pyrimidinediamine compounds and their uses

The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

Embodiments of topical formulations for administering compound I or a pharmaceutically acceptable salt or solvate thereof are disclosed. Embodiments of methods for using the topical formulations in the treatment of dermatological disorders such as cutaneous collagen vascular diseases, e.g., cutaneous lupus, also are disclosed.

Topical formulation for administering a compound

Embodiments of topical formulations for administering compound I or a pharmaceutically acceptable salt or solvate thereof are disclosed. Embodiments of methods for using the topical formulations in the treatment of dermatological disorders such as cutaneous collagen vascular diseases, e.g., cutaneous lupus, also are disclosed. 

Disclosed are tablets comprising hydrolytically stable formulations of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt (Compound 1) prepared by a wet granulation process.

Wet granulation using a water sequestering agent

Disclosed are tablets comprising hydrolytically stable formulations of (6-(5-fluoro-2-(3,4,5 -trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt (Compound 1) prepared by a wet granulation process.

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Fremont, CA, United States of America

Thomas Weitao Sun