Pharmacia Corporation

Jodi L Moe

Michael Mao

Jerry D Clark

Christine B Seymour

Partha Mudipalli

Shaun Raj Selness

Dennis K Anderson

Gopichand Yalamanchili

Win Naing

John Walker

Lisa L McDermott

Patrick H Lau

Tobin C Schilke

Kimberley C Allen

Shekhar Viswanath

John E Baldus

Jon P Lawson

Sastry A Kunda

Clay Little

Gopi Yalamanchili

Thomas P Fraher

Patricia S Miyake

Albert D Edney

Tom Fevig

Kimberly K Allen

Albert D Edeny

Todd Boehlow

Daniel R Dukesherer

Jason A Hanko

Kimberly L Kolbert

Dan R Dukesherer

Ahmad Y Sheikh

This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R, R, R, Y, Y, Y, Y, and Yare as defined in the specification.

Process for making substituted pyrazoles

This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I):wherein R, R, R, Y, Y, Y, Y, and Yare as defined in the specification.

Crystalline forms of the p38 kinase inhibitor N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole are provided. These crystalline forms include (a) a first anhydrous crystalline form possessing improved physical stability relative to other solid-state forms of the compound; (b) a second anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; (c) a third anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; and (d) solvated crystalline forms, hydrated crystalline forms, and crystalline salt forms of the compound that are useful, for example, as intermediate solid-state forms in the preparation of other crystalline forms of the compound. Also provided are combinations and pharmaceutical compositions comprising at least one of these crystalline forms, processes for preparing these crystalline forms and for preparing compositions comprising these crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of at least one of these crystalline forms.

Solid-state forms of N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl) pyrazole

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Buffalo Grove, IL, United States of America

Jodi L Moe