Pharmacia Corporation

Pfizer Corporation

Michael Mao

Donald W Hansen, Jr

Barnett S Pitzele

Timothy J Hagen

E Ann Hallinan

Richard C Durley

Brian S Hickory

Alan E Moormann

Mihaly V Toth

Sofya Tsymbalov

Arija A Bergmanis

Mahima Trivedi

Ronald Keith Webber

Kam F Fok

Alok K Awasthi

Jeffrey A Scholten

Pamela T Manning

Michelle A Promo

Jeffrey S Snyder

Scott S Ganser

Richard R Schartman

Foe Siong Tjoeng

Jerry D Clark

Jodi L Moe

Partha Mudipalli

Christine B Seymour

Shaun Raj Selness

Dennis K Anderson

Gopichand Yalamanchili

Win Naing

John Walker

Lisa L McDermott

Patrick H Lau

Kimberley C Allen

John E Baldus

Gopi Yalamanchili

Tobin C Schilke

Shekhar Viswanath

Jon P Lawson

Sastry A Kunda

George H Klemm

Clay Little

Brian Patrick Chekal

Patricia S Miyake

Ronald J VanderRoest

Thomas P Fraher

Richard Alan Vonder Embse

Daniel Dukesherer

Todd Boehlow

Dan R Dukesherer

Rajappa Vaidyanathan

Albert D Edney

Tom Fevig

Randy Geurink

Kimberly K Allen

Albert D Edeny

Daniel R Dukesherer

Jason A Hanko

Kimberly L Kolbert

Ahmad Y Sheikh

This invention is directed generally to processes for the preparation of compounds of Formula I: wherein R, R, R, R, X, X, X, X, X, Xare as defined in the specification.

Processes for the preparation of 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide

The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.

Amidino compounds useful as nitric oxide synthase inhibitors

Method of making an alpha-amino acid compound having the structure of Formula 32:comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33:where the substituents are described herein.

Methods of making amidino compounds useful as nitric oxide synthase inhibitors

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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Chesterfield, MO, United States of America

Michael Mao