Exelixis, Inc.

Frenel DeMorin

Sagar Shakya

Wei Xu

Stephan D Parent

Yong Wang

Khalid Ali Shah

Melanie Janelle Bevill

Peter H Wong

Courtney S Johnson

Peter Wong

The present invention relates to processes for the synthetic preparation of c-Met inhibitors of Formula I, or pharmaceutically acceptable salts thereof. The present invention further relates to processes for the synthetic preparation of the c-Met inhibitor, Compound 1, or a pharmaceutically acceptable salt thereof. The present invention also relates to processes for the synthetic preparation of Compound 1·hemifumarate. The invention further relates to large scale processes for the synthetic preparation of the c-Met inhibitor, Compound 1 and Compound 1·hemifumarate.

Processes for the preparation of a kinase inhibitor

The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.

Crystalline forms and salt forms of a kinase inhibitor

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Long Beach, CA, United States of America

Frenel DeMorin