Aclaris Therapeutics, Inc.

Confluence Life Sciences, Inc.

Pfizer Corporation

John Robert Springer

Susan Landis Hockerman

James Robert Blinn

Eric Jon Jacobsen

Gary A Decrescenzo

Balekudru Devadas

Margaret Lanahan Grapperhaus

Eddine Saiah

Shaun Raj Selness

Mark E Schnute

Li Huang Xing

Robert Owen Hughes

Christoph Wolfgang Zapf

Daniel Patrick Walker

Joseph B Monahan

Zhao-Kui Wan

Seungil Han

Michelle Ann Schmidt

Danny James Garland

Edward Hellriegel

Walter Smith

Heidi Hope

David Gordon

David R Anderson

Eric Jonathan Jacobsen

Mark Edward Schnute

The present disclosure provides methods of synthesizing a compound of Formula (P)-I. The method proceeds through several different pathways including several novel chiral separations, a Sonogashira coupling, a zinc mediated reductive cyanation, as well as through various halide containing intermediates. Also disclosed is the multi-kilogram preparation of several novel intermediates.

Methods of synthesizing substituted pyridinone-pyridinyl compounds

The present disclosure relates to oral compositions of Compound I or a derivative thereof. Methods of use for treating an inflammatory condition are also disclosed.

Oral compositions of MK2 pathway inhibitor for treatment of immune conditions

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I) 

Bruton's tyrosine kinase inhibitors

Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein R, R, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.

Pyrrolopyrimidine ITK inhibitors for treating inflammation and cancer

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseeases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. 

Disclosed herein are heterocyclic compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein R, R, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.

Heterocyclic ITK inhibitors for treating inflammation and cancer

4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds, pharmaceutically acceptable salts, solvates and pharmaceutical compositions of compounds embraced by Formula (I), provide a therapeutic benefit to subjects with disease conditions, especially cancer, wherein Rand Rare as defined in the detailed description. 

4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds as TAK1 inhibitors in disease treatment

Disclosed herein are substituted pyrrolopyridine and pyrrolopyrazine compounds and compositions useful in the treatment of TAK mediated diseases, such as cancer, having the structure of Formula (I): wherein R, R, R, and Rare as defined in the detailed description. Methods of modulation of TAK activity in a human or animal subject are also provided, providing therapeutic benefit to subjects with disease conditions, especially cancer.

Substituted pyrrolo[2,3-b]pyridines for treating cancer or inflammatory diseases

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Wentzville, MO, United States of America

John Robert Springer