Bruton’s Tyrosine Kinase (BTK) is a nonreceptor cytoplasmic tyrosine kinase belonging to the Tec kinase family, critical for B-cell proliferation, differentiation and signaling. Inhibition of BTK may be an effective way to treat autoimmune diseases such as rheumatoid arthritis (RA) and systemic lupus erythematous (SLE). In this poster, we will describe (1): the quick systematic back-pocket SAR development in the imidazolpyrazine series using library approach; (2): Quick hinge screening in the H3 binder series utilizing parallel synthesis, and hit optimization through a close collaboration between ACE, Med Chem groups, CM&I, and structure chemistry.

Bruton’s Tyrosine Kinase (BTK) program: Quick systematic SAR development utilizing parallel synthesis

253rd National Meeting (2017)

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