4I0R

Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.

Padilla, F., Bhagirath, N., Chen, S., Chiao, E., Goldstein, D.M., Hermann, J.C., Hsu, J., Kennedy-Smith, J.J., Kuglstatter, A., Liao, C., Liu, W., Lowrie, L.E., Luk, K.C., Lynch, S.M., Menke, J., Niu, L., Owens, T.D., O-Yang, C., Railkar, A., Schoenfeld, R.C., Slade, M., Steiner, S., Tan, Y.C., Villasenor, A.G., Wang, C., Wanner, J., Xie, W., Xu, D., Zhang, X., Zhou, M., Lucas, M.C.

(2013) J Med Chem 56: 1677-1692

• PubMed: 23350847 Search on PubMed
• DOI: https://doi.org/10.1021/jm301720p
• Primary Citation of Related Structures:  
  4I0R, 4I0S, 4I0T


• PubMed Abstract: 
  

  We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies. Ultimately, our mouse model revealed unexpected toxicity that precluded us from further advancing this series.

   View More

---

Organizational Affiliation: 

Hoffmann-La Roche Inc., pRED, Pharma Research & Early Development, 340 Kingsland Street, Nutley, New Jersey 07110, United States.