Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson, T.W., Richardson, P.F., Bailey, S., Brooun, A., Burke, B.J., Collins, M.R., Cui, J.J., Deal, J.G., Deng, Y.L., Dinh, D., Engstrom, L.D., He, M., Hoffman, J., Hoffman, R.L., Huang, Q., Kania, R.S., Kath, J.C., Lam, H., Lam, J.L., Le, P.T., Lingardo, L., Liu, W., McTigue, M., Palmer, C.L., Sach, N.W., Smeal, T., Smith, G.L., Stewart, A.E., Timofeevski, S., Zhu, H., Zhu, J., Zou, H.Y., Edwards, M.P.
J. Med. Chem.