- Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors
-
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described.
- Packard, Garrick K.,Papa, Patrick,Riggs, Jennifer R.,Erdman, Paul,Tehrani, Lida,Robinson, Dale,Harris, Roy,Shevlin, Graziella,Perrin-Ninkovic, Sophie,Hilgraf, Robert,McCarrick, Margaret A.,Tran, Tam,Fleming, Yuedi,Bai, April,Richardson, Samantha,Katz, Jason,Tang, Yang,Leisten, Jim,Moghaddam, Mehran,Cathers, Brian,Zhu, Dan,Sakata, Steven
-
p. 747 - 752
(2012/03/11)
-
- INHIBITORS OF TNFα, PDE4 AND B-RAF, COMPOSITIONS THEREOF AND METHODS OF USE THEREWITH
-
Provided herein are compounds having TNFα and/or PDE4 and/or B-RAF inhibitory activity, and compositions thereof. In particular, provided herein are compounds of the formula (I) and pharmaceutically acceptable salts, solvates, hydrates, clathrates, stereoisomers, polymorphs and prodrugs thereof, wherein Ar, R1, R2, R3, R4, n and Z are as described herein. Further provided herein are methods for treating or preventing various diseases and disorders by administering to a patient one or more TNFα and/or PDE4 and/or B-RAF inhibitors. In particular, provided herein are methods for preventing or treating cancer, inflammatory disorders, cognition and memory disorders and autoimmune disorders, or one or more symptoms thereof by administering to a patient one or more TNFα and/or PDE4 and/or B-RAF inhibitors.
- -
-
Page/Page column 221
(2010/11/28)
-