- Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors
-
A series of furano[3,2-d]pyrimidine Syk inhibitors were synthesized and optimized for their enzyme potency and selectivity versus other kinases. In addition, ADME properties were assessed and compounds were prepared with optimized profiles for in vivo experiments. Compound 23 was identified as having acceptable pharmacokinetic properties and demonstrated efficacy in a rat collagen induced arthritis model.
- Hoemann, Michael,Wilson, Noel,Argiriadi, Maria,Banach, David,Burchat, Andrew,Calderwood, David,Clapham, Bruce,Cox, Phil,Duignan, David B.,Konopacki, Don,Somal, Gagandeep,Vasudevan, Anil
-
p. 5562 - 5567
(2016/11/09)
-
- FURO[3,2-d]PYRIMIDINE COMPOUNDS
-
The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
- -
-
-