Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay
A series of novel pyrimidine analogues were synthesized and evaluated for immunosuppressive activity in the Mixed Lymphocyte Reaction assay, which is well-known as the in vitro model for in vivo rejection after organ transplantation. Systematic variation of the substituents at positions 2, 4 and 6 of the pyrimidine scaffold led to the discovery of 2-benzylthio-5-cyano-6-(4- methoxyphenyl)-4-morpholinopyrimidine with an IC50 value of 1.6 μM in the MLR assay.
COMPOUNDS USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES
The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
-
Page 61
(2008/06/13)
Guanidines
Novel substituted phenylquanidine compounds and processes for their preparation are disclosed. Their use as anti-hypertensive agents is also revealed.
-
(2008/06/13)
More Articles about upstream products of 65783-19-9