BOYS MARK LAURENCE,BURGESS LAURENCE E.,GRONEBERG ROBERT D.,HARVEY DARREN M.,HUANG LILY,KERCHER TIMOTHY,KRASER CHRISTOPHER F.,LAIRD ELLEN,TARLTON EUGENE,ZHAO QIAN
申请号:
NZ60344611
公开号:
NZ603446A
申请日:
2011.04.11
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed are 5,7-substituted-imidazo[1,2-C]pyrimidine&rsquos as inhibitors of JAK kinases of formula (I). The compounds are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their comorbidities. Examples of compounds of formula (I) are: 2-(3-(3-(7-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile hydrochloride 3-Cyclopropyl-3-(3-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)propanenitrile and 3-cyclopentyl-3-(4-(7-(4-(1-methylpiperidin-4-yl)phenyl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)propanenitrile. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and the use of a compound of formula (I) in the manufacture of a medicament for the treatment of an autoimmune disease or inflammatory disease organ, tissue or cell transplant rejection or malignancy.