FREEZE BRIAN S.,HIROSE MASAAKI,HU YONGBO,HU ZHIGEN,LEE HONG MYUNG,SELLS TODD B.,SHI ZHAN,VYSKOCIL STEPAN,XU TIANLIN
申请号：
NZ60708711
公开号：
NZ607087A
申请日:
2011.08.11
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
The disclosure relates to a family of substituted heteroaryl/morpholino-thiophene compounds as shown in IA and IB. In these compounds, G1 can refer to either a carbon or nitrogen to form thiophene or thiozole. A, R1, W, HY and R2 and n are all described in the specification, but in most cases, A is aryl or heteroaryl, commonly with chloride bound to it, and W is a substituted alkyl group. HY can either be heteroaryl or a morpholine derivative. This family of compounds are inhibitors of phosphatidylinositol 3-kinase (PI3K) and therefore may be useful for the treatment of proliferative, inflammatory or cardiovascular disorders. These include allergies/anaphylaxis, acute and chronic inflammation, rheumatoid arthritis, autoimmunity disorders, thrombosis, hypertension, cardiac hypertrophy, and heart failure. Example compounds include: N-{ 4-[4-(4-chlorobenyl)-3-cyano-5-(4H-1,2,4-triazol-3-yl)-2-thienyl]pyridin-2-yl} acetamide (4-Methoxyphenyl)[5-pyridin-4-yl-2-(4H-1,2,4-triazol-3-yl)-3-thienyl]methanol 4-(4-Chlorobenzyl)-2-(2-methylpyridin-4-yl)-5-(4H-1,2,4-triazol-3-yl)thiazole 3-[4-(4-chlorobenzyl)-5-(4H-1,2,4-triazol-3-yl)-13-thiazol-2-yI]-2-methylpyrazolo[15-a]pyridine N-({ 3-[4-(4-chlorobenzyl)-5-(4H-1,2,4-triazol-3-yl)-1,3-thiazol-2-yl]-2-methylpyrazolo[1,5-a]pyridin-5-yl} methyl)pyrazine-2-carboxamide N-{ 4-[4-{ (4-chlorophenyl)[3(dimethylamino)azetidin-1-yl]methyl} -5-(4H-1,2,4-triazol-3-yl)-2-thienyl]pyridin-2-yl} acetamide.
