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Heterocyclic ERK2 inhibitors and uses thereof
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
CAO, JINGRONG,GREEN, JEREMY,HALE, MICHAEL,MALTAIS, FRANCOIS,STRAUB, JUDY,TANG, QING,ARONOV, ALEX
申请号:
ES02724922
公开号:
ES2549677T3
申请日:
2002.02.08
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula II or III: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: Sp is selected from the following: ** Formula ** wherein Ring A and QR2 are fixed to Sp in non-adjacent positions; and where Sp has up to two R6 substituents, wherein R6 is selected from an optionally substituted C1-6 aliphatic group, F, Cl, (CH2) and N (R7) 2, N (R7) 2, OR7, SR7, NR7COR7, NR7CON (R7) 2, CON (R7) 2, SO2R7, NR7SO2R7, COR7, CN or 10 SO2N (R7) 2, with the proviso that two atoms in the carbon ring that can be replaced in Sp do not replace simultaneously with R6; T is -CO-, -C (O) C (O) -, -CO2NH-, -C (O) NH-, -C (O) NHNH-, -CO2-, -OC (O) -, -NHCO2 -, -O-, CH2NH-, -N (H) N (H) -, -NHC (O) -, -S-, -S (O) 2-, -SO2NH- or-NHSO2-; Q is -CO-, -CO2-, -CONH-, -OC (O) NH-, -C (O) ONH- or -CONHNH-; U is selected from -NR7-, -NR7CO-, -NR7CONR7-, -NR7CO2-, -O-, -CONR7-, -CO-, -CO2-, -OC (O) -, -NR7SO2-, - SO2NR7-, -NR7SO2NR7- or -SO2-; m and n are each independently selected from zero or one; R1 is selected from hydrogen, CN, halogen, R, N (R7) 2, OR or OH; R2 is selected from - (CH2) and R5, - (CH2) and CH (R5) 2, - (CH2) and CH (R8) CH (R5) 2, -N (R4) 2 or -20 NR4 (CH2) and N (R4) 2; y is 0-6; R3 is selected from R7, R, - (CH2) and CH (R8) R, CN, - (CH2) and CH (R8) CH (R5) 2 or - (CH2) and CH (R8) N (R4) 2; each R is independently selected from an optionally substituted group, selected from C1-6 aliphatic, C6-10 aryl, a heteroaryl ring having 5-10 ring atoms or a heterocyclyl ring having 3-10 atoms in the ring; each R4 is independently selected from R, R7, -COR7, -CO2R, -CON (R7) 2, -SO2R7, - (CH2) and R5 or - (CH2) and CH (R5) 2; Each R5 is independently selected from R, OR, CO2R, (CH2) and N (R7) 2, N (R7) 2, OR7, SR7, NR7COR7, NR7CON (R7) 2, CON (R7) 2, SO2R7, NR7SO2R7 , COR7, CN or SO2N (R7) 2; each R7 is independently selected from hydrogen or an optionally substituted C1-6 aliphatic group or two R7 on the same nitrogen atom are taken together with the nitr
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