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Thiophene or thiazole derivatives and their use as PI3K inhibitors
专利权人:
MILLENNIUM PHARMACEUTICALS; INC.
发明人:
CARDIN, DAVID P.,GAULIN, JEFFREY L.,GREENSPAN, PAUL D.,VYSKOCIL, STEPAN,XU, TIANLIN,RENOU, CHRISTELLE C.
申请号:
ES09767054
公开号:
ES2491522T3
申请日:
2009.06.17
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula I: or a pharmaceutically acceptable salt thereof, in which: Y1 is S; Y2 is C or N, in which when Y2 is C, R1 is H, -CN, halogen, Z-R3, C1-6 aliphatic, or a 3-10 membered cycloaliphatic, and in which when Y2 is N, R1 is absent; where: Z is chosen from an optionally substituted C1-3 alkylene chain, -O-, -N (R1a) -, -S-, -S (O) -, -S (O) 2-, -C (O) -, -CO2-, -C (O) NR1a-, -N (R1a) C (O) -, -N (R1a) CO2-, -S (O) 2NR1a-, - N (R1a) S (O) 2-, -OC (O) N (R1a) -, - N (R1a) C (O) NR1a-, -N (R1a) S (O) 2N (R1a) - or -OC (O) -; R1a is hydrogen or an optionally substituted aliphatic C1-4, and R3 is an optionally substituted group selected from an aliphatic C1-6, a 3-10 membered cycloaliphatic, a 4-10 membered heterocyclyl with 1-5 heteroatoms independently selected from nitrogen, oxygen or sulfur, a 6-10 membered aryl, or a 5-10 membered heteroaryl with 1-5 heteroatoms independently selected from nitrogen, oxygen or sulfur; R2 is H, halogen, -W-R5 or -R5, where: W is chosen from an optionally substituted C1-3 alkylene chain, -O-, -N (R2a) -, - S-, -S (O) - , -S (O) 2-, - C (O) -, -CO2-, -C (O) NR2a-, -N (R2a) C (O) -, -N (R2a) CO2-, -S ( O) 2NR2a-, -N (R2a) S (O) 2-, -OC (O) N (R2a) -, - N (R2a) C (O) NR2a-, -N (R2a) S (O) 2N (R2a) - or -OC (O) -. R2a is hydrogen or an optionally substituted aliphatic C1-4, and R5 is an optionally substituted group selected from an aliphatic C1-6, a 3-10 membered cycloaliphatic, a 4-10 membered heterocyclyl with 1-5 heteroatoms independently selected from nitrogen, oxygen or sulfur, a 6-10 membered aryl, or a 5-10 membered heteroaryl with 1-5 heteroatoms independently selected from nitrogen, oxygen or sulfur; X1, X2 and X3 are each independently N or CR6, where each time it is present, R6 is independently hydrogen, -CN, halogen, -V-R7, an aliphatic C1-6 or a 3-10 membered cycloaliphatic, where : V is chosen from an optionally substituted C1-3 alkylene chain, -O-, -N (R6a) -, -S-, -S (O) -, -S (O) 2-, - C (O) - , -CO2-, -C (
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