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Cyclopropyl dicarboxamides and analogues that present anti-cancer and anti-proliferative activities
专利权人:
DECIPHERA PHARMACEUTICALS; LLC
发明人:
FLYNN, DANIEL L.,KAUFMAN, MICHAEL D.
申请号:
ES11719421
公开号:
ES2475741T3
申请日:
2011.04.29
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, enantiomer, stereoisomer, or tautomer thereof, wherein X is halogen; Z1 and Z2 are CR2; Z3 is CH; each R1 is independently and individually halogen, H, C1-C6 alkyl, branched C3-C7 alkyl, C3-C7 cycloalkyl, or -CN; each R2 is individually and independently H, halogen, C1-C6 alkyl, or cyano; R3 is -C (O) R4, -C (O) -C6-C10 aryl, -C (O) -C4-C6 heterocyclyl, or -C (O) -C5-C6 heteroaryl, wherein aryl is phenyl, naphthyl, tetrahydronaphthyl, indenyl or indanyl; and with the proviso that when R3 is -C (O) -C4-C6 heterocyclyl, the heterocyclyl does not have a point of attachment of N to -C (O); R4 is C3-C8 cycloalkyl, C1-C7 alkyl, - (CH2) p-CN, - (CH2) p-OR6, - (CH2) p-NR6 (R7), - (CH2) p-SO2-C1-alkyl C6, - (CH2) p-aryl C6-C10, - (CH2) p-heteroaryl C5-C6, or - (CH2) p-heterocyclyl C4-C6, in which each alkyl or alkylene is optionally substituted with one or two C1-C6 alkyl; and aryl is phenyl, naphthyl, tetrahydronaphthyl, indenyl or indanyl; each R6 and R7 is individually and independently H, C1-C6 alkyl, or branched C3-C8 alkyl; each cycloalkyl, aryl, heteroaryl and heterocyclyl is independently substituted with - - (R25) m; each R25 is individually and independently C1-C6 alkyl, branched C3-C8 alkyl, halogen, - (CH2) m-CN, - (CH2) m-OR6, - (CH2) m-NR6 (R7), - (CH2) m-SO2-C1-C6 alkyl, - (CH2) mC (O) NR6 (R7), - (CH2) mC (O-heterocyclyl C4-C6, or - (CH2) m-heterocyclyl C4-C6, wherein each alkyl or alkylene is optionally substituted with one or two C1-C6 alkyl; each m is individually and independently 0, 1, 2 or 3; and p is 1, 2 or 3.Un compuesto de Fórmula I, o una sal, enantiómero, estereoisómero, o tautómero farmacéuticamente aceptable del mismo, en la que X es halógeno; Z1 y Z2 son CR2; Z3 es CH; cada R1 es independiente e individualmente halógeno, H, alquilo C1-C6, alquilo C3-C7 ramificado, cicloalquilo C3- C7, o -CN; cada R2 es individual e independientemente H, halógeno, alquilo C1-C6, o ciano; R3 es -C(O)
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