APPLEBY, TODD,FLIRI, HANS G.,KEATS, ANDREW J.,LAZARIDES, LINOS,MACKMAN, RICHARD L.,PETTIT, SIMON N.,POULLENNEC, KARINE G.,SANVOISIN, JONATHAN,STEADMAN, VICTORIA A.,WATT, GREGORY M.
申请号：
ES11805697
公开号：
ES2536321T3
申请日:
2011.12.08
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound of Formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: X1 is O, S, or NR1； each R1 is independently H, optionally substituted (C1-C4) alkyl, optionally substituted (C2-C4) alkenyl or optionally substituted (C2-C4) alkynyl； each R2 or R3 is independently H, optionally substituted (C1-C4) alkyl, optionally substituted (C2-C4) alkenyl, optionally substituted (C2-C4) alkynyl, halogen, cyano, C (O) R1, C (O) OR1 or WITH (R1) 2； or R2 and R3 when taken together with the carbon to which both are attached form -C (>； = O) -, -C (>； = S) - or -C (>； = NR1) -； A is O, S (O) n, NR4 or optionally substituted (C1-C2) alkylene； each n is independently 0, 1 or 2； each R4 is independently H, optionally substituted (C1-C4) alkyl, optionally substituted (C2-C4) alkenyl, optionally substituted alkynyl (C2-C4), cyano, C (O) R7, C (O) OR7, CON (R7 ) 2, S (O) R16, S (O) 2R16, S (O) 2OR7 or S (O) 2N (R ') 2； R5 is optionally substituted aryl (C0-C4) alkyl, optionally substituted heterocyclyl (C0-C4) alkyl, optionally substituted cycloalkyl-alkyl (C0-C4) or optionally substituted (C1-C8) alkyl, wherein each aryl-alkyl Optionally substituted (C0-C4), optionally substituted cycloalkyl-alkyl (C0-C4) or optionally substituted (C1-C8) alkyl is optionally substituted with one or more R6； Each R6 is independently halo, CF3, OR4, CH2OR4, SR4, S (O) R16, S (O) 2R16, N (R1) 2, NHCOR1, NHC (O) OR1, NHC (O) N (R1) 2, NHC (NR1) R1, NHC (NR1) N (R1) 2, C (O) R1, C (O) N (R1) 2, CO2R1, S (O) 2OR1, S (O) 2N (R1) 2, NHS (O) 2OR1, NHS (O) 2R16, NHS (O) 2N (R1) 2, P (O) (OR1) 2, P (O) OR1) (N (R1) 2), P (O) ( R7) (OR1), OP (O) (OR1) 2, OP (O) (OR1) (N (R1) 2), NHP (O) (OR1) 2 or NHP (O) (OR1) (N (R1 )two)； each R7 is H, optionally substituted (C1-C8) alkyl, optionally substituted (C2-C8) alkenyl, optionally substituted (C2-C8) alkynyl, optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted cycloalkyl, aryl (C1-) alkyl C4) optiona
