| abstract |
A compound of formula (I): wherein R 1 is 9 or 10 membered bicyclic heteroaryl, wherein the 9 or 10 membered bicyclic heteroaryl contains from one to three heteroatoms independently selected from oxygen and nitrogen and is optionally substituted with C 1 alkyl. 6, C3-6 cycloalkyl, halo, -CN, -OR13 or -NHSO2R14; or phenyl fused to a 5-membered heterocyclyl, wherein the 5-membered heterocyclyl contains one or two heteroatoms independently selected from oxygen and nitrogen and is substituted with oxo; R2 is 5-membered heteroaryl in which the 5-membered heteroaryl contains from one to three heteroatoms independently selected from oxygen, nitrogen and sulfur and is optionally substituted with one to three substituents independently selected from C16 alkyl optionally substituted with one to three fluorine atoms; C2-6 alkenyl; C3-6 cycloalkyl; -OR5; halo; -COR6; -CO2R7; -CONR8R9; - (CH2) mNR10R11; - CH (CH3) NHCOphenyl; -NHCO2R12; - (CH2) nphenyl; and 5-membered heteroaryl, wherein the second 5-membered heteroaryl contains one or two heteroatoms independently selected from oxygen, nitrogen and sulfur and is optionally substituted with C1-6 alkyl; R3 is hydrogen or fluorine; R4 is hydrogen or methyl; R5, R7, R12 and R13 are each independently hydrogen or C1-6 alkyl; R6, R18 and R1920 are each independently C1-6 alkyl; R8 and R9 are each independently hydrogen or C1-6 alkyl, or R8 and R9, together with the denitrogen atom to which they are attached, are linked to form a 5 or 6 membered heterocyclyl which optionally contains an oxygen atom; R10 and R11 are each independently hydrogen or C1-6 alkyl, or R10 and R11, together with the denitrogen atom to which they are attached, are linked to form a 5-, 6- or 7-membered heterocyclyl or a heterocyclyl cyclicyl in which the heterocyclyl of 5, 6 or 7 members or the 10-membered bicyclic heterocyclyl optionally contains an oxygen atom, a sulfur atom or an additional nitrogen atom and is optionally substituted with one or two substituents independently selected from C1-6 alkyl; C3-6 cycloalkyl; halo; oxo; phenyl optionally substituted with halo; pyridyl; - (CH2) pOR15; - (CH2) qNR16R17; -COR18 and - SO2R19; R14 is C1-6 alkyl or phenyl; R15 is hydrogen, C1-6 alkyl or (CH2) rphenyl; R16 and R17, together with the nitrogen atom to which they are linked, are attached forming a 5- or 6-membered heterocyclyl that optionally contains an oxygen atom; and m, n, p, q, r are each independently 0, 1 or 2. |