| 主权项 |
1. A compound of the Formula (I)wherein
Q is selected from —CH═NR12, —W, —CH2NHR13, —CH═O and —CH(OR17)2; A is —CH2C(O)—; Y is —NR6R7; R1 is —H; each R3 is independently selected from C1-6 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, —Z-heterocyclyl, —Z-aryl, —Z-heteroaryl, —Z—NR6R7, —Z—C(═O)—NR6R7, —Z—NR6—C(═O)—R7, —Z—C(═O)—R7, —Z—OR7, halogen, —Z—SR7, —Z—SOR7, —Z—SO2R7, —Z—SO2NR6R7 and —Z—COOR7, wherein any heterocyclyl may be substituted with one or more R4, and wherein any heteroaryl and any aryl may be substituted with one or more R5; Z is selected from a single bond, C1-4 alkylene, heterocyclylene and C3-6 cycloalkylene; each R4 is independently selected from C1-5 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C1-4 alkoxy, C3-10 cycloalkyl, —N(R10)2, carbamoyl, and —OH; each R5 is independently selected from C1-6 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C1-4 alkoxy, C3-6 cycloalkyl, —CN, —F, —CI, —Br, carbamoyl and —OH; each of R6 and R7 is independently selected from —H, C1-8 alkyl, C1-4 fluoroalkyl, C1-4 perfluoroalkyl, C1-4 hydroxyalkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl, —Z-heterocyclyl, —Z-heteroaryl and —Z-aryl, which alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, heteroaryl and aryl may optionally be substituted with one or more independently selected R8; or, alternatively, R6 and R7 may together with the N-atom to which they are attached form an N-heterocyclic ring optionally substituted with one or more independently selected R8; each R8 is independently selected from C1-5 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C2-5 alkenyl, C2-5 alkynyl, C3-10 cycloalkyl, —Z-heterocyclyl, —Z-heteroaryl, —Z-aryl, —Z—NR10R11, —Z—C(═O)—NR10R11, —Z—OR9, halogen, —CN, —Z—SR9, —Z—SOR9, —Z—SO2R9 and —Z—COOR9, which alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, heteroaryl and aryl may optionally be substituted with one or more selected from C1-4 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C3-5 cycloalkyl, —Z-heterocyclyl, —Z-heteroaryl, —Z-aryl, —Z—NR10R11, —Z—C(═O)—NR10R11, —Z—OR9, halogen, —CN, —Z—SR9, —Z—SOR9, —Z—SO2R9 and —Z—COOR9; wherein any heterocyclyl may be further substituted with one or more R4 as defined above, and wherein any heteroaryl and any aryl may be further substituted with one or more R5 as defined above, and each R9 is independently selected from —H, C1-8 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl, —Z-heterocyclyl, —Z-aryl, and —Z-heteroaryl, wherein any heterocyclyl may be substituted with one or more R4 as defined above, and wherein any heteroaryl and any aryl may be substituted with one or more R5 as defined above; each of R10 and R11 is independently selected from —H, C1-6 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl, heterocyclyl, heteroaryl, and aryl, wherein any heterocyclyl may be substituted with one or more R4 as defined above, and wherein any heteroaryl and any aryl may be substituted with one or more R5 as defined above, or, alternatively, R10 and R11 may together with the N-atom to which they are attached form an N-heterocyclic ring optionally substituted with one or more R4 as defined above; when Q is —CH═NR12, R12 is selected from C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, —Z-heterocyclyl, —Z-aryl, —Z-heteroaryl, —Z—NR6R7, —Z—C(═O)—NR6R7, —Z—NR6—C(═O)—R7, —Z—C(═O)—R7, —Z—OR7, halogen, —Z—SR7, —Z—SOR7, —Z—SO2R7 and —Z—COOR7, which alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, heteroaryl and aryl may optionally be substituted with one or more R3; when Q is —CH2NHR13, R13 is selected from hydrogen, —C(O)R7, —C(O)C(O)R7, —R7, —CR14R15—NR6R7, —CR14R15CN, —CR14R15OR7, wherein each of R14 and R15 is independently selected from —H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl, heterocyclyl, heteroaryl and aryl, and wherein R14 and R15 together with the intervening carbon atom may designate a C3-10 cycloalkyl or C5-10-cycloalkenyl ring, which alkyl, alkenyl, alkynyl, cycloalkyl (ring), cycloalkenyl ring, heterocyclyl, heteroaryl and aryl may optionally be substituted with one or more R3; when Q is W, W is selected from an 1,3-diaza-C5-7-cycloalk-2-yl group which is N-substituted with R16 and optionally further substituted with one or more R3, and an 1,3-oxaza-C5-7-cycloalk-2-yl group which is N-substituted with R16 and optionally further substituted with one or more R3, wherein in both instances two R3's on the same carbon atom may together form a spiro group R16 is selected from hydrogen, —C(O)R7, and —C(O)C(O)R7, and —C(O)C(O)R7; when Q is —CH(OR17)2, each R17 independently is R3, or wherein two R17 substituents together with the intervening —O—CH(−)—O— may form a heterocyclyl optionally substituted with one or more R3 and containing up to two oxo groups; or an isomer or a mixture of isomers thereof, or a pharmaceutically acceptable salt, or solvate or prodrug thereof. |
