| 主权项 |
1. A compound of formula (I):wherein:
X is absent and Y is —CHR3CH2—, —CH2CHR3—, —CHR3CHR4CH2—, —CH2CHR3CHR4—, —CH2CH2CHR3—, —CR3═CHCH2—, —CH═CHR3CH2— or —CH2CH═CR3—; or X is —CHR5 and Y is —CHR3—, —CHR3CHR4—, —CHR3CR4═, —CH2CHR3—, —CR3═CH— or —CH═CR3—, wherein when Y is —CHR3CR4═, R2b is absent, or X is —CH2CHR5— or C(═O)CHR5— and Y is —CHR3—; R1 is —C(═O)CHR6R7, —C(═O)NR6R7, —C(═O)CH2CHR6R7, —C(═O)CH═CR6R7, —C(═S)CHR6R7, —C(═S)NR6R7, —C(═S)CH2CHR6R7, —C(═S)CH═CR6R7, —C(═NR8)CHR6R7, —C(═NR8)NR6R7, —C(═NR8)CH2CHR6R7 or —C(═NR8)CH—CR6R7; R2 is —C1-6alkyl, —C2-6alkenyl, —C2-6alkynyl, —OR8, —SR8, —N(R8)2, —C(═O)R8, —C(═O)N(R8)2, —N(R8)C(═O)R8, —N(R8)C(═O)N(R8)2, —N(R8)SO2R8, —SO2N(R8)2, —N(R8)SO2N(R8)2, —W-cycloalkyl, —W-cycloalkenyl, —W-aryl, —W-heterocyclyl, —W-heteroaryl, —W—Z—W-cycloalkyl, —W—Z—W-cycloalkenyl, —W—Z—W-aryl, —W—Z—W-heterocyclyl or —W—Z—W-heteroaryl, ═CH—C(═O)-J-R10, ═CHC(═O)NH-J-R10, —OCH2CHR10C2R10 or —OCH2C(R10)═CHR10; R2b is hydrogen; R3 is a carboxylic acid, —CH2CH2H, —C(═O)C(═O)OH, —CH2OH, —C(═O)NH2, —CN, —CH2C(═O)NH2, —CH2CN, a carboxylic acid bioisostere or —CH2carboxylic acid bioisostere; R4 is hydrogen or R3 and R4 together form a group: where R11 is a carboxylic acid, —CH2CH2H, —C(═O)C(═O)OH, —CH2OH, —C(═O)NH2, —CN, —CH2C(═O)NH2, —CH2CN, a carboxylic acid bioisostere or —CH2carboxylic acid bioisostere; R5 is hydrogen or together with R2 forms a fusedaryl ring substituted with one or two substituents selected from —C1-6alkyl, —C2-6alkenyl, —C2-6alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, heteroaryl, —C1-6alkyleneR10, —C2-6alkenyleneR10, —C2-6alkynyleneR10, —OCH3, —OCHF2, —OR9, —OC1-6alkyleneR10, —OC2-6alkenyleneR10, —OC2-6alkynyleneR10, —SO2NHR9, —NHSO2R9, —NHC(═O)NHR9, —NHC(═O)OR9 or —CH(OH)CH(OH)R9; or a heterocyclyl or heteroaryl ring optionally substituted with one or two optional substituents selected from —CH1-6alkyl, —C2-6alkenyl, —C2-6alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, heteroaryl, —C1-6alkyleneR10, —C2-6alkenyleneR10, —C2-6alkynyleneR10, —OCH3, —OCHF2, —OR9, —OC1-6alkyleneR10, —OC2-6alkenyleneR10, —OC2-6alkynyleneR10, —SO2NHR9, —NHSO2R9, —NHC(═O)NHR9, —NHC(═O)OR9 or —CH(OH)CH(OH)R9; R6 and R7 are independently —C1-6alkyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, heteroaryl, —CH2aryl, —CH2cycloalkyl, —CH2cycloalkenyl, —CH2heterocyclyl or —CH2heteroaryl; R8 is hydrogen, —C1-8alkyl, —C1-8fluoroalkyl, aryl, —C1-8alkylenearyl, —C2-8alkenylenearyl or —C2-8 alkyylenearyl; R9 is —C1-6alkyl, —C2-6alkenyl, —C2-6alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, heteroaryl, arylcycloalkyl-, arylcycloalkenyl-, arylaryl-, arylheterocyclyl- or arylheteroaryl-; W is a covalent bond, —O—, —S—, —SO—, —SO2—, —N(R8)—, —C(═O)—, —N(R8)C(═O)—, —C(═O)N(R8)—, —CH1-4alkylene-, —C2-4alkenylene-, —CH24 alkynylene-, —C1-3alkyleneQC1-3alkylene-, -QC1-4alkylene-, -QC2-4alkenylene-, -QC2-4alkynylene-, —CH1-4alkyleneQ-, —C2-4alkenyleneQ-, —C2-4 alkynyleneQ-, -QC1-4alkyleneQ-, -QC2-4alkenyleneQ- or —OC2-4alkynyleneQ-; Q is —O—, —S—, —SO—, —SO2—, —N(R8)—, —C(═O)—, —N(R8)C(═O)—, —C(═O)N(R8)—, Z is -cycloalkyl-, -cycloalkenyl-, -aryl-, -heterocyclyl- or -heteroaryl-; J is a covalent bond or —C1-6alkylene-, —C2-6alkenylene- or —C2-6alkynylene, in which one —CH2— group in the alkylene, alkenylene or alkynylene group may be replaced by —O—, —S—, —S(O)—, —S(O)2—, —N(R8)—, —C(═O)—, —C(═O)NH— or —NHC(═O)—; R10 is cycloalkyl, cycloalkenyl, aryl, heterocyclyl or heteroaryl; and wherein each cycloalkyl, cycloalkenyl, aryl, heterocyclyl and heteroaryl may be optionally substituted; or a pharmaceutically acceptable salt thereof. |
