主权项 |
1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: B1 is selected from the group consisting of: R1 is selected from the group consisting of hydrogen, n is 0, 1 or 2; R2 and R3 are independently selected from the group consisting of hydrogen, an optionally substituted C1-6 alkyl and an optionally substituted C1-6 haloalkyl; R4 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-6 alkyl, —OR18 and —OC(═O)R19; R5 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-6 alkyl and —OR20; R6 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-6 alkyl and —OR22 ;
or R5 and R6 are both oxygen atoms and linked together by a carbonyl group; R7 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-6 alkyl, —OR24 and —OC(═O)R25; R8 is selected from the group consisting of hydrogen, an optionally substituted C1-6 alkyl and an optionally substituted C1-6 haloalkyl; R9, R10, each R11, R12 and R13 are independently absent or hydrogen; R14 is selected from the group consisting of an —O-optionally substituted aryl, an —O-optionally substituted heteroaryl and an —O-optionally substituted heterocyclyl, and R15 is or R14 is an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative, and R15 is an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative; or R14 is O−, hydroxy or an —O-optionally substituted C1-6 alkyl, and R15 and R5 together are O; R16 is selected from the group consisting of an —O-optionally substituted aryl, an —O-optionally substituted heteroaryl and an —O-optionally substituted heterocyclyl, and R17 is an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative; or R16 is an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative, and R17 is an optionally substituted N-linked amino acid or an optionally substituted N-linked amino acid ester derivative; or R16 is O−, hydroxy or an —O-optionally substituted C1-6 alkyl, and R17 and R5 together are O; R18, R20, R22 and R24 are independently selected from the group consisting of hydrogen and an optionally substituted C1-6 alkyl; R19 and R25 are independently selected from the group consisting of an optionally substituted C1-6 alkyl and an optionally substituted C3-6 cycloalkyl; R26 is hydrogen or an optionally substituted C1-4-alkyl; R27 is selected from the group consisting of hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C1-6 haloalkyl, an optionally substituted C3-6 cycloalkyl, an optionally substituted C6 aryl, an optionally substituted C10 aryl and an optionally substituted aryl(C1-6 alkyl); and R28 is selected from the group consisting of hydrogen, an optionally substituted C1-6-alkyl, an optionally substituted C3-6 cycloalkyl, an optionally substituted aryl, an optionally substituted aryl(C1-6 alkyl) and an optionally substituted haloalkyl, or R26 and R27 are taken together to form an optionally substituted C3-6 cycloalkyl; RA2 is selected from the group consisting of hydrogen, halogen and NHRJ2, wherein RJ2 is selected from the group consisting of hydrogen, —C(═O)RK2and —C(═O)ORL2; RB2 is halogen or NHRW2, wherein RW2 is selected from the group consisting of hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C2-6 alkenyl, an optionally substituted C3-8 cycloalkyl, —C(═O)RM2 and —C(═O)ORN2; RD2 is selected from the group consisting of hydrogen, halogen, an optionally substituted C1-6 alkyl, an optionally substituted C2-6 alkenyl and an optionally substituted C2-6 alkynyl; RE2 is selected from the group consisting of hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C3-8 cycloalkyl, —C(═O)RR2 and C(═O)ORS2; RF2 is hydrogen; Y2 is N or CRI2, wherein RI2 is selected from the group consisting of hydrogen, halogen, an optionally substituted C1-6-alkyl, an optionally substituted C2-6-alkenyl and an optionally substituted C2-6-alkynyl; RG2 is an optionally substituted C1-6 alkyl; RH2 is hydrogen or NHRT2, wherein RT2 is independently selected from the group consisting of hydrogen, —C(═O)RU2 and C(═O)ORV2, RO2 is selected from the group consisting of hydrogen, —C(═O)RP2 and —C(═O)ORQ2; RY2 is hydrogen or NHRZ2, wherein RZ2 is selected from the group consisting of hydrogen, —C(═O)RAA2 and C(═O)ORBB2; RK2 RL2, RM2, RN2, RP2, RQ2, RR2, RS2, RU2, RV2, RAA2 and RBB2 are independently selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, C3-6 cycloalkynyl, C6-10 aryl, heteroaryl, heteroalicyclyl, aryl(C1-6 alkyl), heteroaryl(C1-6 alkyl) and heteroalicyclyl(C1-6 alkyl); wherein each “optionally substituted” moiety is either unsubstituted or substituted, and wherein each substituted moiety is substituted with one or more substituents individually and independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heteroalicyclyl, aralkyl, heteroaralkyl, (heteroalicyclyl)alkyl, hydroxyl, alkoxy, aryloxy, acyl, mercapto, alkylthio, arylthio, cyano, halogen, thiocarbonyl, O-carbamyl, N-carbamyl, O-thiocarbamyl, N-thiocarbamyl, C-amido, N-amido, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, isocyanato, thiocyanato, isothiocycanato, nitro, silyl, sulfenyl, sulfinyl, sulfonyl, haloalkyl, haloalkoxy, trihalomethanesulfonyl, trihalomethanesulfonamido, an amio, a mono-substituted amino group and a di-substituted amino group; provided that when R2, R3, R4, and R8 are all hydrogen, R1 cannot be hydrogen; provided that when R2 and R3 are both hydrogen, R5 is hydroxy, R4 and R6 are both hydrogen, R7 is halogen, R8 is hydrogen, and B1 is then R1 cannot be wherein n is 0 or 2; and R9, R1° and R11 are hydrogen; provided that when R1 is R2 and R3 are both hydrogen, R4 is hydrogen, R5 is OH, R6 is selected from the group consisting of halogen, hydrogen, and hydroxy, R7 is selected from the group consisting of halogen, hydrogen, methyl, and hydroxy, R8 is hydrogen, B 1 is selected from the group consisting of R14 is an —O-optionally substituted aryl, then R15 cannot be wherein R26 is hydrogen or an optionally substituted C1-4 alkyl; R27 is selected from the group consisting of hydrogen, —CH3, —CH2CH3, —CH(CH3)2, —CH2CH(CH3)2, —CH2CH2SCH3, —CH2CH2COOCH2CH3, —CH2C(═O)OCH2CH3, —CH2-indol-3-yl, —CH2phenyl, unsubstituted cyclopentyl and —CH(CH2CH3)CH3; and R28 is selected from the group consisting of unsubstituted C1-4-alkyl, unsubstituted benzyl and CH2CF3; provided that when R1 is R2, R3, R4, R7 and R8 are all hydrogen, R5 is hydroxy, R6 is hydroxy, R14 is —O-naphthyl, R15 is wherein R26 is hydrogen, R27 is methyl and R28 is benzyl, then B1 cannot be provided that when R1 is R2, R3, R4, R7 and R8 are all hydrogen, R5 is hydroxy, R6 is hydroxy, R14 is —O-phenyl, R15 is wherein R26 and R27 are taken together to form an substituted cyclopentyl ring and R28 is an unsubstituted C1-4 alkyl or benzyl, then B1 cannot be provided that B1 cannot be adenine or an optionally substituted adenine when at least one of R2 and R3 is not hydrogen; and provided that a compound of Formula (I) cannot have the following structure: |