| 主权项 |
1. A compound of Formula (1): or a pharmaceutically acceptable salt thereof, wherein: at least one of R1 and R5 is independently selected from the group consisting of halogen, —N(R10)2, —N+(—O−)(R10)2, —N(OR10)(R10), —NO2, —NO, —N(R10)(S(═O)R10), —N(R10)(S(═O)2R10), —N(R10)(C(O)R), —N(R10)(C(O)OR10), —N(R10)(C(O)N(R10)2, —CN, —COOR10, —CON(R10)2, —OH, —SH, C1-4alkylsulfanyl, C1-4 alkylsulfinyl, C1-4alkylsulfonyl, —S(O)N(R10)2, —S(O)2N(R10)2, C1-4 fluoroalkyl, C1-4 fluoroalkoxy, C1-6 alkyl, substituted C1-6 alkyl, C1-6 alkoxy, substituted C1-6 alkoxy, C3-6 cycloalkyl, substituted C3-6 cycloalkyl, C3-6 cycloalkyloxy, substituted C3-6 cycloalkyloxy, C4-12 cycloalkylalkyl, substituted C4-12 cycloalkylalkyl, C6-10 aryl, substituted C6-10 aryl, C7-16 arylalkyl, substituted C7-16 arylalkyl, C1-6 heteroalkyl, substituted C1-6 heteroalkyl, C1-6 heteroalkoxy, substituted C1-6 heteroalkoxy, C3-6 heterocycloalkyl, substituted C3-6 heterocycloalkyl, C4-12 heterocycloalkylalkyl, substituted C4-12 heterocycloalkylalkyl, C5-10 heteroaryl, substituted C5-10 heteroaryl, C6-16 heteroarylalkyl, and substituted C6-16 heteroarylalkyl; one of R1, R2, R3, R4, and R5 comprises a chemotherapeutic moiety wherein the chemotherapeutic moiety is a moiety of Formula (2), wherein,
A is selected from the group consisting of a bond (“—”), oxygen (—O—), sulfur (—S—), amino (—NR10—), methylene (—CH2—), methyleneoxy (—CH2—O—), oxycarbonyl (—O—C(═O)—), thiocarbonyl (—S—C(═O)—), aminocarbonyl (—NR10—C(═O)—)), oxythiocarbonyl (—O—C(═S)—), thiothiocarbonyl (—S—C(═S)—), aminothiocarbonyl (—NR10—C(═S)—), methyleneoxycarbonyl (—CH2—O—C(═O)—), methylenethiocarbonyl (—CH2—S—C(═O)—), methyleneaminocarbonyl (—CH2—NR10—C(═O)—), methyleneoxythiocarbonyl (—CH2—O—C(═S)—), methylenethiothiocarbonyl (—CH2—S—C(═S)—), methyleneaminothiocarbonyl (—CH2—NR10—C(═S)—), carbonyl (—C(═O)—), methylencarbonyl (—CH2—C(═O)—), thiocarbonyl (—C(═S)—), and methylenethiocarbonyl (—CH2—C(═S)—);Z is selected from the group consisting of a bond (“—”) and oxygen (—O—);Q is selected from the group consisting of —O− (a negatively charged oxygen atom) that is bound to a positively charged nitrogen atom) and a free electron pair (:), with the proviso that when Q is —O− (a negatively charged oxygen atom that is bound to a positively charged nitrogen atom), A is selected from the group consisting of a bond (“—”) and methylene (—CH2—), Z is a bond (“—”), and the chemotherapeutic moiety of Formula (2) is an N-oxide (-A-N+(—O−)(—C(R11)2—C(R11)2—R9)2);each R11 is independently selected from the group consisting of hydrogen, deuterio, and C1-3 alkyl; andeach R9 is independently selected from the group consisting of fluoro (—F), chloro (—Cl), bromo (—Br), iodo (—I), alkyl sulfonate (—OSO2R40, wherein R40 is selected from the group consisting of C1-4 alkyl), C1-4 (per)fluoroalklyl sulfonate (—OSO2R40, wherein R40 is selected from the group consisting of C1-4 (per)fluoroalkyl), and (substituted) aryl sulfonate (—SO2R40, wherein R40 is selected from C6-10 aryl); each of the other of R1, R2, R3, R4, and R5 is independently selected from the group consisting of hydrogen, deuterio, halogen, —OH, —N(R10)2, —NO2, —NO, —CN, —COOR10, —CON(R10)2, C1-4 alkylsulfanyl, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-6 alkyl, substituted C1-6 alkyl, C3-6 cycloalkyl, substituted C3-6 cycloalkyl, C1-6 heteroalkyl, substituted C1-6 heteroalkyl, C1-6 alkoxy, substituted C1-6 alkoxy, C1-6 heteroalkoxy, substituted C1-6 heteroalkoxy, C4-8 cycloalkylalkyl, and C4-8 cycloalkylheteroalkyl; R6 is selected from the group consisting of —COOH, —S(O)OH, —SO2OH, —P(O)(OH)R12, —P(O)(OH)(OR12), —SO2NHR12, —NHSO2R12, —SO2NHCOR12, —CONHSO2R12, —SO2NHCONHR12, —CONHCN, 1H-tetrazol-yl, 5-oxo-1,2,4-oxadiazole, 5-oxo-1,2,4-thiadiazole, 5-thioxo-1,2,4-oxadiazole, thiazolidinedione, oxazolidinedione, oxadiazolidinedione, 3-hydroxyisoxazole, 3-hydroxyisothiazole, cyclopentane-1,3-dione, squaric acid, squareamide, and mixed squaramate; wherein R12 is selected from hydrogen, C1-4alkyl, and C3-5 cycloalkyl; each R7 is independently selected from the group consisting of hydrogen, deuterio, halogen, hydroxyl, C1-6 alkyl, C3-6 cycloalkyl, benzyl, and phenyl; or two R7 together with the carbon to which they are bonded form a ring selected from the group consisting of a C3-6 cycloalkyl ring and a C3-6 heterocycloalkyl ring; R8 is selected from the group consisting of hydrogen, deuterio, halogen, C1-6 alkyl, substituted C1-6 alkyl, C1-6 heteroalkyl, substituted C1-6 heteroalkyl, C1-6 alkoxy, substituted C1-6 alkoxy, C1-6 heteroalkoxy, substituted C1-6 heteroalkoxy, C3-6 cycloalkyl, substituted C3-6 cycloalkyl, C3-6 cycloalkyloxy, substituted C3-6 cycloalkyloxy, —OH, —COOR10, C1-4 fluoroalkyl, C1-4 fluoroalkoxy, C3-6 cycloalkyl, and phenyl; each R10 is independently selected from the group consisting of hydrogen, deuterio, C1-4 alkyl and C1-4 alkoxy, or two geminal R10 together with the nitrogen to which they are bonded form a 3- to 6-membered heterocyclic ring; and L is —(X)a—, wherein,
each X is independently selected from the group consisting of —C(R16)2—, wherein each R16 is independently selected from the group consisting of hydrogen, deuterio, halogen, hydroxyl, C1-4 alkyl and C1-4 alkoxy, or two R16 together with the carbon to which they are bonded form a C3-6 cycloalkyl ring or a C3-6 heterocycloalkyl ring, —O—, —S—, —SO—, —SO2—, —CO—, and —N(R17)—, wherein R17 is selected from the group consisting of hydrogen and C1-4 alkyl; anda is selected from the group consisting of 0, 1, 2, 3, and 4. |
