| 主权项 |
1. A conjugate compound of formula (I): wherein L is a cell-targeting ligand; T is a therapeutic agent, with the proviso that T is not CAS Registry No. 115834-23-6 (SF2446A1) or derivatives or analogues thereof; J is a linker group; X is independently selected from the group consisting of: (1) a bond; (2) O; (3)which is independently and optionally substituted from 1 to 2 times with R8, wherein the wavy lines indicate point of attachment sites and * is the point of attachment to J and ** is the point of attachment to Si; and
(4)which is independently and optionally substituted from 1 to 2 times with R8, wherein the wavy lines indicate point of attachment sites and * is the point of attachment to J and ** is the point of attachment to Si;
Q is —(CH2)n—, —CH2CHR1CH2—, —CH2CR5R6CH2—, —CH2CHR1CH2CH2—, —CH2CH2CHR1CH2CH2—, —CH2X1CH2—, or —CH2CH2X1CH2CH2—; R1 is C1-6 alkyl, aryl, heteroaryl, OR5, NR5R6, or —N(COR2)R7, each of which is optionally substituted with R8; R2 is H, C1-6 alkyl, C3-6 cycloalkyl, aryl, or heteroaryl, each of which is optionally substituted with R8; R3 is H, C1-6 alkyl, C3-6 cycloalkyl, or —COR4, each of which is optionally substituted with R8; R4 is H, C1-6 alkyl, or C3-6 cycloalkyl, each of which is optionally substituted with R8; R5 is H or C1-6 alkyl optionally substituted with R8; R6 is H or C1-6 alkyl optionally substituted with R8; or R5 and R6 are taken together with the nitrogen to which they are attached to form a five- to seven-membered heterocyclic ring, which may be saturated or unsaturated and comprises from 1 to 5 heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur, and is optionally substituted from 1 to 4 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, hydroxyl, cyano, oxo, C1-C4 alkyl, C1-C4 haloalkyl, and C1-C4 alkoxy; R7 is H, C1-6 alkyl, C3-6 cycloalkyl, aryl, or heteroaryl, each of which is optionally substituted with R8; R8 is H, NO2, CN, halogen, oxo, C1-6 alkyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 alkoxyalkyl, C3-6 cycloalkyl, C4-7 cycloalkylalkyl, aryl, heteroaryl, COOR9, COR9, C(O)NR9R10, COONR9R10, SO2R9, SO2NR9R10, or OR9; R9 is H, C1-6 alkyl, C3-6 cycloalkyl, aryl, or heteroaryl, wherein the C1-6 alkyl, C3-6 cycloalkyl, aryl, or heteroaryl is optionally substituted from 1 to 3 times with halogen, hydroxyl, cyano, oxo, C1-C4 alkyl, C1-C4 haloalkyl, or C1-C4 alkoxy; R10 is H, C1-6 alkyl, C3-6 cycloalkyl, aryl, or heteroaryl, wherein the C1-6 alkyl, C3-6 cycloalkyl, aryl, or heteroaryl is optionally substituted from 1 to 3 times with halogen, hydroxyl, cyano, oxo, C1-C4 alkyl, C1-C4 haloalkyl, or C1-C4 alkoxy; or R9 and R10 are taken together with the nitrogen to which they are attached to form a five- to seven-membered heterocyclic ring, which may be saturated or unsaturated and comprises from 1 to 5 heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur, and is optionally substituted from 1 to 4 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, hydroxyl, cyano, oxo, C1-C4 alkyl, C1-C4 haloalkyl, and C1-C4 alkoxy; X1 is O, S, SO, SO2, or NR3; n is 1 to 5; and m is 1 to 8. |
