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US 2014/0178414 A1Published application
Maytansinoid derivatives
AssigneeBio-Thera Solutions, Ltd.
InventorsShengfeng Li, Xiaobin Deng, Songnuan Tan, Weijia Tang, Chao Qin
Life of this patent
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Abstract
Disclosed herein are maytansinoid drug linker derivatives which can be linked to a antigen binding unit (Abu), and maytansinoid drugs linked with an antigen binding unit (Drug-Linker-Antigen binding Unit: D-L-Abu), for targeted delivery to disease tissues. D-L-Abu, D-L-Abu derivatives, and methods relating to the use of such drug conjugates to treat antigen positive cells in cancers and immunological disorders are provided.
Claims18
-102. (canceled)
A compound of Formula Ia:
- or a pharmaceutically acceptable salt or solvate thereof,
- wherein
- X is hydrogen or halo;
- Y is selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, and —C(C═O)R5;
- R1 is selected from the group consisting of hydrogen, —OH, —OC(═O)R5 and —OR5;
- R2 is hydrogen or C1-C6 alkyl;
- R3 is methyl, —CH2OH, or —CH2C(═O)R6;
- R4 is —OH or —SH;
- R5 is C1-C6 alkyl or benzyl;
- R6 is C1-C6 alkyl, phenyl or benzyl;
- R7 is hydrogen, C1-C6 alkyl or an amino acid side chain;
- R8 is hydrogen or C1-6 alkyl;
- p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10;
- L is selected from optionally substituted C1-C20 alkylene, optionally substituted C1-C20 alkylene wherein one or more of the —CH2— groups are independently replaced with —O—, —NR8—, —C(O)—, —C(C═O)NR8—, or —NR8C(═O)—;
- substituted C1-C20 alkylene is C1-C20 alkylene substituted with 1 to 4 R23, wherein each R23 is independently unsubstituted C1-6 alkyl;
- and
- Abu is an antigen binding unit.
14 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.