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US 9,314,536 B2Granted
Compounds and methods for the treatment of EGFR positive diseases
AssigneeBio-Thera Solutions, Ltd.
InventorsChao Qin, Shengfeng Li
Life of this patent
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Abstract
Disclosed herein are anti-EGFR antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods related to the preparation and uses of such antibody drug conjugates to treat EGFR positive cells in cancers are provided.
Claims2
A compound selected from the group consisting of:
- wherein
- X is hydrogen or halo;
- Y is selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, and —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;
- n is 0, 1, 2, 3, 4, 5, 6, 7 or 8;
- or a salt thereof, wherein AA is an amino acid or thiolated amino acid, and wherein the wavy line () represents linkage of the AA through a thioether bond.
10 more elements
Dependencies are inferred from the claim text.