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US 2014/0178413 A1Published application
Compounds and methods for the treatment of erb b2/neu positive diseases
AssigneeBio-Thera Solutions, Ltd.
InventorsWeijia Tang, Shengfeng Li, Jin-Chen Yu, Xiaobin Deng
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Abstract
Disclosed herein are anti-ERB B2/NEU antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods relating to the preparation and uses of such drug conjugates to treat ERB B2/NEU positive cells in cancers are provided.
Claims17
A compound of Formula Ia:
- or a salt thereof,
- 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;
- p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, 10;
- and
- Anti-HER2 is an anti-ERB B2/NEU (HER2) antibody.
13 more elements
Dependencies are inferred from the claim text.