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US 2014/0178411 A1Published application
Compounds and methods for the treatment of cd20 positive diseases
AssigneeBio-Thera Solutions, Ltd.
InventorsChao Qin, Shengfeng Li
Life of this patent
Estimating the term…
Abstract
Disclosed herein are anti-CD20 antibody conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods related to the preparation and uses of such antibody drug conjugates to treat CD20 positive cells in cancers are provided.
Claims15
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;
- p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, 10;
- and
- Anti-CD20 is an anti-CD20 antibody.
12 more elements
A compound of Formula Ib:
- 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-CD20 is an anti-CD20 antibody.
13 more elements
A compound of Formula Ic:
- 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;
- p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, 10;
- and
- Anti-CD20 is an anti-CD20 antibody.
12 more elements
A method of treating a proliferative, inflammatory or immunologic disease or condition characterized by CD20 positive cells in a patient in need thereof comprising administering an effective amount of a compound of Formula IVb,
- or a salt thereof, wherein the compound of Formula IVb is generated as a result of a metabolic chemical reaction following administration of a compound of Formula IIb,
- or a pharmaceutically acceptable salt or solvate thereof, wherein Anti-CD20 is an anti-CD20 antibody, and wherein AA is an amino acid or thiolated amino acid.
Dependencies are inferred from the claim text.