1426151-00-9Relevant articles and documents
Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
-
Page/Page column 141-144; 147; 148, (2019/11/11)
Disclosed are an antibody drug conjugate IB, which uses ether linkages for connection, and improves the water solubility, stability and cytotoxicity in vivo and in intro, and an intermediate, a pharmaceutical composition, and uses of the antibody drug conjugate. The antibody drug conjugate has simple synthetic steps and a high yield.
Preparation method of protein cross-linking agent maleimide-dipolyethylene glycol-acrylic acid succinimide ester
-
Paragraph 0041; 0043; 0044, (2019/04/26)
The invention relates to the technical field of organic chemical synthesis, and in particular relates to a preparation method of a protein cross-linking agent maleimide-dipolyethylene glycol-acrylic acid succinimide ester. The method comprises the following steps: step 1, synthesizing 3-maleimide propionyl chloride; step 2, synthesizing maleimide-dipolyethylene glycol-acrylic acid; step 3, synthesizing maleimide-dipolyethylene glycol-acryloyl chloride; and step 4, synthesizing the maleimide-dipolyethylene glycol-acrylic acid succinimide ester. An acyl chloride reagent adopted by the method foran esterification reaction is cheaper than a condensation reagent, the costs can be reduced, the purification is convenient, and removal of by-products of the condensation reagent is avoided; and themethod is suitable for industrialized production.
POLYMER LINKERS AND THEIR USES
-
Paragraph 0291-0292, (2019/04/08)
Provided herein are poly-1-hydroxymethylethylene hydroxymethyl formal (PHF)-based drug delivery systems. Also disclosed are methods of making antibodydrug conjugates and methods of treatment using these conjugates.
ANTI-FOLATE RECEPTOR APLHA (FRA) ANTIBODY-DRUG CONJUGATES AND METHODS OF USING THEREOF
-
, (2016/06/28)
The present disclosure provides anti-folate receptor alpha (FRA) antibody-drug conjugates comprising a hydrophilic self-immolative linker. The present disclosures further provide compositions and methods for treating cancers.
ANTI-CD22 ANTIBODY-DRUG CONJUGATES AND METHODS OF USING THEREOF
-
Paragraph 0273; 0281, (2016/05/09)
The present disclosure provides anti-CD22 antibody-drug conjugates comprising a hydrophilic self-immolative linker. The present disclosures further provide compositions and methods for treating cancers.
HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF
-
Paragraph 240; 248, (2014/07/08)
The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker.