871133-36-7Relevant articles and documents
Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
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Page/Page column 141; 142; 145; 146, (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
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Paragraph 0033; 0035; 0036, (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.
ANTI-FOLATE RECEPTOR APLHA (FRA) ANTIBODY-DRUG CONJUGATES AND METHODS OF USING THEREOF
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, (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
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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.
Scalable and cost-effective synthesis of a linker for bioconjugation with a peptide and a monoclonal antibody
Magano, Javier,Conway, Brian G.,Farrand, Douglas,Lovdahl, Michael,Maloney, Mark T.,Pozzo, Mark J.,Teixeira, John J.,Rizzo, John,Tumelty, David
, p. 1399 - 1406 (2014/06/09)
An efficient, scalable, and cost-effective synthesis of a linker employed in a bioconjugation process with a peptide and a monoclonal antibody is presented. Several routes were investigated that resulted in the identification of a short synthesis to a key acid intermediate from inexpensive and readily available starting materials. The final coupling of this acid with an aniline to afford the desired linker has been optimized to produce multi-gram quantities of material for clinical studies. The very limited purifications needed for both intermediates and final product make this route amenable to scale. Georg Thieme Verlag Stuttgart New York.
HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF
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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.
Development of novel linkers to conjugate pharmacophores to a carrier antibody
Palanki, Moorthy S.S.,Bhat, Abhijit,Lappe, Rodney W.,Liu, Bin,Oates, Bryan,Rizzo, John,Stankovic, Nebojsa,Bradshaw, Curt
, p. 4249 - 4253 (2012/07/17)
We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such as oligo nucleotides, peptides, and proteins to antibodies to afford novel biologics with well-de
