- Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
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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.
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- ANTI-FOLATE RECEPTOR APLHA (FRA) ANTIBODY-DRUG CONJUGATES AND METHODS OF USING THEREOF
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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.
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- ANTI-CD22 ANTIBODY-DRUG CONJUGATES AND METHODS OF USING THEREOF
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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.
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Paragraph 0273; 0281
(2016/05/09)
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- HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF
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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.
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Paragraph 240; 248
(2014/07/08)
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