- Synthesis of α-Amino Acid N-Carboxyanhydrides
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A simple phosgene- and halogen-free method for synthesizing α-amino acid N-carboxyanhydrides (NCAs) is described. The reaction between Boc-protected α-amino acids and T3P reagent gave the corresponding NCA derivatives in good yield and purity with no detectable epimerization. The process is safe, is easy-to-operate, and does not require any specific installation. It generates nontoxic, easy to remove byproducts. It can apply to the preparation of NCAs for the on-demand on-site production of either little or large quantities.
- Laconde, Guillaume,Amblard, Muriel,Martinez, Jean
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p. 6412 - 6416
(2021/08/30)
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- NOVEL CONNECTED BODY AND USE THEREOF IN SPECIFIC CONJUGATION BETWEEN BIOMOLECULE AND DRUG
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PROBLEM TO BE SOLVED: To provide: a method for producing a connected body; a method for using the connected body in the production of a uniform conjugate; and a method for applying the conjugate in the treatment of cancer, infectious diseases, and autoimmune diseases. SOLUTION: A novel connected body is provided that includes a 2,3-di-substituted succinic acid group or a 2-mono-substituted or 2,3-di-substituted fumaric acid or maleic acid (trans (E)- or cis (Z)-butenedioic acid) group for conjugating 2 or more compounds/cytotoxic agents per connected body with a cell-binding molecule by specifically bridge-linking to a pair of thiol on the cell-binding molecule. The connected body is exemplified by the following general formula. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
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Paragraph 0035; 0061-0062
(2021/05/14)
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- A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS
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Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.
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Page/Page column 233-234
(2021/01/23)
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- METHOD FOR PREPARATION OF N-CARBOXYANHYDRIDES
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The invention discloses a method for the preparation off N-carboxyanhydrides (NCAs) by reaction of amino acids with phosgene.(II)
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Page/Page column 12; 14
(2020/05/12)
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- ANTI-CD22 ANTIBODY-MAYTANSINE CONJUGATES, COMBINATIONS, AND METHODS OF USE THEREOF
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The present disclosure provides methods for treating a cancer or resistant cancer with a combination of an anti-CD22 antibody-maytansine conjugate and one or more anti-cancer agents. The disclosure also encompasses methods for sensitizing a cancer with such combinations. Also provided are pharmaceutical compositions including such combinations.
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Paragraph 0597; 0643
(2019/07/15)
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- ANTI-CD22 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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The present disclosure provides anti-CD22 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
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Paragraph 00481
(2017/08/24)
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- METHOD FOR PREPARING ENANTIOMERICALLY ENRICHED N-CARBOXYANHYDRIDE
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This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.
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Page/Page column 3-4
(2010/05/13)
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- Method for the preparation of maytansinoid esters
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Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytansinol or a maytansinoid bearing a free C-3 hydroxyl moiety and reacting the anion with an activated carboxyl compound to thereby produce the maytansinoid ester.
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Page/Page column 8
(2008/06/13)
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- New routes to 1,4-benzodiazepin-2,5-diones
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1,4-benzodiazepin-2,5-diones have been synthesized in good overall yields by two routes, the first one by cyclisation of dipeptides prepared from Boc anthranilic acid and α-amino acid methyl esters, the second one by reaction of N-carboxy α-amino acid anhydrides with Boc anthranilic acid.
- Akssira,Boumzebra,Kasmi,Dahdouh,Roumestant,Viallefont
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p. 9051 - 9060
(2007/10/02)
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