[EN] OXIME DERIVATIVE SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS [FR] INHIBITEURS D'UNE ASPARTYL PROTEASE DE TYPE HYDROXYETHYLAMINE SUBSTITUEE PAR UN DERIVE D'OXIME
[EN] COMPOSITIONS AND METHODS RELATED TO ANTI-EGFR ANTIBODY DRUG CONJUGATES [FR] COMPOSITIONS ET MÉTHODES ASSOCIÉES À DES CONJUGUÉS ANTICORPS ANTI-EGFR-MÉDICAMENTS
[EN] COMPOSITIONS AND METHODS RELATED TO ANTI-CD19 ANTIBODY DRUG CONJUGATES<br/>[FR] COMPOSITIONS ET MÉTHODES ASSOCIÉES À DES CONJUGUÉS ANTICORPS ANTI-CD19-MÉDICAMENTS
申请人:LEGOCHEM BIOSCIENCES INC
公开号:WO2017051249A1
公开(公告)日:2017-03-30
In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-CD 19 antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
Provided are compounds comprising a self-immolative group, and the compounds comprising a self-immolative group according to the present invention may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity.
The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
constants at neutralpH values. As shown here, dialdehydes react with O‐alkylhydroxylamines at rates of 500 M−1 s−1 at neutralpH values in the absence of catalysts. The key to these conjugations is an unusually stable cyclicintermediate, which ultimately undergoes dehydration to yield an oxime. The scope and limitations of the method are outlined, as well as its application in bioconjugation and a mechanistic
化学生物学面临的开放挑战之一是确定在中性pH值下以大速率常数进行的反应。如此处所示,在没有催化剂的情况下,二醛在中性pH值下与O-烷基羟胺的反应速率为500 M -1 s -1。这些结合的关键是异常稳定的环状中间体,该中间体最终会脱水以生成肟。概述了该方法的范围和局限性,以及其在生物偶联中的应用以及有助于在低底物浓度下进一步发展与烷基羟胺反应的机理的解释。
BIOMOLECULE POLYMER CONJUGATES AND METHODS FOR MAKING THE SAME
申请人:Chilkoti Ashutosh
公开号:US20110294189A1
公开(公告)日:2011-12-01
Methods for producing biomolecule-polymer conjugates, such as polypeptide-polymer conjugates, include attachment of an initiator agent to a biomolecule and in situ polymerization of a polymer from defined sites on the biomolecule. The conjugates may have desirable pharmacological properties and may be used therapeutically.