An efficient reverse Diels–Alder approach for the synthesis of N-alkyl bismaleimides
摘要:
Bismaleimides are useful precursors for Diels-Alder reactions, Michael additions, and thiol-maleimide based conjugation for the synthesis of materials and polymers. Use of bismaleimide cross linkers for generating polymers, bioconjugate molecules, and useful imaging molecules is an active area of research. An efficient and practical synthetic protocol for N-alkyl bis-maleimide cross linkers starting from furan protected maleimide employing a reverse Diels-Alder reaction is reported. (C) 2013 Elsevier Ltd. All rights reserved.
[EN] DERIVATIVES OF AMANITA TOXINS AND THEIR CONJUGATION TO A CELL BINDING MOLECULE<br/>[FR] DÉRIVÉS DE TOXINES D'AMANITES ET LEUR CONJUGAISON À UNE MOLÉCULE DE LIAISON CELLULAIRE
申请人:HANGZHOU DAC BIOTECH CO LTD
公开号:WO2017046658A1
公开(公告)日:2017-03-23
Derivatives of Amernita toxins of Formula (I), wherein, formula (a) R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, X, L, m, n and Q are defined herein. The preparation of the derivatives. The therapeutic use of the derivatives in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
CYTOTOXIC AGENTS COMPRISING NEW ANSAMITOCIN DERIVATIVES
申请人:ImmunoGen, Inc.
公开号:US20160058882A1
公开(公告)日:2016-03-03
New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
[EN] CYTOTOXIC BIS-BENZODIAZEPINE DERIVATIVES AND CONJUGATES THEREOF WITH CELL-BINDING AGENTS FOR INHIBITING ABNORMAL CELL GROWTH OR FOR TREATING PROLIFERATIVE DISEASES<br/>[FR] DÉRIVÉS DE BIS-BENZODIAZÉPINE CYTOTOXIQUES ET LEURS CONJUGUÉS AVEC DES AGENTS DE LIAISON À UNE CELLULE POUR INHIBER LA CROISSANCE CELLULAIRE ANORMALE OU POUR TRAITER DES MALADIES PROLIFÉRATIVES
申请人:IMMUNOGEN INC
公开号:WO2020205564A1
公开(公告)日:2020-10-08
The invention relates to benzodiazepine derivatives with antiproliferative activity and more specifically to benzodiazepine compounds of formulae (I), (II), (TI) and (T2). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
The invention relates to aqueous compositions for hair treatment, comprising polyorganosiloxanes A) or organic compounds B) having certain functional groups, in particular aldehyde and unsaturated dicarboxylic acid moieties, hair treatment or hair care compositions comprising the aqueous compositions, a process for the treatment of hair which comprises the steps of providing the aqueous compositions and applying said aqueous compositions to the hair, and the use of the aqueous compositions for the treatment of hair.
ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS
申请人:Bayer Pharma Aktiengesellschaft
公开号:US20180169256A1
公开(公告)日:2018-06-21
The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.