EP 2486023 A1 20120815 - POTENT CONJUGATES AND HYDROPHILIC LINKERS
Title (en)
POTENT CONJUGATES AND HYDROPHILIC LINKERS
Title (de)
WIRKUNGSSTARKE KONJUGATE UND HYDROPHILE BINDER
Title (fr)
CONJUGUÉS PUISSANTS ET SÉQUENCES DE LIAISON HYDROPHILES
Publication
Application
Priority
US 2009059620 W 20091006
Abstract (en)
[origin: WO2010126551A1] Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.
IPC 8 full level
A61K 47/48 (2006.01); A61P 35/00 (2006.01); C07D 498/18 (2006.01)
CPC (source: EP KR US)
A61K 31/535 (2013.01 - KR); A61K 47/60 (2017.08 - EP); A61K 47/68033 (2023.08 - EP KR US); A61K 47/6851 (2017.08 - EP); A61K 47/6889 (2017.08 - EP); A61P 31/12 (2018.01 - EP); A61P 33/00 (2018.01 - EP); A61P 35/00 (2018.01 - EP); A61P 35/02 (2018.01 - EP); A61P 37/02 (2018.01 - EP); A61P 37/06 (2018.01 - EP); C07D 498/18 (2013.01 - EP KR US)
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR
DOCDB simple family (publication)
WO 2010126551 A1 20101104; CN 102596922 A 20120718; EP 2486023 A1 20120815; EP 2486023 A4 20140507; IL 219020 A0 20120628; IN 2780DEN2012 A 20150918; JP 2013506709 A 20130228; KR 20120080611 A 20120717
DOCDB simple family (application)
US 2009059620 W 20091006; CN 200980162373 A 20091006; EP 09844200 A 20091006; IL 21902012 A 20120403; IN 2780DEN2012 A 20120330; JP 2012533123 A 20091006; KR 20127010084 A 20091006