Title:
酵素及び受容体のモジュレーション
Document Type and Number:
Japanese Patent JP2011513289
Kind Code:
A
Abstract:
Covalent conjugates of an α,α-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the α,α-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.
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Inventors:
Drummond, Alan, Hastings
Davidson, Alan, Hornsby
Moffat, David, Festus, Charles
Donald, Alistair, David, Graham
Davis, Stephen, John
Davidson, Alan, Hornsby
Moffat, David, Festus, Charles
Donald, Alistair, David, Graham
Davis, Stephen, John
Application Number:
JP2010548178A
Publication Date:
April 28, 2011
Filing Date:
February 27, 2009
Export Citation:
Assignee:
CHROMA THERAPEUTICS LTD
International Classes:
C07C259/06; A61K31/196; A61K31/223; A61K31/44; A61K31/4418; A61K47/48; A61P35/00; A61P43/00; C07D213/56; C07D213/73
Domestic Patent References:
| JP2003171381A | 2003-06-20 | |||
| JP2007537268A | 2007-12-20 | |||
| JP2000198735A | 2000-07-18 | |||
| JPH10500702A | 1998-01-20 | |||
| JP2007500727A | 2007-01-18 |
Foreign References:
| WO2008018447A1 | 2008-02-14 | |||
| US5331006A | 1994-07-19 | |||
| WO2006117567A2 | 2006-11-09 |
Other References:
JPN5011009307; ＨＡＲＡＤＡ Ｎ: 'ＳＹＮＴＨＥＳＩＳ ＡＮＤ ＡＮＴＩＴＵＭＯＲ ＡＣＴＩＶＩＴＹ ＯＦ ９-ＡＣＹＬＯＸＹＥＬＬＩＰＴＩＣＩＮＥＳ' ＣＨＥＭＩＣＡＬ ＡＮＤ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ Ｖ４５ Ｎ７, 19970101, Ｐ１１５６-１１６２, ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＳＯＣＩＥＴＹ ＯＦ ＪＡＰＡＮ
Attorney, Agent or Firm:
Shintaro Nogawa
Masanori Akiyama
Shinji Kai
Yusuke Kaneko
Kiyoshi Inamoto
Masanori Akiyama
Shinji Kai
Yusuke Kaneko
Kiyoshi Inamoto