Title:
カルボキシルエステラーゼにより加水分解可能なアルファアミノ酸エステル-薬剤複合体
Document Type and Number:
Japanese Patent JP2008542196
Kind Code:
A
Abstract:
Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by intracellular carboxylesterase enzyme hCE1 and not by hCE2 or hCE3 to the corresponding acid, leads to selective accumulation of the carboxylic acid hydrolysis product in monocyte/macrophage cell and enables improved or more prolonged enzyme or receptor modulation in those cells relative to the unconjugated modulator.
Inventors:
Davidson, Alan, Hornsby
Drummond, Alan, Hastings
Needham, Lindsay, Anne
Drummond, Alan, Hastings
Needham, Lindsay, Anne
Application Number:
JP2008509506A
Publication Date:
November 27, 2008
Filing Date:
May 04, 2006
Export Citation:
Assignee:
CHROMA THERAPEUTICS LTD
International Classes:
C07C259/06; A61K31/198; A61K31/426; A61K31/4418; A61K31/47; A61K31/519; A61P29/00; A61P35/00; A61P43/00; C07D213/73; C07D215/22; C07D277/20; C07D277/46; C07D471/04; C12Q1/00; C12Q1/02; C12Q1/26; C12Q1/44; C12Q1/48
Domestic Patent References:
| JP2002542165A | 2002-12-10 | |||
| JP2007535496A | 2007-12-06 | |||
| JP2008540390A | 2008-11-20 |
Foreign References:
| WO2003076405A1 | 2003-09-18 | |||
| WO2003072557A1 | 2003-09-04 | |||
| US4725687A | 1988-02-16 | |||
| WO2002039997A2 | 2002-05-23 | |||
| WO2005037272A1 | 2005-04-28 |
Other References:
JPN6011068764; 細川 正清 他: 'カルボキシルエステラーゼの分子多様性とプロドラッグの代謝活性化' ファルマシア Ｖ３７， Ｎ２, 2001, Ｐ１１９-１２３
JPN7011004743; 堀江 透 他: 臨床薬物代謝化学 , 20030825, Ｐ８９-９７, 廣川書店
JPN5008005789; ＬＥＥ，Ｗ．Ａ． ｅｔ ａｌ．: 'Ｓｅｌｅｃｔｉｖｅ ｉｎｔｒａｃｅｌｌｕｌａｒ ａｃｔｉｖａｔｉｏｎ ｏｆ ａ ｎｏｖｅｌ ｐｒｏｄｒｕｇ ｏｆ ｔｈｅ ｈｕｍａｎ ｉｍｍｕｎｏｄｅｆｉｃｉｅｎｃｙ ｖｉｒｕｓ ｒｅｖｅｒｓｅ ｔｒ' ＡＮＴＩＭＩＣＲＯＢＩＡＬ ＡＧＥＮＴＳ ＡＮＤ ＣＨＥＭＯＴＨＥＲＡＰＹ Ｖ４９ Ｎ５, 200505, Ｐ１８９８-１９０６, ＡＭＥＲＩＣＡＮ ＳＯＣＩＥＴＹ ＦＯＲ ＭＩＣＲＯＢＩＯＬＯＧＹ
JPN5008005790; ＣＡＨＡＲＤ，Ｄ． ｅｔ ａｌ．: 'Ａｒｙｌｏｘｙ ｐｈｏｓｐｈｏｒａｍｉｄａｔｅ ｔｒｉｅｓｔｅｒｓ ａｓ ｐｒｏｔｉｄｅｓ' ＭＩＮＩ-ＲＥＶＩＥＷＳ ＩＮ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ Ｖ４ Ｎ４, 2004, Ｐ３７１-３８１
JPN6011068763; ＴＨＯＲＮＡＬＬＥＹ，Ｐ．Ｊ． ｅｔ ａｌ．: 'Ａｎｔｉｔｕｍｏｒ Ａｃｔｉｖｉｔｙ ｏｆ Ｓ-（ｐ-Ｂｒｏｍｏｂｅｎｚｙｌ）ｇｌｕｔａｔｈｉｏｎｅ Ｄｉｅｓｔｅｒｓ ｉｎ Ｖｉｔｒｏ： Ａ Ｓｔｒｕｃｔｕｒｅ-Ａｃｔｉｖｉｔｙ Ｓｔｕｄｙ' Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖ３９， Ｎ１７, 1996, Ｐ３４０９-３４１１
JPN7011004743; 堀江 透 他: 臨床薬物代謝化学 , 20030825, Ｐ８９-９７, 廣川書店
JPN5008005789; ＬＥＥ，Ｗ．Ａ． ｅｔ ａｌ．: 'Ｓｅｌｅｃｔｉｖｅ ｉｎｔｒａｃｅｌｌｕｌａｒ ａｃｔｉｖａｔｉｏｎ ｏｆ ａ ｎｏｖｅｌ ｐｒｏｄｒｕｇ ｏｆ ｔｈｅ ｈｕｍａｎ ｉｍｍｕｎｏｄｅｆｉｃｉｅｎｃｙ ｖｉｒｕｓ ｒｅｖｅｒｓｅ ｔｒ' ＡＮＴＩＭＩＣＲＯＢＩＡＬ ＡＧＥＮＴＳ ＡＮＤ ＣＨＥＭＯＴＨＥＲＡＰＹ Ｖ４９ Ｎ５, 200505, Ｐ１８９８-１９０６, ＡＭＥＲＩＣＡＮ ＳＯＣＩＥＴＹ ＦＯＲ ＭＩＣＲＯＢＩＯＬＯＧＹ
JPN5008005790; ＣＡＨＡＲＤ，Ｄ． ｅｔ ａｌ．: 'Ａｒｙｌｏｘｙ ｐｈｏｓｐｈｏｒａｍｉｄａｔｅ ｔｒｉｅｓｔｅｒｓ ａｓ ｐｒｏｔｉｄｅｓ' ＭＩＮＩ-ＲＥＶＩＥＷＳ ＩＮ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ Ｖ４ Ｎ４, 2004, Ｐ３７１-３８１
JPN6011068763; ＴＨＯＲＮＡＬＬＥＹ，Ｐ．Ｊ． ｅｔ ａｌ．: 'Ａｎｔｉｔｕｍｏｒ Ａｃｔｉｖｉｔｙ ｏｆ Ｓ-（ｐ-Ｂｒｏｍｏｂｅｎｚｙｌ）ｇｌｕｔａｔｈｉｏｎｅ Ｄｉｅｓｔｅｒｓ ｉｎ Ｖｉｔｒｏ： Ａ Ｓｔｒｕｃｔｕｒｅ-Ａｃｔｉｖｉｔｙ Ｓｔｕｄｙ' Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖ３９， Ｎ１７, 1996, Ｐ３４０９-３４１１
Attorney, Agent or Firm:
Shintaro Nogawa