Title:
蛍光タグ付きリガンド
Document Type and Number:
Japanese Patent JP2006523203
Kind Code:
A
Abstract:
Library comprising a plurality of tagged non-peptide ligands of formula I (LigJL)mL(JTTag)m(JTL(JLLig)m)p including and salts thereof comprising one or a plurality of same or different ligand moieties Lig each linked to a one or a plurality of same or different tag moieties Tag via same or different linker moieties L and same or different linking site or linking functionality JT and JL wherein Lig comprises a GPCR ligand, an inhibitor of an intracellular enzyme or a substrate or inhibitor of a drug transporter; L is a single bond or is any linking moiety selected from a heteroatom such as N, O, S, P, branched or straight chain saturated or unsaturated, optionally heteroatom containing, C1-600 hydrocarbyl and combinations thereof, which may be monomeric, oligomeric having oligomeric repeat of 2 to 30 or polymeric having polymeric repeat in excess of 30 up to 300; Tag is any known or novel tagging substrate; m are each independently selected from a whole number integer from 1 to 3; p is 0 to 3 characterised in that linking is at same or different linking sites in compounds comprising different Lig, JL, L JT and/or -Tag and is at different linking sites in compounds comprising same Lig, JL, L JT and/or -Tag; process for the preparation thereof; process for the preparation of a library compound of formula I or a precursor of formula IV; method for selecting a compound of formula I from a library thereof; compound of formula I associated with information relating to its pharmacological properties; a novel compound of formula I or precursor of formula IV; uses thereof; methods for binding or inhibition therewith; use of a fluorescent target therewith; a modified cell surface GPCR and cells expressing the same; and a kit comprising a compound of formula I and a target therefor.
Inventors:
George, Michael
Hill, Stephen, John
Keram, Barry
Middleton, Richard, John
Hill, Stephen, John
Keram, Barry
Middleton, Richard, John
Application Number:
JP2006506071A
Publication Date:
October 12, 2006
Filing Date:
March 31, 2004
Export Citation:
Assignee:
University of Nottingham
International Classes:
C07D409/14; C07D209/56; C07D333/02; C07D473/00; C07D473/06; C07F5/02; C07H19/16; C07H19/167; C07H19/20; C09K11/06; C40B40/04; C40B50/00; C40B80/00; G01N21/78; G01N33/533
Foreign References:
| WO2002046395A1 | 2002-06-13 | |||
| WO2002061114A2 | 2002-08-08 |
Attorney, Agent or Firm:
Hideto Asamura
Hajime Asamura
Yukihiro Ikeda
Naganuma Akio
Hajime Asamura
Yukihiro Ikeda
Naganuma Akio