1069087-66-6Relevant articles and documents
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X7 receptor
Abberley, Lee,Bebius, Aude,Beswick, Paul J.,Billinton, Andy,Collis, Katharine L.,Dean, David K.,Fonfria, Elena,Gleave, Robert J.,Medhurst, Stephen J.,Michel, Anton D.,Moses, Andrew P.,Patel, Sadhana,Roman, Shilina A.,Scoccitti, Tiziana,Smith, Beverley,Steadman, Jon G.A.,Walter, Daryl S.
scheme or table, p. 6370 - 6374 (2010/12/18)
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X7 antagonist with very low in vivo clearance and high oral bioavailability in all species examined. Some evidence to support the role of P2X7 in the etiology of pain is also presented.
IMIDAZOLIDINE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS
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, (2008/12/04)
The present invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders / diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.