Water-soluble PDE4 inhibitors for the treatment of dry eye
摘要:
PDE4 inhibitors have the potential to alleviate the symptoms and underlying inflammation associated with dry eye. Disclosed herein is the development of a novel series of water-soluble PDE4 inhibitors. Our studies led to the discovery of coumarin 18, which is effective in a rabbit model of dry eye and a tear secretion test in rats. (C) 2010 Elsevier Ltd. All rights reserved.
[EN] BICYCLIC HETEROARYL INHIBITORS OF PDE4<br/>[FR] INHIBITEURS DE PDE4 À BASE DE COMPOSÉS D'HÉTÉROARYLE BICYCLIQUE
申请人:GOVEK STEVEN P
公开号:WO2008006052A2
公开(公告)日:2008-01-10
[EN] The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. [FR] La présente invention concerne des composés pouvant être utiles comme inhibiteurs de la phosphodiestérase 4 (PDE4), ainsi que des procédés associés. Ces composés et ces procédés sont destinés au traitement ou à la prévention de maladies inflammatoires et d'autres maladies associées à des taux élevés de cytokines et de médiateurs pro-inflammatoires.
Water-soluble PDE4 inhibitors for the treatment of dry eye
作者:Steven P. Govek、Guy Oshiro、John V. Anzola、Clay Beauregard、Jasmine Chen、Avery R. Coyle、Daniel A. Gamache、Mark R. Hellberg、Jennifer N. Hsien、Julia M. Lerch、John C. Liao、James W. Malecha、Lena M. Staszewski、David J. Thomas、John M. Yanni、Stewart A. Noble、Andrew K. Shiau
DOI:10.1016/j.bmcl.2010.03.023
日期:2010.5
PDE4 inhibitors have the potential to alleviate the symptoms and underlying inflammation associated with dry eye. Disclosed herein is the development of a novel series of water-soluble PDE4 inhibitors. Our studies led to the discovery of coumarin 18, which is effective in a rabbit model of dry eye and a tear secretion test in rats. (C) 2010 Elsevier Ltd. All rights reserved.
BICYCLIC HETEROARYL INHIBITORS OF PDE4
申请人:Govek Steven P.
公开号:US20090291950A1
公开(公告)日:2009-11-26
The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.